Biased Signaling Atlas

Ligand source activities (1 row/activity)

Potency
Affinity

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Ligands (move mouse cursor over ligand name to see structure)					Receptor			Assay information							Chemical information
Sel. page	Common name	GPCRdb ID	#Vendors	Reference ligand	Fold selectivity	# Tested GPCRs	Species	p-value (-log)	Activity Type	Activity Relation	Activity Value	AssayType	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI
	4418	40996	85	None	-23	18	Human	5.9	pAC50	=	5.9	Functional	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	40996	85	None	-23	18	Human	5.9	pAC50	=	5.9	Functional	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	10552	33	None	-4897	17	Human	4.8	pAC50	=	4.8	Functional	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	10552	33	None	-4897	17	Human	4.8	pAC50	=	4.8	Functional	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	10552	33	None	-4897	17	Human	4.8	pAC50	=	4.8	Functional	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	10552	33	None	-4897	17	Human	4.8	pAC50	=	4.8	Functional	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	10552	33	None	-4897	17	Human	4.8	pAC50	=	4.8	Functional	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	9383	88	None	-257	8	Human	4.8	pAC50	=	4.8	Functional	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	9383	88	None	-257	8	Human	4.8	pAC50	=	4.8	Functional	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	9383	88	None	-257	8	Human	4.8	pAC50	=	4.8	Functional	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	9383	88	None	-257	8	Human	4.8	pAC50	=	4.8	Functional	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	7516	40	None	-676	29	Human	5.7	pAC50	=	5.7	Functional	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	7516	40	None	-676	29	Human	5.7	pAC50	=	5.7	Functional	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	7516	40	None	-676	29	Human	5.7	pAC50	=	5.7	Functional	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	7516	40	None	-676	29	Human	5.7	pAC50	=	5.7	Functional	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	7516	40	None	-676	29	Human	5.7	pAC50	=	5.7	Functional	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	21265	5	None	-7	25	Human	4.6	pAC50	=	4.6	Functional	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	21265	5	None	-7	25	Human	4.6	pAC50	=	4.6	Functional	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	21265	5	None	-7	25	Human	4.6	pAC50	=	4.6	Functional	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	21265	5	None	-7	25	Human	4.6	pAC50	=	4.6	Functional	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	21265	5	None	-7	25	Human	4.6	pAC50	=	4.6	Functional	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	21265	5	None	-7	25	Human	4.6	pAC50	=	4.6	Functional	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	9292	24	None	-1380	18	Human	5.6	pAC50	=	5.6	Functional	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	9292	24	None	-1380	18	Human	5.6	pAC50	=	5.6	Functional	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	9292	24	None	-1380	18	Human	5.6	pAC50	=	5.6	Functional	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	9292	24	None	-1380	18	Human	5.6	pAC50	=	5.6	Functional	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	9292	24	None	-1380	18	Human	5.6	pAC50	=	5.6	Functional	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	95905	14	None	-234	13	Human	5.5	pAC50	=	5.5	Functional	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	95905	14	None	-234	13	Human	5.5	pAC50	=	5.5	Functional	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	7742	58	None	-93	14	Human	6.4	pAC50	=	6.4	Functional	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	7742	58	None	-93	14	Human	6.4	pAC50	=	6.4	Functional	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	7742	58	None	-93	14	Human	6.4	pAC50	=	6.4	Functional	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	7742	58	None	-93	14	Human	6.4	pAC50	=	6.4	Functional	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	7742	58	None	-93	14	Human	6.4	pAC50	=	6.4	Functional	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	7565	60	None	-891	12	Human	5.4	pAC50	=	5.4	Functional	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	7565	60	None	-891	12	Human	5.4	pAC50	=	5.4	Functional	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	7565	60	None	-891	12	Human	5.4	pAC50	=	5.4	Functional	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	7565	60	None	-891	12	Human	5.4	pAC50	=	5.4	Functional	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	7565	60	None	-891	12	Human	5.4	pAC50	=	5.4	Functional	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	9287	21	None	-22	17	Human	7.2	pAC50	=	7.2	Functional	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	9287	21	None	-22	17	Human	7.2	pAC50	=	7.2	Functional	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	9287	21	None	-22	17	Human	7.2	pAC50	=	7.2	Functional	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	9287	21	None	-22	17	Human	7.2	pAC50	=	7.2	Functional	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	9287	21	None	-22	17	Human	7.2	pAC50	=	7.2	Functional	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	8202	21	None	-467	26	Human	6.2	pAC50	=	6.2	Functional	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	8202	21	None	-467	26	Human	6.2	pAC50	=	6.2	Functional	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	8202	21	None	-467	26	Human	6.2	pAC50	=	6.2	Functional	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	8202	21	None	-467	26	Human	6.2	pAC50	=	6.2	Functional	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	8202	21	None	-467	26	Human	6.2	pAC50	=	6.2	Functional	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	9933	96	None	-234	10	Human	6.1	pAC50	=	6.1	Functional	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	9933	96	None	-234	10	Human	6.1	pAC50	=	6.1	Functional	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	9933	96	None	-234	10	Human	6.1	pAC50	=	6.1	Functional	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	9933	96	None	-234	10	Human	6.1	pAC50	=	6.1	Functional	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	9933	96	None	-234	10	Human	6.1	pAC50	=	6.1	Functional	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	21269	69	None	-	1	Human	6.0	pAC50	=	6.0	Functional	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	21269	69	None	-	1	Human	6.0	pAC50	=	6.0	Functional	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	10606	60	None	-22	6	Human	6.0	pAC50	=	6.0	Functional	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	10606	60	None	-22	6	Human	6.0	pAC50	=	6.0	Functional	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	10606	60	None	-22	6	Human	6.0	pAC50	=	6.0	Functional	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	10606	60	None	-22	6	Human	6.0	pAC50	=	6.0	Functional	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	10606	60	None	-22	6	Human	6.0	pAC50	=	6.0	Functional	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	9828	37	None	-288	24	Human	6.0	pAC50	=	6.0	Functional	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	9828	37	None	-288	24	Human	6.0	pAC50	=	6.0	Functional	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	9828	37	None	-288	24	Human	6.0	pAC50	=	6.0	Functional	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	9828	37	None	-288	24	Human	6.0	pAC50	=	6.0	Functional	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	9828	37	None	-288	24	Human	6.0	pAC50	=	6.0	Functional	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	199797	0	None	50	2	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	367	7	4	5	1.9	CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1	10.1021/acs.jmedchem.1c00692
	CHEMBL5204599	199797	0	None	50	2	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	367	7	4	5	1.9	CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222793	199797	0	None	50	2	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	367	7	4	5	1.9	CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1	10.1021/acs.jmedchem.1c00692
	CHEMBL5093461	222332	0	None	-	1	Human	7.0	pEC50	=	7	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL		None	None	None		CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2nnc(N)s2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1016/j.bmcl.2021.128388
	CHEMBL5095884	222332	0	None	-	1	Human	7.0	pEC50	=	7	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL		None	None	None		CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2nnc(N)s2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1016/j.bmcl.2021.128388
	164611342	191867	0	None	-1	3	Human	7.0	pEC50	=	7	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	346	6	4	4	1.8	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCc1ccccc1	10.1016/j.ejmech.2021.113190
	CHEMBL4856005	191867	0	None	-1	3	Human	7.0	pEC50	=	7	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	346	6	4	4	1.8	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCc1ccccc1	10.1016/j.ejmech.2021.113190
	155559319	181642	0	None	13	2	Human	7.0	pEC50	=	7	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	239	1	1	3	3.2	CC1CCCc2c(-c3ccccc3)nc(N)nc21	10.1021/acs.jmedchem.9b00241
	CHEMBL4563363	181642	0	None	13	2	Human	7.0	pEC50	=	7	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	239	1	1	3	3.2	CC1CCCc2c(-c3ccccc3)nc(N)nc21	10.1021/acs.jmedchem.9b00241
	168290815	199752	0	None	10	2	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	327	9	4	5	1.2	CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5200771	199752	0	None	10	2	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	327	9	4	5	1.2	CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222529	199752	0	None	10	2	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	327	9	4	5	1.2	CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5083588	222313	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	CHEMBL5095633	222313	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	1204	8713	119	None	-181	11	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitment	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	1247	8713	119	None	-181	11	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitment	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	1375	8713	119	None	-181	11	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitment	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	774	8713	119	None	-181	11	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitment	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	CHEMBL90	8713	119	None	-181	11	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitment	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	DB05381	8713	119	None	-181	11	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitment	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	CHEMBL5075713	222308	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitment	ChEMBL		None	None	None		CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2c[nH]cn2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1016/j.bmcl.2021.128388
	CHEMBL5095559	222308	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitment	ChEMBL		None	None	None		CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2c[nH]cn2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1016/j.bmcl.2021.128388
	1204	8713	119	None	-181	11	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.1c00692
	1247	8713	119	None	-181	11	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.1c00692
	1375	8713	119	None	-181	11	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.1c00692
	774	8713	119	None	-181	11	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.1c00692
	CHEMBL90	8713	119	None	-181	11	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.1c00692
	DB05381	8713	119	None	-181	11	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.1c00692
	168268853	199564	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL	389	8	4	5	1.9	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5180504	199564	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL	389	8	4	5	1.9	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221353	199564	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL	389	8	4	5	1.9	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
	46887041	15532	1	None	-5	4	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay	ChEMBL	313	7	4	3	2.2	C[C@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)c1ccccc1	10.1016/j.bmcl.2010.03.082
	CHEMBL1096428	15532	1	None	-5	4	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay	ChEMBL	313	7	4	3	2.2	C[C@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)c1ccccc1	10.1016/j.bmcl.2010.03.082
	CHEMBL5092267	222134	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCC[n+]1c(C)cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc1C	10.1016/j.bmcl.2021.128388
	CHEMBL5075713	222308	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL		None	None	None		CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2c[nH]cn2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1016/j.bmcl.2021.128388
	CHEMBL5095559	222308	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL		None	None	None		CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2c[nH]cn2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1016/j.bmcl.2021.128388
	1204	8713	119	None	-181	11	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm900526h
	1247	8713	119	None	-181	11	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm900526h
	1375	8713	119	None	-181	11	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm900526h
	774	8713	119	None	-181	11	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm900526h
	CHEMBL90	8713	119	None	-181	11	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm900526h
	DB05381	8713	119	None	-181	11	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm900526h
	1204	8713	119	None	-181	11	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1039/C3MD00245D
	1247	8713	119	None	-181	11	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1039/C3MD00245D
	1375	8713	119	None	-181	11	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1039/C3MD00245D
	774	8713	119	None	-181	11	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1039/C3MD00245D
	CHEMBL90	8713	119	None	-181	11	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1039/C3MD00245D
	DB05381	8713	119	None	-181	11	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1039/C3MD00245D
	44482302	12398	0	None	-	1	Human	4.9	pEC50	=	4.9	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	321	6	4	4	1.2	Cc1ccc(S(=O)(=O)NC(=N)NCCCc2c[nH]cn2)cc1	10.1021/jm900526h
	CHEMBL1077596	12398	0	None	-	1	Human	4.9	pEC50	=	4.9	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	321	6	4	4	1.2	Cc1ccc(S(=O)(=O)NC(=N)NCCCc2c[nH]cn2)cc1	10.1021/jm900526h
	44481217	12566	0	None	-	1	Human	4.9	pEC50	=	4.9	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	335	8	4	4	1.0	N=C(NCCCc1c[nH]cn1)NS(=O)(=O)CCc1ccccc1	10.1021/jm900526h
	CHEMBL1078747	12566	0	None	-	1	Human	4.9	pEC50	=	4.9	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	335	8	4	4	1.0	N=C(NCCCc1c[nH]cn1)NS(=O)(=O)CCc1ccccc1	10.1021/jm900526h
	CHEMBL5090859	222062	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCCC[n+]1c(C)cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc1C	10.1016/j.bmcl.2021.128388
	1204	8713	119	None	-181	11	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2010.03.082
	1247	8713	119	None	-181	11	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2010.03.082
	1375	8713	119	None	-181	11	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2010.03.082
	774	8713	119	None	-181	11	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2010.03.082
	CHEMBL90	8713	119	None	-181	11	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2010.03.082
	DB05381	8713	119	None	-181	11	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2010.03.082
	1204	8713	119	None	-181	11	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm201128q
	1247	8713	119	None	-181	11	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm201128q
	1375	8713	119	None	-181	11	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm201128q
	774	8713	119	None	-181	11	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm201128q
	CHEMBL90	8713	119	None	-181	11	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm201128q
	DB05381	8713	119	None	-181	11	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm201128q
	CHEMBL5083588	222313	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitment	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	CHEMBL5095633	222313	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitment	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	168268853	199564	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	389	8	4	5	1.9	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5180504	199564	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	389	8	4	5	1.9	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221353	199564	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	389	8	4	5	1.9	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5077939	222320	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)O)c3ccccc3C2(C)C)c2cc(S(=O)(=O)[O-])ccc2C1(C)C	10.1016/j.bmcl.2021.128388
	CHEMBL5095769	222320	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)O)c3ccccc3C2(C)C)c2cc(S(=O)(=O)[O-])ccc2C1(C)C	10.1016/j.bmcl.2021.128388
	13170764	181858	0	None	2	2	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	255	2	1	4	2.6	COc1ccc(-c2nc(N)nc3c2CCCC3)cc1	10.1021/acs.jmedchem.9b00241
	CHEMBL4568452	181858	0	None	2	2	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	255	2	1	4	2.6	COc1ccc(-c2nc(N)nc3c2CCCC3)cc1	10.1021/acs.jmedchem.9b00241
	168294449	199797	0	None	50	2	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL	367	7	4	5	1.9	CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1	10.1021/acs.jmedchem.1c00692
	CHEMBL5204599	199797	0	None	50	2	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL	367	7	4	5	1.9	CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222793	199797	0	None	50	2	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL	367	7	4	5	1.9	CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1	10.1021/acs.jmedchem.1c00692
	56954513	88858	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	578	17	6	8	2.6	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1cnc(N)s1	10.1021/jm201128q
	CHEMBL2165645	88858	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	578	17	6	8	2.6	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1cnc(N)s1	10.1021/jm201128q
	CHEMBL5092102	222125	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL		None	None	None		NCCCCCCCCNC(=O)/N=C(\N)NCCCc1c[nH]cn1	10.1016/j.bmcl.2021.128388
	164611757	191682	0	None	3	3	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	402	8	4	4	2.8	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1	10.1016/j.ejmech.2021.113190
	CHEMBL4853107	191682	0	None	3	3	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	402	8	4	4	2.8	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1	10.1016/j.ejmech.2021.113190
	168294449	199797	0	None	50	2	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	367	7	4	5	1.9	CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1	10.1021/acs.jmedchem.1c00692
	CHEMBL5204599	199797	0	None	50	2	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	367	7	4	5	1.9	CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222793	199797	0	None	50	2	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	367	7	4	5	1.9	CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1	10.1021/acs.jmedchem.1c00692
	168295528	199810	0	None	31	9	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	333	6	4	5	0.9	N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5206565	199810	0	None	31	9	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	333	6	4	5	0.9	N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222872	199810	0	None	31	9	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	333	6	4	5	0.9	N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5085542	221751	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCC[n+]1c(C)cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc1C	10.1016/j.bmcl.2021.128388
	13170764	181858	0	None	2	2	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	255	2	1	4	2.6	COc1ccc(-c2nc(N)nc3c2CCCC3)cc1	10.1021/acs.jmedchem.9b00241
	CHEMBL4568452	181858	0	None	2	2	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	255	2	1	4	2.6	COc1ccc(-c2nc(N)nc3c2CCCC3)cc1	10.1021/acs.jmedchem.9b00241
	1204	8713	119	None	-181	11	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	1247	8713	119	None	-181	11	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	1375	8713	119	None	-181	11	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	774	8713	119	None	-181	11	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	CHEMBL90	8713	119	None	-181	11	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	DB05381	8713	119	None	-181	11	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	44481489	12485	0	None	-18	2	Human	4.9	pEC50	=	4.9	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	310	8	3	3	2.0	N#C/N=C(\NCCCc1ccccc1)NCCCc1c[nH]cn1	10.1021/jm900526h
	CHEMBL1078210	12485	0	None	-18	2	Human	4.9	pEC50	=	4.9	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	310	8	3	3	2.0	N#C/N=C(\NCCCc1ccccc1)NCCCc1c[nH]cn1	10.1021/jm900526h
	CHEMBL5088914	222341	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	CHEMBL5095949	222341	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	164628701	193246	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	338	5	4	4	1.9	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC1CCCCC1	10.1016/j.ejmech.2021.113190
	CHEMBL4876743	193246	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	338	5	4	4	1.9	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC1CCCCC1	10.1016/j.ejmech.2021.113190
	164626370	193252	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	338	6	4	4	1.8	CCCCCCNC(=O)/N=C(\N)NC1CCc2nc(N)sc2C1	10.1016/j.ejmech.2021.113190
	CHEMBL4876799	193252	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	338	6	4	4	1.8	CCCCCCNC(=O)/N=C(\N)NC1CCc2nc(N)sc2C1	10.1016/j.ejmech.2021.113190
	56954517	88841	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	502	17	6	6	0.5	N/C(=N\C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1ncn[nH]1)NCCCc1ncn[nH]1	10.1021/jm201128q
	CHEMBL2165629	88841	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	502	17	6	6	0.5	N/C(=N\C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1ncn[nH]1)NCCCc1ncn[nH]1	10.1021/jm201128q
	164614645	191911	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	402	8	4	4	3.0	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(c1ccccc1)C(C)C	10.1016/j.ejmech.2021.113190
	CHEMBL4856572	191911	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	402	8	4	4	3.0	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(c1ccccc1)C(C)C	10.1016/j.ejmech.2021.113190
	1204	8713	119	None	-181	11	Human	5.8	pEC50	=	5.8	Functional	Antagonist activity at Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins in presence of histamine by GTPgammaS binding assayAntagonist activity at Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins in presence of histamine by GTPgammaS binding assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acsmedchemlett.0c00033
	1247	8713	119	None	-181	11	Human	5.8	pEC50	=	5.8	Functional	Antagonist activity at Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins in presence of histamine by GTPgammaS binding assayAntagonist activity at Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins in presence of histamine by GTPgammaS binding assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acsmedchemlett.0c00033
	1375	8713	119	None	-181	11	Human	5.8	pEC50	=	5.8	Functional	Antagonist activity at Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins in presence of histamine by GTPgammaS binding assayAntagonist activity at Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins in presence of histamine by GTPgammaS binding assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acsmedchemlett.0c00033
	774	8713	119	None	-181	11	Human	5.8	pEC50	=	5.8	Functional	Antagonist activity at Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins in presence of histamine by GTPgammaS binding assayAntagonist activity at Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins in presence of histamine by GTPgammaS binding assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acsmedchemlett.0c00033
	CHEMBL90	8713	119	None	-181	11	Human	5.8	pEC50	=	5.8	Functional	Antagonist activity at Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins in presence of histamine by GTPgammaS binding assayAntagonist activity at Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins in presence of histamine by GTPgammaS binding assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acsmedchemlett.0c00033
	DB05381	8713	119	None	-181	11	Human	5.8	pEC50	=	5.8	Functional	Antagonist activity at Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins in presence of histamine by GTPgammaS binding assayAntagonist activity at Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins in presence of histamine by GTPgammaS binding assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acsmedchemlett.0c00033
	56954002	88845	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	620	19	6	8	3.7	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1021/jm201128q
	CHEMBL2165633	88845	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	620	19	6	8	3.7	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1021/jm201128q
	44414337	86914	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human H2RAgonist activity at human H2R	ChEMBL	945	24	3	9	8.3	CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCC/N=C(\NC#N)NCCCOc3cccc(CN4CCCCC4)c3)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1016/j.bmcl.2006.05.039
	CHEMBL213357	86914	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human H2RAgonist activity at human H2R	ChEMBL	945	24	3	9	8.3	CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCC/N=C(\NC#N)NCCCOc3cccc(CN4CCCCC4)c3)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1016/j.bmcl.2006.05.039
	90667237	116252	0	None	-	1	Human	4.8	pEC50	=	4.8	Functional	Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting	ChEMBL	356	9	3	4	2.8	Cc1nc(CCCCN/C(=N\C#N)NCCSc2ccccc2)c[nH]1	10.1039/C3MD00245D
	CHEMBL3220638	116252	0	None	-	1	Human	4.8	pEC50	=	4.8	Functional	Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting	ChEMBL	356	9	3	4	2.8	Cc1nc(CCCCN/C(=N\C#N)NCCSc2ccccc2)c[nH]1	10.1039/C3MD00245D
	164622190	192395	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	360	7	4	4	1.8	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCc1ccccc1	10.1016/j.ejmech.2021.113190
	CHEMBL4864067	192395	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	360	7	4	4	1.8	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCc1ccccc1	10.1016/j.ejmech.2021.113190
	119570	9933	96	None	-234	10	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	10.1021/acs.jmedchem.1c00692
	2233	9933	96	None	-234	10	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	10.1021/acs.jmedchem.1c00692
	953	9933	96	None	-234	10	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	10.1021/acs.jmedchem.1c00692
	CHEMBL301265	9933	96	None	-234	10	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	10.1021/acs.jmedchem.1c00692
	DB00413	9933	96	None	-234	10	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	10.1021/acs.jmedchem.1c00692
	164627189	193100	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	298	6	4	4	1.0	CCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1016/j.ejmech.2021.113190
	CHEMBL4874758	193100	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	298	6	4	4	1.0	CCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1016/j.ejmech.2021.113190
	164610892	191977	0	None	4	3	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	394	8	4	4	3.2	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CC1CCCCC1	10.1016/j.ejmech.2021.113190
	CHEMBL4857560	191977	0	None	4	3	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	394	8	4	4	3.2	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CC1CCCCC1	10.1016/j.ejmech.2021.113190
	164612037	192156	0	None	-11	11	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	326	8	4	4	1.8	CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1016/j.ejmech.2021.113190
	CHEMBL4860528	192156	0	None	-11	11	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	326	8	4	4	1.8	CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1016/j.ejmech.2021.113190
	164627189	193100	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	298	6	4	4	1.0	CCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1016/j.ejmech.2021.113190
	CHEMBL4874758	193100	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	298	6	4	4	1.0	CCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1016/j.ejmech.2021.113190
	46887042	15534	0	None	-6	4	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay	ChEMBL	319	7	4	3	2.6	C[C@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)C1CCCCC1	10.1016/j.bmcl.2010.03.082
	CHEMBL1096430	15534	0	None	-6	4	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay	ChEMBL	319	7	4	3	2.6	C[C@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)C1CCCCC1	10.1016/j.bmcl.2010.03.082
	CHEMBL5094663	222285	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](C)c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	168273640	199584	0	None	4	3	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	568	15	8	10	-0.1	N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5176229	199584	0	None	4	3	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	568	15	8	10	-0.1	N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221444	199584	0	None	4	3	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	568	15	8	10	-0.1	N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	168295541	199819	0	None	14	2	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	347	6	4	5	1.4	C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5208845	199819	0	None	14	2	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	347	6	4	5	1.4	C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222926	199819	0	None	14	2	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	347	6	4	5	1.4	C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5094663	222285	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitment	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](C)c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	126688	7192	33	None	57	2	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	157	2	2	4	0.5	NCCc1sc(nc1C)N	10.1021/jm201128q
	4025	7192	33	None	57	2	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	157	2	2	4	0.5	NCCc1sc(nc1C)N	10.1021/jm201128q
	CHEMBL293762	7192	33	None	57	2	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	157	2	2	4	0.5	NCCc1sc(nc1C)N	10.1021/jm201128q
	CHEMBL5092102	222125	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL		None	None	None		NCCCCCCCCNC(=O)/N=C(\N)NCCCc1c[nH]cn1	10.1016/j.bmcl.2021.128388
	44481214	12508	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	314	7	4	2	1.2	NC(=O)/N=C(/NCCCc1ccccc1)NCCc1c[nH]cn1	10.1021/jm900526h
	CHEMBL1078358	12508	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	314	7	4	2	1.2	NC(=O)/N=C(/NCCCc1ccccc1)NCCc1c[nH]cn1	10.1021/jm900526h
	46887080	15317	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay	ChEMBL	365	7	4	5	3.2	Cc1nc(N)sc1CCCNC(=N)NC(=O)C[C@@H](C)C1CCCCC1	10.1016/j.bmcl.2010.03.082
	CHEMBL1094452	15317	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay	ChEMBL	365	7	4	5	3.2	Cc1nc(N)sc1CCCNC(=N)NC(=O)C[C@@H](C)C1CCCCC1	10.1016/j.bmcl.2010.03.082
	71458814	88859	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	345	7	3	4	2.0	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCc1ccccc1	10.1021/jm201128q
	CHEMBL2165646	88859	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	345	7	3	4	2.0	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCc1ccccc1	10.1021/jm201128q
	CHEMBL5076746	222304	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(N)(=O)=O)c3ccccc3C2(C)C)c2cc(S(=O)(=O)[O-])ccc2C1(C)C	10.1016/j.bmcl.2021.128388
	CHEMBL5095519	222304	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(N)(=O)=O)c3ccccc3C2(C)C)c2cc(S(=O)(=O)[O-])ccc2C1(C)C	10.1016/j.bmcl.2021.128388
	CHEMBL5075106	222306	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)O)c3ccccc3C2(C)C)c2cc(S(=O)(=O)[O-])ccc2C1(C)C	10.1016/j.bmcl.2021.128388
	CHEMBL5095549	222306	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)O)c3ccccc3C2(C)C)c2cc(S(=O)(=O)[O-])ccc2C1(C)C	10.1016/j.bmcl.2021.128388
	56954227	88849	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	564	17	6	8	2.3	N/C(=N\C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1cnc(N)s1)NCCCc1cnc(N)s1	10.1021/jm201128q
	CHEMBL2165637	88849	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	564	17	6	8	2.3	N/C(=N\C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1cnc(N)s1)NCCCc1cnc(N)s1	10.1021/jm201128q
	164608815	191233	0	None	3	3	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	380	7	4	4	2.8	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1	10.1016/j.ejmech.2021.113190
	CHEMBL4846638	191233	0	None	3	3	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	380	7	4	4	2.8	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1	10.1016/j.ejmech.2021.113190
	155544816	181812	0	None	2	2	Human	5.7	pEC50	=	5.7	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	269	2	1	4	2.9	COc1ccc(-c2nc(N)nc3c2CC(C)CC3)cc1	10.1021/acs.jmedchem.9b00241
	CHEMBL4567405	181812	0	None	2	2	Human	5.7	pEC50	=	5.7	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	269	2	1	4	2.9	COc1ccc(-c2nc(N)nc3c2CC(C)CC3)cc1	10.1021/acs.jmedchem.9b00241
	56954318	88853	0	None	-2	2	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	444	13	6	4	0.1	N/C(=N\C(=O)CCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1	10.1021/jm201128q
	CHEMBL2165640	88853	0	None	-2	2	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	444	13	6	4	0.1	N/C(=N\C(=O)CCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1	10.1021/jm201128q
	164627774	193344	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	344	3	4	4	1.4	N/C(=N\C(=O)NCc1ccccc1)NC1CCc2nc(N)sc2C1	10.1016/j.ejmech.2021.113190
	CHEMBL4878215	193344	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	344	3	4	4	1.4	N/C(=N\C(=O)NCc1ccccc1)NC1CCc2nc(N)sc2C1	10.1016/j.ejmech.2021.113190
	155544816	181812	0	None	2	2	Human	5.7	pEC50	=	5.7	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	269	2	1	4	2.9	COc1ccc(-c2nc(N)nc3c2CC(C)CC3)cc1	10.1021/acs.jmedchem.9b00241
	CHEMBL4567405	181812	0	None	2	2	Human	5.7	pEC50	=	5.7	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	269	2	1	4	2.9	COc1ccc(-c2nc(N)nc3c2CC(C)CC3)cc1	10.1021/acs.jmedchem.9b00241
	164608815	191233	0	None	3	3	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	380	7	4	4	2.8	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1	10.1016/j.ejmech.2021.113190
	CHEMBL4846638	191233	0	None	3	3	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	380	7	4	4	2.8	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1	10.1016/j.ejmech.2021.113190
	168286426	199705	0	None	5	2	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	403	10	4	5	2.3	CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5198795	199705	0	None	5	2	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	403	10	4	5	2.3	CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222241	199705	0	None	5	2	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	403	10	4	5	2.3	CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	164609493	191215	0	None	-2	3	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	350	6	4	5	1.9	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccco1	10.1016/j.ejmech.2021.113190
	CHEMBL4846380	191215	0	None	-2	3	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	350	6	4	5	1.9	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccco1	10.1016/j.ejmech.2021.113190
	168292954	199776	0	None	7	3	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	388	8	4	4	2.5	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5202592	199776	0	None	7	3	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	388	8	4	4	2.5	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222660	199776	0	None	7	3	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	388	8	4	4	2.5	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
	168294767	199798	0	None	40	10	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	313	8	4	5	0.9	CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5207281	199798	0	None	40	10	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	313	8	4	5	0.9	CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222802	199798	0	None	40	10	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	313	8	4	5	0.9	CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5075106	222306	0	None	-	1	Human	5.6	pEC50	=	5.6	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)O)c3ccccc3C2(C)C)c2cc(S(=O)(=O)[O-])ccc2C1(C)C	10.1016/j.bmcl.2021.128388
	CHEMBL5095549	222306	0	None	-	1	Human	5.6	pEC50	=	5.6	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)O)c3ccccc3C2(C)C)c2cc(S(=O)(=O)[O-])ccc2C1(C)C	10.1016/j.bmcl.2021.128388
	56954425	88856	0	None	13	2	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	584	23	6	4	4.0	N/C(=N\C(=O)CCCCCCCCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1	10.1021/jm201128q
	CHEMBL2165643	88856	0	None	13	2	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	584	23	6	4	4.0	N/C(=N\C(=O)CCCCCCCCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1	10.1021/jm201128q
	155523256	177525	0	None	-3	2	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	269	2	1	4	3.2	COc1cccc(-c2nc(N)nc3c2CCCC3C)c1	10.1021/acs.jmedchem.9b00241
	CHEMBL4452406	177525	0	None	-3	2	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	269	2	1	4	3.2	COc1cccc(-c2nc(N)nc3c2CCCC3C)c1	10.1021/acs.jmedchem.9b00241
	56954125	88846	0	None	-	1	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	676	23	6	8	5.3	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCCCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1021/jm201128q
	CHEMBL2165634	88846	0	None	-	1	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	676	23	6	8	5.3	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCCCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1021/jm201128q
	168290235	199747	0	None	9	9	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	315	6	4	3	1.1	C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5201074	199747	0	None	9	9	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	315	6	4	3	1.1	C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222491	199747	0	None	9	9	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	315	6	4	3	1.1	C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1	10.1021/acs.jmedchem.1c00692
	168294767	199798	0	None	40	10	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL	313	8	4	5	0.9	CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5207281	199798	0	None	40	10	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL	313	8	4	5	0.9	CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222802	199798	0	None	40	10	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL	313	8	4	5	0.9	CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	155523256	177525	0	None	-3	2	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	269	2	1	4	3.2	COc1cccc(-c2nc(N)nc3c2CCCC3C)c1	10.1021/acs.jmedchem.9b00241
	CHEMBL4452406	177525	0	None	-3	2	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	269	2	1	4	3.2	COc1cccc(-c2nc(N)nc3c2CCCC3C)c1	10.1021/acs.jmedchem.9b00241
	CHEMBL5092267	222134	0	None	-	1	Human	5.6	pEC50	=	5.6	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCC[n+]1c(C)cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc1C	10.1016/j.bmcl.2021.128388
	164609017	191204	0	None	-6	3	Human	5.6	pEC50	=	5.6	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	416	10	4	4	3.2	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CCCc1ccccc1	10.1016/j.ejmech.2021.113190
	CHEMBL4846201	191204	0	None	-6	3	Human	5.6	pEC50	=	5.6	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	416	10	4	4	3.2	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CCCc1ccccc1	10.1016/j.ejmech.2021.113190
	CHEMBL5093461	222332	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL		None	None	None		CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2nnc(N)s2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1016/j.bmcl.2021.128388
	CHEMBL5095884	222332	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL		None	None	None		CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2nnc(N)s2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1016/j.bmcl.2021.128388
	164617783	191369	0	None	-2	3	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	388	8	4	4	2.8	CCC(CNC(=O)/N=C(\N)NCCCc1sc(N)nc1C)c1ccccc1	10.1016/j.ejmech.2021.113190
	CHEMBL4848815	191369	0	None	-2	3	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	388	8	4	4	2.8	CCC(CNC(=O)/N=C(\N)NCCCc1sc(N)nc1C)c1ccccc1	10.1016/j.ejmech.2021.113190
	46887078	15776	0	None	-	1	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay	ChEMBL	359	7	4	5	2.8	Cc1nc(N)sc1CCCNC(=N)NC(=O)C[C@H](C)c1ccccc1	10.1016/j.bmcl.2010.03.082
	CHEMBL1098442	15776	0	None	-	1	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay	ChEMBL	359	7	4	5	2.8	Cc1nc(N)sc1CCCNC(=N)NC(=O)C[C@H](C)c1ccccc1	10.1016/j.bmcl.2010.03.082
	46887115	15283	0	None	47	3	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay	ChEMBL	365	7	4	5	3.2	Cc1nc(N)sc1CCCNC(=N)NC(=O)C[C@H](C)C1CCCCC1	10.1016/j.bmcl.2010.03.082
	CHEMBL1094144	15283	0	None	47	3	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay	ChEMBL	365	7	4	5	3.2	Cc1nc(N)sc1CCCNC(=N)NC(=O)C[C@H](C)C1CCCCC1	10.1016/j.bmcl.2010.03.082
	164617783	191369	0	None	-2	3	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	388	8	4	4	2.8	CCC(CNC(=O)/N=C(\N)NCCCc1sc(N)nc1C)c1ccccc1	10.1016/j.ejmech.2021.113190
	CHEMBL4848815	191369	0	None	-2	3	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	388	8	4	4	2.8	CCC(CNC(=O)/N=C(\N)NCCCc1sc(N)nc1C)c1ccccc1	10.1016/j.ejmech.2021.113190
	164611342	191867	0	None	-1	3	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	346	6	4	4	1.8	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCc1ccccc1	10.1016/j.ejmech.2021.113190
	CHEMBL4856005	191867	0	None	-1	3	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	346	6	4	4	1.8	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCc1ccccc1	10.1016/j.ejmech.2021.113190
	164620704	192862	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	416	8	4	4	3.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)c1ccc(C(C)C)cc1	10.1016/j.ejmech.2021.113190
	CHEMBL4871482	192862	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	416	8	4	4	3.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)c1ccc(C(C)C)cc1	10.1016/j.ejmech.2021.113190
	168295541	199819	0	None	14	2	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	347	6	4	5	1.4	C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5208845	199819	0	None	14	2	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	347	6	4	5	1.4	C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222926	199819	0	None	14	2	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	347	6	4	5	1.4	C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1	10.1021/acs.jmedchem.1c00692
	168286426	199705	0	None	5	2	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	403	10	4	5	2.3	CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5198795	199705	0	None	5	2	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	403	10	4	5	2.3	CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222241	199705	0	None	5	2	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	403	10	4	5	2.3	CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	1269	6909	41	None	-67	6	Human	5.5	pEC50	=	5.5	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	125	2	2	2	0.2	Cc1c(CCN)nc[nH]1	10.1021/jm900526h
	37463	6909	41	None	-67	6	Human	5.5	pEC50	=	5.5	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	125	2	2	2	0.2	Cc1c(CCN)nc[nH]1	10.1021/jm900526h
	CHEMBL275443	6909	41	None	-67	6	Human	5.5	pEC50	=	5.5	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	125	2	2	2	0.2	Cc1c(CCN)nc[nH]1	10.1021/jm900526h
	164624107	192501	0	None	8	3	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	402	9	4	4	2.8	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CCc1ccccc1	10.1016/j.ejmech.2021.113190
	CHEMBL4865765	192501	0	None	8	3	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	402	9	4	4	2.8	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CCc1ccccc1	10.1016/j.ejmech.2021.113190
	168295528	199810	0	None	31	9	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	333	6	4	5	0.9	N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5206565	199810	0	None	31	9	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	333	6	4	5	0.9	N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222872	199810	0	None	31	9	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	333	6	4	5	0.9	N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	56954129	88848	0	None	-	1	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	536	15	6	8	1.5	N/C(=N\C(=O)CCCCCCC(=O)/N=C(\N)NCCCc1cnc(N)s1)NCCCc1cnc(N)s1	10.1021/jm201128q
	CHEMBL2165636	88848	0	None	-	1	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	536	15	6	8	1.5	N/C(=N\C(=O)CCCCCCC(=O)/N=C(\N)NCCCc1cnc(N)s1)NCCCc1cnc(N)s1	10.1021/jm201128q
	164614645	191911	0	None	-	1	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	402	8	4	4	3.0	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(c1ccccc1)C(C)C	10.1016/j.ejmech.2021.113190
	CHEMBL4856572	191911	0	None	-	1	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	402	8	4	4	3.0	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(c1ccccc1)C(C)C	10.1016/j.ejmech.2021.113190
	164610892	191977	0	None	4	3	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	394	8	4	4	3.2	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CC1CCCCC1	10.1016/j.ejmech.2021.113190
	CHEMBL4857560	191977	0	None	4	3	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	394	8	4	4	3.2	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CC1CCCCC1	10.1016/j.ejmech.2021.113190
	155565842	182395	0	None	-5	2	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	317	1	1	3	3.9	CC1CCCc2c(-c3cccc(Br)c3)nc(N)nc21	10.1021/acs.jmedchem.9b00241
	CHEMBL4580450	182395	0	None	-5	2	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	317	1	1	3	3.9	CC1CCCc2c(-c3cccc(Br)c3)nc(N)nc21	10.1021/acs.jmedchem.9b00241
	1269	6909	41	None	-67	6	Human	5.5	pEC50	=	5.5	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assay	ChEMBL	125	2	2	2	0.2	Cc1c(CCN)nc[nH]1	10.1016/j.bmcl.2010.10.041
	37463	6909	41	None	-67	6	Human	5.5	pEC50	=	5.5	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assay	ChEMBL	125	2	2	2	0.2	Cc1c(CCN)nc[nH]1	10.1016/j.bmcl.2010.10.041
	CHEMBL275443	6909	41	None	-67	6	Human	5.5	pEC50	=	5.5	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assay	ChEMBL	125	2	2	2	0.2	Cc1c(CCN)nc[nH]1	10.1016/j.bmcl.2010.10.041
	168290235	199747	0	None	9	9	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	315	6	4	3	1.1	C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5201074	199747	0	None	9	9	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	315	6	4	3	1.1	C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222491	199747	0	None	9	9	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	315	6	4	3	1.1	C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5094083	222246	0	None	-	1	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL		None	None	None		C=C(/N=C(\C)NCCCc1nnc(N)s1)NCCCCCCCCN	10.1016/j.bmcl.2021.128388
	164627020	193187	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	422	7	4	4	3.4	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(c1ccccc1)c1ccccc1	10.1016/j.ejmech.2021.113190
	CHEMBL4876025	193187	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	422	7	4	4	3.4	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(c1ccccc1)c1ccccc1	10.1016/j.ejmech.2021.113190
	CHEMBL5075713	222308	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL		None	None	None		CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2c[nH]cn2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1016/j.bmcl.2021.128388
	CHEMBL5095559	222308	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL		None	None	None		CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2c[nH]cn2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1016/j.bmcl.2021.128388
	CHEMBL5093461	222332	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitment	ChEMBL		None	None	None		CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2nnc(N)s2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1016/j.bmcl.2021.128388
	CHEMBL5095884	222332	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitment	ChEMBL		None	None	None		CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2nnc(N)s2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1016/j.bmcl.2021.128388
	CHEMBL5083588	222313	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	CHEMBL5095633	222313	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	164610421	192039	0	None	-	1	Human	5.5	pEC50	=	5.5	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	332	5	4	4	2.1	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)Nc1ccccc1	10.1016/j.ejmech.2021.113190
	CHEMBL4858567	192039	0	None	-	1	Human	5.5	pEC50	=	5.5	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	332	5	4	4	2.1	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)Nc1ccccc1	10.1016/j.ejmech.2021.113190
	168273640	199584	0	None	4	3	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL	568	15	8	10	-0.1	N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5176229	199584	0	None	4	3	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL	568	15	8	10	-0.1	N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221444	199584	0	None	4	3	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL	568	15	8	10	-0.1	N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	164620704	192862	0	None	-	1	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	416	8	4	4	3.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)c1ccc(C(C)C)cc1	10.1016/j.ejmech.2021.113190
	CHEMBL4871482	192862	0	None	-	1	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	416	8	4	4	3.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)c1ccc(C(C)C)cc1	10.1016/j.ejmech.2021.113190
	164624107	192501	0	None	8	3	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	402	9	4	4	2.8	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CCc1ccccc1	10.1016/j.ejmech.2021.113190
	CHEMBL4865765	192501	0	None	8	3	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	402	9	4	4	2.8	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CCc1ccccc1	10.1016/j.ejmech.2021.113190
	155567151	182631	0	None	-1	2	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	245	1	1	3	3.5	CC1CCCc2c1nc(N)nc2C1CCCCC1	10.1021/acs.jmedchem.9b00241
	CHEMBL4585616	182631	0	None	-1	2	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	245	1	1	3	3.5	CC1CCCc2c1nc(N)nc2C1CCCCC1	10.1021/acs.jmedchem.9b00241
	155567151	182631	0	None	-1	2	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	245	1	1	3	3.5	CC1CCCc2c1nc(N)nc2C1CCCCC1	10.1021/acs.jmedchem.9b00241
	CHEMBL4585616	182631	0	None	-1	2	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	245	1	1	3	3.5	CC1CCCc2c1nc(N)nc2C1CCCCC1	10.1021/acs.jmedchem.9b00241
	164616851	191729	0	None	-2	3	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	376	6	4	4	2.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=S)N[C@H](C)c1ccccc1	10.1016/j.ejmech.2021.113190
	CHEMBL4853772	191729	0	None	-2	3	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	376	6	4	4	2.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=S)N[C@H](C)c1ccccc1	10.1016/j.ejmech.2021.113190
	164614549	191722	0	None	-2	3	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	340	9	4	4	2.2	CCCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1016/j.ejmech.2021.113190
	CHEMBL4853668	191722	0	None	-2	3	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	340	9	4	4	2.2	CCCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1016/j.ejmech.2021.113190
	44482300	12565	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	342	9	4	2	2.0	NC(=O)/N=C(/NCCCCc1ccccc1)NCCCc1c[nH]cn1	10.1021/jm900526h
	CHEMBL1078746	12565	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	342	9	4	2	2.0	NC(=O)/N=C(/NCCCCc1ccccc1)NCCCc1c[nH]cn1	10.1021/jm900526h
	1204	8713	119	None	-181	11	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	1247	8713	119	None	-181	11	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	1375	8713	119	None	-181	11	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	774	8713	119	None	-181	11	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	CHEMBL90	8713	119	None	-181	11	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	DB05381	8713	119	None	-181	11	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	1204	8713	119	None	-181	11	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.ejmech.2021.113190
	1247	8713	119	None	-181	11	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.ejmech.2021.113190
	1375	8713	119	None	-181	11	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.ejmech.2021.113190
	774	8713	119	None	-181	11	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.ejmech.2021.113190
	CHEMBL90	8713	119	None	-181	11	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.ejmech.2021.113190
	DB05381	8713	119	None	-181	11	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.ejmech.2021.113190
	1204	8713	119	None	-181	11	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.1c00692
	1247	8713	119	None	-181	11	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.1c00692
	1375	8713	119	None	-181	11	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.1c00692
	774	8713	119	None	-181	11	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.1c00692
	CHEMBL90	8713	119	None	-181	11	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.1c00692
	DB05381	8713	119	None	-181	11	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.1c00692
	164628701	193246	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	338	5	4	4	1.9	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC1CCCCC1	10.1016/j.ejmech.2021.113190
	CHEMBL4876743	193246	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	338	5	4	4	1.9	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC1CCCCC1	10.1016/j.ejmech.2021.113190
	CHEMBL5087637	222334	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	CHEMBL5095891	222334	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	44481487	12879	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	302	7	3	3	2.3	N#C/N=C(/NCCCC1CCCCC1)NCCc1c[nH]cn1	10.1021/jm900526h
	CHEMBL1080772	12879	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	302	7	3	3	2.3	N#C/N=C(/NCCCC1CCCCC1)NCCc1c[nH]cn1	10.1021/jm900526h
	59868	100929	60	None	-	1	Human	4.4	pEC50	=	4.4	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	211	3	2	4	1.6	CCCN[C@@H]1CCc2nc(N)sc2C1	10.1016/j.ejmech.2021.113190
	CHEMBL249420	100929	60	None	-	1	Human	4.4	pEC50	=	4.4	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	211	3	2	4	1.6	CCCN[C@@H]1CCc2nc(N)sc2C1	10.1016/j.ejmech.2021.113190
	168273745	199587	0	None	4	3	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	332	6	4	4	1.5	N/C(=N\C(=O)NCc1ccccc1)NCCCc1cnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5178472	199587	0	None	4	3	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	332	6	4	4	1.5	N/C(=N\C(=O)NCc1ccccc1)NCCCc1cnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221451	199587	0	None	4	3	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	332	6	4	4	1.5	N/C(=N\C(=O)NCc1ccccc1)NCCCc1cnc(N)s1	10.1021/acs.jmedchem.1c00692
	168273640	199584	0	None	4	3	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	568	15	8	10	-0.1	N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5176229	199584	0	None	4	3	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	568	15	8	10	-0.1	N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221444	199584	0	None	4	3	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	568	15	8	10	-0.1	N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5075713	222308	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitment	ChEMBL		None	None	None		CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2c[nH]cn2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1016/j.bmcl.2021.128388
	CHEMBL5095559	222308	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitment	ChEMBL		None	None	None		CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2c[nH]cn2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1016/j.bmcl.2021.128388
	44482299	12509	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	328	8	4	2	1.6	NC(=O)/N=C(/NCCCc1ccccc1)NCCCc1c[nH]cn1	10.1021/jm900526h
	CHEMBL1078359	12509	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	328	8	4	2	1.6	NC(=O)/N=C(/NCCCc1ccccc1)NCCCc1c[nH]cn1	10.1021/jm900526h
	164627774	193344	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	344	3	4	4	1.4	N/C(=N\C(=O)NCc1ccccc1)NC1CCc2nc(N)sc2C1	10.1016/j.ejmech.2021.113190
	CHEMBL4878215	193344	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	344	3	4	4	1.4	N/C(=N\C(=O)NCc1ccccc1)NC1CCc2nc(N)sc2C1	10.1016/j.ejmech.2021.113190
	56953998	88843	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	578	16	6	8	2.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1021/jm201128q
	CHEMBL2165631	88843	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	578	16	6	8	2.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1021/jm201128q
	164622190	192395	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	360	7	4	4	1.8	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCc1ccccc1	10.1016/j.ejmech.2021.113190
	CHEMBL4864067	192395	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	360	7	4	4	1.8	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCc1ccccc1	10.1016/j.ejmech.2021.113190
	164609729	191877	0	None	-2	3	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	360	6	4	4	2.3	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)N[C@H](C)c1ccccc1	10.1016/j.ejmech.2021.113190
	CHEMBL4856059	191877	0	None	-2	3	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	360	6	4	4	2.3	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)N[C@H](C)c1ccccc1	10.1016/j.ejmech.2021.113190
	56953889	88842	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	564	15	6	8	2.1	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1021/jm201128q
	CHEMBL2165630	88842	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	564	15	6	8	2.1	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1021/jm201128q
	168273745	199587	0	None	4	3	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	332	6	4	4	1.5	N/C(=N\C(=O)NCc1ccccc1)NCCCc1cnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5178472	199587	0	None	4	3	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	332	6	4	4	1.5	N/C(=N\C(=O)NCc1ccccc1)NCCCc1cnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221451	199587	0	None	4	3	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	332	6	4	4	1.5	N/C(=N\C(=O)NCc1ccccc1)NCCCc1cnc(N)s1	10.1021/acs.jmedchem.1c00692
	168294767	199798	0	None	40	10	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	313	8	4	5	0.9	CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5207281	199798	0	None	40	10	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	313	8	4	5	0.9	CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222802	199798	0	None	40	10	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	313	8	4	5	0.9	CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	46887076	15730	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay	ChEMBL	359	7	4	5	2.8	Cc1nc(N)sc1CCCNC(=N)NC(=O)CC(C)c1ccccc1	10.1016/j.bmcl.2010.03.082
	CHEMBL1098110	15730	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay	ChEMBL	359	7	4	5	2.8	Cc1nc(N)sc1CCCNC(=N)NC(=O)CC(C)c1ccccc1	10.1016/j.bmcl.2010.03.082
	CHEMBL5094663	222285	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](C)c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	CHEMBL5094663	222285	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitment	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](C)c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	155542256	179863	0	None	-1	2	Human	5.3	pEC50	=	5.3	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	257	5	1	4	3.1	CCCCc1cc(-c2ccc(OC)cc2)nc(N)n1	10.1021/acs.jmedchem.9b00241
	CHEMBL4519923	179863	0	None	-1	2	Human	5.3	pEC50	=	5.3	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	257	5	1	4	3.1	CCCCc1cc(-c2ccc(OC)cc2)nc(N)n1	10.1021/acs.jmedchem.9b00241
	168297879	199127	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at histamine H2 receptor (unknown origin)Agonist activity at histamine H2 receptor (unknown origin)	ChEMBL	640	18	5	9	4.9	CCOC(=O)C1=C(C)NC(CSCCCCCNC(=N)NCCCc2ccc[nH]2)=C(C(=O)OCC)C1c1cccc([N+](=O)[O-])c1	10.1016/j.bmc.2022.116706
	CHEMBL5207008	199127	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at histamine H2 receptor (unknown origin)Agonist activity at histamine H2 receptor (unknown origin)	ChEMBL	640	18	5	9	4.9	CCOC(=O)C1=C(C)NC(CSCCCCCNC(=N)NCCCc2ccc[nH]2)=C(C(=O)OCC)C1c1cccc([N+](=O)[O-])c1	10.1016/j.bmc.2022.116706
	164610421	192039	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	332	5	4	4	2.1	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)Nc1ccccc1	10.1016/j.ejmech.2021.113190
	CHEMBL4858567	192039	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	332	5	4	4	2.1	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)Nc1ccccc1	10.1016/j.ejmech.2021.113190
	155542256	179863	0	None	-1	2	Human	5.3	pEC50	=	5.3	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	257	5	1	4	3.1	CCCCc1cc(-c2ccc(OC)cc2)nc(N)n1	10.1021/acs.jmedchem.9b00241
	CHEMBL4519923	179863	0	None	-1	2	Human	5.3	pEC50	=	5.3	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	257	5	1	4	3.1	CCCCc1cc(-c2ccc(OC)cc2)nc(N)n1	10.1021/acs.jmedchem.9b00241
	155544839	181722	0	None	2	2	Human	5.3	pEC50	=	5.3	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	284	2	1	5	3.1	CC1CCCc2c(-c3ccc([N+](=O)[O-])cc3)nc(N)nc21	10.1021/acs.jmedchem.9b00241
	CHEMBL4565419	181722	0	None	2	2	Human	5.3	pEC50	=	5.3	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	284	2	1	5	3.1	CC1CCCc2c(-c3ccc([N+](=O)[O-])cc3)nc(N)nc21	10.1021/acs.jmedchem.9b00241
	46887077	15775	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay	ChEMBL	359	7	4	5	2.8	Cc1nc(N)sc1CCCNC(=N)NC(=O)C[C@@H](C)c1ccccc1	10.1016/j.bmcl.2010.03.082
	CHEMBL1098441	15775	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay	ChEMBL	359	7	4	5	2.8	Cc1nc(N)sc1CCCNC(=N)NC(=O)C[C@@H](C)c1ccccc1	10.1016/j.bmcl.2010.03.082
	155544839	181722	0	None	2	2	Human	5.3	pEC50	=	5.3	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	284	2	1	5	3.1	CC1CCCc2c(-c3ccc([N+](=O)[O-])cc3)nc(N)nc21	10.1021/acs.jmedchem.9b00241
	CHEMBL4565419	181722	0	None	2	2	Human	5.3	pEC50	=	5.3	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	284	2	1	5	3.1	CC1CCCc2c(-c3ccc([N+](=O)[O-])cc3)nc(N)nc21	10.1021/acs.jmedchem.9b00241
	1204	8713	119	None	-181	11	Human	5.3	pEC50	=	5.3	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitment	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	1247	8713	119	None	-181	11	Human	5.3	pEC50	=	5.3	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitment	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	1375	8713	119	None	-181	11	Human	5.3	pEC50	=	5.3	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitment	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	774	8713	119	None	-181	11	Human	5.3	pEC50	=	5.3	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitment	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	CHEMBL90	8713	119	None	-181	11	Human	5.3	pEC50	=	5.3	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitment	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	DB05381	8713	119	None	-181	11	Human	5.3	pEC50	=	5.3	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitment	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	56954320	88854	0	None	-13	3	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	472	15	6	4	0.9	N/C(=N\C(=O)CCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1	10.1021/jm201128q
	CHEMBL2165641	88854	0	None	-13	3	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	472	15	6	4	0.9	N/C(=N\C(=O)CCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1	10.1021/jm201128q
	168278471	199627	0	None	2	3	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	312	8	4	4	1.5	CCCCCNC(=O)/N=C(\N)NCCCc1cnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5183205	199627	0	None	2	3	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	312	8	4	4	1.5	CCCCCNC(=O)/N=C(\N)NCCCc1cnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221757	199627	0	None	2	3	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	312	8	4	4	1.5	CCCCCNC(=O)/N=C(\N)NCCCc1cnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5087637	222334	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	CHEMBL5095891	222334	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	56953887	88860	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	536	13	6	8	1.4	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1021/jm201128q
	CHEMBL2165647	88860	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	536	13	6	8	1.4	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1021/jm201128q
	168278471	199627	0	None	2	3	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	312	8	4	4	1.5	CCCCCNC(=O)/N=C(\N)NCCCc1cnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5183205	199627	0	None	2	3	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	312	8	4	4	1.5	CCCCCNC(=O)/N=C(\N)NCCCc1cnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221757	199627	0	None	2	3	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	312	8	4	4	1.5	CCCCCNC(=O)/N=C(\N)NCCCc1cnc(N)s1	10.1021/acs.jmedchem.1c00692
	168290815	199752	0	None	10	2	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	327	9	4	5	1.2	CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5200771	199752	0	None	10	2	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	327	9	4	5	1.2	CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222529	199752	0	None	10	2	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	327	9	4	5	1.2	CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	56954322	88855	0	None	-3	3	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	500	17	6	4	1.7	N/C(=N\C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1	10.1021/jm201128q
	CHEMBL2165642	88855	0	None	-3	3	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	500	17	6	4	1.7	N/C(=N\C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1	10.1021/jm201128q
	46887043	15535	0	None	-1	4	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay	ChEMBL	319	7	4	3	2.6	C[C@@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)C1CCCCC1	10.1016/j.bmcl.2010.03.082
	CHEMBL1096431	15535	0	None	-1	4	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay	ChEMBL	319	7	4	3	2.6	C[C@@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)C1CCCCC1	10.1016/j.bmcl.2010.03.082
	164611757	191682	0	None	3	3	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	402	8	4	4	2.8	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1	10.1016/j.ejmech.2021.113190
	CHEMBL4853107	191682	0	None	3	3	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	402	8	4	4	2.8	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1	10.1016/j.ejmech.2021.113190
	168268853	199564	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	389	8	4	5	1.9	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5180504	199564	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	389	8	4	5	1.9	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221353	199564	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	389	8	4	5	1.9	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5083588	222313	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitment	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	CHEMBL5095633	222313	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitment	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	25149712	185765	0	None	-25	3	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assay	ChEMBL	299	7	4	3	1.6	N=C(NCCCc1c[nH]cn1)NC(=O)CCc1ccccc1	10.1016/j.bmcl.2010.10.041
	CHEMBL470790	185765	0	None	-25	3	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assay	ChEMBL	299	7	4	3	1.6	N=C(NCCCc1c[nH]cn1)NC(=O)CCc1ccccc1	10.1016/j.bmcl.2010.10.041
	25149335	191004	0	None	-26	3	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assay	ChEMBL	313	7	3	2	2.0	CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1	10.1016/j.bmcl.2010.10.041
	CHEMBL483406	191004	0	None	-26	3	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assay	ChEMBL	313	7	3	2	2.0	CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1	10.1016/j.bmcl.2010.10.041
	CHEMBL5093461	222332	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitment	ChEMBL		None	None	None		CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2nnc(N)s2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1016/j.bmcl.2021.128388
	CHEMBL5095884	222332	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitment	ChEMBL		None	None	None		CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2nnc(N)s2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1016/j.bmcl.2021.128388
	164626153	193157	0	None	1	3	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	378	6	4	4	2.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1cccc(F)c1	10.1016/j.ejmech.2021.113190
	CHEMBL4875600	193157	0	None	1	3	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	378	6	4	4	2.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1cccc(F)c1	10.1016/j.ejmech.2021.113190
	44482299	12509	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	328	8	4	2	1.6	NC(=O)/N=C(/NCCCc1ccccc1)NCCCc1c[nH]cn1	10.1021/jm900526h
	CHEMBL1078359	12509	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	328	8	4	2	1.6	NC(=O)/N=C(/NCCCc1ccccc1)NCCCc1c[nH]cn1	10.1021/jm900526h
	1204	8713	119	None	-181	11	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human H2 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H2 receptor expressed in 293-EBNA cells by luciferase reporter gene assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm0603318
	1247	8713	119	None	-181	11	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human H2 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H2 receptor expressed in 293-EBNA cells by luciferase reporter gene assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm0603318
	1375	8713	119	None	-181	11	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human H2 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H2 receptor expressed in 293-EBNA cells by luciferase reporter gene assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm0603318
	774	8713	119	None	-181	11	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human H2 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H2 receptor expressed in 293-EBNA cells by luciferase reporter gene assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm0603318
	CHEMBL90	8713	119	None	-181	11	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human H2 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H2 receptor expressed in 293-EBNA cells by luciferase reporter gene assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm0603318
	DB05381	8713	119	None	-181	11	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human H2 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H2 receptor expressed in 293-EBNA cells by luciferase reporter gene assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm0603318
	CHEMBL5076746	222304	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(N)(=O)=O)c3ccccc3C2(C)C)c2cc(S(=O)(=O)[O-])ccc2C1(C)C	10.1016/j.bmcl.2021.128388
	CHEMBL5095519	222304	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(N)(=O)=O)c3ccccc3C2(C)C)c2cc(S(=O)(=O)[O-])ccc2C1(C)C	10.1016/j.bmcl.2021.128388
	CHEMBL5088914	222341	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	CHEMBL5095949	222341	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	CHEMBL5085542	221751	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCC[n+]1c(C)cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc1C	10.1016/j.bmcl.2021.128388
	CHEMBL5092102	222125	0	None	-	1	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitment	ChEMBL		None	None	None		NCCCCCCCCNC(=O)/N=C(\N)NCCCc1c[nH]cn1	10.1016/j.bmcl.2021.128388
	CHEMBL5094083	222246	0	None	-	1	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitment	ChEMBL		None	None	None		C=C(/N=C(\C)NCCCc1nnc(N)s1)NCCCCCCCCN	10.1016/j.bmcl.2021.128388
	56954515	88840	0	None	-2	3	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	546	17	6	6	2.3	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1	10.1021/jm201128q
	CHEMBL2165628	88840	0	None	-2	3	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	546	17	6	6	2.3	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1	10.1021/jm201128q
	56954000	88844	0	None	-	1	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	592	17	6	8	2.9	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1021/jm201128q
	CHEMBL2165632	88844	0	None	-	1	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	592	17	6	8	2.9	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1021/jm201128q
	CHEMBL5078202	222315	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1	10.1016/j.bmcl.2021.128388
	CHEMBL5095695	222315	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1	10.1016/j.bmcl.2021.128388
	44480707	12535	0	None	-5	2	Human	5.1	pEC50	=	5.1	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	328	8	3	4	2.2	N#C/N=C(/NCCCc1c[nH]cn1)NCCSc1ccccc1	10.1021/jm900526h
	CHEMBL1078529	12535	0	None	-5	2	Human	5.1	pEC50	=	5.1	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	328	8	3	4	2.2	N#C/N=C(/NCCCc1c[nH]cn1)NCCSc1ccccc1	10.1021/jm900526h
	168281746	199661	0	None	77	2	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	365	6	4	5	1.6	CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1	10.1021/acs.jmedchem.1c00692
	CHEMBL5184911	199661	0	None	77	2	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	365	6	4	5	1.6	CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221974	199661	0	None	77	2	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	365	6	4	5	1.6	CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1	10.1021/acs.jmedchem.1c00692
	155525816	177833	0	None	7	2	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	257	1	1	3	3.3	CC1CCCc2c(-c3ccc(F)cc3)nc(N)nc21	10.1021/acs.jmedchem.9b00241
	CHEMBL4456972	177833	0	None	7	2	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	257	1	1	3	3.3	CC1CCCc2c(-c3ccc(F)cc3)nc(N)nc21	10.1021/acs.jmedchem.9b00241
	CHEMBL5077939	222320	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)O)c3ccccc3C2(C)C)c2cc(S(=O)(=O)[O-])ccc2C1(C)C	10.1016/j.bmcl.2021.128388
	CHEMBL5095769	222320	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)O)c3ccccc3C2(C)C)c2cc(S(=O)(=O)[O-])ccc2C1(C)C	10.1016/j.bmcl.2021.128388
	168292954	199776	0	None	7	3	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	388	8	4	4	2.5	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5202592	199776	0	None	7	3	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	388	8	4	4	2.5	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222660	199776	0	None	7	3	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	388	8	4	4	2.5	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
	155553964	182236	0	None	11	2	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	273	1	1	3	3.8	CC1CCCc2c(-c3ccc(Cl)cc3)nc(N)nc21	10.1021/acs.jmedchem.9b00241
	CHEMBL4576986	182236	0	None	11	2	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	273	1	1	3	3.8	CC1CCCc2c(-c3ccc(Cl)cc3)nc(N)nc21	10.1021/acs.jmedchem.9b00241
	46830167	15533	0	None	-42	4	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay	ChEMBL	313	7	4	3	2.2	C[C@@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)c1ccccc1	10.1016/j.bmcl.2010.03.082
	CHEMBL1096429	15533	0	None	-42	4	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay	ChEMBL	313	7	4	3	2.2	C[C@@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)c1ccccc1	10.1016/j.bmcl.2010.03.082
	25149521	185831	0	None	-9	2	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assay	ChEMBL	375	8	4	3	3.2	N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1ccccc1	10.1016/j.bmcl.2010.10.041
	CHEMBL471413	185831	0	None	-9	2	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assay	ChEMBL	375	8	4	3	3.2	N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1ccccc1	10.1016/j.bmcl.2010.10.041
	168281746	199661	0	None	77	2	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	365	6	4	5	1.6	CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1	10.1021/acs.jmedchem.1c00692
	CHEMBL5184911	199661	0	None	77	2	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	365	6	4	5	1.6	CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221974	199661	0	None	77	2	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	365	6	4	5	1.6	CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1	10.1021/acs.jmedchem.1c00692
	155525816	177833	0	None	7	2	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	257	1	1	3	3.3	CC1CCCc2c(-c3ccc(F)cc3)nc(N)nc21	10.1021/acs.jmedchem.9b00241
	CHEMBL4456972	177833	0	None	7	2	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	257	1	1	3	3.3	CC1CCCc2c(-c3ccc(F)cc3)nc(N)nc21	10.1021/acs.jmedchem.9b00241
	155553964	182236	0	None	11	2	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	273	1	1	3	3.8	CC1CCCc2c(-c3ccc(Cl)cc3)nc(N)nc21	10.1021/acs.jmedchem.9b00241
	CHEMBL4576986	182236	0	None	11	2	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	273	1	1	3	3.8	CC1CCCc2c(-c3ccc(Cl)cc3)nc(N)nc21	10.1021/acs.jmedchem.9b00241
	155565842	182395	0	None	-5	2	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	317	1	1	3	3.9	CC1CCCc2c(-c3cccc(Br)c3)nc(N)nc21	10.1021/acs.jmedchem.9b00241
	CHEMBL4580450	182395	0	None	-5	2	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	317	1	1	3	3.9	CC1CCCc2c(-c3cccc(Br)c3)nc(N)nc21	10.1021/acs.jmedchem.9b00241
	164614549	191722	0	None	-2	3	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	340	9	4	4	2.2	CCCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1016/j.ejmech.2021.113190
	CHEMBL4853668	191722	0	None	-2	3	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	340	9	4	4	2.2	CCCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1016/j.ejmech.2021.113190
	59868	100929	60	None	-	1	Human	5.1	pEC50	=	5.1	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	211	3	2	4	1.6	CCCN[C@@H]1CCc2nc(N)sc2C1	10.1016/j.ejmech.2021.113190
	CHEMBL249420	100929	60	None	-	1	Human	5.1	pEC50	=	5.1	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	211	3	2	4	1.6	CCCN[C@@H]1CCc2nc(N)sc2C1	10.1016/j.ejmech.2021.113190
	155532722	178564	0	None	3	2	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	253	1	1	3	3.5	Cc1ccc(-c2nc(N)nc3c2CCCC3C)cc1	10.1021/acs.jmedchem.9b00241
	CHEMBL4467878	178564	0	None	3	2	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	253	1	1	3	3.5	Cc1ccc(-c2nc(N)nc3c2CCCC3C)cc1	10.1021/acs.jmedchem.9b00241
	CHEMBL5090859	222062	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCCC[n+]1c(C)cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc1C	10.1016/j.bmcl.2021.128388
	155532722	178564	0	None	3	2	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	253	1	1	3	3.5	Cc1ccc(-c2nc(N)nc3c2CCCC3C)cc1	10.1021/acs.jmedchem.9b00241
	CHEMBL4467878	178564	0	None	3	2	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	253	1	1	3	3.5	Cc1ccc(-c2nc(N)nc3c2CCCC3C)cc1	10.1021/acs.jmedchem.9b00241
	44481758	12486	0	None	-	1	Human	5.1	pEC50	=	5.1	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	324	9	3	3	2.4	N#C/N=C(\NCCCCc1ccccc1)NCCCc1c[nH]cn1	10.1021/jm900526h
	CHEMBL1078212	12486	0	None	-	1	Human	5.1	pEC50	=	5.1	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	324	9	3	3	2.4	N#C/N=C(\NCCCCc1ccccc1)NCCCc1c[nH]cn1	10.1021/jm900526h
	46887079	15281	0	None	478	3	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay	ChEMBL	365	7	4	5	3.2	Cc1nc(N)sc1CCCNC(=N)NC(=O)CC(C)C1CCCCC1	10.1016/j.bmcl.2010.03.082
	CHEMBL1094142	15281	0	None	478	3	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay	ChEMBL	365	7	4	5	3.2	Cc1nc(N)sc1CCCNC(=N)NC(=O)CC(C)C1CCCCC1	10.1016/j.bmcl.2010.03.082
	56954229	88850	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	648	23	6	8	4.7	N/C(=N\C(=O)CCCCCCCCCCCCCCC(=O)/N=C(\N)NCCCc1cnc(N)s1)NCCCc1cnc(N)s1	10.1021/jm201128q
	CHEMBL2165638	88850	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	648	23	6	8	4.7	N/C(=N\C(=O)CCCCCCCCCCCCCCC(=O)/N=C(\N)NCCCc1cnc(N)s1)NCCCc1cnc(N)s1	10.1021/jm201128q
	CHEMBL5094083	222246	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL		None	None	None		C=C(/N=C(\C)NCCCc1nnc(N)s1)NCCCCCCCCN	10.1016/j.bmcl.2021.128388
	155559319	181642	0	None	13	2	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	239	1	1	3	3.2	CC1CCCc2c(-c3ccccc3)nc(N)nc21	10.1021/acs.jmedchem.9b00241
	CHEMBL4563363	181642	0	None	13	2	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	239	1	1	3	3.2	CC1CCCc2c(-c3ccccc3)nc(N)nc21	10.1021/acs.jmedchem.9b00241
	1204	8713	119	None	-181	11	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.ejmech.2021.113190
	1247	8713	119	None	-181	11	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.ejmech.2021.113190
	1375	8713	119	None	-181	11	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.ejmech.2021.113190
	774	8713	119	None	-181	11	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.ejmech.2021.113190
	CHEMBL90	8713	119	None	-181	11	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.ejmech.2021.113190
	DB05381	8713	119	None	-181	11	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.ejmech.2021.113190
	44281005	123509	0	None	-	3	Rat	6.0	pKd	=	6	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	787	17	4	8	6.4	Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CCOC(=O)NCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1	10.1016/S0960-894X(96)00249-1
	CHEMBL33743	123509	0	None	-	3	Rat	6.0	pKd	=	6	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	787	17	4	8	6.4	Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CCOC(=O)NCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1	10.1016/S0960-894X(96)00249-1
	CHEMBL432671	174874	0	None	-	3	Rat	6.0	pKd	=	6	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	784	15	7	12	3.1	CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCNC(=O)CC(=O)NCCSCc3csc(C=C(N)N)n3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00249-1
	44280028	105953	0	None	-	3	Rat	6.0	pKd	=	6	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	768	17	6	9	4.3	CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCCCCC(=O)NCCSCc3csc(N=C(N)N)n3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00248-X
	CHEMBL281318	105953	0	None	-	3	Rat	6.0	pKd	=	6	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	768	17	6	9	4.3	CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCCCCC(=O)NCCSCc3csc(N=C(N)N)n3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00248-X
	9896825	109754	0	None	-	3	Rat	6.0	pKd	=	6	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	742	14	6	10	2.9	Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCC(=O)NCCSCc4csc(N=C(N)N)n4)c3)c3ccccc3N(C)C2=O)c1	10.1016/S0960-894X(96)00248-X
	CHEMBL30656	109754	0	None	-	3	Rat	6.0	pKd	=	6	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	742	14	6	10	2.9	Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCC(=O)NCCSCc4csc(N=C(N)N)n4)c3)c3ccccc3N(C)C2=O)c1	10.1016/S0960-894X(96)00248-X
	44281078	106519	0	None	-	3	Rat	5.9	pKd	=	5.9	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	773	16	4	8	5.9	CN1C(=O)[C@H](NC(=O)Nc2cccc(CCOC(=O)NCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00249-1
	CHEMBL284975	106519	0	None	-	3	Rat	5.9	pKd	=	5.9	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	773	16	4	8	5.9	CN1C(=O)[C@H](NC(=O)Nc2cccc(CCOC(=O)NCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00249-1
	44280714	106809	0	None	-	3	Rat	5.9	pKd	=	5.9	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	726	14	6	9	3.2	Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCC(=O)NCCSCc3csc(N=C(N)N)n3)C2=O)c1	10.1016/S0960-894X(96)00248-X
	CHEMBL286908	106809	0	None	-	3	Rat	5.9	pKd	=	5.9	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	726	14	6	9	3.2	Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCC(=O)NCCSCc3csc(N=C(N)N)n3)C2=O)c1	10.1016/S0960-894X(96)00248-X
	44281291	106601	0	None	-	0	Rat	7.8	pKd	=	7.8	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	433	11	2	5	3.9	CC(C)(C)OC(=O)NCCCC(=O)NCCCOc1cccc(CN2CCCCC2)c1	10.1016/S0960-894X(96)00249-1
	CHEMBL285556	106601	0	None	-	0	Rat	7.8	pKd	=	7.8	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	433	11	2	5	3.9	CC(C)(C)OC(=O)NCCCC(=O)NCCCOc1cccc(CN2CCCCC2)c1	10.1016/S0960-894X(96)00249-1
	44281292	121572	0	None	-	3	Rat	6.8	pKd	=	6.8	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	816	17	5	9	5.0	CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCCNC(=O)CC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00249-1
	CHEMBL33398	121572	0	None	-	3	Rat	6.8	pKd	=	6.8	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	816	17	5	9	5.0	CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCCNC(=O)CC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00249-1
	CHEMBL286835	106795	0	None	-	0	Rat	5.7	pKd	=	5.7	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	755	14	6	11	4.5	Cc1cccc(NC(=O)N[C@@H]2N=C(c3cccc(OC(=O)NCCCC(=O)NCCSCc4csc(C=C(N)N)n4)c3)c3ccccc3N(C)C2=O)c1	10.1016/S0960-894X(96)00249-1
	1231	7724	116	None	-	4	Rat	6.6	pKd	=	6.6	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/S0960-894X(96)00249-1
	2756	7724	116	None	-	4	Rat	6.6	pKd	=	6.6	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/S0960-894X(96)00249-1
	645	7724	116	None	-	4	Rat	6.6	pKd	=	6.6	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/S0960-894X(96)00249-1
	CHEMBL30	7724	116	None	-	4	Rat	6.6	pKd	=	6.6	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/S0960-894X(96)00249-1
	DB00501	7724	116	None	-	4	Rat	6.6	pKd	=	6.6	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/S0960-894X(96)00249-1
	44281020	123422	0	None	-	3	Rat	6.6	pKd	=	6.6	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	773	16	4	8	6.2	CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00249-1
	CHEMBL33698	123422	0	None	-	3	Rat	6.6	pKd	=	6.6	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	773	16	4	8	6.2	CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00249-1
	1231	7724	116	None	-	4	Rat	6.6	pKd	=	6.6	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/S0960-894X(96)00248-X
	2756	7724	116	None	-	4	Rat	6.6	pKd	=	6.6	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/S0960-894X(96)00248-X
	645	7724	116	None	-	4	Rat	6.6	pKd	=	6.6	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/S0960-894X(96)00248-X
	CHEMBL30	7724	116	None	-	4	Rat	6.6	pKd	=	6.6	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/S0960-894X(96)00248-X
	DB00501	7724	116	None	-	4	Rat	6.6	pKd	=	6.6	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/S0960-894X(96)00248-X
	44279811	103700	0	None	-	3	Rat	6.6	pKd	=	6.6	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	743	15	4	7	5.3	CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00248-X
	CHEMBL265987	103700	0	None	-	3	Rat	6.6	pKd	=	6.6	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	743	15	4	7	5.3	CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00248-X
	44281204	106626	0	None	-	3	Rat	6.5	pKd	=	6.5	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	871	18	4	10	5.5	CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCCCN3CCN(C(=O)CNCCCOc4cccc(CN5CCCCC5)c4)CC3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00249-1
	CHEMBL285719	106626	0	None	-	3	Rat	6.5	pKd	=	6.5	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	871	18	4	10	5.5	CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCCCN3CCN(C(=O)CNCCCOc4cccc(CN5CCCCC5)c4)CC3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00249-1
	44280741	163341	0	None	-	3	Rat	6.5	pKd	=	6.5	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	759	15	4	8	5.8	CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00249-1
	CHEMBL406844	163341	0	None	-	3	Rat	6.5	pKd	=	6.5	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	759	15	4	8	5.8	CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00249-1
	44280372	106163	0	None	-	3	Rat	6.5	pKd	=	6.5	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	787	17	4	8	5.8	Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1	10.1016/S0960-894X(96)00248-X
	CHEMBL282645	106163	0	None	-	3	Rat	6.5	pKd	=	6.5	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	787	17	4	8	5.8	Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1	10.1016/S0960-894X(96)00248-X
	CHEMBL282175	106097	0	None	-	3	Rat	5.5	pKd	=	5.5	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	769	16	6	11	4.6	Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CCOC(=O)NCCCC(=O)NCCSCc3csc(C=C(N)N)n3)C2=O)c1	10.1016/S0960-894X(96)00249-1
	44280713	106808	0	None	-	3	Rat	5.5	pKd	=	5.5	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	740	15	6	9	3.6	Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCCC(=O)NCCSCc3csc(N=C(N)N)n3)C2=O)c1	10.1016/S0960-894X(96)00248-X
	CHEMBL286907	106808	0	None	-	3	Rat	5.5	pKd	=	5.5	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	740	15	6	9	3.6	Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCCC(=O)NCCSCc3csc(N=C(N)N)n3)C2=O)c1	10.1016/S0960-894X(96)00248-X
	44280740	107183	0	None	-	3	Rat	6.4	pKd	=	6.4	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	787	17	4	8	6.3	CN1C(=O)[C@H](NC(=O)Nc2cccc(CCOC(=O)NCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00249-1
	CHEMBL290122	107183	0	None	-	3	Rat	6.4	pKd	=	6.4	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	787	17	4	8	6.3	CN1C(=O)[C@H](NC(=O)Nc2cccc(CCOC(=O)NCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00249-1
	44280200	107601	0	None	-	3	Rat	6.4	pKd	=	6.4	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	785	18	4	7	6.6	Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1	10.1016/S0960-894X(96)00248-X
	CHEMBL29331	107601	0	None	-	3	Rat	6.4	pKd	=	6.4	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	785	18	4	7	6.6	Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1	10.1016/S0960-894X(96)00248-X
	44279861	109961	0	None	-	3	Rat	6.4	pKd	=	6.4	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	726	14	6	9	3.1	CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCC(=O)NCCSCc3csc(N=C(N)N)n3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00248-X
	CHEMBL30821	109961	0	None	-	3	Rat	6.4	pKd	=	6.4	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	726	14	6	9	3.1	CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCC(=O)NCCSCc3csc(N=C(N)N)n3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00248-X
	44279810	110621	0	None	-	3	Rat	6.4	pKd	=	6.4	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	757	16	4	7	5.7	CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00248-X
	CHEMBL30917	110621	0	None	-	3	Rat	6.4	pKd	=	6.4	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	757	16	4	7	5.7	CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00248-X
	44279808	105917	0	None	-	3	Rat	5.4	pKd	=	5.4	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	712	13	6	9	2.9	Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCC(=O)NCCSCc3csc(N=C(N)N)n3)C2=O)c1	10.1016/S0960-894X(96)00248-X
	CHEMBL281082	105917	0	None	-	3	Rat	5.4	pKd	=	5.4	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	712	13	6	9	2.9	Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCC(=O)NCCSCc3csc(N=C(N)N)n3)C2=O)c1	10.1016/S0960-894X(96)00248-X
	135881774	106434	0	None	-	0	Rat	7.3	pKd	=	7.3	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	415	10	4	8	2.0	CC(C)(C)OC(=O)NCCCC(=O)NCCSCc1csc(C=C(N)N)n1	10.1016/S0960-894X(96)00249-1
	CHEMBL284374	106434	0	None	-	0	Rat	7.3	pKd	=	7.3	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	415	10	4	8	2.0	CC(C)(C)OC(=O)NCCCC(=O)NCCSCc1csc(C=C(N)N)n1	10.1016/S0960-894X(96)00249-1
	44281004	106855	0	None	-	3	Rat	6.3	pKd	=	6.3	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	773	15	4	8	6.4	Cc1cccc(NC(=O)N[C@@H]2N=C(c3cccc(OC(=O)NCCCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1	10.1016/S0960-894X(96)00249-1
	CHEMBL287295	106855	0	None	-	3	Rat	6.3	pKd	=	6.3	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	773	15	4	8	6.4	Cc1cccc(NC(=O)N[C@@H]2N=C(c3cccc(OC(=O)NCCCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1	10.1016/S0960-894X(96)00249-1
	44280029	103216	0	None	-	3	Rat	6.3	pKd	=	6.3	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	740	15	6	9	3.5	CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCCC(=O)NCCSCc3csc(N=C(N)N)n3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00248-X
	CHEMBL262125	103216	0	None	-	3	Rat	6.3	pKd	=	6.3	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	740	15	6	9	3.5	CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCCC(=O)NCCSCc3csc(N=C(N)N)n3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00248-X
	44280373	106164	0	None	-	3	Rat	6.3	pKd	=	6.3	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	773	16	4	8	5.4	Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1	10.1016/S0960-894X(96)00248-X
	CHEMBL282646	106164	0	None	-	3	Rat	6.3	pKd	=	6.3	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	773	16	4	8	5.4	Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1	10.1016/S0960-894X(96)00248-X
	44280388	123647	0	None	-	3	Rat	6.3	pKd	=	6.3	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	759	15	4	8	5.0	Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1	10.1016/S0960-894X(96)00248-X
	CHEMBL33819	123647	0	None	-	3	Rat	6.3	pKd	=	6.3	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	759	15	4	8	5.0	Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1	10.1016/S0960-894X(96)00248-X
	44279862	105906	0	None	-	3	Rat	5.3	pKd	=	5.3	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	702	13	3	7	5.9	Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1	10.1016/S0960-894X(96)00248-X
	CHEMBL281017	105906	0	None	-	3	Rat	5.3	pKd	=	5.3	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	702	13	3	7	5.9	Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1	10.1016/S0960-894X(96)00248-X
	44280213	108395	0	None	-	3	Rat	5.3	pKd	=	5.3	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	685	12	5	9	3.7	Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCSCc4csc(N=C(N)N)n4)c3)c3ccccc3N(C)C2=O)c1	10.1016/S0960-894X(96)00248-X
	CHEMBL29888	108395	0	None	-	3	Rat	5.3	pKd	=	5.3	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	685	12	5	9	3.7	Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCSCc4csc(N=C(N)N)n4)c3)c3ccccc3N(C)C2=O)c1	10.1016/S0960-894X(96)00248-X
	44281205	121596	0	None	-	3	Rat	6.2	pKd	=	6.2	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	857	17	4	10	5.1	CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCCN3CCN(C(=O)CNCCCOc4cccc(CN5CCCCC5)c4)CC3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00249-1
	CHEMBL33412	121596	0	None	-	3	Rat	6.2	pKd	=	6.2	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	857	17	4	10	5.1	CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCCN3CCN(C(=O)CNCCCOc4cccc(CN5CCCCC5)c4)CC3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00249-1
	44279809	105743	0	None	-	3	Rat	6.2	pKd	=	6.2	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	785	18	4	7	6.4	CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00248-X
	CHEMBL279778	105743	0	None	-	3	Rat	6.2	pKd	=	6.2	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	785	18	4	7	6.4	CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00248-X
	44280371	109805	0	None	-	3	Rat	6.2	pKd	=	6.2	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	815	19	4	8	6.6	Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCCCCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1	10.1016/S0960-894X(96)00248-X
	CHEMBL30701	109805	0	None	-	3	Rat	6.2	pKd	=	6.2	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	815	19	4	8	6.6	Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCCCCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1	10.1016/S0960-894X(96)00248-X
	44280214	114079	0	None	-	3	Rat	6.2	pKd	=	6.2	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	770	16	6	10	3.6	Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCCC(=O)NCCSCc4csc(N=C(N)N)n4)c3)c3ccccc3N(C)C2=O)c1	10.1016/S0960-894X(96)00248-X
	CHEMBL31726	114079	0	None	-	3	Rat	6.2	pKd	=	6.2	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	770	16	6	10	3.6	Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCCC(=O)NCCSCc4csc(N=C(N)N)n4)c3)c3ccccc3N(C)C2=O)c1	10.1016/S0960-894X(96)00248-X
	44280266	105553	0	None	-	3	Rat	5.2	pKd	=	5.2	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	729	14	4	7	5.0	Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1	10.1016/S0960-894X(96)00248-X
	CHEMBL278217	105553	0	None	-	3	Rat	5.2	pKd	=	5.2	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	729	14	4	7	5.0	Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1	10.1016/S0960-894X(96)00248-X
	44280996	106520	0	None	-	3	Rat	6.1	pKd	=	6.1	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	745	14	4	8	5.4	CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00249-1
	CHEMBL284976	106520	0	None	-	3	Rat	6.1	pKd	=	6.1	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	745	14	4	8	5.4	CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00249-1
	CHEMBL285995	106668	0	None	-	3	Rat	6.1	pKd	=	6.1	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	741	16	6	11	4.5	CN1C(=O)[C@H](NC(=O)Nc2cccc(CCOC(=O)NCCCNCCSCc3csc(C=C(N)N)n3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00249-1
	44280215	106606	0	None	-	3	Rat	6.1	pKd	=	6.1	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	756	15	6	10	3.3	Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCC(=O)NCCSCc4csc(N=C(N)N)n4)c3)c3ccccc3N(C)C2=O)c1	10.1016/S0960-894X(96)00248-X
	CHEMBL285586	106606	0	None	-	3	Rat	6.1	pKd	=	6.1	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	756	15	6	10	3.3	Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCC(=O)NCCSCc4csc(N=C(N)N)n4)c3)c3ccccc3N(C)C2=O)c1	10.1016/S0960-894X(96)00248-X
	44280225	106739	0	None	-	3	Rat	6.1	pKd	=	6.1	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	743	15	4	7	5.4	Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1	10.1016/S0960-894X(96)00248-X
	CHEMBL286475	106739	0	None	-	3	Rat	6.1	pKd	=	6.1	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	743	15	4	7	5.4	Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1	10.1016/S0960-894X(96)00248-X
	44280224	111561	0	None	-	3	Rat	6.1	pKd	=	6.1	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	757	16	4	7	5.8	Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1	10.1016/S0960-894X(96)00248-X
	CHEMBL31090	111561	0	None	-	3	Rat	6.1	pKd	=	6.1	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	757	16	4	7	5.8	Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1	10.1016/S0960-894X(96)00248-X
	54754351	74992	0	None	-	0	Human	5.5	pKi	=	5.5	Functional	Antagonist activity at histamine H2 receptorAntagonist activity at histamine H2 receptor	ChEMBL	277	4	1	5	2.1	CN1CCN(c2cc(NCCC(C)(C)C)ncn2)CC1	10.1016/j.bmcl.2011.07.114
	CHEMBL1915535	74992	0	None	-	0	Human	5.5	pKi	=	5.5	Functional	Antagonist activity at histamine H2 receptorAntagonist activity at histamine H2 receptor	ChEMBL	277	4	1	5	2.1	CN1CCN(c2cc(NCCC(C)(C)C)ncn2)CC1	10.1016/j.bmcl.2011.07.114
	57395620	74991	0	None	-	0	Human	5.1	pKi	=	5.1	Functional	Antagonist activity at histamine H2 receptorAntagonist activity at histamine H2 receptor	ChEMBL	263	5	3	5	2.1	CC(C)(C)CCNc1cc(N[C@H]2CCNC2)ncn1	10.1016/j.bmcl.2011.07.114
	CHEMBL1915534	74991	0	None	-	0	Human	5.1	pKi	=	5.1	Functional	Antagonist activity at histamine H2 receptorAntagonist activity at histamine H2 receptor	ChEMBL	263	5	3	5	2.1	CC(C)(C)CCNc1cc(N[C@H]2CCNC2)ncn1	10.1016/j.bmcl.2011.07.114
	1204	8713	119	None	2	11	Guinea pig	8.2	pEC50	=	8.2	Functional	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	8713	119	None	2	11	Guinea pig	8.2	pEC50	=	8.2	Functional	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	8713	119	None	2	11	Guinea pig	8.2	pEC50	=	8.2	Functional	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	8713	119	None	2	11	Guinea pig	8.2	pEC50	=	8.2	Functional	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	8713	119	None	2	11	Guinea pig	8.2	pEC50	=	8.2	Functional	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	8713	119	None	2	11	Guinea pig	8.2	pEC50	=	8.2	Functional	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	7192	33	None	57	2	Human	6.4	pEC50	=	6.4	Functional	UnclassifiedUnclassified	Guide to Pharmacology	157	2	2	4	0.5	NCCc1sc(nc1C)N	19072936
	4025	7192	33	None	57	2	Human	6.4	pEC50	=	6.4	Functional	UnclassifiedUnclassified	Guide to Pharmacology	157	2	2	4	0.5	NCCc1sc(nc1C)N	19072936
	CHEMBL293762	7192	33	None	57	2	Human	6.4	pEC50	=	6.4	Functional	UnclassifiedUnclassified	Guide to Pharmacology	157	2	2	4	0.5	NCCc1sc(nc1C)N	19072936
	1229	7530	0	None	-	1	Human	5.7	pEC50	None	5.7	Functional	UnclassifiedUnclassified	Guide to Pharmacology	262	5	3	2	2.0	CNC(=S)NCCCCc1cccc2c1cn[nH]2	9681472
	5311293	7530	0	None	-	1	Human	5.7	pEC50	None	5.7	Functional	UnclassifiedUnclassified	Guide to Pharmacology	262	5	3	2	2.0	CNC(=S)NCCCCc1cccc2c1cn[nH]2	9681472
	18381	224486	0	None	1	4	Human	8.3	pIC50	=	8.3	Functional	NoneNone	Drug Central	469	4	2	6	3.2	CC1=C(C(=O)N[C@H]2[C@H]3SC(C)(C)[C@@H](N3C2=O)C(O)=O)C(=NO1)C1=C(Cl)C=CC=C1Cl	None
	30699	224483	0	None	-1	14	Human	8.3	pIC50	=	8.3	Functional	NoneNone	Drug Central	423	7	2	8	0.5	CC(=O)OCC1=C(N2[C@H](SC1)[C@H](NC(=O)CSC1=CC=NC=C1)C2=O)C(O)=O	None
	180	7189	56	None	-100	38	Human	8.2	pIC50	=	8.2	Functional	NoneNone	Drug Central	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	None
	200	7189	56	None	-100	38	Human	8.2	pIC50	=	8.2	Functional	NoneNone	Drug Central	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	None
	2160	7189	56	None	-100	38	Human	8.2	pIC50	=	8.2	Functional	NoneNone	Drug Central	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	None
	CHEMBL629	7189	56	None	-100	38	Human	8.2	pIC50	=	8.2	Functional	NoneNone	Drug Central	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	None
	DB00321	7189	56	None	-100	38	Human	8.2	pIC50	=	8.2	Functional	NoneNone	Drug Central	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	None
	46780481	114308	20	None	-40	15	Human	8.1	pIC50	=	8.1	Functional	NoneNone	Drug Central	285	0	0	2	4.3	CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1	None
	9903970	114308	20	None	-40	15	Human	8.1	pIC50	=	8.1	Functional	NoneNone	Drug Central	285	0	0	2	4.3	CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1	None
	CHEMBL3187365	114308	20	None	-40	15	Human	8.1	pIC50	=	8.1	Functional	NoneNone	Drug Central	285	0	0	2	4.3	CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1	None
	CHEMBL3544974	114308	20	None	-40	15	Human	8.1	pIC50	=	8.1	Functional	NoneNone	Drug Central	285	0	0	2	4.3	CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1	None

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Ligands (move mouse cursor over ligand name to see structure)					Receptor			Assay information							Chemical information
Sel. page	Similar- ity	Common name	GPCRdb ID	#Vendors	Reference ligand	Fold selectivity	# Tested GPCRs	Species	p-value (-log)	Activity Type	Activity Relation	Activity Value	Assay Type	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI
		213	10625	55	None	-12	43	Human	5.0	pAC50	=	5.0	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10625	55	None	-12	43	Human	5.0	pAC50	=	5.0	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10625	55	None	-12	43	Human	5.0	pAC50	=	5.0	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10625	55	None	-12	43	Human	5.0	pAC50	=	5.0	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10625	55	None	-12	43	Human	5.0	pAC50	=	5.0	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10103	96	None	-	6	Human	5.0	pAC50	=	5.0	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10103	96	None	-	6	Human	5.0	pAC50	=	5.0	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10103	96	None	-	6	Human	5.0	pAC50	=	5.0	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10103	96	None	-	6	Human	5.0	pAC50	=	5.0	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10103	96	None	-	6	Human	5.0	pAC50	=	5.0	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9956	33	None	-53	29	Human	7.0	pAC50	=	7.0	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9956	33	None	-53	29	Human	7.0	pAC50	=	7.0	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9956	33	None	-53	29	Human	7.0	pAC50	=	7.0	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9956	33	None	-53	29	Human	7.0	pAC50	=	7.0	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9956	33	None	-53	29	Human	7.0	pAC50	=	7.0	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8692	93	None	-131	85	Human	6.9	pAC50	=	6.9	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8692	93	None	-131	85	Human	6.9	pAC50	=	6.9	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8692	93	None	-131	85	Human	6.9	pAC50	=	6.9	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8692	93	None	-131	85	Human	6.9	pAC50	=	6.9	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8692	93	None	-131	85	Human	6.9	pAC50	=	6.9	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	205458	82	None	-	4	Human	4.9	pAC50	=	4.9	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	205458	82	None	-	4	Human	4.9	pAC50	=	4.9	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	205458	82	None	-	4	Human	4.9	pAC50	=	4.9	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	92710	54	None	-	2	Human	4.9	pAC50	=	4.9	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	92710	54	None	-	2	Human	4.9	pAC50	=	4.9	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	70316	93	None	-	0	Human	5.9	pAC50	=	5.9	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	70316	93	None	-	0	Human	5.9	pAC50	=	5.9	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	212597	75	None	-	3	Human	4.9	pAC50	=	4.9	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	212597	75	None	-	3	Human	4.9	pAC50	=	4.9	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	212597	75	None	-	3	Human	4.9	pAC50	=	4.9	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	96369	85	None	-	0	Human	4.9	pAC50	=	4.9	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	96369	85	None	-	0	Human	4.9	pAC50	=	4.9	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9127	53	None	-10	44	Human	6.9	pAC50	=	6.9	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9127	53	None	-10	44	Human	6.9	pAC50	=	6.9	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9127	53	None	-10	44	Human	6.9	pAC50	=	6.9	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9127	53	None	-10	44	Human	6.9	pAC50	=	6.9	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9127	53	None	-10	44	Human	6.9	pAC50	=	6.9	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9535	49	None	-	16	Human	5.8	pAC50	=	5.8	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9535	49	None	-	16	Human	5.8	pAC50	=	5.8	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9535	49	None	-	16	Human	5.8	pAC50	=	5.8	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9535	49	None	-	16	Human	5.8	pAC50	=	5.8	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9535	49	None	-	16	Human	5.8	pAC50	=	5.8	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10578	47	None	-6	25	Human	6.8	pAC50	=	6.8	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10578	47	None	-6	25	Human	6.8	pAC50	=	6.8	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10578	47	None	-6	25	Human	6.8	pAC50	=	6.8	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10578	47	None	-6	25	Human	6.8	pAC50	=	6.8	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10578	47	None	-6	25	Human	6.8	pAC50	=	6.8	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	62596	55	None	-	1	Human	5.8	pAC50	=	5.8	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	62596	55	None	-	1	Human	5.8	pAC50	=	5.8	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8439	75	None	-	32	Human	5.8	pAC50	=	5.8	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8439	75	None	-	32	Human	5.8	pAC50	=	5.8	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8439	75	None	-	32	Human	5.8	pAC50	=	5.8	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8439	75	None	-	32	Human	5.8	pAC50	=	5.8	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8439	75	None	-	32	Human	5.8	pAC50	=	5.8	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7590	103	None	-	22	Human	5.8	pAC50	=	5.8	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7590	103	None	-	22	Human	5.8	pAC50	=	5.8	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7590	103	None	-	22	Human	5.8	pAC50	=	5.8	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7590	103	None	-	22	Human	5.8	pAC50	=	5.8	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7590	103	None	-	22	Human	5.8	pAC50	=	5.8	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	113858	46	None	-	0	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	113858	46	None	-	0	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7516	40	None	-	35	Human	5.8	pAC50	=	5.8	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7516	40	None	-	35	Human	5.8	pAC50	=	5.8	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7516	40	None	-	35	Human	5.8	pAC50	=	5.8	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7516	40	None	-	35	Human	5.8	pAC50	=	5.8	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7516	40	None	-	35	Human	5.8	pAC50	=	5.8	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7706	68	None	-85	72	Human	6.8	pAC50	=	6.8	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7706	68	None	-85	72	Human	6.8	pAC50	=	6.8	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7706	68	None	-85	72	Human	6.8	pAC50	=	6.8	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7706	68	None	-85	72	Human	6.8	pAC50	=	6.8	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7706	68	None	-85	72	Human	6.8	pAC50	=	6.8	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10551	74	None	-	13	Human	5.8	pAC50	=	5.8	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10551	74	None	-	13	Human	5.8	pAC50	=	5.8	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10551	74	None	-	13	Human	5.8	pAC50	=	5.8	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10551	74	None	-	13	Human	5.8	pAC50	=	5.8	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10551	74	None	-	13	Human	5.8	pAC50	=	5.8	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	11551	101	None	-33	34	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	11551	101	None	-33	34	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10519	78	None	-41	35	Human	5.8	pAC50	=	5.8	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10519	78	None	-41	35	Human	5.8	pAC50	=	5.8	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10519	78	None	-41	35	Human	5.8	pAC50	=	5.8	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10519	78	None	-41	35	Human	5.8	pAC50	=	5.8	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10519	78	None	-41	35	Human	5.8	pAC50	=	5.8	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10519	78	None	-41	35	Human	5.8	pAC50	=	5.8	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7668	0	None	-	2	Human	5.7	pAC50	=	5.7	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7668	0	None	-	2	Human	5.7	pAC50	=	5.7	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7668	0	None	-	2	Human	5.7	pAC50	=	5.7	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7668	0	None	-	2	Human	5.7	pAC50	=	5.7	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7668	0	None	-	2	Human	5.7	pAC50	=	5.7	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8738	70	None	-	3	Human	6.7	pAC50	=	6.7	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8738	70	None	-	3	Human	6.7	pAC50	=	6.7	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8738	70	None	-	3	Human	6.7	pAC50	=	6.7	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8738	70	None	-	3	Human	6.7	pAC50	=	6.7	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8738	70	None	-	3	Human	6.7	pAC50	=	6.7	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8738	70	None	-	3	Human	6.7	pAC50	=	6.7	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10899	48	None	-	49	Human	4.7	pAC50	=	4.7	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10899	48	None	-	49	Human	4.7	pAC50	=	4.7	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10899	48	None	-	49	Human	4.7	pAC50	=	4.7	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10899	48	None	-	49	Human	4.7	pAC50	=	4.7	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10899	48	None	-	49	Human	4.7	pAC50	=	4.7	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7724	116	None	-4	8	Human	6.7	pAC50	=	6.7	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7724	116	None	-4	8	Human	6.7	pAC50	=	6.7	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7724	116	None	-4	8	Human	6.7	pAC50	=	6.7	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7724	116	None	-4	8	Human	6.7	pAC50	=	6.7	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7724	116	None	-4	8	Human	6.7	pAC50	=	6.7	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7189	56	None	-1412	40	Human	7.7	pAC50	=	7.7	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7189	56	None	-1412	40	Human	7.7	pAC50	=	7.7	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7189	56	None	-1412	40	Human	7.7	pAC50	=	7.7	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7189	56	None	-1412	40	Human	7.7	pAC50	=	7.7	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7189	56	None	-1412	40	Human	7.7	pAC50	=	7.7	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	106992	107	None	-	0	Human	5.7	pAC50	=	5.7	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	106992	107	None	-	0	Human	5.7	pAC50	=	5.7	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7258	124	None	-7244	51	Human	5.7	pAC50	=	5.7	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7258	124	None	-7244	51	Human	5.7	pAC50	=	5.7	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7258	124	None	-7244	51	Human	5.7	pAC50	=	5.7	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7258	124	None	-7244	51	Human	5.7	pAC50	=	5.7	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7258	124	None	-7244	51	Human	5.7	pAC50	=	5.7	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	69957	17	None	-	1	Human	6.6	pAC50	=	6.6	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	69957	17	None	-	1	Human	6.6	pAC50	=	6.6	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8252	71	None	-	12	Human	5.6	pAC50	=	5.6	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8252	71	None	-	12	Human	5.6	pAC50	=	5.6	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8252	71	None	-	12	Human	5.6	pAC50	=	5.6	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8252	71	None	-	12	Human	5.6	pAC50	=	5.6	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8252	71	None	-	12	Human	5.6	pAC50	=	5.6	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9292	24	None	-8511	67	Human	5.6	pAC50	=	5.6	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9292	24	None	-8511	67	Human	5.6	pAC50	=	5.6	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9292	24	None	-8511	67	Human	5.6	pAC50	=	5.6	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9292	24	None	-8511	67	Human	5.6	pAC50	=	5.6	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9292	24	None	-8511	67	Human	5.6	pAC50	=	5.6	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8214	83	None	-	13	Human	6.6	pAC50	=	6.6	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8214	83	None	-	13	Human	6.6	pAC50	=	6.6	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8214	83	None	-	13	Human	6.6	pAC50	=	6.6	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8214	83	None	-	13	Human	6.6	pAC50	=	6.6	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8214	83	None	-	13	Human	6.6	pAC50	=	6.6	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8214	83	None	-	13	Human	6.6	pAC50	=	6.6	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8202	21	None	-	24	Human	6.6	pAC50	=	6.6	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8202	21	None	-	24	Human	6.6	pAC50	=	6.6	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8202	21	None	-	24	Human	6.6	pAC50	=	6.6	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8202	21	None	-	24	Human	6.6	pAC50	=	6.6	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8202	21	None	-	24	Human	6.6	pAC50	=	6.6	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8443	50	None	-323	65	Human	6.6	pAC50	=	6.6	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8443	50	None	-323	65	Human	6.6	pAC50	=	6.6	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8443	50	None	-323	65	Human	6.6	pAC50	=	6.6	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8443	50	None	-323	65	Human	6.6	pAC50	=	6.6	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8443	50	None	-323	65	Human	6.6	pAC50	=	6.6	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7191	98	None	-	29	Human	6.6	pAC50	=	6.6	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7191	98	None	-	29	Human	6.6	pAC50	=	6.6	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7191	98	None	-	29	Human	6.6	pAC50	=	6.6	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7191	98	None	-	29	Human	6.6	pAC50	=	6.6	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7191	98	None	-	29	Human	6.6	pAC50	=	6.6	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7186	66	None	-6	31	Human	5.6	pAC50	=	5.6	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7186	66	None	-6	31	Human	5.6	pAC50	=	5.6	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7186	66	None	-6	31	Human	5.6	pAC50	=	5.6	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7186	66	None	-6	31	Human	5.6	pAC50	=	5.6	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7186	66	None	-6	31	Human	5.6	pAC50	=	5.6	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8171	114	None	-29	15	Human	8.5	pAC50	=	8.5	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8171	114	None	-29	15	Human	8.5	pAC50	=	8.5	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8171	114	None	-29	15	Human	8.5	pAC50	=	8.5	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8171	114	None	-29	15	Human	8.5	pAC50	=	8.5	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8171	114	None	-29	15	Human	8.5	pAC50	=	8.5	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	21245	41	None	-	0	Human	5.5	pAC50	=	5.5	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	21245	41	None	-	0	Human	5.5	pAC50	=	5.5	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10614	64	None	-	10	Human	5.5	pAC50	=	5.5	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10614	64	None	-	10	Human	5.5	pAC50	=	5.5	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10614	64	None	-	10	Human	5.5	pAC50	=	5.5	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10614	64	None	-	10	Human	5.5	pAC50	=	5.5	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10614	64	None	-	10	Human	5.5	pAC50	=	5.5	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	210787	70	None	-20	12	Human	5.5	pAC50	=	5.5	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	210787	70	None	-20	12	Human	5.5	pAC50	=	5.5	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	210787	70	None	-20	12	Human	5.5	pAC50	=	5.5	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	201796	74	None	-	27	Human	6.5	pAC50	=	6.5	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	201796	74	None	-	27	Human	6.5	pAC50	=	6.5	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	201796	74	None	-	27	Human	6.5	pAC50	=	6.5	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9828	37	None	-	32	Human	5.4	pAC50	=	5.4	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9828	37	None	-	32	Human	5.4	pAC50	=	5.4	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9828	37	None	-	32	Human	5.4	pAC50	=	5.4	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9828	37	None	-	32	Human	5.4	pAC50	=	5.4	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9828	37	None	-	32	Human	5.4	pAC50	=	5.4	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9933	96	None	-169	39	Human	5.4	pAC50	=	5.4	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9933	96	None	-169	39	Human	5.4	pAC50	=	5.4	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9933	96	None	-169	39	Human	5.4	pAC50	=	5.4	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9933	96	None	-169	39	Human	5.4	pAC50	=	5.4	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9933	96	None	-169	39	Human	5.4	pAC50	=	5.4	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	210812	89	None	-	2	Human	5.4	pAC50	=	5.4	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	210812	89	None	-	2	Human	5.4	pAC50	=	5.4	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10030	77	None	-1122	62	Human	6.4	pAC50	=	6.4	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10030	77	None	-1122	62	Human	6.4	pAC50	=	6.4	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10030	77	None	-1122	62	Human	6.4	pAC50	=	6.4	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10030	77	None	-1122	62	Human	6.4	pAC50	=	6.4	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10030	77	None	-1122	62	Human	6.4	pAC50	=	6.4	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7293	81	None	-56	42	Human	6.4	pAC50	=	6.4	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7293	81	None	-56	42	Human	6.4	pAC50	=	6.4	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7293	81	None	-56	42	Human	6.4	pAC50	=	6.4	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7293	81	None	-56	42	Human	6.4	pAC50	=	6.4	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7293	81	None	-56	42	Human	6.4	pAC50	=	6.4	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	193699	64	None	-	25	Human	5.4	pAC50	=	5.4	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	193699	64	None	-	25	Human	5.4	pAC50	=	5.4	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	193699	64	None	-	25	Human	5.4	pAC50	=	5.4	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7705	51	None	-446	21	Human	6.4	pAC50	=	6.4	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7705	51	None	-446	21	Human	6.4	pAC50	=	6.4	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7705	51	None	-446	21	Human	6.4	pAC50	=	6.4	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7705	51	None	-446	21	Human	6.4	pAC50	=	6.4	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7705	51	None	-446	21	Human	6.4	pAC50	=	6.4	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7705	51	None	-446	21	Human	6.4	pAC50	=	6.4	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7705	51	None	-446	21	Human	6.4	pAC50	=	6.4	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7705	51	None	-446	21	Human	6.4	pAC50	=	6.4	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7705	51	None	-446	21	Human	6.4	pAC50	=	6.4	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7705	51	None	-446	21	Human	6.4	pAC50	=	6.4	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7705	51	None	-446	21	Human	6.4	pAC50	=	6.4	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7705	51	None	-446	21	Human	6.4	pAC50	=	6.4	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7705	51	None	-446	21	Human	6.4	pAC50	=	6.4	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	207716	94	None	-	0	Human	5.4	pAC50	=	5.4	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	207716	94	None	-	0	Human	5.4	pAC50	=	5.4	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9688	112	None	-9	65	Human	6.4	pAC50	=	6.4	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9688	112	None	-9	65	Human	6.4	pAC50	=	6.4	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9688	112	None	-9	65	Human	6.4	pAC50	=	6.4	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9688	112	None	-9	65	Human	6.4	pAC50	=	6.4	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10104	118	None	-288	66	Human	7.3	pAC50	=	7.3	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10104	118	None	-288	66	Human	7.3	pAC50	=	7.3	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10104	118	None	-288	66	Human	7.3	pAC50	=	7.3	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10104	118	None	-288	66	Human	7.3	pAC50	=	7.3	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10104	118	None	-288	66	Human	7.3	pAC50	=	7.3	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10632	58	None	-	30	Human	6.3	pAC50	=	6.3	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10632	58	None	-	30	Human	6.3	pAC50	=	6.3	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10632	58	None	-	30	Human	6.3	pAC50	=	6.3	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10632	58	None	-	30	Human	6.3	pAC50	=	6.3	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10632	58	None	-	30	Human	6.3	pAC50	=	6.3	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10632	58	None	-	30	Human	6.3	pAC50	=	6.3	Binding	Binding affinity towards human HRH2 in an in vitro assay 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
		CHEMBL3039583	217728	0	None	-	0	Human	5.3	pAC50	=	5.3	Binding	Binding affinity towards human HRH2 in an in vitro assay 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		NCCCC[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](c2ccccc2)NC(=O)[C@@H]2C[C@H](OC(=O)NCCN)CN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(OCc3ccccc3)cc2)NC1=O	10.1038/s41467-023-40064-9
		135398737	7745	93	None	-64	90	Human	7.3	pAC50	=	7.3	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7745	93	None	-64	90	Human	7.3	pAC50	=	7.3	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7745	93	None	-64	90	Human	7.3	pAC50	=	7.3	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7745	93	None	-64	90	Human	7.3	pAC50	=	7.3	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	7745	93	None	-64	90	Human	7.3	pAC50	=	7.3	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	22066	12	None	-	0	Human	5.3	pAC50	=	5.3	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	22066	12	None	-	0	Human	5.3	pAC50	=	5.3	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	63041	27	None	-12589	20	Human	7.3	pAC50	=	7.3	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	63041	27	None	-12589	20	Human	7.3	pAC50	=	7.3	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9957	51	None	-26	30	Human	7.3	pAC50	=	7.3	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9957	51	None	-26	30	Human	7.3	pAC50	=	7.3	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9957	51	None	-26	30	Human	7.3	pAC50	=	7.3	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9957	51	None	-26	30	Human	7.3	pAC50	=	7.3	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9957	51	None	-26	30	Human	7.3	pAC50	=	7.3	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9310	43	None	-39	56	Human	7.3	pAC50	=	7.3	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9310	43	None	-39	56	Human	7.3	pAC50	=	7.3	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9310	43	None	-39	56	Human	7.3	pAC50	=	7.3	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9310	43	None	-39	56	Human	7.3	pAC50	=	7.3	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9310	43	None	-39	56	Human	7.3	pAC50	=	7.3	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10915	73	None	-281	53	Human	6.2	pAC50	=	6.2	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10915	73	None	-281	53	Human	6.2	pAC50	=	6.2	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10915	73	None	-281	53	Human	6.2	pAC50	=	6.2	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10915	73	None	-281	53	Human	6.2	pAC50	=	6.2	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10915	73	None	-281	53	Human	6.2	pAC50	=	6.2	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8402	96	None	-1	2	Human	8.2	pAC50	=	8.2	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8402	96	None	-1	2	Human	8.2	pAC50	=	8.2	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8402	96	None	-1	2	Human	8.2	pAC50	=	8.2	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8402	96	None	-1	2	Human	8.2	pAC50	=	8.2	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8402	96	None	-1	2	Human	8.2	pAC50	=	8.2	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8402	96	None	-1	2	Human	8.2	pAC50	=	8.2	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8402	96	None	-1	2	Human	8.2	pAC50	=	8.2	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8106	44	None	-	9	Human	6.2	pAC50	=	6.2	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8106	44	None	-	9	Human	6.2	pAC50	=	6.2	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8106	44	None	-	9	Human	6.2	pAC50	=	6.2	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8106	44	None	-	9	Human	6.2	pAC50	=	6.2	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8106	44	None	-	9	Human	6.2	pAC50	=	6.2	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8106	44	None	-	9	Human	6.2	pAC50	=	6.2	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	52998	91	None	-	0	Human	5.2	pAC50	=	5.2	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	52998	91	None	-	0	Human	5.2	pAC50	=	5.2	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	52998	91	None	-	0	Human	5.2	pAC50	=	5.2	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9899	71	None	-	29	Human	6.2	pAC50	=	6.2	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9899	71	None	-	29	Human	6.2	pAC50	=	6.2	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9899	71	None	-	29	Human	6.2	pAC50	=	6.2	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9899	71	None	-	29	Human	6.2	pAC50	=	6.2	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9899	71	None	-	29	Human	6.2	pAC50	=	6.2	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8794	54	None	-	27	Human	7.2	pAC50	=	7.2	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8794	54	None	-	27	Human	7.2	pAC50	=	7.2	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8794	54	None	-	27	Human	7.2	pAC50	=	7.2	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8794	54	None	-	27	Human	7.2	pAC50	=	7.2	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	8794	54	None	-	27	Human	7.2	pAC50	=	7.2	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9121	117	None	-	4	Human	6.2	pAC50	=	6.2	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9121	117	None	-	4	Human	6.2	pAC50	=	6.2	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9121	117	None	-	4	Human	6.2	pAC50	=	6.2	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9121	117	None	-	4	Human	6.2	pAC50	=	6.2	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	9121	117	None	-	4	Human	6.2	pAC50	=	6.2	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	24764	31	None	-	6	Human	6.2	pAC50	=	6.2	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	24764	31	None	-	6	Human	6.2	pAC50	=	6.2	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	215810	40	None	-	5	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	215810	40	None	-	5	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	190314	112	None	-	0	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	190314	112	None	-	0	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10059	64	None	-	21	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10059	64	None	-	21	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10059	64	None	-	21	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10059	64	None	-	21	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	10059	64	None	-	21	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	48288	100	None	-	6	Human	5.0	pAC50	=	5.0	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	48288	100	None	-	6	Human	5.0	pAC50	=	5.0	Binding	Binding affinity towards human HRH2 in an in vitro assay 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	195215	0	None	-	0	Human	7.0	pEC50	=	7.0	Binding	Activity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay	ChEMBL	319	7	4	4	2.2	CC(CC(=O)NC(=N)NCCCc1c[nH]cn1)c1cccs1	10.1021/jm800841w
		CHEMBL502339	195215	0	None	-	0	Human	7.0	pEC50	=	7.0	Binding	Activity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay	ChEMBL	319	7	4	4	2.2	CC(CC(=O)NC(=N)NCCCc1c[nH]cn1)c1cccs1	10.1021/jm800841w
		42625304	185879	0	None	-	1	Human	7.0	pEC50	=	7.0	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	237	5	3	2	0.4	CC(C)C(=O)/N=C(\N)NCCCc1c[nH]cn1	10.1021/jm9000693
		CHEMBL471724	185879	0	None	-	1	Human	7.0	pEC50	=	7.0	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	237	5	3	2	0.4	CC(C)C(=O)/N=C(\N)NCCCc1c[nH]cn1	10.1021/jm9000693
		25149613	185979	0	None	-	1	Human	6.9	pEC50	=	6.9	Binding	Activity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay	ChEMBL	382	8	4	5	2.7	N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1nccs1	10.1021/jm800841w
		CHEMBL472441	185979	0	None	-	1	Human	6.9	pEC50	=	6.9	Binding	Activity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay	ChEMBL	382	8	4	5	2.7	N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1nccs1	10.1021/jm800841w
		1204	8713	119	None	-173	25	Human	5.9	pEC50	=	5.9	Binding	Activity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm800841w
		1247	8713	119	None	-173	25	Human	5.9	pEC50	=	5.9	Binding	Activity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm800841w
		1375	8713	119	None	-173	25	Human	5.9	pEC50	=	5.9	Binding	Activity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm800841w
		774	8713	119	None	-173	25	Human	5.9	pEC50	=	5.9	Binding	Activity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm800841w
		CHEMBL90	8713	119	None	-173	25	Human	5.9	pEC50	=	5.9	Binding	Activity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm800841w
		DB05381	8713	119	None	-173	25	Human	5.9	pEC50	=	5.9	Binding	Activity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm800841w
		1204	8713	119	None	-173	25	Human	5.9	pEC50	=	5.9	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm9000693
		1247	8713	119	None	-173	25	Human	5.9	pEC50	=	5.9	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm9000693
		1375	8713	119	None	-173	25	Human	5.9	pEC50	=	5.9	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm9000693
		774	8713	119	None	-173	25	Human	5.9	pEC50	=	5.9	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm9000693
		CHEMBL90	8713	119	None	-173	25	Human	5.9	pEC50	=	5.9	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm9000693
		DB05381	8713	119	None	-173	25	Human	5.9	pEC50	=	5.9	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm9000693
		1204	8713	119	None	-173	25	Human	5.9	pEC50	=	5.9	Binding	Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1039/C3MD00245D
		1247	8713	119	None	-173	25	Human	5.9	pEC50	=	5.9	Binding	Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1039/C3MD00245D
		1375	8713	119	None	-173	25	Human	5.9	pEC50	=	5.9	Binding	Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1039/C3MD00245D
		774	8713	119	None	-173	25	Human	5.9	pEC50	=	5.9	Binding	Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1039/C3MD00245D
		CHEMBL90	8713	119	None	-173	25	Human	5.9	pEC50	=	5.9	Binding	Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1039/C3MD00245D
		DB05381	8713	119	None	-173	25	Human	5.9	pEC50	=	5.9	Binding	Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1039/C3MD00245D
		46890166	14088	0	None	-	2	Human	6.9	pEC50	=	6.9	Binding	Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cellsDisplacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells	ChEMBL	419	6	2	4	4.5	Cc1cc(OCCCN2CCc3nc[nH]c3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1	10.1016/j.bmcl.2010.04.017
		CHEMBL1086105	14088	0	None	-	2	Human	6.9	pEC50	=	6.9	Binding	Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cellsDisplacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells	ChEMBL	419	6	2	4	4.5	Cc1cc(OCCCN2CCc3nc[nH]c3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1	10.1016/j.bmcl.2010.04.017
		42625386	185132	0	None	-	1	Human	6.9	pEC50	=	6.9	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	237	6	3	2	0.6	CCCC(=O)/N=C(\N)NCCCc1c[nH]cn1	10.1021/jm9000693
		CHEMBL465170	185132	0	None	-	1	Human	6.9	pEC50	=	6.9	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	237	6	3	2	0.6	CCCC(=O)/N=C(\N)NCCCc1c[nH]cn1	10.1021/jm9000693
		90667232	116248	0	None	-	1	Human	6.6	pEC50	=	6.6	Binding	Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay	ChEMBL	313	7	3	2	2.0	CC(CC(=O)/N=C(\N)NCCCc1cn[nH]c1)c1ccccc1	10.1039/C3MD00245D
		CHEMBL3220633	116248	0	None	-	1	Human	6.6	pEC50	=	6.6	Binding	Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay	ChEMBL	313	7	3	2	2.0	CC(CC(=O)/N=C(\N)NCCCc1cn[nH]c1)c1ccccc1	10.1039/C3MD00245D
		10103168	32876	5	None	-	2	Human	5.6	pEC50	=	5.6	Binding	Inhibition of human Histamine H2 receptor using [3H]tiotidineInhibition of human Histamine H2 receptor using [3H]tiotidine	ChEMBL	123	1	2	2	0.2	N[C@@H]1C[C@H]1c1c[nH]cn1	10.1021/jm020415q
		CHEMBL13559	32876	5	None	-	2	Human	5.6	pEC50	=	5.6	Binding	Inhibition of human Histamine H2 receptor using [3H]tiotidineInhibition of human Histamine H2 receptor using [3H]tiotidine	ChEMBL	123	1	2	2	0.2	N[C@@H]1C[C@H]1c1c[nH]cn1	10.1021/jm020415q
		182527	117345	8	None	-	0	Human	5.6	pEC50	=	5.6	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	167	4	4	2	-0.2	N=C(N)NCCCc1c[nH]cn1	10.1021/jm9000693
		CHEMBL325327	117345	8	None	-	0	Human	5.6	pEC50	=	5.6	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	167	4	4	2	-0.2	N=C(N)NCCCc1c[nH]cn1	10.1021/jm9000693
		42626110	186548	0	None	-	0	Human	6.5	pEC50	=	6.5	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	310	5	4	2	1.6	N/C(=N\C(=O)c1cc2ccccc2[nH]1)NCCCc1c[nH]cn1	10.1021/jm9000693
		CHEMBL474448	186548	0	None	-	0	Human	6.5	pEC50	=	6.5	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	310	5	4	2	1.6	N/C(=N\C(=O)c1cc2ccccc2[nH]1)NCCCc1c[nH]cn1	10.1021/jm9000693
		42625224	187543	0	None	-	1	Human	7.5	pEC50	=	7.5	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	395	9	5	3	1.5	N/C(=N\C(=O)CCCNC(=O)c1cc2ccccc2[nH]1)NCCCc1c[nH]cn1	10.1021/jm9000693
		CHEMBL475620	187543	0	None	-	1	Human	7.5	pEC50	=	7.5	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	395	9	5	3	1.5	N/C(=N\C(=O)CCCNC(=O)c1cc2ccccc2[nH]1)NCCCc1c[nH]cn1	10.1021/jm9000693
		42625223	186704	0	None	-	1	Human	6.5	pEC50	=	6.5	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	395	8	4	3	1.4	CN(CCC(=O)/N=C(\N)NCCCc1c[nH]cn1)C(=O)c1cc2ccccc2[nH]1	10.1021/jm9000693
		CHEMBL474617	186704	0	None	-	1	Human	6.5	pEC50	=	6.5	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	395	8	4	3	1.4	CN(CCC(=O)/N=C(\N)NCCCc1c[nH]cn1)C(=O)c1cc2ccccc2[nH]1	10.1021/jm9000693
		42626109	186547	0	None	-	1	Human	7.4	pEC50	=	7.4	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	324	6	4	2	1.5	N/C(=N\C(=O)Cc1c[nH]c2ccccc12)NCCCc1c[nH]cn1	10.1021/jm9000693
		CHEMBL474447	186547	0	None	-	1	Human	7.4	pEC50	=	7.4	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	324	6	4	2	1.5	N/C(=N\C(=O)Cc1c[nH]c2ccccc12)NCCCc1c[nH]cn1	10.1021/jm9000693
		42625303	187545	0	None	-	1	Human	6.4	pEC50	=	6.4	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	223	5	3	2	0.2	CCC(=O)/N=C(\N)NCCCc1c[nH]cn1	10.1021/jm9000693
		CHEMBL475621	187545	0	None	-	1	Human	6.4	pEC50	=	6.4	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	223	5	3	2	0.2	CCC(=O)/N=C(\N)NCCCc1c[nH]cn1	10.1021/jm9000693
		90667235	116251	0	None	-	1	Human	6.4	pEC50	=	6.4	Binding	Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay	ChEMBL	376	8	3	3	2.4	N/C(=N\C(=O)CC(c1ccccc1)c1ccccc1)NCCCc1ncn[nH]1	10.1039/C3MD00245D
		CHEMBL3220636	116251	0	None	-	1	Human	6.4	pEC50	=	6.4	Binding	Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay	ChEMBL	376	8	3	3	2.4	N/C(=N\C(=O)CC(c1ccccc1)c1ccccc1)NCCCc1ncn[nH]1	10.1039/C3MD00245D
		1204	8713	119	None	-173	25	Human	6.3	pEC50	=	6.3	Binding	Inhibition of human Histamine H2 receptor using [3H]tiotidineInhibition of human Histamine H2 receptor using [3H]tiotidine	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm020415q
		1247	8713	119	None	-173	25	Human	6.3	pEC50	=	6.3	Binding	Inhibition of human Histamine H2 receptor using [3H]tiotidineInhibition of human Histamine H2 receptor using [3H]tiotidine	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm020415q
		1375	8713	119	None	-173	25	Human	6.3	pEC50	=	6.3	Binding	Inhibition of human Histamine H2 receptor using [3H]tiotidineInhibition of human Histamine H2 receptor using [3H]tiotidine	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm020415q
		774	8713	119	None	-173	25	Human	6.3	pEC50	=	6.3	Binding	Inhibition of human Histamine H2 receptor using [3H]tiotidineInhibition of human Histamine H2 receptor using [3H]tiotidine	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm020415q
		CHEMBL90	8713	119	None	-173	25	Human	6.3	pEC50	=	6.3	Binding	Inhibition of human Histamine H2 receptor using [3H]tiotidineInhibition of human Histamine H2 receptor using [3H]tiotidine	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm020415q
		DB05381	8713	119	None	-173	25	Human	6.3	pEC50	=	6.3	Binding	Inhibition of human Histamine H2 receptor using [3H]tiotidineInhibition of human Histamine H2 receptor using [3H]tiotidine	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm020415q
		25149335	191004	0	None	-	1	Human	7.2	pEC50	=	7.2	Binding	Activity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay	ChEMBL	313	7	3	2	2.0	CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1	10.1021/jm800841w
		CHEMBL483406	191004	0	None	-	1	Human	7.2	pEC50	=	7.2	Binding	Activity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay	ChEMBL	313	7	3	2	2.0	CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1	10.1021/jm800841w
		25149335	191004	0	None	-	1	Human	7.2	pEC50	=	7.2	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	313	7	3	2	2.0	CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1	10.1021/jm9000693
		CHEMBL483406	191004	0	None	-	1	Human	7.2	pEC50	=	7.2	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	313	7	3	2	2.0	CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1	10.1021/jm9000693
		25149335	191004	0	None	-	1	Human	7.2	pEC50	=	7.2	Binding	Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay	ChEMBL	313	7	3	2	2.0	CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1	10.1039/C3MD00245D
		CHEMBL483406	191004	0	None	-	1	Human	7.2	pEC50	=	7.2	Binding	Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay	ChEMBL	313	7	3	2	2.0	CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1	10.1039/C3MD00245D
		10374457	35668	2	None	-	2	Human	6.2	pEC50	=	6.2	Binding	Inhibition of human Histamine H2 receptor using [3H]tiotidineInhibition of human Histamine H2 receptor using [3H]tiotidine	ChEMBL	123	1	2	2	0.2	N[C@H]1C[C@@H]1c1c[nH]cn1	10.1021/jm020415q
		CHEMBL13795	35668	2	None	-	2	Human	6.2	pEC50	=	6.2	Binding	Inhibition of human Histamine H2 receptor using [3H]tiotidineInhibition of human Histamine H2 receptor using [3H]tiotidine	ChEMBL	123	1	2	2	0.2	N[C@H]1C[C@@H]1c1c[nH]cn1	10.1021/jm020415q
		42625384	176552	0	None	-	1	Human	6.1	pEC50	=	6.1	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	209	4	3	2	-0.2	CC(=O)/N=C(\N)NCCCc1c[nH]cn1	10.1021/jm9000693
		CHEMBL443896	176552	0	None	-	1	Human	6.1	pEC50	=	6.1	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	209	4	3	2	-0.2	CC(=O)/N=C(\N)NCCCc1c[nH]cn1	10.1021/jm9000693
		90667234	116250	0	None	-	1	Human	6.1	pEC50	=	6.1	Binding	Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay	ChEMBL	314	7	3	3	1.4	CC(CC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1	10.1039/C3MD00245D
		CHEMBL3220635	116250	0	None	-	1	Human	6.1	pEC50	=	6.1	Binding	Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay	ChEMBL	314	7	3	3	1.4	CC(CC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1	10.1039/C3MD00245D
		25149521	185831	0	None	-	1	Human	7.1	pEC50	=	7.1	Binding	Activity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay	ChEMBL	375	8	4	3	3.2	N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1ccccc1	10.1021/jm800841w
		CHEMBL471413	185831	0	None	-	1	Human	7.1	pEC50	=	7.1	Binding	Activity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay	ChEMBL	375	8	4	3	3.2	N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1ccccc1	10.1021/jm800841w
		42625221	196367	0	None	-	1	Human	7.1	pEC50	=	7.1	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	338	7	4	2	1.9	N/C(=N\C(=O)CCc1c[nH]c2ccccc12)NCCCc1c[nH]cn1	10.1021/jm9000693
		CHEMBL514641	196367	0	None	-	1	Human	7.1	pEC50	=	7.1	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	338	7	4	2	1.9	N/C(=N\C(=O)CCc1c[nH]c2ccccc12)NCCCc1c[nH]cn1	10.1021/jm9000693
		42626111	196473	0	None	-	0	Human	7.1	pEC50	=	7.1	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	381	8	5	3	1.1	N/C(=N\C(=O)CCNC(=O)c1cc2ccccc2[nH]1)NCCCc1c[nH]cn1	10.1021/jm9000693
		CHEMBL515428	196473	0	None	-	0	Human	7.1	pEC50	=	7.1	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	381	8	5	3	1.1	N/C(=N\C(=O)CCNC(=O)c1cc2ccccc2[nH]1)NCCCc1c[nH]cn1	10.1021/jm9000693
		90667262	116257	0	None	-	0	Human	6.1	pEC50	=	6.1	Binding	Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay	ChEMBL	324	7	2	2	2.6	CC(CC(=O)/N=C(\N)NCCCc1ccccn1)c1ccccc1	10.1039/C3MD00245D
		CHEMBL3220665	116257	0	None	-	0	Human	6.1	pEC50	=	6.1	Binding	Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay	ChEMBL	324	7	2	2	2.6	CC(CC(=O)/N=C(\N)NCCCc1ccccn1)c1ccccc1	10.1039/C3MD00245D
		11829635	170018	4	None	-	1	Human	7.0	pEC50	=	7.0	Binding	Inhibition of human Histamine H2 receptor using [3H]tiotidineInhibition of human Histamine H2 receptor using [3H]tiotidine	ChEMBL	151	3	2	2	0.9	NCC[C@H]1C[C@H]1c1c[nH]cn1	10.1021/jm020415q
		CHEMBL418470	170018	4	None	-	1	Human	7.0	pEC50	=	7.0	Binding	Inhibition of human Histamine H2 receptor using [3H]tiotidineInhibition of human Histamine H2 receptor using [3H]tiotidine	ChEMBL	151	3	2	2	0.9	NCC[C@H]1C[C@H]1c1c[nH]cn1	10.1021/jm020415q
		42625222	186549	0	None	-	0	Human	6.0	pEC50	=	6.0	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	367	7	5	3	0.7	N/C(=N\C(=O)CNC(=O)c1cc2ccccc2[nH]1)NCCCc1c[nH]cn1	10.1021/jm9000693
		CHEMBL474449	186549	0	None	-	0	Human	6.0	pEC50	=	6.0	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	367	7	5	3	0.7	N/C(=N\C(=O)CNC(=O)c1cc2ccccc2[nH]1)NCCCc1c[nH]cn1	10.1021/jm9000693
		11539632	77336	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Inhibitory concentration against histamine H2 receptorInhibitory concentration against histamine H2 receptor	ChEMBL	447	8	1	5	4.8	Cc1cc(OCCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12	10.1021/jm050103y
		CHEMBL194837	77336	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Inhibitory concentration against histamine H2 receptorInhibitory concentration against histamine H2 receptor	ChEMBL	447	8	1	5	4.8	Cc1cc(OCCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12	10.1021/jm050103y
		132609385	164874	0	None	-	0	Human	6.0	pIC50	=	6	Binding	Displacement of [125I]-aminopotentidine receptor from histamine H2 receptor (unknown origin)Displacement of [125I]-aminopotentidine receptor from histamine H2 receptor (unknown origin)	ChEMBL	324	5	0	3	3.8	COc1ccc(CN2CCCN(Cc3ccccc3)[C@@H](C)C2)cc1	10.1016/j.bmc.2017.07.027
		CHEMBL4086541	164874	0	None	-	0	Human	6.0	pIC50	=	6	Binding	Displacement of [125I]-aminopotentidine receptor from histamine H2 receptor (unknown origin)Displacement of [125I]-aminopotentidine receptor from histamine H2 receptor (unknown origin)	ChEMBL	324	5	0	3	3.8	COc1ccc(CN2CCCN(Cc3ccccc3)[C@@H](C)C2)cc1	10.1016/j.bmc.2017.07.027
		1231	7724	116	None	-4	8	Human	6.0	pIC50	=	6	Binding	Displacement of [125I]APT from human recombinant H2 receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [125I]APT from human recombinant H2 receptor expressed in CHO cells measured after 120 mins by scintillation counting method	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.bmc.2016.11.014
		2756	7724	116	None	-4	8	Human	6.0	pIC50	=	6	Binding	Displacement of [125I]APT from human recombinant H2 receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [125I]APT from human recombinant H2 receptor expressed in CHO cells measured after 120 mins by scintillation counting method	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.bmc.2016.11.014
		645	7724	116	None	-4	8	Human	6.0	pIC50	=	6	Binding	Displacement of [125I]APT from human recombinant H2 receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [125I]APT from human recombinant H2 receptor expressed in CHO cells measured after 120 mins by scintillation counting method	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.bmc.2016.11.014
		CHEMBL30	7724	116	None	-4	8	Human	6.0	pIC50	=	6	Binding	Displacement of [125I]APT from human recombinant H2 receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [125I]APT from human recombinant H2 receptor expressed in CHO cells measured after 120 mins by scintillation counting method	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.bmc.2016.11.014
		DB00501	7724	116	None	-4	8	Human	6.0	pIC50	=	6	Binding	Displacement of [125I]APT from human recombinant H2 receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [125I]APT from human recombinant H2 receptor expressed in CHO cells measured after 120 mins by scintillation counting method	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.bmc.2016.11.014
		1231	7724	116	None	-4	8	Human	6.0	pIC50	=	6	Binding	Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cellsDisplacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.bmc.2016.03.006
		2756	7724	116	None	-4	8	Human	6.0	pIC50	=	6	Binding	Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cellsDisplacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.bmc.2016.03.006
		645	7724	116	None	-4	8	Human	6.0	pIC50	=	6	Binding	Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cellsDisplacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.bmc.2016.03.006
		CHEMBL30	7724	116	None	-4	8	Human	6.0	pIC50	=	6	Binding	Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cellsDisplacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.bmc.2016.03.006
		DB00501	7724	116	None	-4	8	Human	6.0	pIC50	=	6	Binding	Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cellsDisplacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.bmc.2016.03.006
		17747460	68103	12	None	-	4	Human	5.0	pIC50	=	5	Binding	Binding affinity to human histamine H2 receptorBinding affinity to human histamine H2 receptor	ChEMBL	640	14	0	6	7.8	O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1	10.1021/jm1013874
		CHEMBL1767164	68103	12	None	-	4	Human	5.0	pIC50	=	5	Binding	Binding affinity to human histamine H2 receptorBinding affinity to human histamine H2 receptor	ChEMBL	640	14	0	6	7.8	O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1	10.1021/jm1013874
		10205121	73466	0	None	-	0	Human	5.0	pIC50	=	5	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	464	6	1	4	6.5	O=C(O)c1cccc(CN2CCC(c3cn(Cc4ccc(Cl)s4)c4ccccc34)CC2)c1	10.1021/jm0498203
		CHEMBL185489	73466	0	None	-	0	Human	5.0	pIC50	=	5	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	464	6	1	4	6.5	O=C(O)c1cccc(CN2CCC(c3cn(Cc4ccc(Cl)s4)c4ccccc34)CC2)c1	10.1021/jm0498203
		10138404	143660	0	None	-	0	Human	5.0	pIC50	=	5	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	444	8	1	5	5.2	O=C(O)c1ccccc1OCCN1CCC(c2cn(Cc3ccco3)c3ccccc23)CC1	10.1021/jm0498203
		CHEMBL374218	143660	0	None	-	0	Human	5.0	pIC50	=	5	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	444	8	1	5	5.2	O=C(O)c1ccccc1OCCN1CCC(c2cn(Cc3ccco3)c3ccccc23)CC1	10.1021/jm0498203
		9932752	148761	0	None	-	0	Human	5.0	pIC50	=	5	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	436	8	1	4	5.1	O=C(O)c1ccccc1OCCN1CCC(c2cn(CC3CC3)c3cc(F)ccc23)CC1	10.1021/jm0498203
		CHEMBL387391	148761	0	None	-	0	Human	5.0	pIC50	=	5	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	436	8	1	4	5.1	O=C(O)c1ccccc1OCCN1CCC(c2cn(CC3CC3)c3cc(F)ccc23)CC1	10.1021/jm0498203
		44326821	214690	0	None	-	0	Rat	4.0	pIC50	=	4	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL	559	12	5	6	2.2	CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)C	10.1021/jm00381a002
		CHEMBL96738	214690	0	None	-	0	Rat	4.0	pIC50	=	4	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL	559	12	5	6	2.2	CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)C	10.1021/jm00381a002
		CHEMBL95063	222696	0	None	-	0	Rat	4.0	pIC50	=	4	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL		None	None	None		CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(N)=O	10.1021/jm00381a002
		135	9310	43	None	-39	56	Human	6.0	pIC50	=	6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	264	0	0	2	3.1	CN1CCN2C(C1)c1ccccc1Cc1c2cccc1	nan
		1796	9310	43	None	-39	56	Human	6.0	pIC50	=	6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	264	0	0	2	3.1	CN1CCN2C(C1)c1ccccc1Cc1c2cccc1	nan
		4184	9310	43	None	-39	56	Human	6.0	pIC50	=	6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	264	0	0	2	3.1	CN1CCN2C(C1)c1ccccc1Cc1c2cccc1	nan
		CHEMBL6437	9310	43	None	-39	56	Human	6.0	pIC50	=	6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	264	0	0	2	3.1	CN1CCN2C(C1)c1ccccc1Cc1c2cccc1	nan
		DB06148	9310	43	None	-39	56	Human	6.0	pIC50	=	6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	264	0	0	2	3.1	CN1CCN2C(C1)c1ccccc1Cc1c2cccc1	nan
		11785584	143742	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	512	8	1	5	6.5	O=C(O)c1ccccc1OCCN1CCC(c2cn(Cc3ccc(Cl)s3)c3cc(F)ccc23)CC1	10.1021/jm0498203
		CHEMBL374459	143742	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	512	8	1	5	6.5	O=C(O)c1ccccc1OCCN1CCC(c2cn(Cc3ccc(Cl)s3)c3cc(F)ccc23)CC1	10.1021/jm0498203
		10885636	117793	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Inhibition of histamine H2 receptorInhibition of histamine H2 receptor	ChEMBL	503	9	0	4	5.7	N#Cc1ccc(CCOC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1	10.1021/jm010878g
		CHEMBL326263	117793	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Inhibition of histamine H2 receptorInhibition of histamine H2 receptor	ChEMBL	503	9	0	4	5.7	N#Cc1ccc(CCOC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1	10.1021/jm010878g
		1588	9105	27	None	-223	44	Human	6.0	pIC50	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	338	3	2	2	2.8	CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC	nan
		28864	9105	27	None	-223	44	Human	6.0	pIC50	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	338	3	2	2	2.8	CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC	nan
		43	9105	27	None	-223	44	Human	6.0	pIC50	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	338	3	2	2	2.8	CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC	nan
		CHEMBL157138	9105	27	None	-223	44	Human	6.0	pIC50	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	338	3	2	2	2.8	CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC	nan
		DB00589	9105	27	None	-223	44	Human	6.0	pIC50	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	338	3	2	2	2.8	CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC	nan
		176	7186	66	None	-6	31	Human	5.0	pIC50	=	5.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	nan
		2157	7186	66	None	-6	31	Human	5.0	pIC50	=	5.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	nan
		2566	7186	66	None	-6	31	Human	5.0	pIC50	=	5.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	nan
		CHEMBL633	7186	66	None	-6	31	Human	5.0	pIC50	=	5.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	nan
		DB01118	7186	66	None	-6	31	Human	5.0	pIC50	=	5.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	nan
		657255	205863	34	None	-3	15	Human	7.0	pIC50	=	7.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	337	12	2	3	5.6	CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1	nan
		CHEMBL588119	205863	34	None	-3	15	Human	7.0	pIC50	=	7.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	337	12	2	3	5.6	CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1	nan
		124087	8171	114	None	-29	15	Human	6.0	pIC50	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	310	0	1	2	4.0	Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1	nan
		7157	8171	114	None	-29	15	Human	6.0	pIC50	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	310	0	1	2	4.0	Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1	nan
		814	8171	114	None	-29	15	Human	6.0	pIC50	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	310	0	1	2	4.0	Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1	nan
		CHEMBL1172	8171	114	None	-29	15	Human	6.0	pIC50	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	310	0	1	2	4.0	Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1	nan
		DB00967	8171	114	None	-29	15	Human	6.0	pIC50	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	310	0	1	2	4.0	Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1	nan
		11057	182928	23	None	-2	20	Human	5.9	pIC50	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	372	4	0	2	4.5	CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1	nan
		3468	182928	23	None	-2	20	Human	5.9	pIC50	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	372	4	0	2	4.5	CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1	nan
		CHEMBL459265	182928	23	None	-2	20	Human	5.9	pIC50	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	372	4	0	2	4.5	CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1	nan
		CHEMBL64894	182928	23	None	-2	20	Human	5.9	pIC50	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	372	4	0	2	4.5	CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1	nan
		2286	9957	51	None	-26	30	Human	5.9	pIC50	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	nan
		4927	9957	51	None	-26	30	Human	5.9	pIC50	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	nan
		7282	9957	51	None	-26	30	Human	5.9	pIC50	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	nan
		CHEMBL643	9957	51	None	-26	30	Human	5.9	pIC50	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	nan
		DB01069	9957	51	None	-26	30	Human	5.9	pIC50	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	nan
		1353	8692	93	None	-131	85	Human	5.9	pIC50	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	nan
		3559	8692	93	None	-131	85	Human	5.9	pIC50	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	nan
		86	8692	93	None	-131	85	Human	5.9	pIC50	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	nan
		CHEMBL54	8692	93	None	-131	85	Human	5.9	pIC50	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	nan
		DB00502	8692	93	None	-131	85	Human	5.9	pIC50	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	nan
		11362693	148390	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	440	9	1	5	4.4	COCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccc(F)cc21	10.1021/jm0498203
		CHEMBL385133	148390	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	440	9	1	5	4.4	COCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccc(F)cc21	10.1021/jm0498203
		1201549	7384	24	None	-74	20	Human	5.9	pIC50	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	307	4	0	2	4.4	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1	nan
		333	7384	24	None	-74	20	Human	5.9	pIC50	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	307	4	0	2	4.4	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1	nan
		7601	7384	24	None	-74	20	Human	5.9	pIC50	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	307	4	0	2	4.4	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1	nan
		CHEMBL1201203	7384	24	None	-74	20	Human	5.9	pIC50	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	307	4	0	2	4.4	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1	nan
		CHEMBL438151	7384	24	None	-74	20	Human	5.9	pIC50	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	307	4	0	2	4.4	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1	nan
		DB00245	7384	24	None	-74	20	Human	5.9	pIC50	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	307	4	0	2	4.4	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1	nan
		1212	8443	50	None	-323	65	Human	5.9	pIC50	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	nan
		204	8443	50	None	-323	65	Human	5.9	pIC50	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	nan
		3372	8443	50	None	-323	65	Human	5.9	pIC50	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	nan
		CHEMBL726	8443	50	None	-323	65	Human	5.9	pIC50	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	nan
		DB00623	8443	50	None	-323	65	Human	5.9	pIC50	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	nan
		9889247	91536	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	436	10	1	5	4.6	CCOCCn1cc(C2CCN(CCOc3cccc(C(=O)O)c3)CC2)c2ccccc21	10.1021/jm0498203
		CHEMBL223024	91536	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	436	10	1	5	4.6	CCOCCn1cc(C2CCN(CCOc3cccc(C(=O)O)c3)CC2)c2ccccc21	10.1021/jm0498203
		11071079	117370	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Inhibition of histamine H2 receptorInhibition of histamine H2 receptor	ChEMBL	496	9	0	3	6.0	O=C(OCCc1ccc(F)cc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1	10.1021/jm010878g
		CHEMBL325516	117370	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Inhibition of histamine H2 receptorInhibition of histamine H2 receptor	ChEMBL	496	9	0	3	6.0	O=C(OCCc1ccc(F)cc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1	10.1021/jm010878g
		10202996	91417	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	430	6	1	4	5.8	O=C(O)c1cccc(CN2CCC(c3cn(Cc4cccs4)c4ccccc34)CC2)c1	10.1021/jm0498203
		CHEMBL222372	91417	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	430	6	1	4	5.8	O=C(O)c1cccc(CN2CCC(c3cn(Cc4cccs4)c4ccccc34)CC2)c1	10.1021/jm0498203
		11113605	17279	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Inhibition of histamine H2 receptorInhibition of histamine H2 receptor	ChEMBL	480	9	0	2	5.8	O=C(CCc1ccc(F)cc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1	10.1021/jm010878g
		CHEMBL116735	17279	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Inhibition of histamine H2 receptorInhibition of histamine H2 receptor	ChEMBL	480	9	0	2	5.8	O=C(CCc1ccc(F)cc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1	10.1021/jm010878g
		11329753	91338	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	514	10	1	5	5.4	CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2cccc(Br)c21	10.1021/jm0498203
		CHEMBL222083	91338	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	514	10	1	5	5.4	CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2cccc(Br)c21	10.1021/jm0498203
		1231	7724	116	None	-4	8	Human	6.9	pIC50	=	6.9	Binding	Binding affinity to human histamine H2 receptor by radioligand displacement assayBinding affinity to human histamine H2 receptor by radioligand displacement assay	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.ejmech.2013.01.044
		2756	7724	116	None	-4	8	Human	6.9	pIC50	=	6.9	Binding	Binding affinity to human histamine H2 receptor by radioligand displacement assayBinding affinity to human histamine H2 receptor by radioligand displacement assay	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.ejmech.2013.01.044
		645	7724	116	None	-4	8	Human	6.9	pIC50	=	6.9	Binding	Binding affinity to human histamine H2 receptor by radioligand displacement assayBinding affinity to human histamine H2 receptor by radioligand displacement assay	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.ejmech.2013.01.044
		CHEMBL30	7724	116	None	-4	8	Human	6.9	pIC50	=	6.9	Binding	Binding affinity to human histamine H2 receptor by radioligand displacement assayBinding affinity to human histamine H2 receptor by radioligand displacement assay	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.ejmech.2013.01.044
		DB00501	7724	116	None	-4	8	Human	6.9	pIC50	=	6.9	Binding	Binding affinity to human histamine H2 receptor by radioligand displacement assayBinding affinity to human histamine H2 receptor by radioligand displacement assay	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.ejmech.2013.01.044
		104903	63118	17	None	-5	6	Human	4.9	pIC50	=	4.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	624	6	0	8	5.5	C[C@@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)C3=CC[C@]2(C)[C@H]1C(=O)CN1CCN(c2cc(N3CCCC3)nc(N3CCCC3)n2)CC1	nan
		CHEMBL1630578	63118	17	None	-5	6	Human	4.9	pIC50	=	4.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	624	6	0	8	5.5	C[C@@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)C3=CC[C@]2(C)[C@H]1C(=O)CN1CCN(c2cc(N3CCCC3)nc(N3CCCC3)n2)CC1	nan
		72548703	168346	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Displacement of [125I]APT from human recombinant histamine H2 receptor after 120 mins by scintillation counting analysisDisplacement of [125I]APT from human recombinant histamine H2 receptor after 120 mins by scintillation counting analysis	ChEMBL	583	8	3	6	5.8	CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12	10.1016/j.bmcl.2018.03.093
		CHEMBL4128926	168346	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Displacement of [125I]APT from human recombinant histamine H2 receptor after 120 mins by scintillation counting analysisDisplacement of [125I]APT from human recombinant histamine H2 receptor after 120 mins by scintillation counting analysis	ChEMBL	583	8	3	6	5.8	CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12	10.1016/j.bmcl.2018.03.093
		2389	10104	118	None	-288	66	Human	5.8	pIC50	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	nan
		5073	10104	118	None	-288	66	Human	5.8	pIC50	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	nan
		96	10104	118	None	-288	66	Human	5.8	pIC50	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	nan
		CHEMBL85	10104	118	None	-288	66	Human	5.8	pIC50	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	nan
		DB00734	10104	118	None	-288	66	Human	5.8	pIC50	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	nan
		10139591	91415	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	462	7	1	5	5.5	COc1ccc(CN2CCC(c3cn(Cc4ccoc4)c4cc(F)ccc34)CC2)cc1C(=O)O	10.1021/jm0498203
		CHEMBL222356	91415	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	462	7	1	5	5.5	COc1ccc(CN2CCC(c3cn(Cc4ccoc4)c4cc(F)ccc34)CC2)cc1C(=O)O	10.1021/jm0498203
		11329754	148760	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	514	10	1	5	5.4	CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2cc(Br)ccc21	10.1021/jm0498203
		CHEMBL387390	148760	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	514	10	1	5	5.4	CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2cc(Br)ccc21	10.1021/jm0498203
		CHEMBL96946	222701	0	None	-	0	Rat	4.8	pIC50	=	4.8	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL		None	None	None		CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(N)=O	10.1021/jm00381a002
		57469	25638	125	None	-1	3	Human	5.8	pIC50	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	240	2	1	4	2.8	CC(C)Cn1cnc2c(N)nc3ccccc3c21	nan
		CHEMBL1282	25638	125	None	-1	3	Human	5.8	pIC50	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	240	2	1	4	2.8	CC(C)Cn1cnc2c(N)nc3ccccc3c21	nan
		3198	212292	76	None	-19	34	Human	5.8	pIC50	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	380	6	0	3	5.8	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1	nan
		CHEMBL1201049	212292	76	None	-19	34	Human	5.8	pIC50	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	380	6	0	3	5.8	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1	nan
		CHEMBL808	212292	76	None	-19	34	Human	5.8	pIC50	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	380	6	0	3	5.8	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1	nan
		3042	8196	35	None	-53	15	Human	5.8	pIC50	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	309	7	0	3	4.4	CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC	nan
		355	8196	35	None	-53	15	Human	5.8	pIC50	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	309	7	0	3	4.4	CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC	nan
		868	8196	35	None	-53	15	Human	5.8	pIC50	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	309	7	0	3	4.4	CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC	nan
		CHEMBL1123	8196	35	None	-53	15	Human	5.8	pIC50	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	309	7	0	3	4.4	CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC	nan
		DB00804	8196	35	None	-53	15	Human	5.8	pIC50	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	309	7	0	3	4.4	CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC	nan
		2247	7293	81	None	-56	42	Human	5.8	pIC50	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	nan
		249	7293	81	None	-56	42	Human	5.8	pIC50	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	nan
		2603	7293	81	None	-56	42	Human	5.8	pIC50	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	nan
		CHEMBL296419	7293	81	None	-56	42	Human	5.8	pIC50	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	nan
		DB00637	7293	81	None	-56	42	Human	5.8	pIC50	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	nan
		9822631	129737	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	406	8	1	4	4.8	CCOCCn1cc(C2CCN(Cc3cccc(C(=O)O)c3)CC2)c2ccccc21	10.1021/jm0498203
		CHEMBL360791	129737	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	406	8	1	4	4.8	CCOCCn1cc(C2CCN(Cc3cccc(C(=O)O)c3)CC2)c2ccccc21	10.1021/jm0498203
		1231	7724	116	None	-4	8	Human	6.8	pIC50	=	6.8	Binding	Displacement of radiolabeled cimetidine from human histamine H2 receptorDisplacement of radiolabeled cimetidine from human histamine H2 receptor	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1021/jm8007618
		2756	7724	116	None	-4	8	Human	6.8	pIC50	=	6.8	Binding	Displacement of radiolabeled cimetidine from human histamine H2 receptorDisplacement of radiolabeled cimetidine from human histamine H2 receptor	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1021/jm8007618
		645	7724	116	None	-4	8	Human	6.8	pIC50	=	6.8	Binding	Displacement of radiolabeled cimetidine from human histamine H2 receptorDisplacement of radiolabeled cimetidine from human histamine H2 receptor	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1021/jm8007618
		CHEMBL30	7724	116	None	-4	8	Human	6.8	pIC50	=	6.8	Binding	Displacement of radiolabeled cimetidine from human histamine H2 receptorDisplacement of radiolabeled cimetidine from human histamine H2 receptor	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1021/jm8007618
		DB00501	7724	116	None	-4	8	Human	6.8	pIC50	=	6.8	Binding	Displacement of radiolabeled cimetidine from human histamine H2 receptorDisplacement of radiolabeled cimetidine from human histamine H2 receptor	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1021/jm8007618
		10141470	130335	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	494	8	1	5	6.4	O=C(O)c1ccccc1OCCN1CCC(c2cn(Cc3ccc(Cl)s3)c3ccccc23)CC1	10.1021/jm0498203
		CHEMBL361805	130335	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	494	8	1	5	6.4	O=C(O)c1ccccc1OCCN1CCC(c2cn(Cc3ccc(Cl)s3)c3ccccc23)CC1	10.1021/jm0498203
		3158	63041	27	None	-12589	20	Human	5.7	pIC50	=	5.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	279	3	0	2	4.0	CN(C)CCC=C1c2ccccc2COc2ccccc21	nan
		CHEMBL1628227	63041	27	None	-12589	20	Human	5.7	pIC50	=	5.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	279	3	0	2	4.0	CN(C)CCC=C1c2ccccc2COc2ccccc21	nan
		11476077	143185	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	436	10	1	5	4.5	CCOCCn1cc(C2CCN(Cc3cccc(OCC(=O)O)c3)CC2)c2ccccc21	10.1021/jm0498203
		CHEMBL373534	143185	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	436	10	1	5	4.5	CCOCCn1cc(C2CCN(Cc3cccc(OCC(=O)O)c3)CC2)c2ccccc21	10.1021/jm0498203
		5291	214216	120	None	-1	2	Human	5.7	pIC50	=	5.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	493	7	2	7	4.6	Cc1ccc(NC(=O)c2ccc(CN3CCN(C)CC3)cc2)cc1Nc1nccc(-c2cccnc2)n1	nan
		CHEMBL941	214216	120	None	-1	2	Human	5.7	pIC50	=	5.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	493	7	2	7	4.6	Cc1ccc(NC(=O)c2ccc(CN3CCN(C)CC3)cc2)cc1Nc1nccc(-c2cccnc2)n1	nan
		277	8083	62	None	-43	50	Human	6.7	pIC50	=	6.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	287	0	0	1	4.7	CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1	nan
		2913	8083	62	None	-43	50	Human	6.7	pIC50	=	6.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	287	0	0	1	4.7	CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1	nan
		765	8083	62	None	-43	50	Human	6.7	pIC50	=	6.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	287	0	0	1	4.7	CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1	nan
		CHEMBL516	8083	62	None	-43	50	Human	6.7	pIC50	=	6.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	287	0	0	1	4.7	CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1	nan
		DB00434	8083	62	None	-43	50	Human	6.7	pIC50	=	6.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	287	0	0	1	4.7	CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1	nan
		11730467	17800	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Inhibition of histamine H2 receptorInhibition of histamine H2 receptor	ChEMBL	476	10	0	2	6.0	O=C(CCCc1ccccc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1	10.1021/jm010878g
		CHEMBL117537	17800	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Inhibition of histamine H2 receptorInhibition of histamine H2 receptor	ChEMBL	476	10	0	2	6.0	O=C(CCCc1ccccc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1	10.1021/jm010878g
		CHEMBL328512	218076	0	None	-	0	Rat	4.7	pIC50	=	4.7	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(N)=O	10.1021/jm00381a002
		CHEMBL96681	222697	0	None	-	0	Rat	4.7	pIC50	=	4.7	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL		None	None	None		CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CCC(=O)O)C(N)=O	10.1021/jm00381a002
		2398	7741	62	None	-13	29	Human	5.7	pIC50	=	5.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	314	4	0	2	4.5	CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C	nan
		2801	7741	62	None	-13	29	Human	5.7	pIC50	=	5.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	314	4	0	2	4.5	CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C	nan
		701	7741	62	None	-13	29	Human	5.7	pIC50	=	5.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	314	4	0	2	4.5	CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C	nan
		CHEMBL415	7741	62	None	-13	29	Human	5.7	pIC50	=	5.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	314	4	0	2	4.5	CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C	nan
		DB01242	7741	62	None	-13	29	Human	5.7	pIC50	=	5.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	314	4	0	2	4.5	CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C	nan
		11430513	91406	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	436	10	1	5	4.5	CCOCCn1cc(C2CCN(Cc3ccccc3OCC(=O)O)CC2)c2ccccc21	10.1021/jm0498203
		CHEMBL222217	91406	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	436	10	1	5	4.5	CCOCCn1cc(C2CCN(Cc3ccccc3OCC(=O)O)CC2)c2ccccc21	10.1021/jm0498203
		10140544	148417	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	478	9	1	6	4.4	O=C(O)c1ccccc1OCCN1CCC(c2cn(CCC3COCCO3)c3ccccc23)CC1	10.1021/jm0498203
		CHEMBL385311	148417	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	478	9	1	6	4.4	O=C(O)c1ccccc1OCCN1CCC(c2cn(CCC3COCCO3)c3ccccc23)CC1	10.1021/jm0498203
		11189839	91109	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	438	9	1	4	5.5	CCCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccc(F)cc21	10.1021/jm0498203
		CHEMBL221664	91109	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	438	9	1	4	5.5	CCCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccc(F)cc21	10.1021/jm0498203
		3823	56995	42	None	-66	11	Human	4.7	pIC50	=	4.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	530	7	0	7	4.2	CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1	nan
		76973198	56995	42	None	-66	11	Human	4.7	pIC50	=	4.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	530	7	0	7	4.2	CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1	nan
		CHEMBL157101	56995	42	None	-66	11	Human	4.7	pIC50	=	4.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	530	7	0	7	4.2	CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1	nan
		1235	10595	36	None	-2	5	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I]Aminopotentidine from human recombinant histamine H2 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Aminopotentidine from human recombinant histamine H2 receptor expressed in CHOK1 cells after 2 hrs	ChEMBL	312	6	4	6	-0.1	N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N	10.1016/j.bmcl.2013.01.025
		3959	10595	36	None	-2	5	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I]Aminopotentidine from human recombinant histamine H2 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Aminopotentidine from human recombinant histamine H2 receptor expressed in CHOK1 cells after 2 hrs	ChEMBL	312	6	4	6	-0.1	N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N	10.1016/j.bmcl.2013.01.025
		50287	10595	36	None	-2	5	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I]Aminopotentidine from human recombinant histamine H2 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Aminopotentidine from human recombinant histamine H2 receptor expressed in CHOK1 cells after 2 hrs	ChEMBL	312	6	4	6	-0.1	N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N	10.1016/j.bmcl.2013.01.025
		CHEMBL269646	10595	36	None	-2	5	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I]Aminopotentidine from human recombinant histamine H2 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Aminopotentidine from human recombinant histamine H2 receptor expressed in CHOK1 cells after 2 hrs	ChEMBL	312	6	4	6	-0.1	N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N	10.1016/j.bmcl.2013.01.025
		11166846	91076	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	450	10	1	5	4.9	CCOCCn1cc(C2CCN(CCOc3ccc(C)cc3C(=O)O)CC2)c2ccccc21	10.1021/jm0498203
		CHEMBL221462	91076	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	450	10	1	5	4.9	CCOCCn1cc(C2CCN(CCOc3ccc(C)cc3C(=O)O)CC2)c2ccccc21	10.1021/jm0498203
		1971	9641	38	None	-22	30	Human	5.6	pIC50	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	263	3	1	1	3.8	CNCCC=C1c2ccccc2CCc2c1cccc2	nan
		2404	9641	38	None	-22	30	Human	5.6	pIC50	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	263	3	1	1	3.8	CNCCC=C1c2ccccc2CCc2c1cccc2	nan
		4543	9641	38	None	-22	30	Human	5.6	pIC50	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	263	3	1	1	3.8	CNCCC=C1c2ccccc2CCc2c1cccc2	nan
		CHEMBL445	9641	38	None	-22	30	Human	5.6	pIC50	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	263	3	1	1	3.8	CNCCC=C1c2ccccc2CCc2c1cccc2	nan
		DB00540	9641	38	None	-22	30	Human	5.6	pIC50	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	263	3	1	1	3.8	CNCCC=C1c2ccccc2CCc2c1cccc2	nan
		CHEMBL44345	220701	0	None	-	0	Rat	4.6	pIC50	=	4.6	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(N)=O	10.1021/jm00381a002
		2060890	209827	34	None	-	0	Rat	3.6	pIC50	=	3.6	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL	342	5	3	2	3.2	O=C(N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)c1ccc(Cl)cc1	10.1021/jm00381a002
		CHEMBL63544	209827	34	None	-	0	Rat	3.6	pIC50	=	3.6	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL	342	5	3	2	3.2	O=C(N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)c1ccc(Cl)cc1	10.1021/jm00381a002
		2281	9949	82	None	-	0	Rat	2.6	pIC50	=	2.6	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL	334	10	2	3	2.3	CCCN(C(=O)C(NC(=O)c1ccccc1)CCC(=O)O)CCC	10.1021/jm00381a002
		4922	9949	82	None	-	0	Rat	2.6	pIC50	=	2.6	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL	334	10	2	3	2.3	CCCN(C(=O)C(NC(=O)c1ccccc1)CCC(=O)O)CCC	10.1021/jm00381a002
		893	9949	82	None	-	0	Rat	2.6	pIC50	=	2.6	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL	334	10	2	3	2.3	CCCN(C(=O)C(NC(=O)c1ccccc1)CCC(=O)O)CCC	10.1021/jm00381a002
		CHEMBL316561	9949	82	None	-	0	Rat	2.6	pIC50	=	2.6	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL	334	10	2	3	2.3	CCCN(C(=O)C(NC(=O)c1ccccc1)CCC(=O)O)CCC	10.1021/jm00381a002
		DB13431	9949	82	None	-	0	Rat	2.6	pIC50	=	2.6	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL	334	10	2	3	2.3	CCCN(C(=O)C(NC(=O)c1ccccc1)CCC(=O)O)CCC	10.1021/jm00381a002
		2520	210787	70	None	-20	12	Human	5.6	pIC50	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	454	13	0	6	5.1	COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC	nan
		CHEMBL1280	210787	70	None	-20	12	Human	5.6	pIC50	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	454	13	0	6	5.1	COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC	nan
		CHEMBL6966	210787	70	None	-20	12	Human	5.6	pIC50	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	454	13	0	6	5.1	COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC	nan
		11293983	91066	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	454	10	1	5	4.8	CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccc(F)cc21	10.1021/jm0498203
		CHEMBL221413	91066	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	454	10	1	5	4.8	CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccc(F)cc21	10.1021/jm0498203
		2726	7706	68	None	-85	72	Human	5.6	pIC50	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	nan
		621	7706	68	None	-85	72	Human	5.6	pIC50	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	nan
		83	7706	68	None	-85	72	Human	5.6	pIC50	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	nan
		CHEMBL71	7706	68	None	-85	72	Human	5.6	pIC50	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	nan
		DB00477	7706	68	None	-85	72	Human	5.6	pIC50	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	nan
		118139356	186502	28	None	-	0	Human	4.6	pIC50	=	4.6	Binding	Antagonist activity at human H2 receptorAntagonist activity at human H2 receptor	ChEMBL	435	7	2	7	3.2	Cc1cc(-c2ccnc(Nc3cnn(C)c3)n2)ccc1CNC(=O)N1CC(OC(C)C)C1	10.1021/acs.jmedchem.0c00702
		CHEMBL4744041	186502	28	None	-	0	Human	4.6	pIC50	=	4.6	Binding	Antagonist activity at human H2 receptorAntagonist activity at human H2 receptor	ChEMBL	435	7	2	7	3.2	Cc1cc(-c2ccnc(Nc3cnn(C)c3)n2)ccc1CNC(=O)N1CC(OC(C)C)C1	10.1021/acs.jmedchem.0c00702
		1231	7724	116	None	-4	8	Human	6.6	pIC50	=	6.6	Binding	Binding affinity to human histamine H2 receptor by radioligand displacement assayBinding affinity to human histamine H2 receptor by radioligand displacement assay	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.bmc.2013.03.016
		2756	7724	116	None	-4	8	Human	6.6	pIC50	=	6.6	Binding	Binding affinity to human histamine H2 receptor by radioligand displacement assayBinding affinity to human histamine H2 receptor by radioligand displacement assay	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.bmc.2013.03.016
		645	7724	116	None	-4	8	Human	6.6	pIC50	=	6.6	Binding	Binding affinity to human histamine H2 receptor by radioligand displacement assayBinding affinity to human histamine H2 receptor by radioligand displacement assay	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.bmc.2013.03.016
		CHEMBL30	7724	116	None	-4	8	Human	6.6	pIC50	=	6.6	Binding	Binding affinity to human histamine H2 receptor by radioligand displacement assayBinding affinity to human histamine H2 receptor by radioligand displacement assay	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.bmc.2013.03.016
		DB00501	7724	116	None	-4	8	Human	6.6	pIC50	=	6.6	Binding	Binding affinity to human histamine H2 receptor by radioligand displacement assayBinding affinity to human histamine H2 receptor by radioligand displacement assay	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.bmc.2013.03.016
		18609376	211138	63	None	-	1	Human	4.6	pIC50	=	4.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	386	2	0	4	4.7	CC(=O)O[C@]1(C(C)=O)CC[C@H]2[C@@H]3C[C@H](C)C4=CC(=O)CC[C@]4(C)[C@H]3CC[C@@]21C	nan
		6279	211138	63	None	-	1	Human	4.6	pIC50	=	4.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	386	2	0	4	4.7	CC(=O)O[C@]1(C(C)=O)CC[C@H]2[C@@H]3C[C@H](C)C4=CC(=O)CC[C@]4(C)[C@H]3CC[C@@]21C	nan
		CHEMBL717	211138	63	None	-	1	Human	4.6	pIC50	=	4.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	386	2	0	4	4.7	CC(=O)O[C@]1(C(C)=O)CC[C@H]2[C@@H]3C[C@H](C)C4=CC(=O)CC[C@]4(C)[C@H]3CC[C@@]21C	nan
		2284	9956	33	None	-53	29	Human	5.5	pIC50	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	284	4	0	3	4.2	CN(CCCN1c2ccccc2Sc2c1cccc2)C	nan
		4926	9956	33	None	-53	29	Human	5.5	pIC50	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	284	4	0	3	4.2	CN(CCCN1c2ccccc2Sc2c1cccc2)C	nan
		7281	9956	33	None	-53	29	Human	5.5	pIC50	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	284	4	0	3	4.2	CN(CCCN1c2ccccc2Sc2c1cccc2)C	nan
		CHEMBL564	9956	33	None	-53	29	Human	5.5	pIC50	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	284	4	0	3	4.2	CN(CCCN1c2ccccc2Sc2c1cccc2)C	nan
		DB00420	9956	33	None	-53	29	Human	5.5	pIC50	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	284	4	0	3	4.2	CN(CCCN1c2ccccc2Sc2c1cccc2)C	nan
		11443495	91125	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	504	10	1	5	5.7	CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccc(C(F)(F)F)cc21	10.1021/jm0498203
		CHEMBL221718	91125	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	504	10	1	5	5.7	CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccc(C(F)(F)F)cc21	10.1021/jm0498203
		10298838	175573	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	469	9	1	5	5.2	O=C(O)c1ccccc1OCCN1CCC(c2cn(CCc3ccccn3)c3ccccc23)CC1	10.1021/jm0498203
		CHEMBL437519	175573	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	469	9	1	5	5.2	O=C(O)c1ccccc1OCCN1CCC(c2cn(CCc3ccccn3)c3ccccc23)CC1	10.1021/jm0498203
		3191	109635	97	None	-24	25	Human	5.5	pIC50	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	469	9	0	3	7.2	CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1	nan
		CHEMBL305660	109635	97	None	-24	25	Human	5.5	pIC50	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	469	9	0	3	7.2	CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1	nan
		10162727	91393	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	478	7	1	5	6.0	COc1ccc(CN2CCC(c3cn(Cc4cccs4)c4cc(F)ccc34)CC2)cc1C(=O)O	10.1021/jm0498203
		CHEMBL222139	91393	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	478	7	1	5	6.0	COc1ccc(CN2CCC(c3cn(Cc4cccs4)c4cc(F)ccc34)CC2)cc1C(=O)O	10.1021/jm0498203
		CHEMBL2370238	216590	0	None	-	0	Rat	4.5	pIC50	=	4.5	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL		None	None	None		CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N1CCCC[C@H]1C(=O)O	10.1021/jm00381a002
		CHEMBL262692	217324	0	None	-	0	Rat	4.5	pIC50	=	4.5	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(N)=O	10.1021/jm00381a002
		CHEMBL289310	217650	0	None	-	0	Rat	4.5	pIC50	=	4.5	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(N)=O	10.1021/jm00381a002
		CHEMBL318221	217991	0	None	-	0	Rat	4.5	pIC50	=	4.5	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL		None	None	None		CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)O	10.1021/jm00381a002
		CHEMBL91765	222683	0	None	-	0	Rat	4.5	pIC50	=	4.5	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL		None	None	None		CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(N)=O	10.1021/jm00381a002
		11211919	91528	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	406	8	1	4	4.8	CCOCCn1cc(C2CCN(Cc3ccccc3C(=O)O)CC2)c2ccccc21	10.1021/jm0498203
		CHEMBL222984	91528	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	406	8	1	4	4.8	CCOCCn1cc(C2CCN(Cc3ccccc3C(=O)O)CC2)c2ccccc21	10.1021/jm0498203
		10279311	91126	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	512	7	1	5	6.6	COc1ccc(CN2CCC(c3cn(Cc4ccc(Cl)s4)c4cc(F)ccc34)CC2)cc1C(=O)O	10.1021/jm0498203
		CHEMBL221730	91126	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	512	7	1	5	6.6	COc1ccc(CN2CCC(c3cn(Cc4ccc(Cl)s4)c4cc(F)ccc34)CC2)cc1C(=O)O	10.1021/jm0498203
		1599	9120	50	None	-154	16	Human	5.5	pIC50	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	476	7	1	3	5.1	Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1	nan
		3955	9120	50	None	-154	16	Human	5.5	pIC50	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	476	7	1	3	5.1	Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1	nan
		7215	9120	50	None	-154	16	Human	5.5	pIC50	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	476	7	1	3	5.1	Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1	nan
		CHEMBL841	9120	50	None	-154	16	Human	5.5	pIC50	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	476	7	1	3	5.1	Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1	nan
		DB00836	9120	50	None	-154	16	Human	5.5	pIC50	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	476	7	1	3	5.1	Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1	nan
		11247939	143883	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	450	10	1	5	4.9	CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2cccc(C)c21	10.1021/jm0498203
		CHEMBL374754	143883	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	450	10	1	5	4.9	CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2cccc(C)c21	10.1021/jm0498203
		10226501	144652	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	460	7	1	5	5.8	COc1ccc(CN2CCC(c3cn(Cc4cccs4)c4ccccc34)CC2)cc1C(=O)O	10.1021/jm0498203
		CHEMBL376202	144652	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	460	7	1	5	5.8	COc1ccc(CN2CCC(c3cn(Cc4cccs4)c4ccccc34)CC2)cc1C(=O)O	10.1021/jm0498203
		11282005	72840	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	436	10	1	5	4.6	CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccccc21	10.1021/jm0498203
		CHEMBL183706	72840	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	436	10	1	5	4.6	CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccccc21	10.1021/jm0498203
		CHEMBL330142	218105	0	None	-	0	Rat	4.5	pIC50	=	4.5	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL		None	None	None		CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@H](CC(=O)O)C(N)=O	10.1021/jm00381a002
		237	211644	48	None	-3	13	Human	5.5	pIC50	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	399	9	1	4	6.0	CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12	nan
		CHEMBL546257	211644	48	None	-3	13	Human	5.5	pIC50	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	399	9	1	4	6.0	CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12	nan
		CHEMBL554190	211644	48	None	-3	13	Human	5.5	pIC50	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	399	9	1	4	6.0	CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12	nan
		CHEMBL7568	211644	48	None	-3	13	Human	5.5	pIC50	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	399	9	1	4	6.0	CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12	nan
		135398737	7745	93	None	-64	90	Human	5.4	pIC50	=	5.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	nan
		38	7745	93	None	-64	90	Human	5.4	pIC50	=	5.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	nan
		722	7745	93	None	-64	90	Human	5.4	pIC50	=	5.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	nan
		CHEMBL42	7745	93	None	-64	90	Human	5.4	pIC50	=	5.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	nan
		DB00363	7745	93	None	-64	90	Human	5.4	pIC50	=	5.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	nan
		11005810	17238	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Inhibition of histamine H2 receptorInhibition of histamine H2 receptor	ChEMBL	517	10	1	4	6.2	N#Cc1ccc(CCOC(=O)NC2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1	10.1021/jm010878g
		CHEMBL116463	17238	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Inhibition of histamine H2 receptorInhibition of histamine H2 receptor	ChEMBL	517	10	1	4	6.2	N#Cc1ccc(CCOC(=O)NC2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1	10.1021/jm010878g
		26987	7736	33	None	-177	21	Human	6.4	pIC50	=	6.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	343	6	0	2	5.1	Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C	nan
		6063	7736	33	None	-177	21	Human	6.4	pIC50	=	6.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	343	6	0	2	5.1	Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C	nan
		671	7736	33	None	-177	21	Human	6.4	pIC50	=	6.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	343	6	0	2	5.1	Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C	nan
		CHEMBL1626	7736	33	None	-177	21	Human	6.4	pIC50	=	6.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	343	6	0	2	5.1	Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C	nan
		DB00283	7736	33	None	-177	21	Human	6.4	pIC50	=	6.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	343	6	0	2	5.1	Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C	nan
		11212029	91394	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	410	7	1	4	4.5	COCCn1cc(C2CCN(Cc3cccc(C(=O)O)c3)CC2)c2ccc(F)cc21	10.1021/jm0498203
		CHEMBL222142	91394	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	410	7	1	4	4.5	COCCn1cc(C2CCN(Cc3cccc(C(=O)O)c3)CC2)c2ccc(F)cc21	10.1021/jm0498203
		11259138	91787	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	436	10	1	5	4.5	CCOCCn1cc(C2CCN(Cc3ccc(OCC(=O)O)cc3)CC2)c2ccccc21	10.1021/jm0498203
		CHEMBL223882	91787	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	436	10	1	5	4.5	CCOCCn1cc(C2CCN(Cc3ccc(OCC(=O)O)cc3)CC2)c2ccccc21	10.1021/jm0498203
		4011	89183	49	None	-27	24	Human	6.4	pIC50	=	6.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	277	4	1	1	4.2	CNCCCC12CCC(c3ccccc31)c1ccccc12	nan
		CHEMBL21731	89183	49	None	-27	24	Human	6.4	pIC50	=	6.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	277	4	1	1	4.2	CNCCCC12CCC(c3ccccc31)c1ccccc12	nan
		CHEMBL94917	222694	0	None	-	0	Rat	4.4	pIC50	=	4.4	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL		None	None	None		CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OCc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(N)=O	10.1021/jm00381a002
		1530	8963	50	None	-151	21	Human	5.4	pIC50	=	5.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	309	0	0	3	4.0	CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1	nan
		3827	8963	50	None	-151	21	Human	5.4	pIC50	=	5.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	309	0	0	3	4.0	CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1	nan
		7206	8963	50	None	-151	21	Human	5.4	pIC50	=	5.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	309	0	0	3	4.0	CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1	nan
		CHEMBL534	8963	50	None	-151	21	Human	5.4	pIC50	=	5.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	309	0	0	3	4.0	CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1	nan
		DB00920	8963	50	None	-151	21	Human	5.4	pIC50	=	5.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	309	0	0	3	4.0	CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1	nan
		1129	8402	96	None	-1	2	Human	7.4	pIC50	=	7.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	nan
		3325	8402	96	None	-1	2	Human	7.4	pIC50	=	7.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	nan
		5353622	8402	96	None	-1	2	Human	7.4	pIC50	=	7.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	nan
		5702160	8402	96	None	-1	2	Human	7.4	pIC50	=	7.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	nan
		7074	8402	96	None	-1	2	Human	7.4	pIC50	=	7.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	nan
		CHEMBL902	8402	96	None	-1	2	Human	7.4	pIC50	=	7.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	nan
		DB00927	8402	96	None	-1	2	Human	7.4	pIC50	=	7.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	nan
		10161929	143965	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	464	9	1	6	4.4	O=C(O)c1ccccc1OCCN1CCC(c2cn(CCC3OCCO3)c3ccccc23)CC1	10.1021/jm0498203
		CHEMBL374869	143965	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	464	9	1	6	4.4	O=C(O)c1ccccc1OCCN1CCC(c2cn(CCC3OCCO3)c3ccccc23)CC1	10.1021/jm0498203
		1231	7724	116	None	-4	8	Human	6.3	pIC50	=	6.3	Binding	Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation counting	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1021/acs.jmedchem.6b01422
		2756	7724	116	None	-4	8	Human	6.3	pIC50	=	6.3	Binding	Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation counting	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1021/acs.jmedchem.6b01422
		645	7724	116	None	-4	8	Human	6.3	pIC50	=	6.3	Binding	Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation counting	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1021/acs.jmedchem.6b01422
		CHEMBL30	7724	116	None	-4	8	Human	6.3	pIC50	=	6.3	Binding	Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation counting	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1021/acs.jmedchem.6b01422
		DB00501	7724	116	None	-4	8	Human	6.3	pIC50	=	6.3	Binding	Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation counting	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1021/acs.jmedchem.6b01422
		11238716	91067	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	592	10	1	5	6.2	CCOCCn1cc(C2CCN(CCOc3c(Br)cc(Br)cc3C(=O)O)CC2)c2ccccc21	10.1021/jm0498203
		CHEMBL221414	91067	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	592	10	1	5	6.2	CCOCCn1cc(C2CCN(CCOc3c(Br)cc(Br)cc3C(=O)O)CC2)c2ccccc21	10.1021/jm0498203
		10204866	91511	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	460	8	1	5	5.7	O=C(O)c1ccccc1OCCN1CCC(c2cn(Cc3cccs3)c3ccccc23)CC1	10.1021/jm0498203
		CHEMBL222881	91511	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	460	8	1	5	5.7	O=C(O)c1ccccc1OCCN1CCC(c2cn(Cc3cccs3)c3ccccc23)CC1	10.1021/jm0498203
		11396873	143763	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	454	10	1	5	4.8	CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2cc(F)ccc21	10.1021/jm0498203
		CHEMBL374585	143763	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	454	10	1	5	4.8	CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2cc(F)ccc21	10.1021/jm0498203
		44326564	214651	0	None	-	0	Rat	4.3	pIC50	=	4.3	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL	531	12	6	6	1.6	CC(C)CC(NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(N)=O	10.1021/jm00381a002
		CHEMBL96530	214651	0	None	-	0	Rat	4.3	pIC50	=	4.3	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL	531	12	6	6	1.6	CC(C)CC(NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(N)=O	10.1021/jm00381a002
		CHEMBL1790763	215684	0	None	-	0	Rat	4.3	pIC50	=	4.3	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(N)=O	10.1021/jm00381a002
		2812	11551	101	None	-33	34	Human	5.3	pIC50	=	5.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	344	4	0	2	5.4	Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1	nan
		CHEMBL104	11551	101	None	-33	34	Human	5.3	pIC50	=	5.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	344	4	0	2	5.4	Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1	nan
		10478188	129720	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	436	9	1	5	4.8	CCOCCn1cc(C2CCN(Cc3ccc(OC)c(C(=O)O)c3)CC2)c2ccccc21	10.1021/jm0498203
		CHEMBL360712	129720	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	436	9	1	5	4.8	CCOCCn1cc(C2CCN(Cc3ccc(OC)c(C(=O)O)c3)CC2)c2ccccc21	10.1021/jm0498203
		1231	7724	116	None	-4	8	Human	5.3	pIC50	=	5.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	nan
		2756	7724	116	None	-4	8	Human	5.3	pIC50	=	5.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	nan
		645	7724	116	None	-4	8	Human	5.3	pIC50	=	5.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	nan
		CHEMBL30	7724	116	None	-4	8	Human	5.3	pIC50	=	5.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	nan
		DB00501	7724	116	None	-4	8	Human	5.3	pIC50	=	5.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	nan
		11363750	91405	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	484	8	1	4	5.5	CCOCCn1cc(C2CCN(Cc3cc(C(=O)O)ccc3Br)CC2)c2ccccc21	10.1021/jm0498203
		CHEMBL222214	91405	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	484	8	1	4	5.5	CCOCCn1cc(C2CCN(Cc3cc(C(=O)O)ccc3Br)CC2)c2ccccc21	10.1021/jm0498203
		11247290	143481	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	424	8	1	4	4.9	CCOCCn1cc(C2CCN(Cc3ccc(F)c(C(=O)O)c3)CC2)c2ccccc21	10.1021/jm0498203
		CHEMBL374059	143481	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	424	8	1	4	4.9	CCOCCn1cc(C2CCN(Cc3ccc(F)c(C(=O)O)c3)CC2)c2ccccc21	10.1021/jm0498203
		10273238	91529	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	414	6	1	4	5.4	O=C(O)c1cccc(CN2CCC(c3cn(Cc4ccco4)c4ccccc34)CC2)c1	10.1021/jm0498203
		CHEMBL222985	91529	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	414	6	1	4	5.4	O=C(O)c1cccc(CN2CCC(c3cn(Cc4ccco4)c4ccccc34)CC2)c1	10.1021/jm0498203
		11351801	91124	0	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	466	11	1	6	4.6	CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2cc(OC)ccc21	10.1021/jm0498203
		CHEMBL221716	91124	0	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	466	11	1	6	4.6	CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2cc(OC)ccc21	10.1021/jm0498203
		4189	213701	96	None	-36	34	Human	5.2	pIC50	=	5.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	414	6	0	3	6.5	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1	nan
		CHEMBL1559	213701	96	None	-36	34	Human	5.2	pIC50	=	5.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	414	6	0	3	6.5	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1	nan
		CHEMBL91	213701	96	None	-36	34	Human	5.2	pIC50	=	5.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	414	6	0	3	6.5	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1	nan
		9889248	91505	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	436	10	1	5	4.6	CCOCCn1cc(C2CCN(CCOc3ccc(C(=O)O)cc3)CC2)c2ccccc21	10.1021/jm0498203
		CHEMBL222853	91505	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	436	10	1	5	4.6	CCOCCn1cc(C2CCN(CCOc3ccc(C(=O)O)cc3)CC2)c2ccccc21	10.1021/jm0498203
		4601	213526	35	None	-7	17	Human	5.2	pIC50	=	5.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	269	6	0	2	3.7	Cc1ccccc1C(OCCN(C)C)c1ccccc1	nan
		CHEMBL1201023	213526	35	None	-7	17	Human	5.2	pIC50	=	5.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	269	6	0	2	3.7	Cc1ccccc1C(OCCN(C)C)c1ccccc1	nan
		CHEMBL900	213526	35	None	-7	17	Human	5.2	pIC50	=	5.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	269	6	0	2	3.7	Cc1ccccc1C(OCCN(C)C)c1ccccc1	nan
		CHEMBL91752	222682	0	None	-	0	Rat	4.2	pIC50	=	4.2	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(N)=O	10.1021/jm00381a002
		CHEMBL94448	222689	0	None	-	0	Rat	4.2	pIC50	=	4.2	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL		None	None	None		CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)O	10.1021/jm00381a002
		CHEMBL94902	222692	1	None	-	0	Rat	4.2	pIC50	=	4.2	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL		None	None	None		CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)O	10.1021/jm00381a002
		180	7189	56	None	-1412	40	Human	6.1	pIC50	=	6.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	nan
		200	7189	56	None	-1412	40	Human	6.1	pIC50	=	6.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	nan
		2160	7189	56	None	-1412	40	Human	6.1	pIC50	=	6.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	nan
		CHEMBL629	7189	56	None	-1412	40	Human	6.1	pIC50	=	6.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	nan
		DB00321	7189	56	None	-1412	40	Human	6.1	pIC50	=	6.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	nan
		10907460	16600	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Inhibition of histamine H2 receptorInhibition of histamine H2 receptor	ChEMBL	521	11	1	3	5.8	CCOc1ccc(CCNC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1	10.1021/jm010878g
		CHEMBL113956	16600	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Inhibition of histamine H2 receptorInhibition of histamine H2 receptor	ChEMBL	521	11	1	3	5.8	CCOc1ccc(CCNC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1	10.1021/jm010878g
		11340290	71138	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	466	11	1	6	4.6	CCOCCn1cc(C2CCN(CCOc3cc(OC)ccc3C(=O)O)CC2)c2ccccc21	10.1021/jm0498203
		CHEMBL181278	71138	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	466	11	1	6	4.6	CCOCCn1cc(C2CCN(CCOc3cc(OC)ccc3C(=O)O)CC2)c2ccccc21	10.1021/jm0498203
		1231	7724	116	None	-4	8	Human	6.1	pIC50	=	6.1	Binding	Inhibition of histamine H2 receptorInhibition of histamine H2 receptor	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1021/jm701575k
		2756	7724	116	None	-4	8	Human	6.1	pIC50	=	6.1	Binding	Inhibition of histamine H2 receptorInhibition of histamine H2 receptor	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1021/jm701575k
		645	7724	116	None	-4	8	Human	6.1	pIC50	=	6.1	Binding	Inhibition of histamine H2 receptorInhibition of histamine H2 receptor	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1021/jm701575k
		CHEMBL30	7724	116	None	-4	8	Human	6.1	pIC50	=	6.1	Binding	Inhibition of histamine H2 receptorInhibition of histamine H2 receptor	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1021/jm701575k
		DB00501	7724	116	None	-4	8	Human	6.1	pIC50	=	6.1	Binding	Inhibition of histamine H2 receptorInhibition of histamine H2 receptor	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1021/jm701575k
		1210	7705	51	None	-446	21	Human	5.1	pIC50	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	nan
		1213	7705	51	None	-446	21	Human	5.1	pIC50	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	nan
		2725	7705	51	None	-446	21	Human	5.1	pIC50	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	nan
		33036	7705	51	None	-446	21	Human	5.1	pIC50	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	nan
		4411	7705	51	None	-446	21	Human	5.1	pIC50	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	nan
		616	7705	51	None	-446	21	Human	5.1	pIC50	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	nan
		6976	7705	51	None	-446	21	Human	5.1	pIC50	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	nan
		716121	7705	51	None	-446	21	Human	5.1	pIC50	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	nan
		CHEMBL1201353	7705	51	None	-446	21	Human	5.1	pIC50	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	nan
		CHEMBL1554789	7705	51	None	-446	21	Human	5.1	pIC50	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	nan
		CHEMBL505	7705	51	None	-446	21	Human	5.1	pIC50	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	nan
		DB01114	7705	51	None	-446	21	Human	5.1	pIC50	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	nan
		DB13679	7705	51	None	-446	21	Human	5.1	pIC50	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	nan
		11328514	144636	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	454	10	1	5	4.8	CCOCCn1cc(C2CCN(CCOc3cccc(F)c3C(=O)O)CC2)c2ccccc21	10.1021/jm0498203
		CHEMBL376025	144636	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	454	10	1	5	4.8	CCOCCn1cc(C2CCN(CCOc3cccc(F)c3C(=O)O)CC2)c2ccccc21	10.1021/jm0498203
		9804849	74230	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Inhibitory concentration against Histamine H2 receptorInhibitory concentration against Histamine H2 receptor	ChEMBL	472	8	1	5	5.1	Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12	10.1021/jm050103y
		CHEMBL189118	74230	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Inhibitory concentration against Histamine H2 receptorInhibitory concentration against Histamine H2 receptor	ChEMBL	472	8	1	5	5.1	Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12	10.1021/jm050103y
		10139592	91779	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	462	8	1	5	5.4	O=C(O)c1ccccc1OCCN1CCC(c2cn(Cc3ccco3)c3cc(F)ccc23)CC1	10.1021/jm0498203
		CHEMBL223837	91779	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	462	8	1	5	5.4	O=C(O)c1ccccc1OCCN1CCC(c2cn(Cc3ccco3)c3cc(F)ccc23)CC1	10.1021/jm0498203
		11385692	143827	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	462	8	1	5	5.4	O=C(O)c1ccccc1OCCN1CCC(c2cn(Cc3ccoc3)c3cc(F)ccc23)CC1	10.1021/jm0498203
		CHEMBL374675	143827	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	462	8	1	5	5.4	O=C(O)c1ccccc1OCCN1CCC(c2cn(Cc3ccoc3)c3cc(F)ccc23)CC1	10.1021/jm0498203
		9802248	173022	0	None	-	0	Human	5.0	pIC50	=	5.0	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	420	9	1	4	5.4	CCCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccccc21	10.1021/jm0498203
		CHEMBL426786	173022	0	None	-	0	Human	5.0	pIC50	=	5.0	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	420	9	1	4	5.4	CCCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccccc21	10.1021/jm0498203
		1016	10519	78	None	-41	35	Human	5.0	pIC50	=	5.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	nan
		2561	10519	78	None	-41	35	Human	5.0	pIC50	=	5.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	nan
		2733526	10519	78	None	-41	35	Human	5.0	pIC50	=	5.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	nan
		5384	10519	78	None	-41	35	Human	5.0	pIC50	=	5.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	nan
		CHEMBL83	10519	78	None	-41	35	Human	5.0	pIC50	=	5.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	nan
		DB00675	10519	78	None	-41	35	Human	5.0	pIC50	=	5.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	nan
		100	10577	58	None	-46	54	Human	6.0	pIC50	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	nan
		2637	10577	58	None	-46	54	Human	6.0	pIC50	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	nan
		5452	10577	58	None	-46	54	Human	6.0	pIC50	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	nan
		CHEMBL479	10577	58	None	-46	54	Human	6.0	pIC50	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	nan
		DB00679	10577	58	None	-46	54	Human	6.0	pIC50	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	nan
		11202401	143885	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	478	11	1	6	4.8	CCOCCn1cc(C2CCN(CCOc3ccc(C(C)=O)cc3C(=O)O)CC2)c2ccccc21	10.1021/jm0498203
		CHEMBL374755	143885	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	478	11	1	6	4.8	CCOCCn1cc(C2CCN(CCOc3ccc(C(C)=O)cc3C(=O)O)CC2)c2ccccc21	10.1021/jm0498203
		133	9274	52	None	-141	43	Human	6.0	pIC50	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	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	9274	52	None	-141	43	Human	6.0	pIC50	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	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	9274	52	None	-141	43	Human	6.0	pIC50	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	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	9274	52	None	-141	43	Human	6.0	pIC50	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	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	9274	52	None	-141	43	Human	6.0	pIC50	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	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	222334	0	None	-	1	Human	6.0	pKd	=	6	Binding	Binding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysisBinding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
		CHEMBL5095891	222334	0	None	-	1	Human	6.0	pKd	=	6	Binding	Binding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysisBinding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
		CHEMBL5093461	222332	0	None	-	1	Human	7.0	pKd	=	7.0	Binding	Binding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysisBinding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysis	ChEMBL		None	None	None		CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2nnc(N)s2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1016/j.bmcl.2021.128388
		CHEMBL5095884	222332	0	None	-	1	Human	7.0	pKd	=	7.0	Binding	Binding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysisBinding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysis	ChEMBL		None	None	None		CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2nnc(N)s2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1016/j.bmcl.2021.128388
		126688	7192	33	None	-2	3	Rat	4.9	pKd	=	4.9	Binding	Affinity to the Histamine H2 receptor was determined expressed in CHO cell using [125I]iodoaminopotentidine as radioligandAffinity to the Histamine H2 receptor was determined expressed in CHO cell using [125I]iodoaminopotentidine as radioligand	ChEMBL	157	2	2	4	0.5	NCCc1sc(nc1C)N	10.1016/S0960-894X(01)80533-3
		4025	7192	33	None	-2	3	Rat	4.9	pKd	=	4.9	Binding	Affinity to the Histamine H2 receptor was determined expressed in CHO cell using [125I]iodoaminopotentidine as radioligandAffinity to the Histamine H2 receptor was determined expressed in CHO cell using [125I]iodoaminopotentidine as radioligand	ChEMBL	157	2	2	4	0.5	NCCc1sc(nc1C)N	10.1016/S0960-894X(01)80533-3
		CHEMBL293762	7192	33	None	-2	3	Rat	4.9	pKd	=	4.9	Binding	Affinity to the Histamine H2 receptor was determined expressed in CHO cell using [125I]iodoaminopotentidine as radioligandAffinity to the Histamine H2 receptor was determined expressed in CHO cell using [125I]iodoaminopotentidine as radioligand	ChEMBL	157	2	2	4	0.5	NCCc1sc(nc1C)N	10.1016/S0960-894X(01)80533-3
		1204	8713	119	None	-173	25	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.1c00692
		1247	8713	119	None	-173	25	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.1c00692
		1375	8713	119	None	-173	25	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.1c00692
		774	8713	119	None	-173	25	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.1c00692
		CHEMBL90	8713	119	None	-173	25	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.1c00692
		DB05381	8713	119	None	-173	25	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.1c00692
		119570	9933	96	None	-169	39	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	10.1021/acs.jmedchem.1c00692
		2233	9933	96	None	-169	39	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	10.1021/acs.jmedchem.1c00692
		953	9933	96	None	-169	39	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	10.1021/acs.jmedchem.1c00692
		CHEMBL301265	9933	96	None	-169	39	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	10.1021/acs.jmedchem.1c00692
		DB00413	9933	96	None	-169	39	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	10.1021/acs.jmedchem.1c00692
		168268716	199541	0	None	1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	372	3	4	4	3.5	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NC2CCCCC2)cc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5170276	199541	0	None	1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	372	3	4	4	3.5	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NC2CCCCC2)cc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5221176	199541	0	None	1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	372	3	4	4	3.5	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NC2CCCCC2)cc1	10.1021/acs.jmedchem.1c00692
		168268680	199545	0	None	1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	662	11	8	8	4.8	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5172675	199545	0	None	1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	662	11	8	8	4.8	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5221210	199545	0	None	1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	662	11	8	8	4.8	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1	10.1021/acs.jmedchem.1c00692
		168268827	199558	0	None	3	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	450	8	4	4	4.8	Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)c1	10.1021/acs.jmedchem.1c00692
		CHEMBL5179906	199558	0	None	3	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	450	8	4	4	4.8	Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)c1	10.1021/acs.jmedchem.1c00692
		CHEMBL5221314	199558	0	None	3	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	450	8	4	4	4.8	Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)c1	10.1021/acs.jmedchem.1c00692
		168268853	199564	0	None	-2	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	389	8	4	5	1.9	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5180504	199564	0	None	-2	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	389	8	4	5	1.9	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5221353	199564	0	None	-2	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	389	8	4	5	1.9	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
		168273471	199580	0	None	12	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	596	17	8	10	0.7	N/C(=N\C(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
		CHEMBL5173079	199580	0	None	12	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	596	17	8	10	0.7	N/C(=N\C(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
		CHEMBL5221433	199580	0	None	12	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	596	17	8	10	0.7	N/C(=N\C(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
		168273549	199582	0	None	1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	436	6	4	4	4.3	Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5174342	199582	0	None	1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	436	6	4	4	4.3	Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5221438	199582	0	None	1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	436	6	4	4	4.3	Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1	10.1021/acs.jmedchem.1c00692
		168273640	199584	0	None	-6	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	568	15	8	10	-0.1	N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
		CHEMBL5176229	199584	0	None	-6	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	568	15	8	10	-0.1	N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
		CHEMBL5221444	199584	0	None	-6	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	568	15	8	10	-0.1	N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
		168273745	199587	0	None	-13	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	332	6	4	4	1.5	N/C(=N\C(=O)NCc1ccccc1)NCCCc1cnc(N)s1	10.1021/acs.jmedchem.1c00692
		CHEMBL5178472	199587	0	None	-13	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	332	6	4	4	1.5	N/C(=N\C(=O)NCc1ccccc1)NCCCc1cnc(N)s1	10.1021/acs.jmedchem.1c00692
		CHEMBL5221451	199587	0	None	-13	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	332	6	4	4	1.5	N/C(=N\C(=O)NCc1ccccc1)NCCCc1cnc(N)s1	10.1021/acs.jmedchem.1c00692
		168274129	199588	0	None	-6	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	370	12	5	6	1.0	NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
		CHEMBL5176780	199588	0	None	-6	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	370	12	5	6	1.0	NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
		CHEMBL5221468	199588	0	None	-6	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	370	12	5	6	1.0	NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
		168275750	199605	0	None	-87	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	332	6	3	4	1.6	Cc1nnc(CCCN/C(N)=N/C(=O)NCc2ccccc2)s1	10.1021/acs.jmedchem.1c00692
		CHEMBL5175558	199605	0	None	-87	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	332	6	3	4	1.6	Cc1nnc(CCCN/C(N)=N/C(=O)NCc2ccccc2)s1	10.1021/acs.jmedchem.1c00692
		CHEMBL5221581	199605	0	None	-87	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	332	6	3	4	1.6	Cc1nnc(CCCN/C(N)=N/C(=O)NCc2ccccc2)s1	10.1021/acs.jmedchem.1c00692
		168276867	199614	0	None	-1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	662	11	8	8	4.8	Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)c1	10.1021/acs.jmedchem.1c00692
		CHEMBL5174278	199614	0	None	-1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	662	11	8	8	4.8	Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)c1	10.1021/acs.jmedchem.1c00692
		CHEMBL5221653	199614	0	None	-1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	662	11	8	8	4.8	Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)c1	10.1021/acs.jmedchem.1c00692
		168277996	199625	0	None	-20	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	380	4	4	4	3.3	Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCc2ccccc2)c1	10.1021/acs.jmedchem.1c00692
		CHEMBL5173373	199625	0	None	-20	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	380	4	4	4	3.3	Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCc2ccccc2)c1	10.1021/acs.jmedchem.1c00692
		CHEMBL5221736	199625	0	None	-20	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	380	4	4	4	3.3	Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCc2ccccc2)c1	10.1021/acs.jmedchem.1c00692
		168278471	199627	0	None	-18	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	312	8	4	4	1.5	CCCCCNC(=O)/N=C(\N)NCCCc1cnc(N)s1	10.1021/acs.jmedchem.1c00692
		CHEMBL5183205	199627	0	None	-18	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	312	8	4	4	1.5	CCCCCNC(=O)/N=C(\N)NCCCc1cnc(N)s1	10.1021/acs.jmedchem.1c00692
		CHEMBL5221757	199627	0	None	-18	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	312	8	4	4	1.5	CCCCCNC(=O)/N=C(\N)NCCCc1cnc(N)s1	10.1021/acs.jmedchem.1c00692
		168278543	199630	0	None	2	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	358	4	4	4	1.6	N/C(=N\C(=O)NCc1ccccc1)NCC1CCc2nc(N)sc2C1	10.1021/acs.jmedchem.1c00692
		CHEMBL5184846	199630	0	None	2	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	358	4	4	4	1.6	N/C(=N\C(=O)NCc1ccccc1)NCC1CCc2nc(N)sc2C1	10.1021/acs.jmedchem.1c00692
		CHEMBL5221764	199630	0	None	2	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	358	4	4	4	1.6	N/C(=N\C(=O)NCc1ccccc1)NCC1CCc2nc(N)sc2C1	10.1021/acs.jmedchem.1c00692
		168280339	199644	0	None	-52	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	372	8	3	5	1.1	C[C@@H](NC(=O)/N=C(\N)NCCCn1cc(CN(C)C)nn1)c1ccccc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5188592	199644	0	None	-52	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	372	8	3	5	1.1	C[C@@H](NC(=O)/N=C(\N)NCCCn1cc(CN(C)C)nn1)c1ccccc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5221885	199644	0	None	-52	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	372	8	3	5	1.1	C[C@@H](NC(=O)/N=C(\N)NCCCn1cc(CN(C)C)nn1)c1ccccc1	10.1021/acs.jmedchem.1c00692
		168281536	199660	0	None	-9	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	369	12	4	5	1.7	Cc1nnc(CCCN/C(N)=N/C(=O)NCCCCCCCCN)s1	10.1021/acs.jmedchem.1c00692
		CHEMBL5189006	199660	0	None	-9	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	369	12	4	5	1.7	Cc1nnc(CCCN/C(N)=N/C(=O)NCCCCCCCCN)s1	10.1021/acs.jmedchem.1c00692
		CHEMBL5221966	199660	0	None	-9	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	369	12	4	5	1.7	Cc1nnc(CCCN/C(N)=N/C(=O)NCCCCCCCCN)s1	10.1021/acs.jmedchem.1c00692
		168281746	199661	0	None	-676	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	365	6	4	5	1.6	CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1	10.1021/acs.jmedchem.1c00692
		CHEMBL5184911	199661	0	None	-676	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	365	6	4	5	1.6	CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1	10.1021/acs.jmedchem.1c00692
		CHEMBL5221974	199661	0	None	-676	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	365	6	4	5	1.6	CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1	10.1021/acs.jmedchem.1c00692
		168283097	199672	0	None	-22	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	311	9	4	5	0.8	CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)o1	10.1021/acs.jmedchem.1c00692
		CHEMBL5186770	199672	0	None	-22	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	311	9	4	5	0.8	CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)o1	10.1021/acs.jmedchem.1c00692
		CHEMBL5222043	199672	0	None	-22	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	311	9	4	5	0.8	CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)o1	10.1021/acs.jmedchem.1c00692
		168283321	199674	0	None	2	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	364	7	4	4	2.3	Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1	10.1021/acs.jmedchem.1c00692
		CHEMBL5183015	199674	0	None	2	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	364	7	4	4	2.3	Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1	10.1021/acs.jmedchem.1c00692
		CHEMBL5222057	199674	0	None	2	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	364	7	4	4	2.3	Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1	10.1021/acs.jmedchem.1c00692
		168283536	199679	0	None	-53	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	312	8	3	4	1.6	CCCCCNC(=O)/N=C(/N)NCCCc1nnc(C)s1	10.1021/acs.jmedchem.1c00692
		CHEMBL5187758	199679	0	None	-53	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	312	8	3	4	1.6	CCCCCNC(=O)/N=C(/N)NCCCc1nnc(C)s1	10.1021/acs.jmedchem.1c00692
		CHEMBL5222074	199679	0	None	-53	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	312	8	3	4	1.6	CCCCCNC(=O)/N=C(/N)NCCCc1nnc(C)s1	10.1021/acs.jmedchem.1c00692
		168284289	199685	0	None	1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	428	8	4	4	3.1	CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1	10.1021/acs.jmedchem.1c00692
		CHEMBL5194860	199685	0	None	1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	428	8	4	4	3.1	CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1	10.1021/acs.jmedchem.1c00692
		CHEMBL5222123	199685	0	None	1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	428	8	4	4	3.1	CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1	10.1021/acs.jmedchem.1c00692
		168284480	199689	0	None	-22	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	330	6	4	4	1.3	Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCc1ccccc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5197548	199689	0	None	-22	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	330	6	4	4	1.3	Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCc1ccccc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5222137	199689	0	None	-22	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	330	6	4	4	1.3	Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCc1ccccc1	10.1021/acs.jmedchem.1c00692
		168286141	199703	0	None	2	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	450	8	4	4	4.8	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)cc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5192993	199703	0	None	2	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	450	8	4	4	4.8	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)cc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5222231	199703	0	None	2	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	450	8	4	4	4.8	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)cc1	10.1021/acs.jmedchem.1c00692
		168286426	199705	0	None	-5	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	403	10	4	5	2.3	CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
		CHEMBL5198795	199705	0	None	-5	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	403	10	4	5	2.3	CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
		CHEMBL5222241	199705	0	None	-5	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	403	10	4	5	2.3	CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
		168290235	199747	0	None	-1737	20	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	315	6	4	3	1.1	C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5201074	199747	0	None	-1737	20	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	315	6	4	3	1.1	C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5222491	199747	0	None	-1737	20	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	315	6	4	3	1.1	C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1	10.1021/acs.jmedchem.1c00692
		168290815	199752	0	None	-537	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	327	9	4	5	1.2	CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
		CHEMBL5200771	199752	0	None	-537	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	327	9	4	5	1.2	CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
		CHEMBL5222529	199752	0	None	-537	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	327	9	4	5	1.2	CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
		168291233	199758	0	None	-5	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	373	8	4	5	1.4	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)o2)cc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5200106	199758	0	None	-5	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	373	8	4	5	1.4	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)o2)cc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5222556	199758	0	None	-5	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	373	8	4	5	1.4	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)o2)cc1	10.1021/acs.jmedchem.1c00692
		168292954	199776	0	None	-11	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	388	8	4	4	2.5	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5202592	199776	0	None	-11	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	388	8	4	4	2.5	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5222660	199776	0	None	-11	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	388	8	4	4	2.5	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
		168294161	199785	0	None	3	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	360	6	4	4	3.3	CCCCCNC(=O)/N=C(\N)Nc1cccc(-c2sc(N)nc2C)c1	10.1021/acs.jmedchem.1c00692
		CHEMBL5204739	199785	0	None	3	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	360	6	4	4	3.3	CCCCCNC(=O)/N=C(\N)Nc1cccc(-c2sc(N)nc2C)c1	10.1021/acs.jmedchem.1c00692
		CHEMBL5222742	199785	0	None	3	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	360	6	4	4	3.3	CCCCCNC(=O)/N=C(\N)Nc1cccc(-c2sc(N)nc2C)c1	10.1021/acs.jmedchem.1c00692
		168294445	199789	0	None	-1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	414	6	4	4	2.6	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCC2CCc3nc(N)sc3C2)cc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5208113	199789	0	None	-1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	414	6	4	4	2.6	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCC2CCc3nc(N)sc3C2)cc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5222768	199789	0	None	-1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	414	6	4	4	2.6	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCC2CCc3nc(N)sc3C2)cc1	10.1021/acs.jmedchem.1c00692
		168294166	199793	0	None	1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	360	6	4	4	3.3	CCCCCNC(=O)/N=C(\N)Nc1ccc(-c2sc(N)nc2C)cc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5209081	199793	0	None	1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	360	6	4	4	3.3	CCCCCNC(=O)/N=C(\N)Nc1ccc(-c2sc(N)nc2C)cc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5222775	199793	0	None	1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	360	6	4	4	3.3	CCCCCNC(=O)/N=C(\N)Nc1ccc(-c2sc(N)nc2C)cc1	10.1021/acs.jmedchem.1c00692
		168294449	199797	0	None	-6	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	367	7	4	5	1.9	CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1	10.1021/acs.jmedchem.1c00692
		CHEMBL5204599	199797	0	None	-6	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	367	7	4	5	1.9	CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1	10.1021/acs.jmedchem.1c00692
		CHEMBL5222793	199797	0	None	-6	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	367	7	4	5	1.9	CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1	10.1021/acs.jmedchem.1c00692
		168294767	199798	0	None	-117	20	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	313	8	4	5	0.9	CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
		CHEMBL5207281	199798	0	None	-117	20	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	313	8	4	5	0.9	CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
		CHEMBL5222802	199798	0	None	-117	20	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	313	8	4	5	0.9	CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
		168294770	199799	0	None	2	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	436	6	4	4	4.3	Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)cc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5208327	199799	0	None	2	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	436	6	4	4	4.3	Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)cc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5222806	199799	0	None	2	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	436	6	4	4	4.3	Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)cc1	10.1021/acs.jmedchem.1c00692
		168294776	199805	0	None	-7	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	366	7	3	4	2.6	Cc1nnc(CCCN/C(N)=N/C(=O)NCC(C)C2CCCCC2)s1	10.1021/acs.jmedchem.1c00692
		CHEMBL5209479	199805	0	None	-7	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	366	7	3	4	2.6	Cc1nnc(CCCN/C(N)=N/C(=O)NCC(C)C2CCCCC2)s1	10.1021/acs.jmedchem.1c00692
		CHEMBL5222831	199805	0	None	-7	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	366	7	3	4	2.6	Cc1nnc(CCCN/C(N)=N/C(=O)NCC(C)C2CCCCC2)s1	10.1021/acs.jmedchem.1c00692
		168295528	199810	0	None	-147	20	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	333	6	4	5	0.9	N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
		CHEMBL5206565	199810	0	None	-147	20	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	333	6	4	5	0.9	N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
		CHEMBL5222872	199810	0	None	-147	20	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	333	6	4	5	0.9	N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
		168294178	199814	0	None	1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	414	5	4	4	4.4	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)C2CCCCC2)cc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5205197	199814	0	None	1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	414	5	4	4	4.4	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)C2CCCCC2)cc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5222887	199814	0	None	1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	414	5	4	4	4.4	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)C2CCCCC2)cc1	10.1021/acs.jmedchem.1c00692
		168295541	199819	0	None	-851	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	347	6	4	5	1.4	C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5208845	199819	0	None	-851	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	347	6	4	5	1.4	C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5222926	199819	0	None	-851	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	347	6	4	5	1.4	C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1	10.1021/acs.jmedchem.1c00692
		168295543	199820	0	None	1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	380	4	4	4	3.3	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCc2ccccc2)cc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5209021	199820	0	None	1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	380	4	4	4	3.3	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCc2ccccc2)cc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5222929	199820	0	None	1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	380	4	4	4	3.3	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCc2ccccc2)cc1	10.1021/acs.jmedchem.1c00692
		168295803	199824	0	None	3	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	338	6	4	4	1.6	CCCCCNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1	10.1021/acs.jmedchem.1c00692
		CHEMBL5207206	199824	0	None	3	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	338	6	4	4	1.6	CCCCCNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1	10.1021/acs.jmedchem.1c00692
		CHEMBL5222937	199824	0	None	3	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	338	6	4	4	1.6	CCCCCNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1	10.1021/acs.jmedchem.1c00692
		168294182	199827	0	None	-3	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	314	6	4	2	1.7	C[C@@H](NC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5208722	199827	0	None	-3	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	314	6	4	2	1.7	C[C@@H](NC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5222960	199827	0	None	-3	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	314	6	4	2	1.7	C[C@@H](NC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1	10.1021/acs.jmedchem.1c00692
		156021166	185116	0	None	-	1	Human	7.9	pKd	=	7.9	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry	ChEMBL	908	25	3	8	10.3	C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21	10.1021/acsmedchemlett.0c00033
		CHEMBL4647775	185116	0	None	-	1	Human	7.9	pKd	=	7.9	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry	ChEMBL	908	25	3	8	10.3	C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21	10.1021/acsmedchemlett.0c00033
		CHEMBL4651205	185116	0	None	-	1	Human	7.9	pKd	=	7.9	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry	ChEMBL	908	25	3	8	10.3	C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21	10.1021/acsmedchemlett.0c00033
		156015793	185038	0	None	-	1	Human	6.9	pKd	=	6.9	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis	ChEMBL	880	23	3	8	9.5	C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21	10.1021/acsmedchemlett.0c00033
		CHEMBL4645867	185038	0	None	-	1	Human	6.9	pKd	=	6.9	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis	ChEMBL	880	23	3	8	9.5	C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21	10.1021/acsmedchemlett.0c00033
		CHEMBL4650701	185038	0	None	-	1	Human	6.9	pKd	=	6.9	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis	ChEMBL	880	23	3	8	9.5	C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21	10.1021/acsmedchemlett.0c00033
		156011186	185022	0	None	-	1	Human	7.8	pKd	=	7.8	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry	ChEMBL	704	20	2	7	7.5	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
		CHEMBL4637893	185022	0	None	-	1	Human	7.8	pKd	=	7.8	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry	ChEMBL	704	20	2	7	7.5	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
		CHEMBL4650588	185022	0	None	-	1	Human	7.8	pKd	=	7.8	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry	ChEMBL	704	20	2	7	7.5	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
		156021166	185116	0	None	-	1	Human	7.8	pKd	=	7.8	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis	ChEMBL	908	25	3	8	10.3	C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21	10.1021/acsmedchemlett.0c00033
		CHEMBL4647775	185116	0	None	-	1	Human	7.8	pKd	=	7.8	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis	ChEMBL	908	25	3	8	10.3	C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21	10.1021/acsmedchemlett.0c00033
		CHEMBL4651205	185116	0	None	-	1	Human	7.8	pKd	=	7.8	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis	ChEMBL	908	25	3	8	10.3	C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21	10.1021/acsmedchemlett.0c00033
		156015041	185012	0	None	-	1	Human	7.8	pKd	=	7.8	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis	ChEMBL	1029	30	3	11	10.0	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
		CHEMBL4637356	185012	0	None	-	1	Human	7.8	pKd	=	7.8	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis	ChEMBL	1029	30	3	11	10.0	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
		CHEMBL4650547	185012	0	None	-	1	Human	7.8	pKd	=	7.8	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis	ChEMBL	1029	30	3	11	10.0	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
		156015643	185074	0	None	-	1	Human	6.8	pKd	=	6.8	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis	ChEMBL	1001	28	3	11	9.2	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
		CHEMBL4645213	185074	0	None	-	1	Human	6.8	pKd	=	6.8	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis	ChEMBL	1001	28	3	11	9.2	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
		CHEMBL4650968	185074	0	None	-	1	Human	6.8	pKd	=	6.8	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis	ChEMBL	1001	28	3	11	9.2	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
		156015722	185052	0	None	-	1	Human	7.7	pKd	=	7.7	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry	ChEMBL	718	21	2	7	7.9	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
		CHEMBL4644467	185052	0	None	-	1	Human	7.7	pKd	=	7.7	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry	ChEMBL	718	21	2	7	7.9	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
		CHEMBL4650837	185052	0	None	-	1	Human	7.7	pKd	=	7.7	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry	ChEMBL	718	21	2	7	7.9	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
		CHEMBL5088914	222341	0	None	-	1	Human	6.6	pKd	=	6.6	Binding	Binding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysisBinding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
		CHEMBL5095949	222341	0	None	-	1	Human	6.6	pKd	=	6.6	Binding	Binding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysisBinding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
		44403829	78227	0	None	-	1	Human	6.6	pKd	=	6.6	Binding	Negative logarithm of the drug concentration against H2 histamine receptorNegative logarithm of the drug concentration against H2 histamine receptor	ChEMBL	743	15	4	7	5.3	CN1C(=O)[C@H](NC(=O)Nc2ccc(CC(=O)NCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)cc2)N=C(c2ccccc2)c2ccccc21	10.1021/jm058225d
		CHEMBL196143	78227	0	None	-	1	Human	6.6	pKd	=	6.6	Binding	Negative logarithm of the drug concentration against H2 histamine receptorNegative logarithm of the drug concentration against H2 histamine receptor	ChEMBL	743	15	4	7	5.3	CN1C(=O)[C@H](NC(=O)Nc2ccc(CC(=O)NCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)cc2)N=C(c2ccccc2)c2ccccc21	10.1021/jm058225d
		5105	183606	52	None	-	1	Human	6.6	pKd	=	6.6	Binding	Negative logarithm of the drug concentration against H2 histamine receptorNegative logarithm of the drug concentration against H2 histamine receptor	ChEMBL	348	9	1	5	2.1	CC(=O)OCC(=O)NCCCOc1cccc(CN2CCCCC2)c1	10.1021/jm058225d
		CHEMBL46102	183606	52	None	-	1	Human	6.6	pKd	=	6.6	Binding	Negative logarithm of the drug concentration against H2 histamine receptorNegative logarithm of the drug concentration against H2 histamine receptor	ChEMBL	348	9	1	5	2.1	CC(=O)OCC(=O)NCCCOc1cccc(CN2CCCCC2)c1	10.1021/jm058225d
		156015152	185085	0	None	-	1	Human	7.6	pKd	=	7.6	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry	ChEMBL	676	18	2	7	6.7	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
		CHEMBL4641916	185085	0	None	-	1	Human	7.6	pKd	=	7.6	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry	ChEMBL	676	18	2	7	6.7	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
		CHEMBL4651017	185085	0	None	-	1	Human	7.6	pKd	=	7.6	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry	ChEMBL	676	18	2	7	6.7	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
		156015793	185038	0	None	-	1	Human	6.5	pKd	=	6.5	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry	ChEMBL	880	23	3	8	9.5	C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21	10.1021/acsmedchemlett.0c00033
		CHEMBL4645867	185038	0	None	-	1	Human	6.5	pKd	=	6.5	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry	ChEMBL	880	23	3	8	9.5	C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21	10.1021/acsmedchemlett.0c00033
		CHEMBL4650701	185038	0	None	-	1	Human	6.5	pKd	=	6.5	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry	ChEMBL	880	23	3	8	9.5	C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21	10.1021/acsmedchemlett.0c00033
		156015633	185034	0	None	-	1	Human	7.5	pKd	=	7.5	Binding	Binding affinity to human H2R expressing Sf9 cells incubated for 60 mins by microbeta scintillation counter methodBinding affinity to human H2R expressing Sf9 cells incubated for 60 mins by microbeta scintillation counter method	ChEMBL	498	17	3	7	3.6	CCC(=O)NCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
		156020426	185034	0	None	-	1	Human	7.5	pKd	=	7.5	Binding	Binding affinity to human H2R expressing Sf9 cells incubated for 60 mins by microbeta scintillation counter methodBinding affinity to human H2R expressing Sf9 cells incubated for 60 mins by microbeta scintillation counter method	ChEMBL	498	17	3	7	3.6	CCC(=O)NCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
		CHEMBL4648685	185034	0	None	-	1	Human	7.5	pKd	=	7.5	Binding	Binding affinity to human H2R expressing Sf9 cells incubated for 60 mins by microbeta scintillation counter methodBinding affinity to human H2R expressing Sf9 cells incubated for 60 mins by microbeta scintillation counter method	ChEMBL	498	17	3	7	3.6	CCC(=O)NCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
		CHEMBL4650687	185034	0	None	-	1	Human	7.5	pKd	=	7.5	Binding	Binding affinity to human H2R expressing Sf9 cells incubated for 60 mins by microbeta scintillation counter methodBinding affinity to human H2R expressing Sf9 cells incubated for 60 mins by microbeta scintillation counter method	ChEMBL	498	17	3	7	3.6	CCC(=O)NCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
		CHEMBL5094663	222285	0	None	-	1	Human	7.5	pKd	=	7.5	Binding	Binding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysisBinding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](C)c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
		156014823	185106	0	None	-	1	Human	6.4	pKd	=	6.4	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis	ChEMBL	1109	31	4	13	9.2	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3cc(S(=O)(=O)O)ccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
		CHEMBL4641747	185106	0	None	-	1	Human	6.4	pKd	=	6.4	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis	ChEMBL	1109	31	4	13	9.2	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3cc(S(=O)(=O)O)ccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
		CHEMBL4651132	185106	0	None	-	1	Human	6.4	pKd	=	6.4	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis	ChEMBL	1109	31	4	13	9.2	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3cc(S(=O)(=O)O)ccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
		156015041	185012	0	None	-	1	Human	7.3	pKd	=	7.3	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry	ChEMBL	1029	30	3	11	10.0	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
		CHEMBL4637356	185012	0	None	-	1	Human	7.3	pKd	=	7.3	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry	ChEMBL	1029	30	3	11	10.0	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
		CHEMBL4650547	185012	0	None	-	1	Human	7.3	pKd	=	7.3	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry	ChEMBL	1029	30	3	11	10.0	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
		CHEMBL5075713	222308	0	None	-	1	Human	7.3	pKd	=	7.3	Binding	Binding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysisBinding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysis	ChEMBL		None	None	None		CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2c[nH]cn2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1016/j.bmcl.2021.128388
		CHEMBL5095559	222308	0	None	-	1	Human	7.3	pKd	=	7.3	Binding	Binding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysisBinding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysis	ChEMBL		None	None	None		CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2c[nH]cn2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1016/j.bmcl.2021.128388
		156015643	185074	0	None	-	1	Human	6.3	pKd	=	6.3	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry	ChEMBL	1001	28	3	11	9.2	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
		CHEMBL4645213	185074	0	None	-	1	Human	6.3	pKd	=	6.3	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry	ChEMBL	1001	28	3	11	9.2	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
		CHEMBL4650968	185074	0	None	-	1	Human	6.3	pKd	=	6.3	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry	ChEMBL	1001	28	3	11	9.2	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
		5039	69957	17	None	-	1	Human	7.2	pKd	=	7.2	Binding	Binding affinity to histamine H2 receptor (unknown origin)Binding affinity to histamine H2 receptor (unknown origin)	ChEMBL	314	10	2	7	1.5	CNC(=C[N+](=O)[O-])NCCSCc1ccc(CN(C)C)o1	10.1007/s00044-004-0012-z
		CHEMBL1790041	69957	17	None	-	1	Human	7.2	pKd	=	7.2	Binding	Binding affinity to histamine H2 receptor (unknown origin)Binding affinity to histamine H2 receptor (unknown origin)	ChEMBL	314	10	2	7	1.5	CNC(=C[N+](=O)[O-])NCCSCc1ccc(CN(C)C)o1	10.1007/s00044-004-0012-z
		156015722	185052	0	None	-	1	Human	7.2	pKd	=	7.2	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by imaging flow cytometry analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by imaging flow cytometry analysis	ChEMBL	718	21	2	7	7.9	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
		CHEMBL4644467	185052	0	None	-	1	Human	7.2	pKd	=	7.2	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by imaging flow cytometry analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by imaging flow cytometry analysis	ChEMBL	718	21	2	7	7.9	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
		CHEMBL4650837	185052	0	None	-	1	Human	7.2	pKd	=	7.2	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by imaging flow cytometry analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by imaging flow cytometry analysis	ChEMBL	718	21	2	7	7.9	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
		CHEMBL5083588	222313	0	None	-	1	Human	7.2	pKd	=	7.2	Binding	Binding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysisBinding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
		CHEMBL5095633	222313	0	None	-	1	Human	7.2	pKd	=	7.2	Binding	Binding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysisBinding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
		156015152	185085	0	None	-	1	Human	7.1	pKd	=	7.1	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis	ChEMBL	676	18	2	7	6.7	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
		CHEMBL4641916	185085	0	None	-	1	Human	7.1	pKd	=	7.1	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis	ChEMBL	676	18	2	7	6.7	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
		CHEMBL4651017	185085	0	None	-	1	Human	7.1	pKd	=	7.1	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis	ChEMBL	676	18	2	7	6.7	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
		3032915	22267	24	None	-25	7	Human	5.1	pKd	=	5.1	Binding	Binding affinity to histamine H2 receptor (unknown origin)Binding affinity to histamine H2 receptor (unknown origin)	ChEMBL	212	5	3	2	1.2	C/N=C(\S)NCCCCc1c[nH]cn1	10.1007/s00044-004-0012-z
		CHEMBL12160	22267	24	None	-25	7	Human	5.1	pKd	=	5.1	Binding	Binding affinity to histamine H2 receptor (unknown origin)Binding affinity to histamine H2 receptor (unknown origin)	ChEMBL	212	5	3	2	1.2	C/N=C(\S)NCCCCc1c[nH]cn1	10.1007/s00044-004-0012-z
		24824726	167888	1	None	-10232	6	Human	5.1	pKd	=	5.1	Binding	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	167888	1	None	-10232	6	Human	5.1	pKd	=	5.1	Binding	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	167888	1	None	-10232	6	Human	5.1	pKd	=	5.1	Binding	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	167888	1	None	-10232	6	Human	5.1	pKd	=	5.1	Binding	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	167888	1	None	-10232	6	Human	5.1	pKd	=	5.1	Binding	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	222315	0	None	-	1	Human	7.1	pKd	=	7.1	Binding	Binding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysisBinding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1	10.1016/j.bmcl.2021.128388
		CHEMBL5095695	222315	0	None	-	1	Human	7.1	pKd	=	7.1	Binding	Binding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysisBinding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1	10.1016/j.bmcl.2021.128388
		156015152	185085	0	None	-	1	Human	7.1	pKd	=	7.1	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by imaging flow cytometry analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by imaging flow cytometry analysis	ChEMBL	676	18	2	7	6.7	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
		CHEMBL4641916	185085	0	None	-	1	Human	7.1	pKd	=	7.1	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by imaging flow cytometry analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by imaging flow cytometry analysis	ChEMBL	676	18	2	7	6.7	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
		CHEMBL4651017	185085	0	None	-	1	Human	7.1	pKd	=	7.1	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by imaging flow cytometry analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by imaging flow cytometry analysis	ChEMBL	676	18	2	7	6.7	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
		156015722	185052	0	None	-	1	Human	7.1	pKd	=	7.1	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis	ChEMBL	718	21	2	7	7.9	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
		CHEMBL4644467	185052	0	None	-	1	Human	7.1	pKd	=	7.1	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis	ChEMBL	718	21	2	7	7.9	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
		CHEMBL4650837	185052	0	None	-	1	Human	7.1	pKd	=	7.1	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis	ChEMBL	718	21	2	7	7.9	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
		9990475	63251	0	None	-3	3	Rat	5.0	pKd	=	5.0	Binding	Affinity to the Histamine H2 receptor was determined expressed in CHO cell using [125I]iodoaminopotentidine as radioligandAffinity to the Histamine H2 receptor was determined expressed in CHO cell using [125I]iodoaminopotentidine as radioligand	ChEMBL	205	2	2	3	-0.5	Cc1nc(N)[se]c1CCN	10.1016/S0960-894X(01)80533-3
		CHEMBL1632408	63251	0	None	-3	3	Rat	5.0	pKd	=	5.0	Binding	Affinity to the Histamine H2 receptor was determined expressed in CHO cell using [125I]iodoaminopotentidine as radioligandAffinity to the Histamine H2 receptor was determined expressed in CHO cell using [125I]iodoaminopotentidine as radioligand	ChEMBL	205	2	2	3	-0.5	Cc1nc(N)[se]c1CCN	10.1016/S0960-894X(01)80533-3
		CHEMBL2448450	63251	0	None	-3	3	Rat	5.0	pKd	=	5.0	Binding	Affinity to the Histamine H2 receptor was determined expressed in CHO cell using [125I]iodoaminopotentidine as radioligandAffinity to the Histamine H2 receptor was determined expressed in CHO cell using [125I]iodoaminopotentidine as radioligand	ChEMBL	205	2	2	3	-0.5	Cc1nc(N)[se]c1CCN	10.1016/S0960-894X(01)80533-3
		9805944	63001	37	None	-2	9	Human	8.8	pKi	=	8.8	Binding	Displacement of [3H]tiotidine from human histamine H2 receptorDisplacement of [3H]tiotidine from human histamine H2 receptor	ChEMBL	462	7	2	3	4.7	CNC(=O)C(CCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1	10.1021/jm800510m
		CHEMBL1627	63001	37	None	-2	9	Human	8.8	pKi	=	8.8	Binding	Displacement of [3H]tiotidine from human histamine H2 receptorDisplacement of [3H]tiotidine from human histamine H2 receptor	ChEMBL	462	7	2	3	4.7	CNC(=O)C(CCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1	10.1021/jm800510m
		164622259	192509	0	None	2290	4	Human	8.0	pKi	=	8.0	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	336	6	4	5	1.4	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCc1ccco1	10.1016/j.ejmech.2021.113190
		CHEMBL4865965	192509	0	None	2290	4	Human	8.0	pKi	=	8.0	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	336	6	4	5	1.4	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCc1ccco1	10.1016/j.ejmech.2021.113190
		164610648	191617	0	None	87	4	Human	7.0	pKi	=	7	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	374	7	4	4	2.4	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC[C@H](C)c1ccccc1	10.1016/j.ejmech.2021.113190
		CHEMBL4852212	191617	0	None	87	4	Human	7.0	pKi	=	7	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	374	7	4	4	2.4	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC[C@H](C)c1ccccc1	10.1016/j.ejmech.2021.113190
		44334025	11319	0	None	-269	3	Human	6.0	pKi	=	6	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	462	10	1	5	3.8	O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccccc3Cl)C2)cc1)C1CC1	10.1016/s0960-894x(02)00685-6
		CHEMBL102384	11319	0	None	-269	3	Human	6.0	pKi	=	6	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	462	10	1	5	3.8	O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccccc3Cl)C2)cc1)C1CC1	10.1016/s0960-894x(02)00685-6
		44334781	12178	0	None	-346	3	Human	6.0	pKi	=	6	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	458	11	1	6	3.1	COc1ccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)cc1	10.1016/s0960-894x(02)00685-6
		CHEMBL107162	12178	0	None	-346	3	Human	6.0	pKi	=	6	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	458	11	1	6	3.1	COc1ccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)cc1	10.1016/s0960-894x(02)00685-6
		33630	185736	99	None	-13	28	Human	6.0	pKi	=	6	Binding	Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assay	ChEMBL	523	7	1	2	7.5	OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1	10.1016/j.bmcl.2018.10.036
		CHEMBL47050	185736	99	None	-13	28	Human	6.0	pKi	=	6	Binding	Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assay	ChEMBL	523	7	1	2	7.5	OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1	10.1016/j.bmcl.2018.10.036
		4023	6986	24	None	-3467	4	Human	5.0	pKi	=	5	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	349	7	0	4	3.6	N#Cc1ccc(cc1)c1ccc(cc1)OCCCN1CC[C@H](C1)N(C)C	10.1016/s0960-894x(02)00648-0
		9884746	6986	24	None	-3467	4	Human	5.0	pKi	=	5	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	349	7	0	4	3.6	N#Cc1ccc(cc1)c1ccc(cc1)OCCCN1CC[C@H](C1)N(C)C	10.1016/s0960-894x(02)00648-0
		CHEMBL319000	6986	24	None	-3467	4	Human	5.0	pKi	=	5	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	349	7	0	4	3.6	N#Cc1ccc(cc1)c1ccc(cc1)OCCCN1CC[C@H](C1)N(C)C	10.1016/s0960-894x(02)00648-0
		44335456	11325	0	None	-316	4	Human	5.0	pKi	=	5	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	336	6	1	4	3.5	N#Cc1ccc(-c2ccc(OCCCN3CCC(O)CC3)cc2)cc1	10.1016/s0960-894x(02)00648-0
		CHEMBL102416	11325	0	None	-316	4	Human	5.0	pKi	=	5	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	336	6	1	4	3.5	N#Cc1ccc(-c2ccc(OCCCN3CCC(O)CC3)cc2)cc1	10.1016/s0960-894x(02)00648-0
		10268636	12055	0	None	-1174	4	Human	5.0	pKi	=	5	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	335	7	1	4	3.3	CN[C@@H]1CCN(CCCOc2ccc(-c3ccc(C#N)cc3)cc2)C1	10.1016/s0960-894x(02)00648-0
		CHEMBL106545	12055	0	None	-1174	4	Human	5.0	pKi	=	5	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	335	7	1	4	3.3	CN[C@@H]1CCN(CCCOc2ccc(-c3ccc(C#N)cc3)cc2)C1	10.1016/s0960-894x(02)00648-0
		44304327	207661	0	None	-2511	3	Human	5.0	pKi	=	5	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	535	11	1	6	4.3	CC(C)(C)OC(=O)N[C@H](Cc1ccccc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		CHEMBL60143	207661	0	None	-2511	3	Human	5.0	pKi	=	5	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	535	11	1	6	4.3	CC(C)(C)OC(=O)N[C@H](Cc1ccccc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		44304295	209648	0	None	-2290	3	Human	5.0	pKi	=	5	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	357	8	1	5	1.5	O=C1C[C@@H](N2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)CC2)N1	10.1016/s0960-894x(02)00310-4
		CHEMBL62596	209648	0	None	-2290	3	Human	5.0	pKi	=	5	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	357	8	1	5	1.5	O=C1C[C@@H](N2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)CC2)N1	10.1016/s0960-894x(02)00310-4
		44304331	209900	0	None	-2187	3	Human	5.0	pKi	=	5	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	449	11	1	5	3.2	N[C@H](CCc1ccccc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		CHEMBL64059	209900	0	None	-2187	3	Human	5.0	pKi	=	5	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	449	11	1	5	3.2	N[C@H](CCc1ccccc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		44275807	105746	0	None	-9120	10	Human	5.0	pKi	=	5	Binding	Binding affinity towards human histaminergic (H2) receptorBinding affinity towards human histaminergic (H2) receptor	ChEMBL	422	7	0	4	4.5	C[C@H]1CC[C@H](C)N1CCCOc1ccc(-c2ccc(C(=O)N3CCOCC3)cc2)cc1	10.1016/s0960-894x(03)00118-5
		CHEMBL27979	105746	0	None	-9120	10	Human	5.0	pKi	=	5	Binding	Binding affinity towards human histaminergic (H2) receptorBinding affinity towards human histaminergic (H2) receptor	ChEMBL	422	7	0	4	4.5	C[C@H]1CC[C@H](C)N1CCCOc1ccc(-c2ccc(C(=O)N3CCOCC3)cc2)cc1	10.1016/s0960-894x(03)00118-5
		10422468	210937	0	None	-501	3	Human	5.0	pKi	=	5	Binding	Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors	ChEMBL	254	7	3	2	2.4	CC(C)/N=C(\S)NCCCCCc1c[nH]cn1	10.1021/jm00012a025
		CHEMBL70603	210937	0	None	-501	3	Human	5.0	pKi	=	5	Binding	Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors	ChEMBL	254	7	3	2	2.4	CC(C)/N=C(\S)NCCCCCc1c[nH]cn1	10.1021/jm00012a025
		10466840	211260	0	None	-1000	4	Human	5.0	pKi	=	5	Binding	Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors	ChEMBL	240	7	3	2	2.0	CC/N=C(\S)NCCCCCc1c[nH]cn1	10.1021/jm00012a025
		CHEMBL72424	211260	0	None	-1000	4	Human	5.0	pKi	=	5	Binding	Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors	ChEMBL	240	7	3	2	2.0	CC/N=C(\S)NCCCCCc1c[nH]cn1	10.1021/jm00012a025
		9990475	63251	0	None	-3	3	Human	5.0	pKi	=	5	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	205	2	2	3	-0.5	Cc1nc(N)[se]c1CCN	10.1016/j.bmcl.2010.10.041
		CHEMBL1632408	63251	0	None	-3	3	Human	5.0	pKi	=	5	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	205	2	2	3	-0.5	Cc1nc(N)[se]c1CCN	10.1016/j.bmcl.2010.10.041
		CHEMBL2448450	63251	0	None	-3	3	Human	5.0	pKi	=	5	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	205	2	2	3	-0.5	Cc1nc(N)[se]c1CCN	10.1016/j.bmcl.2010.10.041
		10466840	211260	0	None	-1000	4	Human	5.0	pKi	=	5	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	240	7	3	2	2.0	CC/N=C(\S)NCCCCCc1c[nH]cn1	10.1016/j.bmcl.2010.10.041
		CHEMBL72424	211260	0	None	-1000	4	Human	5.0	pKi	=	5	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	240	7	3	2	2.0	CC/N=C(\S)NCCCCCc1c[nH]cn1	10.1016/j.bmcl.2010.10.041
		44334252	11320	0	None	-323	3	Human	4.0	pKi	=	4	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	449	10	3	7	1.7	CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)[C@@H](CO)NC(=O)OC(C)(C)C)C2)cc1	10.1016/s0960-894x(02)00685-6
		CHEMBL102390	11320	0	None	-323	3	Human	4.0	pKi	=	4	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	449	10	3	7	1.7	CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)[C@@H](CO)NC(=O)OC(C)(C)C)C2)cc1	10.1016/s0960-894x(02)00685-6
		44335350	11852	0	None	-389	3	Human	4.0	pKi	=	4	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	398	8	0	5	3.9	CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc(OC)cc3)cc2)CC1	10.1016/s0960-894x(02)00648-0
		CHEMBL105483	11852	0	None	-389	3	Human	4.0	pKi	=	4	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	398	8	0	5	3.9	CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc(OC)cc3)cc2)CC1	10.1016/s0960-894x(02)00648-0
		44304211	108974	0	None	-19054	3	Human	4.0	pKi	=	4	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	373	9	1	5	1.9	CC[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		CHEMBL302829	108974	0	None	-19054	3	Human	4.0	pKi	=	4	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	373	9	1	5	1.9	CC[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		10451094	209252	0	None	-199526	3	Human	4.0	pKi	=	4	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	359	9	1	5	1.5	NCCC(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		CHEMBL61120	209252	0	None	-199526	3	Human	4.0	pKi	=	4	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	359	9	1	5	1.5	NCCC(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		29298	210229	1	None	-1047	4	Human	5.0	pKi	=	5.0	Binding	Compound was tested for its binding affinity towards human H2 receptorCompound was tested for its binding affinity towards human H2 receptor	ChEMBL	297	5	1	3	3.9	CN(C)CCCNc1c2c(nc3ccccc13)CCCCC2	10.1016/s0960-894x(03)00356-1
		CHEMBL65849	210229	1	None	-1047	4	Human	5.0	pKi	=	5.0	Binding	Compound was tested for its binding affinity towards human H2 receptorCompound was tested for its binding affinity towards human H2 receptor	ChEMBL	297	5	1	3	3.9	CN(C)CCCNc1c2c(nc3ccccc13)CCCCC2	10.1016/s0960-894x(03)00356-1
		164614645	191911	0	None	57	4	Human	7.0	pKi	=	7.0	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	402	8	4	4	3.0	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(c1ccccc1)C(C)C	10.1016/j.ejmech.2021.113190
		CHEMBL4856572	191911	0	None	57	4	Human	7.0	pKi	=	7.0	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	402	8	4	4	3.0	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(c1ccccc1)C(C)C	10.1016/j.ejmech.2021.113190
		164622886	192721	0	None	93	4	Human	7.0	pKi	=	7.0	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	374	7	4	4	2.4	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC[C@@H](C)c1ccccc1	10.1016/j.ejmech.2021.113190
		CHEMBL4869389	192721	0	None	93	4	Human	7.0	pKi	=	7.0	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	374	7	4	4	2.4	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC[C@@H](C)c1ccccc1	10.1016/j.ejmech.2021.113190
		1588	9105	27	None	-223	44	Human	6.0	pKi	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	338	3	2	2	2.8	CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC	nan
		28864	9105	27	None	-223	44	Human	6.0	pKi	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	338	3	2	2	2.8	CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC	nan
		43	9105	27	None	-223	44	Human	6.0	pKi	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	338	3	2	2	2.8	CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC	nan
		CHEMBL157138	9105	27	None	-223	44	Human	6.0	pKi	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	338	3	2	2	2.8	CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC	nan
		DB00589	9105	27	None	-223	44	Human	6.0	pKi	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	338	3	2	2	2.8	CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC	nan
		10069595	209907	0	None	-3235	3	Human	5.0	pKi	=	5.0	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	400	11	0	4	4.2	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)C3CCC3)CC2)cc1	10.1016/s0960-894x(02)00309-8
		CHEMBL64100	209907	0	None	-3235	3	Human	5.0	pKi	=	5.0	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	400	11	0	4	4.2	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)C3CCC3)CC2)cc1	10.1016/s0960-894x(02)00309-8
		44304318	210040	0	None	-1584	3	Human	5.0	pKi	=	5.0	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	373	9	1	5	1.8	C[C@@H](CN)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		CHEMBL64608	210040	0	None	-1584	3	Human	5.0	pKi	=	5.0	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	373	9	1	5	1.8	C[C@@H](CN)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		112936251	144044	1	None	-10	4	Human	5.0	pKi	=	5.0	Binding	Displacement of [3H]UR-DE257 from human histamine 2 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]UR-DE257 from human histamine 2 receptor expressed in Sf9 cell membranes by liquid scintillation counting	ChEMBL	359	5	1	5	3.5	CN1CCN(c2cc(-c3ccccc3)nc(NCc3ccccc3)n2)CC1	10.1016/j.bmcl.2015.12.035
		CHEMBL3752085	144044	1	None	-10	4	Human	5.0	pKi	=	5.0	Binding	Displacement of [3H]UR-DE257 from human histamine 2 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]UR-DE257 from human histamine 2 receptor expressed in Sf9 cell membranes by liquid scintillation counting	ChEMBL	359	5	1	5	3.5	CN1CCN(c2cc(-c3ccccc3)nc(NCc3ccccc3)n2)CC1	10.1016/j.bmcl.2015.12.035
		127052293	147016	3	None	-218	4	Human	5.0	pKi	=	5.0	Binding	Displacement of [3H]tiotidine from human histamine H2 receptor expressed in sf9 cell membrane co-expressing Gsalphas incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]tiotidine from human histamine H2 receptor expressed in sf9 cell membrane co-expressing Gsalphas incubated for 60 mins by liquid scintillation counting method	ChEMBL	368	7	3	4	3.1	N#C/N=C(/NCCSc1ccccc1)NC[C@H]1CC[C@H](c2c[nH]cn2)C1	10.1021/acs.jmedchem.6b00120
		CHEMBL3805361	147016	3	None	-218	4	Human	5.0	pKi	=	5.0	Binding	Displacement of [3H]tiotidine from human histamine H2 receptor expressed in sf9 cell membrane co-expressing Gsalphas incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]tiotidine from human histamine H2 receptor expressed in sf9 cell membrane co-expressing Gsalphas incubated for 60 mins by liquid scintillation counting method	ChEMBL	368	7	3	4	3.1	N#C/N=C(/NCCSc1ccccc1)NC[C@H]1CC[C@H](c2c[nH]cn2)C1	10.1021/acs.jmedchem.6b00120
		176	7186	66	None	-6	31	Human	5.0	pKi	=	5.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	nan
		2157	7186	66	None	-6	31	Human	5.0	pKi	=	5.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	nan
		2566	7186	66	None	-6	31	Human	5.0	pKi	=	5.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	nan
		CHEMBL633	7186	66	None	-6	31	Human	5.0	pKi	=	5.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	nan
		DB01118	7186	66	None	-6	31	Human	5.0	pKi	=	5.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	nan
		164627189	193100	0	None	275	4	Human	7.0	pKi	=	7.0	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	298	6	4	4	1.0	CCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1016/j.ejmech.2021.113190
		CHEMBL4874758	193100	0	None	275	4	Human	7.0	pKi	=	7.0	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	298	6	4	4	1.0	CCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1016/j.ejmech.2021.113190
		168294776	199805	0	None	-7	4	Human	6.0	pKi	=	6.0	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	366	7	3	4	2.6	Cc1nnc(CCCN/C(N)=N/C(=O)NCC(C)C2CCCCC2)s1	10.1021/acs.jmedchem.1c00692
		CHEMBL5209479	199805	0	None	-7	4	Human	6.0	pKi	=	6.0	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	366	7	3	4	2.6	Cc1nnc(CCCN/C(N)=N/C(=O)NCC(C)C2CCCCC2)s1	10.1021/acs.jmedchem.1c00692
		CHEMBL5222831	199805	0	None	-7	4	Human	6.0	pKi	=	6.0	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	366	7	3	4	2.6	Cc1nnc(CCCN/C(N)=N/C(=O)NCC(C)C2CCCCC2)s1	10.1021/acs.jmedchem.1c00692
		168294445	199789	0	None	-1	4	Human	7.0	pKi	=	7.0	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	414	6	4	4	2.6	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCC2CCc3nc(N)sc3C2)cc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5208113	199789	0	None	-1	4	Human	7.0	pKi	=	7.0	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	414	6	4	4	2.6	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCC2CCc3nc(N)sc3C2)cc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5222768	199789	0	None	-1	4	Human	7.0	pKi	=	7.0	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	414	6	4	4	2.6	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCC2CCc3nc(N)sc3C2)cc1	10.1021/acs.jmedchem.1c00692
		44304320	170053	0	None	-4265	3	Human	5.0	pKi	=	5.0	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	373	9	1	5	1.9	CC[C@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		CHEMBL418666	170053	0	None	-4265	3	Human	5.0	pKi	=	5.0	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	373	9	1	5	1.9	CC[C@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		44304319	209413	0	None	-1202	3	Human	5.0	pKi	=	5.0	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	373	9	1	5	1.8	C[C@H](CN)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		CHEMBL61288	209413	0	None	-1202	3	Human	5.0	pKi	=	5.0	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	373	9	1	5	1.8	C[C@H](CN)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		44304494	209771	0	None	-8709	3	Human	5.0	pKi	=	5.0	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	489	12	1	6	4.3	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](C)NC(=O)OC(C)(C)C)CC2)cc1	10.1016/s0960-894x(02)00310-4
		CHEMBL63125	209771	0	None	-8709	3	Human	5.0	pKi	=	5.0	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	489	12	1	6	4.3	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](C)NC(=O)OC(C)(C)C)CC2)cc1	10.1016/s0960-894x(02)00310-4
		132060746	169849	0	None	-6	5	Human	6.0	pKi	=	6.0	Binding	Displacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method	ChEMBL	405	4	0	4	4.4	O=C(OCc1ccccc1)N1Cc2ccc(N3CCN(C4CCCC4)CC3)cc2C1	10.1016/j.ejmech.2018.02.024
		CHEMBL4176474	169849	0	None	-6	5	Human	6.0	pKi	=	6.0	Binding	Displacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method	ChEMBL	405	4	0	4	4.4	O=C(OCc1ccccc1)N1Cc2ccc(N3CCN(C4CCCC4)CC3)cc2C1	10.1016/j.ejmech.2018.02.024
		124087	8171	114	None	-29	15	Human	6.0	pKi	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	310	0	1	2	4.0	Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1	nan
		7157	8171	114	None	-29	15	Human	6.0	pKi	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	310	0	1	2	4.0	Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1	nan
		814	8171	114	None	-29	15	Human	6.0	pKi	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	310	0	1	2	4.0	Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1	nan
		CHEMBL1172	8171	114	None	-29	15	Human	6.0	pKi	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	310	0	1	2	4.0	Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1	nan
		DB00967	8171	114	None	-29	15	Human	6.0	pKi	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	310	0	1	2	4.0	Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1	nan
		168284289	199685	0	None	1	4	Human	7.0	pKi	=	7.0	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	428	8	4	4	3.1	CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1	10.1021/acs.jmedchem.1c00692
		CHEMBL5194860	199685	0	None	1	4	Human	7.0	pKi	=	7.0	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	428	8	4	4	3.1	CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1	10.1021/acs.jmedchem.1c00692
		CHEMBL5222123	199685	0	None	1	4	Human	7.0	pKi	=	7.0	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	428	8	4	4	3.1	CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1	10.1021/acs.jmedchem.1c00692
		44304211	108974	0	None	-19054	3	Human	5.0	pKi	=	5.0	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	373	9	1	5	1.9	CC[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		CHEMBL302829	108974	0	None	-19054	3	Human	5.0	pKi	=	5.0	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	373	9	1	5	1.9	CC[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		132060752	169705	0	None	-3	4	Human	6.0	pKi	=	6.0	Binding	Displacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method	ChEMBL	437	7	0	6	3.4	CCOC(=O)CCN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)C3)CC1	10.1016/j.ejmech.2018.02.024
		CHEMBL4174189	169705	0	None	-3	4	Human	6.0	pKi	=	6.0	Binding	Displacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method	ChEMBL	437	7	0	6	3.4	CCOC(=O)CCN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)C3)CC1	10.1016/j.ejmech.2018.02.024
		CHEMBL5085542	221751	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCC[n+]1c(C)cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc1C	10.1016/j.bmcl.2021.128388
		164626370	193252	0	None	1	6	Human	6.0	pKi	=	6.0	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	338	6	4	4	1.8	CCCCCCNC(=O)/N=C(\N)NC1CCc2nc(N)sc2C1	10.1016/j.ejmech.2021.113190
		CHEMBL4876799	193252	0	None	1	6	Human	6.0	pKi	=	6.0	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	338	6	4	4	1.8	CCCCCCNC(=O)/N=C(\N)NC1CCc2nc(N)sc2C1	10.1016/j.ejmech.2021.113190
		44304382	210081	0	None	-1174	3	Human	5.0	pKi	=	5.0	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	403	11	1	4	4.0	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)NC(C)C)CC2)cc1	10.1016/s0960-894x(02)00309-8
		CHEMBL64773	210081	0	None	-1174	3	Human	5.0	pKi	=	5.0	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	403	11	1	4	4.0	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)NC(C)C)CC2)cc1	10.1016/s0960-894x(02)00309-8
		11057	182928	23	None	-2	20	Human	6.0	pKi	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	372	4	0	2	4.5	CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1	nan
		3468	182928	23	None	-2	20	Human	6.0	pKi	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	372	4	0	2	4.5	CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1	nan
		CHEMBL459265	182928	23	None	-2	20	Human	6.0	pKi	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	372	4	0	2	4.5	CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1	nan
		CHEMBL64894	182928	23	None	-2	20	Human	6.0	pKi	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	372	4	0	2	4.5	CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1	nan
		164616851	191729	0	None	-1	5	Human	6.9	pKi	=	6.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	376	6	4	4	2.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=S)N[C@H](C)c1ccccc1	10.1016/j.ejmech.2021.113190
		CHEMBL4853772	191729	0	None	-1	5	Human	6.9	pKi	=	6.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	376	6	4	4	2.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=S)N[C@H](C)c1ccccc1	10.1016/j.ejmech.2021.113190
		2286	9957	51	None	-26	30	Human	5.9	pKi	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	nan
		4927	9957	51	None	-26	30	Human	5.9	pKi	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	nan
		7282	9957	51	None	-26	30	Human	5.9	pKi	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	nan
		CHEMBL643	9957	51	None	-26	30	Human	5.9	pKi	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	nan
		DB01069	9957	51	None	-26	30	Human	5.9	pKi	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	nan
		1353	8692	93	None	-131	85	Human	5.9	pKi	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	nan
		3559	8692	93	None	-131	85	Human	5.9	pKi	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	nan
		86	8692	93	None	-131	85	Human	5.9	pKi	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	nan
		CHEMBL54	8692	93	None	-131	85	Human	5.9	pKi	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	nan
		DB00502	8692	93	None	-131	85	Human	5.9	pKi	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	nan
		164612760	191497	0	None	38	4	Human	5.9	pKi	=	5.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	390	7	4	4	2.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NC[C@H](C)c1ccccc1	10.1016/j.ejmech.2021.113190
		CHEMBL4850490	191497	0	None	38	4	Human	5.9	pKi	=	5.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	390	7	4	4	2.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NC[C@H](C)c1ccccc1	10.1016/j.ejmech.2021.113190
		44582678	188353	0	None	-7	10	Human	5.9	pKi	=	5.9	Binding	Inhibition of human cloned histamine H2 receptor by competitive binding experimentInhibition of human cloned histamine H2 receptor by competitive binding experiment	ChEMBL	401	9	1	4	4.3	COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(C)cc2)CC1	10.1016/j.bmc.2009.03.021
		CHEMBL476839	188353	0	None	-7	10	Human	5.9	pKi	=	5.9	Binding	Inhibition of human cloned histamine H2 receptor by competitive binding experimentInhibition of human cloned histamine H2 receptor by competitive binding experiment	ChEMBL	401	9	1	4	4.3	COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(C)cc2)CC1	10.1016/j.bmc.2009.03.021
		73353884	99097	0	None	2	8	Human	5.9	pKi	=	5.9	Binding	Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	295	3	1	3	2.7	c1cc2c(cc1CN[C@H]1C3C4CC5C6C4CC3C6C51)OCO2	10.1016/j.bmc.2013.07.045
		CHEMBL2429890	99097	0	None	2	8	Human	5.9	pKi	=	5.9	Binding	Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	295	3	1	3	2.7	c1cc2c(cc1CN[C@H]1C3C4CC5C6C4CC3C6C51)OCO2	10.1016/j.bmc.2013.07.045
		44304245	210107	0	None	-2884	3	Human	4.9	pKi	=	4.9	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	425	11	0	5	4.0	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3cccn3C)CC2)cc1	10.1016/s0960-894x(02)00309-8
		CHEMBL64884	210107	0	None	-2884	3	Human	4.9	pKi	=	4.9	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	425	11	0	5	4.0	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3cccn3C)CC2)cc1	10.1016/s0960-894x(02)00309-8
		44335559	116486	0	None	-6918	4	Human	4.9	pKi	=	4.9	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	334	6	0	3	4.7	CC1CCCN(CCCOc2ccc(-c3ccc(C#N)cc3)cc2)C1	10.1016/s0960-894x(02)00648-0
		CHEMBL322873	116486	0	None	-6918	4	Human	4.9	pKi	=	4.9	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	334	6	0	3	4.7	CC1CCCN(CCCOc2ccc(-c3ccc(C#N)cc3)cc2)C1	10.1016/s0960-894x(02)00648-0
		1201549	7384	24	None	-74	20	Human	5.9	pKi	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	307	4	0	2	4.4	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1	nan
		333	7384	24	None	-74	20	Human	5.9	pKi	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	307	4	0	2	4.4	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1	nan
		7601	7384	24	None	-74	20	Human	5.9	pKi	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	307	4	0	2	4.4	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1	nan
		CHEMBL1201203	7384	24	None	-74	20	Human	5.9	pKi	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	307	4	0	2	4.4	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1	nan
		CHEMBL438151	7384	24	None	-74	20	Human	5.9	pKi	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	307	4	0	2	4.4	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1	nan
		DB00245	7384	24	None	-74	20	Human	5.9	pKi	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	307	4	0	2	4.4	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1	nan
		168295541	199819	0	None	-851	6	Human	7.9	pKi	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	347	6	4	5	1.4	C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5208845	199819	0	None	-851	6	Human	7.9	pKi	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	347	6	4	5	1.4	C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5222926	199819	0	None	-851	6	Human	7.9	pKi	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	347	6	4	5	1.4	C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1	10.1021/acs.jmedchem.1c00692
		44334430	11226	0	None	-398	3	Human	5.9	pKi	=	5.9	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	428	10	1	5	3.1	O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccccc3)C2)cc1)C1CC1	10.1016/s0960-894x(02)00685-6
		CHEMBL101691	11226	0	None	-398	3	Human	5.9	pKi	=	5.9	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	428	10	1	5	3.1	O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccccc3)C2)cc1)C1CC1	10.1016/s0960-894x(02)00685-6
		44304457	209992	0	None	-3981	3	Human	4.9	pKi	=	4.9	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	376	10	0	5	3.6	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OC)CC2)cc1	10.1016/s0960-894x(02)00309-8
		CHEMBL64408	209992	0	None	-3981	3	Human	4.9	pKi	=	4.9	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	376	10	0	5	3.6	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OC)CC2)cc1	10.1016/s0960-894x(02)00309-8
		44304431	209720	0	None	-512	3	Human	4.9	pKi	=	4.9	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	566	14	1	7	4.9	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](Cc3ccncc3)NC(=O)OC(C)(C)C)CC2)cc1	10.1016/s0960-894x(02)00310-4
		CHEMBL62903	209720	0	None	-512	3	Human	4.9	pKi	=	4.9	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	566	14	1	7	4.9	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](Cc3ccncc3)NC(=O)OC(C)(C)C)CC2)cc1	10.1016/s0960-894x(02)00310-4
		1212	8443	50	None	-323	65	Human	5.9	pKi	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	nan
		204	8443	50	None	-323	65	Human	5.9	pKi	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	nan
		3372	8443	50	None	-323	65	Human	5.9	pKi	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	nan
		CHEMBL726	8443	50	None	-323	65	Human	5.9	pKi	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	nan
		DB00623	8443	50	None	-323	65	Human	5.9	pKi	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	nan
		9872676	84970	0	None	-3090	17	Human	5.9	pKi	=	5.9	Binding	Binding affinity to H2 receptorBinding affinity to H2 receptor	ChEMBL	565	11	2	10	4.8	COc1nc(NCCCN2CCOCC2)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1	10.1021/jm060012g
		CHEMBL210514	84970	0	None	-3090	17	Human	5.9	pKi	=	5.9	Binding	Binding affinity to H2 receptorBinding affinity to H2 receptor	ChEMBL	565	11	2	10	4.8	COc1nc(NCCCN2CCOCC2)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1	10.1021/jm060012g
		44304751	107800	0	None	-338	3	Human	4.9	pKi	=	4.9	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	422	11	0	4	4.7	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3ccccc3)CC2)cc1	10.1016/s0960-894x(02)00309-8
		CHEMBL294519	107800	0	None	-338	3	Human	4.9	pKi	=	4.9	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	422	11	0	4	4.7	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3ccccc3)CC2)cc1	10.1016/s0960-894x(02)00309-8
		44304990	209841	0	None	-331	3	Human	4.9	pKi	=	4.9	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	483	12	0	6	4.1	CCCCCC(=O)c1ccc(OCCCN2CCN(S(=O)(=O)c3ccc(C#N)cc3)CC2)cc1	10.1016/s0960-894x(02)00309-8
		CHEMBL63632	209841	0	None	-331	3	Human	4.9	pKi	=	4.9	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	483	12	0	6	4.1	CCCCCC(=O)c1ccc(OCCCN2CCN(S(=O)(=O)c3ccc(C#N)cc3)CC2)cc1	10.1016/s0960-894x(02)00309-8
		44335225	170934	0	None	-812	4	Human	4.9	pKi	=	4.9	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	347	6	1	4	3.1	N#Cc1ccc(-c2ccc(OCCCN3CC4CNCC4C3)cc2)cc1	10.1016/s0960-894x(02)00648-0
		CHEMBL421026	170934	0	None	-812	4	Human	4.9	pKi	=	4.9	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	347	6	1	4	3.1	N#Cc1ccc(-c2ccc(OCCCN3CC4CNCC4C3)cc2)cc1	10.1016/s0960-894x(02)00648-0
		44304303	210108	0	None	-954	3	Human	4.9	pKi	=	4.9	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	371	8	1	5	1.6	O=C(c1ccc(OCCCN2CCN(C(=O)[C@@H]3CCN3)CC2)cc1)C1CC1	10.1016/s0960-894x(02)00310-4
		CHEMBL64896	210108	0	None	-954	3	Human	4.9	pKi	=	4.9	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	371	8	1	5	1.6	O=C(c1ccc(OCCCN2CCN(C(=O)[C@@H]3CCN3)CC2)cc1)C1CC1	10.1016/s0960-894x(02)00310-4
		164621681	192359	0	None	64	4	Human	6.9	pKi	=	6.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	444	7	4	5	3.2	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(OC(F)(F)F)cc1	10.1016/j.ejmech.2021.113190
		CHEMBL4863523	192359	0	None	64	4	Human	6.9	pKi	=	6.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	444	7	4	5	3.2	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(OC(F)(F)F)cc1	10.1016/j.ejmech.2021.113190
		409544	209693	4	None	-8912	3	Human	4.9	pKi	=	4.9	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	390	11	0	5	4.0	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OCC)CC2)cc1	10.1016/s0960-894x(02)00309-8
		CHEMBL62803	209693	4	None	-8912	3	Human	4.9	pKi	=	4.9	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	390	11	0	5	4.0	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OCC)CC2)cc1	10.1016/s0960-894x(02)00309-8
		44304035	210088	0	None	-181	3	Human	4.9	pKi	=	4.9	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	410	9	0	5	3.7	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)Cc3ccccc3)cc2)CC1	10.1016/s0960-894x(02)00309-8
		CHEMBL64799	210088	0	None	-181	3	Human	4.9	pKi	=	4.9	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	410	9	0	5	3.7	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)Cc3ccccc3)cc2)CC1	10.1016/s0960-894x(02)00309-8
		44304393	112734	0	None	-128	3	Human	4.9	pKi	=	4.9	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	517	13	1	6	4.9	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](NC(=O)OC(C)(C)C)C(C)C)CC2)cc1	10.1016/s0960-894x(02)00310-4
		CHEMBL312958	112734	0	None	-128	3	Human	4.9	pKi	=	4.9	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	517	13	1	6	4.9	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](NC(=O)OC(C)(C)C)C(C)C)CC2)cc1	10.1016/s0960-894x(02)00310-4
		10039772	111138	0	None	-501	3	Human	4.9	pKi	=	4.9	Binding	Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors	ChEMBL	288	7	3	2	3.1	S=C(NCCCCCc1c[nH]cn1)Nc1ccccc1	10.1021/jm00012a025
		CHEMBL310087	111138	0	None	-501	3	Human	4.9	pKi	=	4.9	Binding	Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors	ChEMBL	288	7	3	2	3.1	S=C(NCCCCCc1c[nH]cn1)Nc1ccccc1	10.1021/jm00012a025
		44304246	209430	0	None	-1513	3	Human	4.9	pKi	=	4.9	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	426	11	0	5	4.6	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3occc3C)CC2)cc1	10.1016/s0960-894x(02)00309-8
		CHEMBL61396	209430	0	None	-1513	3	Human	4.9	pKi	=	4.9	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	426	11	0	5	4.6	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3occc3C)CC2)cc1	10.1016/s0960-894x(02)00309-8
		44335463	11227	0	None	-229	4	Human	4.9	pKi	=	4.9	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	357	7	1	4	3.2	CCOC(=O)N1CCN(CCCOc2ccc(-c3cc[nH]c3)cc2)CC1	10.1016/s0960-894x(02)00648-0
		CHEMBL101692	11227	0	None	-229	4	Human	4.9	pKi	=	4.9	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	357	7	1	4	3.2	CCOC(=O)N1CCN(CCCOc2ccc(-c3cc[nH]c3)cc2)CC1	10.1016/s0960-894x(02)00648-0
		44335483	12065	0	None	-426	4	Human	4.9	pKi	=	4.9	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	336	6	1	4	3.5	N#Cc1ccc(-c2ccc(OCCCN3CCCC(O)C3)cc2)cc1	10.1016/s0960-894x(02)00648-0
		CHEMBL106596	12065	0	None	-426	4	Human	4.9	pKi	=	4.9	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	336	6	1	4	3.5	N#Cc1ccc(-c2ccc(OCCCN3CCCC(O)C3)cc2)cc1	10.1016/s0960-894x(02)00648-0
		156017225	185124	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	442	15	3	7	3.1	NCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
		CHEMBL4642548	185124	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	442	15	3	7	3.1	NCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
		CHEMBL4651234	185124	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	442	15	3	7	3.1	NCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
		156015555	185091	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	456	16	3	7	3.5	NCCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
		CHEMBL4644794	185091	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	456	16	3	7	3.5	NCCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
		CHEMBL4651059	185091	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	456	16	3	7	3.5	NCCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
		156014823	185106	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	1109	31	4	13	9.2	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3cc(S(=O)(=O)O)ccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
		CHEMBL4641747	185106	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	1109	31	4	13	9.2	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3cc(S(=O)(=O)O)ccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
		CHEMBL4651132	185106	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	1109	31	4	13	9.2	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3cc(S(=O)(=O)O)ccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
		44304412	208427	0	None	-912	3	Human	4.9	pKi	=	4.9	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	517	13	1	6	4.9	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](NC(=O)OC(C)(C)C)C(C)C)CC2)cc1	10.1016/s0960-894x(02)00310-4
		CHEMBL60598	208427	0	None	-912	3	Human	4.9	pKi	=	4.9	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	517	13	1	6	4.9	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](NC(=O)OC(C)(C)C)C(C)C)CC2)cc1	10.1016/s0960-894x(02)00310-4
		59868	100929	60	None	-20892	3	Human	4.9	pKi	=	4.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	211	3	2	4	1.6	CCCN[C@@H]1CCc2nc(N)sc2C1	10.1016/j.ejmech.2021.113190
		CHEMBL249420	100929	60	None	-20892	3	Human	4.9	pKi	=	4.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	211	3	2	4	1.6	CCCN[C@@H]1CCc2nc(N)sc2C1	10.1016/j.ejmech.2021.113190
		119570	9933	96	None	-169	39	Human	4.9	pKi	=	4.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	10.1021/acs.jmedchem.1c00692
		2233	9933	96	None	-169	39	Human	4.9	pKi	=	4.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	10.1021/acs.jmedchem.1c00692
		953	9933	96	None	-169	39	Human	4.9	pKi	=	4.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	10.1021/acs.jmedchem.1c00692
		CHEMBL301265	9933	96	None	-169	39	Human	4.9	pKi	=	4.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	10.1021/acs.jmedchem.1c00692
		DB00413	9933	96	None	-169	39	Human	4.9	pKi	=	4.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	10.1021/acs.jmedchem.1c00692
		104903	63118	17	None	-5	6	Human	4.9	pKi	=	4.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	624	6	0	8	5.5	C[C@@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)C3=CC[C@]2(C)[C@H]1C(=O)CN1CCN(c2cc(N3CCCC3)nc(N3CCCC3)n2)CC1	nan
		CHEMBL1630578	63118	17	None	-5	6	Human	4.9	pKi	=	4.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	624	6	0	8	5.5	C[C@@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)C3=CC[C@]2(C)[C@H]1C(=O)CN1CCN(c2cc(N3CCCC3)nc(N3CCCC3)n2)CC1	nan
		CHEMBL4535474	220767	39	None	-1	6	Human	6.9	pKi	=	6.9	Binding	Selectivity interaction (GPCR panel (PDSP screen)) EUB0000320b HRH2Selectivity interaction (GPCR panel (PDSP screen)) EUB0000320b HRH2	ChEMBL		None	None	None		CNCc1ccccc1-c1csc([C@@H](C)Nc2nc(C)nc3cc(OC)c(OC)cc23)c1	10.6019/CHEMBL5212743
		1231	7724	116	None	-4	8	Human	6.9	pKi	=	6.9	Binding	Binding affinity to human histamine H2 receptor by radioligand displacement assayBinding affinity to human histamine H2 receptor by radioligand displacement assay	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.ejmech.2013.01.044
		2756	7724	116	None	-4	8	Human	6.9	pKi	=	6.9	Binding	Binding affinity to human histamine H2 receptor by radioligand displacement assayBinding affinity to human histamine H2 receptor by radioligand displacement assay	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.ejmech.2013.01.044
		645	7724	116	None	-4	8	Human	6.9	pKi	=	6.9	Binding	Binding affinity to human histamine H2 receptor by radioligand displacement assayBinding affinity to human histamine H2 receptor by radioligand displacement assay	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.ejmech.2013.01.044
		CHEMBL30	7724	116	None	-4	8	Human	6.9	pKi	=	6.9	Binding	Binding affinity to human histamine H2 receptor by radioligand displacement assayBinding affinity to human histamine H2 receptor by radioligand displacement assay	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.ejmech.2013.01.044
		DB00501	7724	116	None	-4	8	Human	6.9	pKi	=	6.9	Binding	Binding affinity to human histamine H2 receptor by radioligand displacement assayBinding affinity to human histamine H2 receptor by radioligand displacement assay	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.ejmech.2013.01.044
		44568347	198430	0	None	-67	15	Human	5.9	pKi	=	5.9	Binding	Antagonist activity at histamine H2 receptor (unknown origin) by PDSP assayAntagonist activity at histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	356	6	0	4	5.2	CCN(CC)CCCOC(=O)N1c2ccccc2Sc2ccccc21	10.1016/j.bmcl.2013.04.082
		CHEMBL519609	198430	0	None	-67	15	Human	5.9	pKi	=	5.9	Binding	Antagonist activity at histamine H2 receptor (unknown origin) by PDSP assayAntagonist activity at histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	356	6	0	4	5.2	CCN(CC)CCCOC(=O)N1c2ccccc2Sc2ccccc21	10.1016/j.bmcl.2013.04.082
		44304560	109540	0	None	-10715	3	Human	4.9	pKi	=	4.9	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	371	8	1	5	1.6	O=C(c1ccc(OCCCN2CCN(C(=O)[C@H]3CCN3)CC2)cc1)C1CC1	10.1016/s0960-894x(02)00310-4
		CHEMBL305144	109540	0	None	-10715	3	Human	4.9	pKi	=	4.9	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	371	8	1	5	1.6	O=C(c1ccc(OCCCN2CCN(C(=O)[C@H]3CCN3)CC2)cc1)C1CC1	10.1016/s0960-894x(02)00310-4
		44304760	209680	0	None	-229	3	Human	4.9	pKi	=	4.9	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	431	13	1	5	3.7	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](N)CC(C)C)CC2)cc1	10.1016/s0960-894x(02)00310-4
		CHEMBL62741	209680	0	None	-229	3	Human	4.9	pKi	=	4.9	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	431	13	1	5	3.7	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](N)CC(C)C)CC2)cc1	10.1016/s0960-894x(02)00310-4
		71525678	96500	0	None	-1479	6	Human	4.9	pKi	=	4.9	Binding	Displacement of [3H]histamine from human histamine H2 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H2 receptor expressed in HEK cells	ChEMBL	258	3	2	6	0.6	CCc1cnc2c(N3CC(NC)C3)nc(N)nc2c1	10.1016/j.bmcl.2013.02.091
		CHEMBL2376800	96500	0	None	-1479	6	Human	4.9	pKi	=	4.9	Binding	Displacement of [3H]histamine from human histamine H2 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H2 receptor expressed in HEK cells	ChEMBL	258	3	2	6	0.6	CCc1cnc2c(N3CC(NC)C3)nc(N)nc2c1	10.1016/j.bmcl.2013.02.091
		CHEMBL4748908	220814	1	None	-1	12	Human	6.8	pKi	=	6.8	Binding	GPCRScan assay: inhibition of H2GPCRScan assay: inhibition of H2	ChEMBL		None	None	None		CN1CCN(c2ccnc(NCCc3ccccc3)n2)CC1	10.6019/CHEMBL4800732
		164610824	191889	0	None	14	4	Human	5.8	pKi	=	5.8	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	452	8	4	4	3.6	Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NCC(c1ccccc1)c1ccccc1	10.1016/j.ejmech.2021.113190
		CHEMBL4856200	191889	0	None	14	4	Human	5.8	pKi	=	5.8	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	452	8	4	4	3.6	Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NCC(c1ccccc1)c1ccccc1	10.1016/j.ejmech.2021.113190
		18539962	108908	0	None	-537	3	Human	4.8	pKi	=	4.8	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	318	10	1	4	3.1	CCCCCC(=O)c1ccc(OCCCN2CCNCC2)cc1	10.1016/s0960-894x(02)00309-8
		CHEMBL302445	108908	0	None	-537	3	Human	4.8	pKi	=	4.8	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	318	10	1	4	3.1	CCCCCC(=O)c1ccc(OCCCN2CCNCC2)cc1	10.1016/s0960-894x(02)00309-8
		2389	10104	118	None	-288	66	Human	5.8	pKi	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	nan
		5073	10104	118	None	-288	66	Human	5.8	pKi	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	nan
		96	10104	118	None	-288	66	Human	5.8	pKi	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	nan
		CHEMBL85	10104	118	None	-288	66	Human	5.8	pKi	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	nan
		DB00734	10104	118	None	-288	66	Human	5.8	pKi	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	nan
		164620704	192862	0	None	17	4	Human	6.8	pKi	=	6.8	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	416	8	4	4	3.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)c1ccc(C(C)C)cc1	10.1016/j.ejmech.2021.113190
		CHEMBL4871482	192862	0	None	17	4	Human	6.8	pKi	=	6.8	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	416	8	4	4	3.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)c1ccc(C(C)C)cc1	10.1016/j.ejmech.2021.113190
		44304287	209677	0	None	-912	3	Human	4.8	pKi	=	4.8	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	428	11	0	5	4.7	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3cccs3)CC2)cc1	10.1016/s0960-894x(02)00309-8
		CHEMBL62726	209677	0	None	-912	3	Human	4.8	pKi	=	4.8	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	428	11	0	5	4.7	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3cccs3)CC2)cc1	10.1016/s0960-894x(02)00309-8
		44304310	210053	0	None	-1995	3	Human	4.8	pKi	=	4.8	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	415	10	0	4	4.1	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)N3CCCC3)CC2)cc1	10.1016/s0960-894x(02)00309-8
		CHEMBL64667	210053	0	None	-1995	3	Human	4.8	pKi	=	4.8	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	415	10	0	4	4.1	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)N3CCCC3)CC2)cc1	10.1016/s0960-894x(02)00309-8
		44304349	209580	0	None	-275	3	Human	4.8	pKi	=	4.8	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	566	14	1	7	4.9	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](Cc3ccncc3)NC(=O)OC(C)(C)C)CC2)cc1	10.1016/s0960-894x(02)00310-4
		CHEMBL62266	209580	0	None	-275	3	Human	4.8	pKi	=	4.8	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	566	14	1	7	4.9	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](Cc3ccncc3)NC(=O)OC(C)(C)C)CC2)cc1	10.1016/s0960-894x(02)00310-4
		CHEMBL4748908	220814	1	None	-1	12	Human	6.8	pKi	=	6.8	Binding	GPCRScan assay: inhibition of H2GPCRScan assay: inhibition of H2	ChEMBL		None	None	None		CN1CCN(c2ccnc(NCCc3ccccc3)n2)CC1	10.6019/CHEMBL4800732
		73347825	99315	0	None	-1	3	Human	5.8	pKi	=	5.8	Binding	Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	311	5	1	3	2.9	COc1ccc(CN[C@H]2C3C4CC5C6C4CC3C6C52)cc1OC	10.1016/j.bmc.2013.07.045
		CHEMBL2432046	99315	0	None	-1	3	Human	5.8	pKi	=	5.8	Binding	Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	311	5	1	3	2.9	COc1ccc(CN[C@H]2C3C4CC5C6C4CC3C6C52)cc1OC	10.1016/j.bmc.2013.07.045
		57469	25638	125	None	-1	3	Human	5.8	pKi	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	240	2	1	4	2.8	CC(C)Cn1cnc2c(N)nc3ccccc3c21	nan
		CHEMBL1282	25638	125	None	-1	3	Human	5.8	pKi	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	240	2	1	4	2.8	CC(C)Cn1cnc2c(N)nc3ccccc3c21	nan
		168286426	199705	0	None	-5	6	Human	7.8	pKi	=	7.8	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	403	10	4	5	2.3	CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
		CHEMBL5198795	199705	0	None	-5	6	Human	7.8	pKi	=	7.8	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	403	10	4	5	2.3	CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
		CHEMBL5222241	199705	0	None	-5	6	Human	7.8	pKi	=	7.8	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	403	10	4	5	2.3	CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
		135156	184582	12	None	-	1	Human	7.8	pKi	=	7.8	Binding	Binding affinity to human H2R expressing Sf9 cells incubated for 60 mins by microbeta scintillation counter methodBinding affinity to human H2R expressing Sf9 cells incubated for 60 mins by microbeta scintillation counter method	ChEMBL	343	8	2	6	1.7	Nc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
		CHEMBL4643501	184582	12	None	-	1	Human	7.8	pKi	=	7.8	Binding	Binding affinity to human H2R expressing Sf9 cells incubated for 60 mins by microbeta scintillation counter methodBinding affinity to human H2R expressing Sf9 cells incubated for 60 mins by microbeta scintillation counter method	ChEMBL	343	8	2	6	1.7	Nc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
		69355600	85460	0	None	-3715	4	Human	4.8	pKi	=	4.8	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	336	6	1	4	3.5	C[C@@]1(O)CCN(CCCOc2ccc(-c3ccc(C#N)cc3)cc2)C1	10.1016/s0960-894x(02)00648-0
		CHEMBL2112461	85460	0	None	-3715	4	Human	4.8	pKi	=	4.8	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	336	6	1	4	3.5	C[C@@]1(O)CCN(CCCOc2ccc(-c3ccc(C#N)cc3)cc2)C1	10.1016/s0960-894x(02)00648-0
		44304293	209741	0	None	-52	3	Human	4.8	pKi	=	4.8	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	491	10	1	6	4.0	N[C@H](Cc1cc2ccccc2s1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		CHEMBL63002	209741	0	None	-52	3	Human	4.8	pKi	=	4.8	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	491	10	1	6	4.0	N[C@H](Cc1cc2ccccc2s1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		168295803	199824	0	None	3	4	Human	6.8	pKi	=	6.8	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	338	6	4	4	1.6	CCCCCNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1	10.1021/acs.jmedchem.1c00692
		CHEMBL5207206	199824	0	None	3	4	Human	6.8	pKi	=	6.8	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	338	6	4	4	1.6	CCCCCNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1	10.1021/acs.jmedchem.1c00692
		CHEMBL5222937	199824	0	None	3	4	Human	6.8	pKi	=	6.8	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	338	6	4	4	1.6	CCCCCNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1	10.1021/acs.jmedchem.1c00692
		44304283	209952	0	None	-117	3	Human	5.8	pKi	=	5.8	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	452	8	0	5	4.8	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)c3ccc(C(C)(C)C)cc3)cc2)CC1	10.1016/s0960-894x(02)00309-8
		CHEMBL64247	209952	0	None	-117	3	Human	5.8	pKi	=	5.8	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	452	8	0	5	4.8	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)c3ccc(C(C)(C)C)cc3)cc2)CC1	10.1016/s0960-894x(02)00309-8
		44334396	11688	0	None	-575	3	Human	5.8	pKi	=	5.8	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	446	10	1	5	3.2	O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccccc3F)C2)cc1)C1CC1	10.1016/s0960-894x(02)00685-6
		CHEMBL104618	11688	0	None	-575	3	Human	5.8	pKi	=	5.8	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	446	10	1	5	3.2	O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccccc3F)C2)cc1)C1CC1	10.1016/s0960-894x(02)00685-6
		3198	212292	76	None	-19	34	Human	5.8	pKi	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	380	6	0	3	5.8	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1	nan
		CHEMBL1201049	212292	76	None	-19	34	Human	5.8	pKi	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	380	6	0	3	5.8	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1	nan
		CHEMBL808	212292	76	None	-19	34	Human	5.8	pKi	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	380	6	0	3	5.8	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1	nan
		164622190	192395	0	None	93	2	Human	6.8	pKi	=	6.8	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	360	7	4	4	1.8	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCc1ccccc1	10.1016/j.ejmech.2021.113190
		CHEMBL4864067	192395	0	None	93	2	Human	6.8	pKi	=	6.8	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	360	7	4	4	1.8	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCc1ccccc1	10.1016/j.ejmech.2021.113190
		10017820	210974	0	None	-79	3	Human	5.8	pKi	=	5.8	Binding	Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors	ChEMBL	302	8	3	2	2.8	S=C(NCCCCCc1c[nH]cn1)NCc1ccccc1	10.1021/jm00012a025
		CHEMBL70811	210974	0	None	-79	3	Human	5.8	pKi	=	5.8	Binding	Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors	ChEMBL	302	8	3	2	2.8	S=C(NCCCCCc1c[nH]cn1)NCc1ccccc1	10.1021/jm00012a025
		9974306	211253	0	None	-199	4	Human	5.8	pKi	=	5.8	Binding	Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors	ChEMBL	336	8	3	2	3.4	S=C(NCCCCCc1c[nH]cn1)NCc1ccc(Cl)cc1	10.1021/jm00012a025
		CHEMBL72372	211253	0	None	-199	4	Human	5.8	pKi	=	5.8	Binding	Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors	ChEMBL	336	8	3	2	3.4	S=C(NCCCCCc1c[nH]cn1)NCc1ccc(Cl)cc1	10.1021/jm00012a025
		9974306	211253	0	None	-199	4	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	336	8	3	2	3.4	S=C(NCCCCCc1c[nH]cn1)NCc1ccc(Cl)cc1	10.1016/j.bmcl.2010.10.041
		CHEMBL72372	211253	0	None	-199	4	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	336	8	3	2	3.4	S=C(NCCCCCc1c[nH]cn1)NCc1ccc(Cl)cc1	10.1016/j.bmcl.2010.10.041
		3042	8196	35	None	-53	15	Human	5.8	pKi	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	309	7	0	3	4.4	CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC	nan
		355	8196	35	None	-53	15	Human	5.8	pKi	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	309	7	0	3	4.4	CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC	nan
		868	8196	35	None	-53	15	Human	5.8	pKi	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	309	7	0	3	4.4	CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC	nan
		CHEMBL1123	8196	35	None	-53	15	Human	5.8	pKi	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	309	7	0	3	4.4	CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC	nan
		DB00804	8196	35	None	-53	15	Human	5.8	pKi	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	309	7	0	3	4.4	CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC	nan
		10343536	11734	0	None	-1000	3	Human	5.8	pKi	=	5.8	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	446	10	1	5	3.2	O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3cccc(F)c3)C2)cc1)C1CC1	10.1016/s0960-894x(02)00685-6
		CHEMBL104809	11734	0	None	-1000	3	Human	5.8	pKi	=	5.8	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	446	10	1	5	3.2	O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3cccc(F)c3)C2)cc1)C1CC1	10.1016/s0960-894x(02)00685-6
		71452695	85458	0	None	-398	3	Human	5.8	pKi	=	5.8	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	453	10	1	6	3.0	N#Cc1ccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)cc1	10.1016/s0960-894x(02)00685-6
		CHEMBL2112451	85458	0	None	-398	3	Human	5.8	pKi	=	5.8	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	453	10	1	6	3.0	N#Cc1ccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)cc1	10.1016/s0960-894x(02)00685-6
		CHEMBL4576555	220796	5	None	-1	19	Human	5.8	pKi	=	5.8	Binding	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	7293	81	None	-56	42	Human	5.8	pKi	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	nan
		249	7293	81	None	-56	42	Human	5.8	pKi	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	nan
		2603	7293	81	None	-56	42	Human	5.8	pKi	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	nan
		CHEMBL296419	7293	81	None	-56	42	Human	5.8	pKi	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	nan
		DB00637	7293	81	None	-56	42	Human	5.8	pKi	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	nan
		44335185	114168	0	None	-14	3	Human	5.8	pKi	=	5.8	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	446	7	0	4	4.7	CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc(Br)cc3)cc2)CC1	10.1016/s0960-894x(02)00648-0
		CHEMBL317900	114168	0	None	-14	3	Human	5.8	pKi	=	5.8	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	446	7	0	4	4.7	CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc(Br)cc3)cc2)CC1	10.1016/s0960-894x(02)00648-0
		44304743	107385	0	None	-97	3	Human	4.8	pKi	=	4.8	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	431	13	1	5	3.7	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](N)CC(C)C)CC2)cc1	10.1016/s0960-894x(02)00310-4
		CHEMBL291847	107385	0	None	-97	3	Human	4.8	pKi	=	4.8	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	431	13	1	5	3.7	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](N)CC(C)C)CC2)cc1	10.1016/s0960-894x(02)00310-4
		164628701	193246	0	None	144	3	Human	6.8	pKi	=	6.8	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	338	5	4	4	1.9	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC1CCCCC1	10.1016/j.ejmech.2021.113190
		CHEMBL4876743	193246	0	None	144	3	Human	6.8	pKi	=	6.8	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	338	5	4	4	1.9	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC1CCCCC1	10.1016/j.ejmech.2021.113190
		9880208	11696	0	None	-2041	4	Human	4.8	pKi	=	4.8	Binding	Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor	ChEMBL	322	6	1	4	3.1	N#Cc1ccc(-c2ccc(OCCCN3CC[C@@H](O)C3)cc2)cc1	10.1016/s0960-894x(02)00648-0
		CHEMBL104669	11696	0	None	-2041	4	Human	4.8	pKi	=	4.8	Binding	Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor	ChEMBL	322	6	1	4	3.1	N#Cc1ccc(-c2ccc(OCCCN3CC[C@@H](O)C3)cc2)cc1	10.1016/s0960-894x(02)00648-0
		156015722	185052	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	718	21	2	7	7.9	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
		CHEMBL4644467	185052	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	718	21	2	7	7.9	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
		CHEMBL4650837	185052	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	718	21	2	7	7.9	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
		156015152	185085	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	676	18	2	7	6.7	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
		CHEMBL4641916	185085	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	676	18	2	7	6.7	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
		CHEMBL4651017	185085	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	676	18	2	7	6.7	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
		164609729	191877	0	None	-2	6	Human	7.8	pKi	=	7.8	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	360	6	4	4	2.3	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)N[C@H](C)c1ccccc1	10.1016/j.ejmech.2021.113190
		CHEMBL4856059	191877	0	None	-2	6	Human	7.8	pKi	=	7.8	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	360	6	4	4	2.3	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)N[C@H](C)c1ccccc1	10.1016/j.ejmech.2021.113190
		1231	7724	116	None	-4	8	Human	6.8	pKi	=	6.8	Binding	Displacement of radiolabeled cimetidine from human histamine H2 receptorDisplacement of radiolabeled cimetidine from human histamine H2 receptor	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1021/jm8007618
		2756	7724	116	None	-4	8	Human	6.8	pKi	=	6.8	Binding	Displacement of radiolabeled cimetidine from human histamine H2 receptorDisplacement of radiolabeled cimetidine from human histamine H2 receptor	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1021/jm8007618
		645	7724	116	None	-4	8	Human	6.8	pKi	=	6.8	Binding	Displacement of radiolabeled cimetidine from human histamine H2 receptorDisplacement of radiolabeled cimetidine from human histamine H2 receptor	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1021/jm8007618
		CHEMBL30	7724	116	None	-4	8	Human	6.8	pKi	=	6.8	Binding	Displacement of radiolabeled cimetidine from human histamine H2 receptorDisplacement of radiolabeled cimetidine from human histamine H2 receptor	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1021/jm8007618
		DB00501	7724	116	None	-4	8	Human	6.8	pKi	=	6.8	Binding	Displacement of radiolabeled cimetidine from human histamine H2 receptorDisplacement of radiolabeled cimetidine from human histamine H2 receptor	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1021/jm8007618
		9906447	202356	2	None	-2344	13	Human	5.8	pKi	=	5.8	Binding	Binding affinity to human recombinant H2 receptorBinding affinity to human recombinant H2 receptor	ChEMBL	351	5	0	3	4.8	C[C@@H]1CCCN1CCc1cc2cc(C(=O)c3ccc(F)cc3)ccc2o1	10.1021/jm201690h
		CHEMBL2031738	202356	2	None	-2344	13	Human	5.8	pKi	=	5.8	Binding	Binding affinity to human recombinant H2 receptorBinding affinity to human recombinant H2 receptor	ChEMBL	351	5	0	3	4.8	C[C@@H]1CCCN1CCc1cc2cc(C(=O)c3ccc(F)cc3)ccc2o1	10.1021/jm201690h
		CHEMBL555146	202356	2	None	-2344	13	Human	5.8	pKi	=	5.8	Binding	Binding affinity to human recombinant H2 receptorBinding affinity to human recombinant H2 receptor	ChEMBL	351	5	0	3	4.8	C[C@@H]1CCCN1CCc1cc2cc(C(=O)c3ccc(F)cc3)ccc2o1	10.1021/jm201690h
		CHEMBL4576555	220796	5	None	-1	19	Human	5.8	pKi	=	5.8	Binding	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	109153	0	None	-95	4	Human	5.8	pKi	=	5.8	Binding	Compound was tested for its binding affinity towards human H2 receptorCompound was tested for its binding affinity towards human H2 receptor	ChEMBL	323	4	1	3	4.4	CN1CCCC1CCNc1c2c(nc3ccccc13)CCCCC2	10.1016/s0960-894x(03)00356-1
		CHEMBL303824	109153	0	None	-95	4	Human	5.8	pKi	=	5.8	Binding	Compound was tested for its binding affinity towards human H2 receptorCompound was tested for its binding affinity towards human H2 receptor	ChEMBL	323	4	1	3	4.4	CN1CCCC1CCNc1c2c(nc3ccccc13)CCCCC2	10.1016/s0960-894x(03)00356-1
		73349359	99318	0	None	-2	8	Human	5.8	pKi	=	5.8	Binding	Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	341	6	1	4	2.9	COc1cc(CN[C@H]2C3C4CC5C6C4CC3C6C52)cc(OC)c1OC	10.1016/j.bmc.2013.07.045
		CHEMBL2432051	99318	0	None	-2	8	Human	5.8	pKi	=	5.8	Binding	Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	341	6	1	4	2.9	COc1cc(CN[C@H]2C3C4CC5C6C4CC3C6C52)cc(OC)c1OC	10.1016/j.bmc.2013.07.045
		44304308	109262	0	None	-691	3	Human	4.8	pKi	=	4.8	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	432	8	0	5	3.7	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)c3cccc(F)c3F)cc2)CC1	10.1016/s0960-894x(02)00309-8
		CHEMBL304027	109262	0	None	-691	3	Human	4.8	pKi	=	4.8	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	432	8	0	5	3.7	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)c3cccc(F)c3F)cc2)CC1	10.1016/s0960-894x(02)00309-8
		44582676	196558	0	None	-13	17	Human	5.8	pKi	=	5.8	Binding	Inhibition of human cloned histamine H2 receptor by competitive binding experimentInhibition of human cloned histamine H2 receptor by competitive binding experiment	ChEMBL	403	9	0	4	4.3	COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(F)cc2)CC1	10.1016/j.bmc.2009.03.021
		CHEMBL516088	196558	0	None	-13	17	Human	5.8	pKi	=	5.8	Binding	Inhibition of human cloned histamine H2 receptor by competitive binding experimentInhibition of human cloned histamine H2 receptor by competitive binding experiment	ChEMBL	403	9	0	4	4.3	COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(F)cc2)CC1	10.1016/j.bmc.2009.03.021
		132060776	169181	0	None	-6	16	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method	ChEMBL	419	4	0	4	4.4	O=C(OCc1ccccc1)N1CCc2ccc(N3CCN(C4CCCC4)CC3)cc2C1	10.1016/j.ejmech.2018.02.024
		CHEMBL4165863	169181	0	None	-6	16	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method	ChEMBL	419	4	0	4	4.4	O=C(OCc1ccccc1)N1CCc2ccc(N3CCN(C4CCCC4)CC3)cc2C1	10.1016/j.ejmech.2018.02.024
		73346042	98609	5	None	-17782	17	Human	5.8	pKi	=	5.8	Binding	Binding affinity to histamine H2 receptor (unknown origin)Binding affinity to histamine H2 receptor (unknown origin)	ChEMBL	405	9	0	8	0.9	Cn1c(=O)cnn(CCCCN2CCN(c3ccccc3OCCF)CC2)c1=O	10.1016/j.bmc.2013.05.050
		CHEMBL2413153	98609	5	None	-17782	17	Human	5.8	pKi	=	5.8	Binding	Binding affinity to histamine H2 receptor (unknown origin)Binding affinity to histamine H2 receptor (unknown origin)	ChEMBL	405	9	0	8	0.9	Cn1c(=O)cnn(CCCCN2CCN(c3ccccc3OCCF)CC2)c1=O	10.1016/j.bmc.2013.05.050
		44304385	209957	0	None	-3548	3	Human	4.8	pKi	=	4.8	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	404	11	0	5	4.4	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OC(C)C)CC2)cc1	10.1016/s0960-894x(02)00309-8
		CHEMBL64259	209957	0	None	-3548	3	Human	4.8	pKi	=	4.8	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	404	11	0	5	4.4	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OC(C)C)CC2)cc1	10.1016/s0960-894x(02)00309-8
		10455457	210182	0	None	-3019	3	Human	4.8	pKi	=	4.8	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	431	10	0	5	3.3	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)N3CCOCC3)CC2)cc1	10.1016/s0960-894x(02)00309-8
		CHEMBL65518	210182	0	None	-3019	3	Human	4.8	pKi	=	4.8	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	431	10	0	5	3.3	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)N3CCOCC3)CC2)cc1	10.1016/s0960-894x(02)00309-8
		44304066	209544	0	None	-407	3	Human	4.8	pKi	=	4.8	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	449	11	1	5	3.0	CN[C@H](Cc1ccccc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		CHEMBL62050	209544	0	None	-407	3	Human	4.8	pKi	=	4.8	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	449	11	1	5	3.0	CN[C@H](Cc1ccccc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		71452383	90571	0	None	1	3	Human	5.8	pKi	=	5.8	Binding	Binding affinity to Histamine H2 receptorBinding affinity to Histamine H2 receptor	ChEMBL	339	5	1	4	2.0	COc1ccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1OC	10.1016/j.bmcl.2012.08.046
		CHEMBL2205814	90571	0	None	1	3	Human	5.8	pKi	=	5.8	Binding	Binding affinity to Histamine H2 receptorBinding affinity to Histamine H2 receptor	ChEMBL	339	5	1	4	2.0	COc1ccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1OC	10.1016/j.bmcl.2012.08.046
		1235	10595	36	None	-2	5	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]Aminopotentidine from human recombinant histamine H2 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Aminopotentidine from human recombinant histamine H2 receptor expressed in CHOK1 cells after 2 hrs	ChEMBL	312	6	4	6	-0.1	N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N	10.1016/j.bmcl.2013.01.025
		3959	10595	36	None	-2	5	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]Aminopotentidine from human recombinant histamine H2 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Aminopotentidine from human recombinant histamine H2 receptor expressed in CHOK1 cells after 2 hrs	ChEMBL	312	6	4	6	-0.1	N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N	10.1016/j.bmcl.2013.01.025
		50287	10595	36	None	-2	5	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]Aminopotentidine from human recombinant histamine H2 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Aminopotentidine from human recombinant histamine H2 receptor expressed in CHOK1 cells after 2 hrs	ChEMBL	312	6	4	6	-0.1	N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N	10.1016/j.bmcl.2013.01.025
		CHEMBL269646	10595	36	None	-2	5	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]Aminopotentidine from human recombinant histamine H2 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Aminopotentidine from human recombinant histamine H2 receptor expressed in CHOK1 cells after 2 hrs	ChEMBL	312	6	4	6	-0.1	N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N	10.1016/j.bmcl.2013.01.025
		4806	10780	88	None	-5	13	Human	6.8	pKi	=	6.8	Binding	Binding affinity to human histamine H2 receptorBinding affinity to human histamine H2 receptor	ChEMBL	298	3	1	3	3.9	Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1	10.1021/jm101459g
		7351	10780	88	None	-5	13	Human	6.8	pKi	=	6.8	Binding	Binding affinity to human histamine H2 receptorBinding affinity to human histamine H2 receptor	ChEMBL	298	3	1	3	3.9	Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1	10.1021/jm101459g
		9966051	10780	88	None	-5	13	Human	6.8	pKi	=	6.8	Binding	Binding affinity to human histamine H2 receptorBinding affinity to human histamine H2 receptor	ChEMBL	298	3	1	3	3.9	Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1	10.1021/jm101459g
		CHEMBL2104993	10780	88	None	-5	13	Human	6.8	pKi	=	6.8	Binding	Binding affinity to human histamine H2 receptorBinding affinity to human histamine H2 receptor	ChEMBL	298	3	1	3	3.9	Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1	10.1021/jm101459g
		DB09068	10780	88	None	-5	13	Human	6.8	pKi	=	6.8	Binding	Binding affinity to human histamine H2 receptorBinding affinity to human histamine H2 receptor	ChEMBL	298	3	1	3	3.9	Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1	10.1021/jm101459g
		10003483	11416	0	None	-660	3	Human	5.8	pKi	=	5.8	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	442	10	1	5	3.4	Cc1cccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)c1	10.1016/s0960-894x(02)00685-6
		CHEMBL103027	11416	0	None	-660	3	Human	5.8	pKi	=	5.8	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	442	10	1	5	3.4	Cc1cccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)c1	10.1016/s0960-894x(02)00685-6
		CHEMBL5076746	222304	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(N)(=O)=O)c3ccccc3C2(C)C)c2cc(S(=O)(=O)[O-])ccc2C1(C)C	10.1016/j.bmcl.2021.128388
		CHEMBL5095519	222304	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(N)(=O)=O)c3ccccc3C2(C)C)c2cc(S(=O)(=O)[O-])ccc2C1(C)C	10.1016/j.bmcl.2021.128388
		156015638	185051	0	None	-1819	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human recombinant H2R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]UR-DE257 from Gsalphas-coupled human recombinant H2R expressed in baculovirus infected Sf9 insect cell membranes	ChEMBL	415	10	1	2	5.5	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCc1c[nH]cn1	10.1021/acs.jmedchem.0c00160
		CHEMBL4642520	185051	0	None	-1819	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human recombinant H2R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]UR-DE257 from Gsalphas-coupled human recombinant H2R expressed in baculovirus infected Sf9 insect cell membranes	ChEMBL	415	10	1	2	5.5	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCc1c[nH]cn1	10.1021/acs.jmedchem.0c00160
		CHEMBL4650832	185051	0	None	-1819	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human recombinant H2R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]UR-DE257 from Gsalphas-coupled human recombinant H2R expressed in baculovirus infected Sf9 insect cell membranes	ChEMBL	415	10	1	2	5.5	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCc1c[nH]cn1	10.1021/acs.jmedchem.0c00160
		168281536	199660	0	None	-9	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	369	12	4	5	1.7	Cc1nnc(CCCN/C(N)=N/C(=O)NCCCCCCCCN)s1	10.1021/acs.jmedchem.1c00692
		CHEMBL5189006	199660	0	None	-9	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	369	12	4	5	1.7	Cc1nnc(CCCN/C(N)=N/C(=O)NCCCCCCCCN)s1	10.1021/acs.jmedchem.1c00692
		CHEMBL5221966	199660	0	None	-9	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	369	12	4	5	1.7	Cc1nnc(CCCN/C(N)=N/C(=O)NCCCCCCCCN)s1	10.1021/acs.jmedchem.1c00692
		3158	63041	27	None	-12589	20	Human	5.7	pKi	=	5.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	279	3	0	2	4.0	CN(C)CCC=C1c2ccccc2COc2ccccc21	nan
		CHEMBL1628227	63041	27	None	-12589	20	Human	5.7	pKi	=	5.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	279	3	0	2	4.0	CN(C)CCC=C1c2ccccc2COc2ccccc21	nan
		44304399	209972	0	None	-91	3	Human	5.7	pKi	=	5.7	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	418	13	0	5	4.8	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OCCCC)CC2)cc1	10.1016/s0960-894x(02)00309-8
		CHEMBL64317	209972	0	None	-91	3	Human	5.7	pKi	=	5.7	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	418	13	0	5	4.8	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OCCCC)CC2)cc1	10.1016/s0960-894x(02)00309-8
		44304376	209749	0	None	-354	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	423	11	0	5	4.1	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3ccccn3)CC2)cc1	10.1016/s0960-894x(02)00309-8
		CHEMBL63036	209749	0	None	-354	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	423	11	0	5	4.1	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3ccccn3)CC2)cc1	10.1016/s0960-894x(02)00309-8
		44304244	209955	0	None	-1174	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	372	12	0	4	4.2	CCCCCC(=O)c1ccc(OCCCN2CCN(CC3CC3)CC2)cc1	10.1016/s0960-894x(02)00309-8
		CHEMBL64253	209955	0	None	-1174	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	372	12	0	4	4.2	CCCCCC(=O)c1ccc(OCCCN2CCN(CC3CC3)CC2)cc1	10.1016/s0960-894x(02)00309-8
		44335384	11410	0	None	-2630	4	Human	4.7	pKi	=	4.7	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	334	6	0	3	4.9	CC1CCCCN1CCCOc1ccc(-c2ccc(C#N)cc2)cc1	10.1016/s0960-894x(02)00648-0
		CHEMBL102984	11410	0	None	-2630	4	Human	4.7	pKi	=	4.7	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	334	6	0	3	4.9	CC1CCCCN1CCCOc1ccc(-c2ccc(C#N)cc2)cc1	10.1016/s0960-894x(02)00648-0
		73355418	99321	0	None	-1	3	Human	5.7	pKi	=	5.7	Binding	Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	325	5	0	3	3.3	COc1ccc(CN(C)[C@H]2C3C4CC5C6C4CC3C6C52)cc1OC	10.1016/j.bmc.2013.07.045
		CHEMBL2432056	99321	0	None	-1	3	Human	5.7	pKi	=	5.7	Binding	Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	325	5	0	3	3.3	COc1ccc(CN(C)[C@H]2C3C4CC5C6C4CC3C6C52)cc1OC	10.1016/j.bmc.2013.07.045
		156011186	185022	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	704	20	2	7	7.5	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
		CHEMBL4637893	185022	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	704	20	2	7	7.5	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
		CHEMBL4650588	185022	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	704	20	2	7	7.5	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
		168294449	199797	0	None	-6	6	Human	7.7	pKi	=	7.7	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	367	7	4	5	1.9	CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1	10.1021/acs.jmedchem.1c00692
		CHEMBL5204599	199797	0	None	-6	6	Human	7.7	pKi	=	7.7	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	367	7	4	5	1.9	CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1	10.1021/acs.jmedchem.1c00692
		CHEMBL5222793	199797	0	None	-6	6	Human	7.7	pKi	=	7.7	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	367	7	4	5	1.9	CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1	10.1021/acs.jmedchem.1c00692
		168294161	199785	0	None	3	4	Human	6.7	pKi	=	6.7	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	360	6	4	4	3.3	CCCCCNC(=O)/N=C(\N)Nc1cccc(-c2sc(N)nc2C)c1	10.1021/acs.jmedchem.1c00692
		CHEMBL5204739	199785	0	None	3	4	Human	6.7	pKi	=	6.7	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	360	6	4	4	3.3	CCCCCNC(=O)/N=C(\N)Nc1cccc(-c2sc(N)nc2C)c1	10.1021/acs.jmedchem.1c00692
		CHEMBL5222742	199785	0	None	3	4	Human	6.7	pKi	=	6.7	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	360	6	4	4	3.3	CCCCCNC(=O)/N=C(\N)Nc1cccc(-c2sc(N)nc2C)c1	10.1021/acs.jmedchem.1c00692
		9923186	114319	0	None	-977	4	Human	4.7	pKi	=	4.7	Binding	Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor	ChEMBL	322	6	1	4	3.1	N#Cc1ccc(-c2ccc(OCCCN3CC[C@H](O)C3)cc2)cc1	10.1016/s0960-894x(02)00648-0
		CHEMBL318801	114319	0	None	-977	4	Human	4.7	pKi	=	4.7	Binding	Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor	ChEMBL	322	6	1	4	3.1	N#Cc1ccc(-c2ccc(OCCCN3CC[C@H](O)C3)cc2)cc1	10.1016/s0960-894x(02)00648-0
		12192007	175187	44	None	-724	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	191	2	2	2	0.8	N[C@@H](C(=O)O)C1Cc2ccccc2C1	10.1016/s0960-894x(02)00310-4
		CHEMBL434785	175187	44	None	-724	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	191	2	2	2	0.8	N[C@@H](C(=O)O)C1Cc2ccccc2C1	10.1016/s0960-894x(02)00310-4
		44304013	209673	0	None	-363	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	401	8	1	5	2.6	CC(C)(C)[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		CHEMBL62716	209673	0	None	-363	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	401	8	1	5	2.6	CC(C)(C)[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		72901200	126555	25	None	-1318	4	Human	5.7	pKi	=	5.7	Binding	Selectivity interaction (PRESTO-Tango GPCR-ome screening) EUB0000539a HRH2Selectivity interaction (PRESTO-Tango GPCR-ome screening) EUB0000539a HRH2	ChEMBL	322	7	2	4	3.8	Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1	10.6019/CHEMBL5212743
		CHEMBL3480577	126555	25	None	-1318	4	Human	5.7	pKi	=	5.7	Binding	Selectivity interaction (PRESTO-Tango GPCR-ome screening) EUB0000539a HRH2Selectivity interaction (PRESTO-Tango GPCR-ome screening) EUB0000539a HRH2	ChEMBL	322	7	2	4	3.8	Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1	10.6019/CHEMBL5212743
		5291	214216	120	None	-1	2	Human	5.7	pKi	=	5.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	493	7	2	7	4.6	Cc1ccc(NC(=O)c2ccc(CN3CCN(C)CC3)cc2)cc1Nc1nccc(-c2cccnc2)n1	nan
		CHEMBL941	214216	120	None	-1	2	Human	5.7	pKi	=	5.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	493	7	2	7	4.6	Cc1ccc(NC(=O)c2ccc(CN3CCN(C)CC3)cc2)cc1Nc1nccc(-c2cccnc2)n1	nan
		44304259	107391	0	None	-660	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	462	11	0	5	5.4	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3sccc3Cl)CC2)cc1	10.1016/s0960-894x(02)00309-8
		CHEMBL291882	107391	0	None	-660	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	462	11	0	5	5.4	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3sccc3Cl)CC2)cc1	10.1016/s0960-894x(02)00309-8
		10341609	207049	0	None	-4365	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	412	11	1	5	3.4	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3c[nH]cn3)CC2)cc1	10.1016/s0960-894x(02)00309-8
		CHEMBL59715	207049	0	None	-4365	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	412	11	1	5	3.4	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3c[nH]cn3)CC2)cc1	10.1016/s0960-894x(02)00309-8
		277	8083	62	None	-43	50	Human	6.7	pKi	=	6.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	287	0	0	1	4.7	CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1	nan
		2913	8083	62	None	-43	50	Human	6.7	pKi	=	6.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	287	0	0	1	4.7	CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1	nan
		765	8083	62	None	-43	50	Human	6.7	pKi	=	6.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	287	0	0	1	4.7	CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1	nan
		CHEMBL516	8083	62	None	-43	50	Human	6.7	pKi	=	6.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	287	0	0	1	4.7	CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1	nan
		DB00434	8083	62	None	-43	50	Human	6.7	pKi	=	6.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	287	0	0	1	4.7	CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1	nan
		153287553	177883	0	None	-316	6	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]-Iodoaminopotentidine from human recombinant histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-Iodoaminopotentidine from human recombinant histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method	ChEMBL	264	1	1	2	3.7	C[C@@]12CN(c3ccccc3)c3ccccc3[C@@H]1CCN2	10.1021/acsmedchemlett.9b00225
		CHEMBL4457754	177883	0	None	-316	6	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]-Iodoaminopotentidine from human recombinant histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-Iodoaminopotentidine from human recombinant histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method	ChEMBL	264	1	1	2	3.7	C[C@@]12CN(c3ccccc3)c3ccccc3[C@@H]1CCN2	10.1021/acsmedchemlett.9b00225
		164619039	192927	0	None	17	2	Human	5.7	pKi	=	5.7	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	366	4	4	4	3.0	N/C(=N\C(=O)NCc1ccccc1)Nc1cccc(-c2csc(N)n2)c1	10.1016/j.ejmech.2021.113190
		CHEMBL4872277	192927	0	None	17	2	Human	5.7	pKi	=	5.7	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	366	4	4	4	3.0	N/C(=N\C(=O)NCc1ccccc1)Nc1cccc(-c2csc(N)n2)c1	10.1016/j.ejmech.2021.113190
		10263017	214241	2	None	-31	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.	ChEMBL	223	10	2	2	3.0	NCCCCCCCCCCc1c[nH]cn1	10.1021/jm00002a008
		CHEMBL94249	214241	2	None	-31	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.	ChEMBL	223	10	2	2	3.0	NCCCCCCCCCCc1c[nH]cn1	10.1021/jm00002a008
		44304247	209588	0	None	-1905	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	412	11	0	5	4.3	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3ccco3)CC2)cc1	10.1016/s0960-894x(02)00309-8
		CHEMBL62312	209588	0	None	-1905	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	412	11	0	5	4.3	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3ccco3)CC2)cc1	10.1016/s0960-894x(02)00309-8
		5250783	176166	3	None	-1995	3	Human	4.7	pKi	=	4.7	Binding	Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors	ChEMBL	226	6	3	2	1.6	C/N=C(\S)NCCCCCc1c[nH]cn1	10.1021/jm00012a025
		CHEMBL44220	176166	3	None	-1995	3	Human	4.7	pKi	=	4.7	Binding	Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors	ChEMBL	226	6	3	2	1.6	C/N=C(\S)NCCCCCc1c[nH]cn1	10.1021/jm00012a025
		CHEMBL5276441	200679	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	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	193157	0	None	4	6	Human	8.7	pKi	=	8.7	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	378	6	4	4	2.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1cccc(F)c1	10.1016/j.ejmech.2021.113190
		CHEMBL4875600	193157	0	None	4	6	Human	8.7	pKi	=	8.7	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	378	6	4	4	2.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1cccc(F)c1	10.1016/j.ejmech.2021.113190
		2398	7741	62	None	-13	29	Human	5.7	pKi	=	5.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	314	4	0	2	4.5	CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C	nan
		2801	7741	62	None	-13	29	Human	5.7	pKi	=	5.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	314	4	0	2	4.5	CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C	nan
		701	7741	62	None	-13	29	Human	5.7	pKi	=	5.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	314	4	0	2	4.5	CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C	nan
		CHEMBL415	7741	62	None	-13	29	Human	5.7	pKi	=	5.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	314	4	0	2	4.5	CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C	nan
		DB01242	7741	62	None	-13	29	Human	5.7	pKi	=	5.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	314	4	0	2	4.5	CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C	nan
		156015243	185017	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	1081	29	4	13	8.5	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3cc(S(=O)(=O)O)ccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
		CHEMBL4648203	185017	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	1081	29	4	13	8.5	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3cc(S(=O)(=O)O)ccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
		CHEMBL4650564	185017	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	1081	29	4	13	8.5	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3cc(S(=O)(=O)O)ccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
		44304068	109124	0	None	-125	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	441	10	1	5	3.5	N[C@H](CC1CCCCC1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		CHEMBL303737	109124	0	None	-125	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	441	10	1	5	3.5	N[C@H](CC1CCCCC1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		44304030	207741	0	None	-154	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	511	11	1	5	4.4	N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		CHEMBL60189	207741	0	None	-154	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	511	11	1	5	4.4	N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		44304991	209840	0	None	-1659	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	424	12	0	5	3.6	CCCCCC(=O)c1ccc(OCCCN2CCN(S(=O)(=O)C(C)C)CC2)cc1	10.1016/s0960-894x(02)00309-8
		CHEMBL63631	209840	0	None	-1659	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	424	12	0	5	3.6	CCCCCC(=O)c1ccc(OCCCN2CCN(S(=O)(=O)C(C)C)CC2)cc1	10.1016/s0960-894x(02)00309-8
		44304294	209742	0	None	-97	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	485	10	1	5	3.9	N[C@H](Cc1cccc2ccccc12)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		CHEMBL63003	209742	0	None	-97	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	485	10	1	5	3.9	N[C@H](Cc1cccc2ccccc12)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		CHEMBL4520788	220754	10	None	3	25	Human	7.7	pKi	=	7.7	Binding	Selectivity interaction (GPCR panel (PDSP screen)) EUB0000743a HRH2Selectivity interaction (GPCR panel (PDSP screen)) EUB0000743a HRH2	ChEMBL		None	None	None		CNCc1ccccc1-c1csc([C@H](C)Nc2nc(C)nc3cc(OC)c(OC)cc23)c1	10.6019/CHEMBL5212743
		156021166	185116	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	908	25	3	8	10.3	C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21	10.1021/acsmedchemlett.0c00033
		CHEMBL4647775	185116	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	908	25	3	8	10.3	C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21	10.1021/acsmedchemlett.0c00033
		CHEMBL4651205	185116	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	908	25	3	8	10.3	C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21	10.1021/acsmedchemlett.0c00033
		CHEMBL5094663	222285	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](C)c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
		21830793	98610	10	None	-14125	46	Human	5.7	pKi	=	5.7	Binding	Binding affinity to histamine H2 receptor (unknown origin)Binding affinity to histamine H2 receptor (unknown origin)	ChEMBL	373	7	0	8	0.6	COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1	10.1016/j.bmc.2013.05.050
		CHEMBL2413154	98610	10	None	-14125	46	Human	5.7	pKi	=	5.7	Binding	Binding affinity to histamine H2 receptor (unknown origin)Binding affinity to histamine H2 receptor (unknown origin)	ChEMBL	373	7	0	8	0.6	COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1	10.1016/j.bmc.2013.05.050
		11948707	172946	0	None	-5248	13	Human	5.7	pKi	=	5.7	Binding	Binding affinity to histamine H2 receptor by radioligand binding assayBinding affinity to histamine H2 receptor by radioligand binding assay	ChEMBL	373	7	0	8	0.6	COc1cccc(N2CCN(CCCCn3ncc(=O)n(C)c3=O)CC2)c1	10.1016/j.bmcl.2006.01.052
		CHEMBL426317	172946	0	None	-5248	13	Human	5.7	pKi	=	5.7	Binding	Binding affinity to histamine H2 receptor by radioligand binding assayBinding affinity to histamine H2 receptor by radioligand binding assay	ChEMBL	373	7	0	8	0.6	COc1cccc(N2CCN(CCCCn3ncc(=O)n(C)c3=O)CC2)c1	10.1016/j.bmcl.2006.01.052
		168295543	199820	0	None	1	4	Human	6.7	pKi	=	6.7	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	380	4	4	4	3.3	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCc2ccccc2)cc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5209021	199820	0	None	1	4	Human	6.7	pKi	=	6.7	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	380	4	4	4	3.3	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCc2ccccc2)cc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5222929	199820	0	None	1	4	Human	6.7	pKi	=	6.7	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	380	4	4	4	3.3	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCc2ccccc2)cc1	10.1021/acs.jmedchem.1c00692
		44304459	179379	0	None	-575	3	Human	5.7	pKi	=	5.7	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	418	13	0	5	4.8	CCCCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OCC)CC2)cc1	10.1016/s0960-894x(02)00309-8
		CHEMBL449040	179379	0	None	-575	3	Human	5.7	pKi	=	5.7	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	418	13	0	5	4.8	CCCCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OCC)CC2)cc1	10.1016/s0960-894x(02)00309-8
		53320569	63628	0	None	3	2	Human	5.7	pKi	=	5.7	Binding	Inhibition of H2 receptorInhibition of H2 receptor	ChEMBL	269	3	1	1	3.1	Fc1cccc(CN[C@H]2C3C4CC5C6C4CC3C6C52)c1	10.1016/j.bmcl.2010.11.075
		CHEMBL1643899	63628	0	None	3	2	Human	5.7	pKi	=	5.7	Binding	Inhibition of H2 receptorInhibition of H2 receptor	ChEMBL	269	3	1	1	3.1	Fc1cccc(CN[C@H]2C3C4CC5C6C4CC3C6C52)c1	10.1016/j.bmcl.2010.11.075
		53320569	63628	0	None	3	2	Human	5.7	pKi	=	5.7	Binding	Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	269	3	1	1	3.1	Fc1cccc(CN[C@H]2C3C4CC5C6C4CC3C6C52)c1	10.1016/j.bmc.2013.07.045
		CHEMBL1643899	63628	0	None	3	2	Human	5.7	pKi	=	5.7	Binding	Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	269	3	1	1	3.1	Fc1cccc(CN[C@H]2C3C4CC5C6C4CC3C6C52)c1	10.1016/j.bmc.2013.07.045
		3823	56995	42	None	-66	11	Human	4.7	pKi	=	4.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	530	7	0	7	4.2	CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1	nan
		76973198	56995	42	None	-66	11	Human	4.7	pKi	=	4.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	530	7	0	7	4.2	CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1	nan
		CHEMBL157101	56995	42	None	-66	11	Human	4.7	pKi	=	4.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	530	7	0	7	4.2	CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1	nan
		168283536	199679	0	None	-53	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	312	8	3	4	1.6	CCCCCNC(=O)/N=C(/N)NCCCc1nnc(C)s1	10.1021/acs.jmedchem.1c00692
		CHEMBL5187758	199679	0	None	-53	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	312	8	3	4	1.6	CCCCCNC(=O)/N=C(/N)NCCCc1nnc(C)s1	10.1021/acs.jmedchem.1c00692
		CHEMBL5222074	199679	0	None	-53	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	312	8	3	4	1.6	CCCCCNC(=O)/N=C(/N)NCCCc1nnc(C)s1	10.1021/acs.jmedchem.1c00692
		44304021	109572	0	None	-562	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	374	8	0	5	3.4	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)C=C(C)C)cc2)CC1	10.1016/s0960-894x(02)00309-8
		CHEMBL305313	109572	0	None	-562	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	374	8	0	5	3.4	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)C=C(C)C)cc2)CC1	10.1016/s0960-894x(02)00309-8
		168278471	199627	0	None	-18	6	Human	7.6	pKi	=	7.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	312	8	4	4	1.5	CCCCCNC(=O)/N=C(\N)NCCCc1cnc(N)s1	10.1021/acs.jmedchem.1c00692
		CHEMBL5183205	199627	0	None	-18	6	Human	7.6	pKi	=	7.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	312	8	4	4	1.5	CCCCCNC(=O)/N=C(\N)NCCCc1cnc(N)s1	10.1021/acs.jmedchem.1c00692
		CHEMBL5221757	199627	0	None	-18	6	Human	7.6	pKi	=	7.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	312	8	4	4	1.5	CCCCCNC(=O)/N=C(\N)NCCCc1cnc(N)s1	10.1021/acs.jmedchem.1c00692
		44334235	11403	0	None	-199	3	Human	5.7	pKi	=	5.7	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	442	10	1	5	3.4	Cc1ccccc1S(=O)(=O)N[C@H]1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)C1	10.1016/s0960-894x(02)00685-6
		CHEMBL102929	11403	0	None	-199	3	Human	5.7	pKi	=	5.7	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	442	10	1	5	3.4	Cc1ccccc1S(=O)(=O)N[C@H]1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)C1	10.1016/s0960-894x(02)00685-6
		44334503	11767	0	None	-144	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	349	9	3	6	0.2	CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)[C@@H](N)CO)C2)cc1	10.1016/s0960-894x(02)00685-6
		CHEMBL104994	11767	0	None	-144	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	349	9	3	6	0.2	CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)[C@@H](N)CO)C2)cc1	10.1016/s0960-894x(02)00685-6
		44304036	103557	0	None	-407	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	360	8	0	5	3.0	C=C(C)C(=O)c1ccc(OCCCN2CCN(C(=O)OCC)CC2)cc1	10.1016/s0960-894x(02)00309-8
		CHEMBL264761	103557	0	None	-407	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	360	8	0	5	3.0	C=C(C)C(=O)c1ccc(OCCCN2CCN(C(=O)OCC)CC2)cc1	10.1016/s0960-894x(02)00309-8
		44304269	107320	0	None	-3548	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	423	11	0	5	4.1	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3ccncc3)CC2)cc1	10.1016/s0960-894x(02)00309-8
		CHEMBL291394	107320	0	None	-3548	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	423	11	0	5	4.1	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3ccncc3)CC2)cc1	10.1016/s0960-894x(02)00309-8
		44304037	109470	0	None	-6165	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	362	9	0	5	3.2	CCCC(=O)c1ccc(OCCCN2CCN(C(=O)OCC)CC2)cc1	10.1016/s0960-894x(02)00309-8
		CHEMBL304714	109470	0	None	-6165	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	362	9	0	5	3.2	CCCC(=O)c1ccc(OCCCN2CCN(C(=O)OCC)CC2)cc1	10.1016/s0960-894x(02)00309-8
		CHEMBL5094083	222246	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL		None	None	None		C=C(/N=C(\C)NCCCc1nnc(N)s1)NCCCCCCCCN	10.1016/j.bmcl.2021.128388
		164611143	191495	0	None	75	4	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	414	6	4	4	2.9	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(c1ccccc1)C(F)(F)F	10.1016/j.ejmech.2021.113190
		CHEMBL4850448	191495	0	None	75	4	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	414	6	4	4	2.9	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(c1ccccc1)C(F)(F)F	10.1016/j.ejmech.2021.113190
		44304438	209947	0	None	-2089	3	Human	4.6	pKi	=	4.6	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	420	13	0	5	4.1	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)CSCC)CC2)cc1	10.1016/s0960-894x(02)00309-8
		CHEMBL64235	209947	0	None	-2089	3	Human	4.6	pKi	=	4.6	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	420	13	0	5	4.1	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)CSCC)CC2)cc1	10.1016/s0960-894x(02)00309-8
		44304307	210012	0	None	-3548	3	Human	4.6	pKi	=	4.6	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	388	12	0	4	4.2	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)CCC)CC2)cc1	10.1016/s0960-894x(02)00309-8
		CHEMBL64479	210012	0	None	-3548	3	Human	4.6	pKi	=	4.6	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	388	12	0	4	4.2	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)CCC)CC2)cc1	10.1016/s0960-894x(02)00309-8
		44335405	11875	0	None	-194	4	Human	4.6	pKi	=	4.6	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	321	6	1	4	2.9	N#Cc1ccc(-c2ccc(OCCCN3CCNCC3)cc2)cc1	10.1016/s0960-894x(02)00648-0
		CHEMBL105594	11875	0	None	-194	4	Human	4.6	pKi	=	4.6	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	321	6	1	4	2.9	N#Cc1ccc(-c2ccc(OCCCN3CCNCC3)cc2)cc1	10.1016/s0960-894x(02)00648-0
		44304415	208807	0	None	-9549	3	Human	4.6	pKi	=	4.6	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	505	13	2	7	3.2	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](CO)NC(=O)OC(C)(C)C)CC2)cc1	10.1016/s0960-894x(02)00310-4
		CHEMBL60837	208807	0	None	-9549	3	Human	4.6	pKi	=	4.6	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	505	13	2	7	3.2	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](CO)NC(=O)OC(C)(C)C)CC2)cc1	10.1016/s0960-894x(02)00310-4
		1971	9641	38	None	-22	30	Human	5.6	pKi	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	263	3	1	1	3.8	CNCCC=C1c2ccccc2CCc2c1cccc2	nan
		2404	9641	38	None	-22	30	Human	5.6	pKi	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	263	3	1	1	3.8	CNCCC=C1c2ccccc2CCc2c1cccc2	nan
		4543	9641	38	None	-22	30	Human	5.6	pKi	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	263	3	1	1	3.8	CNCCC=C1c2ccccc2CCc2c1cccc2	nan
		CHEMBL445	9641	38	None	-22	30	Human	5.6	pKi	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	263	3	1	1	3.8	CNCCC=C1c2ccccc2CCc2c1cccc2	nan
		DB00540	9641	38	None	-22	30	Human	5.6	pKi	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	263	3	1	1	3.8	CNCCC=C1c2ccccc2CCc2c1cccc2	nan
		44334214	11387	0	None	-380	3	Human	5.6	pKi	=	5.6	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	427	9	1	6	2.6	CC(=O)c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccc(C#N)cc3)C2)cc1	10.1016/s0960-894x(02)00685-6
		CHEMBL102840	11387	0	None	-380	3	Human	5.6	pKi	=	5.6	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	427	9	1	6	2.6	CC(=O)c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccc(C#N)cc3)C2)cc1	10.1016/s0960-894x(02)00685-6
		168268827	199558	0	None	3	4	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	450	8	4	4	4.8	Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)c1	10.1021/acs.jmedchem.1c00692
		CHEMBL5179906	199558	0	None	3	4	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	450	8	4	4	4.8	Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)c1	10.1021/acs.jmedchem.1c00692
		CHEMBL5221314	199558	0	None	3	4	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	450	8	4	4	4.8	Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)c1	10.1021/acs.jmedchem.1c00692
		168294770	199799	0	None	2	4	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	436	6	4	4	4.3	Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)cc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5208327	199799	0	None	2	4	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	436	6	4	4	4.3	Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)cc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5222806	199799	0	None	2	4	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	436	6	4	4	4.3	Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)cc1	10.1021/acs.jmedchem.1c00692
		44304325	208457	0	None	-1096	3	Human	4.6	pKi	=	4.6	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	389	11	1	4	3.6	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)NCC)CC2)cc1	10.1016/s0960-894x(02)00309-8
		CHEMBL60620	208457	0	None	-1096	3	Human	4.6	pKi	=	4.6	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	389	11	1	4	3.6	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)NCC)CC2)cc1	10.1016/s0960-894x(02)00309-8
		44335368	11822	0	None	-63	3	Human	4.6	pKi	=	4.6	Binding	Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor	ChEMBL	393	7	0	5	3.8	CCOC(=O)N1CCN(CCCOc2ccc(-c3cccc(C#N)c3)cc2)CC1	10.1016/s0960-894x(02)00648-0
		CHEMBL105268	11822	0	None	-63	3	Human	4.6	pKi	=	4.6	Binding	Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor	ChEMBL	393	7	0	5	3.8	CCOC(=O)N1CCN(CCCOc2ccc(-c3cccc(C#N)c3)cc2)CC1	10.1016/s0960-894x(02)00648-0
		44335238	11861	0	None	-11220	4	Human	4.6	pKi	=	4.6	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	348	6	0	3	5.3	CC1CCCC(C)N1CCCOc1ccc(-c2ccc(C#N)cc2)cc1	10.1016/s0960-894x(02)00648-0
		CHEMBL105515	11861	0	None	-11220	4	Human	4.6	pKi	=	4.6	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	348	6	0	3	5.3	CC1CCCC(C)N1CCCOc1ccc(-c2ccc(C#N)cc2)cc1	10.1016/s0960-894x(02)00648-0
		44333987	115326	0	None	-26	3	Human	4.6	pKi	=	4.6	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	433	9	2	6	2.8	CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)[C@H](C)NC(=O)OC(C)(C)C)C2)cc1	10.1016/s0960-894x(02)00685-6
		CHEMBL320174	115326	0	None	-26	3	Human	4.6	pKi	=	4.6	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	433	9	2	6	2.8	CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)[C@H](C)NC(=O)OC(C)(C)C)C2)cc1	10.1016/s0960-894x(02)00685-6
		44582675	196480	0	None	-40	15	Human	5.6	pKi	=	5.6	Binding	Inhibition of human cloned histamine H2 receptor by competitive binding experimentInhibition of human cloned histamine H2 receptor by competitive binding experiment	ChEMBL	405	9	1	4	4.2	COc1c(OCCF)cccc1[C@H](O)C1CCN(CCc2ccc(F)cc2)CC1	10.1016/j.bmc.2009.03.021
		CHEMBL515472	196480	0	None	-40	15	Human	5.6	pKi	=	5.6	Binding	Inhibition of human cloned histamine H2 receptor by competitive binding experimentInhibition of human cloned histamine H2 receptor by competitive binding experiment	ChEMBL	405	9	1	4	4.2	COc1c(OCCF)cccc1[C@H](O)C1CCN(CCc2ccc(F)cc2)CC1	10.1016/j.bmc.2009.03.021
		168283321	199674	0	None	2	4	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	364	7	4	4	2.3	Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1	10.1021/acs.jmedchem.1c00692
		CHEMBL5183015	199674	0	None	2	4	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	364	7	4	4	2.3	Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1	10.1021/acs.jmedchem.1c00692
		CHEMBL5222057	199674	0	None	2	4	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	364	7	4	4	2.3	Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1	10.1021/acs.jmedchem.1c00692
		44304437	107773	0	None	-426	3	Human	4.6	pKi	=	4.6	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	404	11	1	5	3.1	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)C(C)(C)O)CC2)cc1	10.1016/s0960-894x(02)00309-8
		CHEMBL294349	107773	0	None	-426	3	Human	4.6	pKi	=	4.6	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	404	11	1	5	3.1	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)C(C)(C)O)CC2)cc1	10.1016/s0960-894x(02)00309-8
		44304049	108915	0	None	-891	3	Human	4.6	pKi	=	4.6	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	421	9	1	5	2.9	N[C@@H](C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1)c1ccccc1	10.1016/s0960-894x(02)00310-4
		CHEMBL302468	108915	0	None	-891	3	Human	4.6	pKi	=	4.6	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	421	9	1	5	2.9	N[C@@H](C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1)c1ccccc1	10.1016/s0960-894x(02)00310-4
		146025727	178464	0	None	-93	27	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method	ChEMBL	411	3	0	5	6.4	FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12	10.1021/acs.jmedchem.9b00351
		CHEMBL4466483	178464	0	None	-93	27	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method	ChEMBL	411	3	0	5	6.4	FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12	10.1021/acs.jmedchem.9b00351
		CHEMBL5087637	222334	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
		CHEMBL5095891	222334	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
		44304304	176842	0	None	-3981	3	Human	4.6	pKi	=	4.6	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	423	9	0	6	3.5	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)/C=C/c3cccnc3)cc2)CC1	10.1016/s0960-894x(02)00309-8
		CHEMBL444307	176842	0	None	-3981	3	Human	4.6	pKi	=	4.6	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	423	9	0	6	3.5	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)/C=C/c3cccnc3)cc2)CC1	10.1016/s0960-894x(02)00309-8
		1248	8206	28	None	-123	7	Human	4.6	pKi	=	4.6	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	161	4	2	3	0.6	CN(CCCSC(=N)N)C	10.1016/j.bmcl.2010.10.041
		3077	8206	28	None	-123	7	Human	4.6	pKi	=	4.6	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	161	4	2	3	0.6	CN(CCCSC(=N)N)C	10.1016/j.bmcl.2010.10.041
		90045	8206	28	None	-123	7	Human	4.6	pKi	=	4.6	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	161	4	2	3	0.6	CN(CCCSC(=N)N)C	10.1016/j.bmcl.2010.10.041
		CHEMBL12344	8206	28	None	-123	7	Human	4.6	pKi	=	4.6	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	161	4	2	3	0.6	CN(CCCSC(=N)N)C	10.1016/j.bmcl.2010.10.041
		145988693	173945	0	None	-10	17	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assay	ChEMBL	524	7	1	3	7.1	OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCN(c2ccc(F)cc2)c2ccc(F)cc2)CC1	10.1016/j.bmcl.2018.10.036
		CHEMBL4291048	173945	0	None	-10	17	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assay	ChEMBL	524	7	1	3	7.1	OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCN(c2ccc(F)cc2)c2ccc(F)cc2)CC1	10.1016/j.bmcl.2018.10.036
		2520	210787	70	None	-20	12	Human	5.6	pKi	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	454	13	0	6	5.1	COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC	nan
		CHEMBL1280	210787	70	None	-20	12	Human	5.6	pKi	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	454	13	0	6	5.1	COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC	nan
		CHEMBL6966	210787	70	None	-20	12	Human	5.6	pKi	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	454	13	0	6	5.1	COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC	nan
		2726	7706	68	None	-85	72	Human	5.6	pKi	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	nan
		621	7706	68	None	-85	72	Human	5.6	pKi	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	nan
		83	7706	68	None	-85	72	Human	5.6	pKi	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	nan
		CHEMBL71	7706	68	None	-85	72	Human	5.6	pKi	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	nan
		DB00477	7706	68	None	-85	72	Human	5.6	pKi	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	nan
		CHEMBL5273718	200553	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	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	199587	0	None	-13	6	Human	7.6	pKi	=	7.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	332	6	4	4	1.5	N/C(=N\C(=O)NCc1ccccc1)NCCCc1cnc(N)s1	10.1021/acs.jmedchem.1c00692
		CHEMBL5178472	199587	0	None	-13	6	Human	7.6	pKi	=	7.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	332	6	4	4	1.5	N/C(=N\C(=O)NCc1ccccc1)NCCCc1cnc(N)s1	10.1021/acs.jmedchem.1c00692
		CHEMBL5221451	199587	0	None	-13	6	Human	7.6	pKi	=	7.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	332	6	4	4	1.5	N/C(=N\C(=O)NCc1ccccc1)NCCCc1cnc(N)s1	10.1021/acs.jmedchem.1c00692
		155543832	179990	0	None	-234	7	Human	5.6	pKi	=	5.6	Binding	Inhibition of histamine H2 receptor (unknown origin)Inhibition of histamine H2 receptor (unknown origin)	ChEMBL	451	6	3	7	3.4	O[C@H]1[C@H](n2cnc3c(NC(C4CCC4)C4CCC4)nc(Cl)nc32)[C@H]2C[C@@]2(CCl)[C@H]1O	10.1021/acs.jmedchem.8b01662
		CHEMBL4522864	179990	0	None	-234	7	Human	5.6	pKi	=	5.6	Binding	Inhibition of histamine H2 receptor (unknown origin)Inhibition of histamine H2 receptor (unknown origin)	ChEMBL	451	6	3	7	3.4	O[C@H]1[C@H](n2cnc3c(NC(C4CCC4)C4CCC4)nc(Cl)nc32)[C@H]2C[C@@]2(CCl)[C@H]1O	10.1021/acs.jmedchem.8b01662
		1204	8713	119	None	-173	25	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
		1247	8713	119	None	-173	25	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
		1375	8713	119	None	-173	25	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
		774	8713	119	None	-173	25	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
		CHEMBL90	8713	119	None	-173	25	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
		DB05381	8713	119	None	-173	25	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
		CHEMBL5077939	222320	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)O)c3ccccc3C2(C)C)c2cc(S(=O)(=O)[O-])ccc2C1(C)C	10.1016/j.bmcl.2021.128388
		CHEMBL5095769	222320	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)O)c3ccccc3C2(C)C)c2cc(S(=O)(=O)[O-])ccc2C1(C)C	10.1016/j.bmcl.2021.128388
		CHEMBL5093461	222332	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL		None	None	None		CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2nnc(N)s2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1016/j.bmcl.2021.128388
		CHEMBL5095884	222332	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL		None	None	None		CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2nnc(N)s2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1016/j.bmcl.2021.128388
		1204	8713	119	None	-173	25	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.ejmech.2021.113190
		1247	8713	119	None	-173	25	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.ejmech.2021.113190
		1375	8713	119	None	-173	25	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.ejmech.2021.113190
		774	8713	119	None	-173	25	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.ejmech.2021.113190
		CHEMBL90	8713	119	None	-173	25	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.ejmech.2021.113190
		DB05381	8713	119	None	-173	25	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.ejmech.2021.113190
		1204	8713	119	None	-173	25	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.1c00692
		1247	8713	119	None	-173	25	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.1c00692
		1375	8713	119	None	-173	25	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.1c00692
		774	8713	119	None	-173	25	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.1c00692
		CHEMBL90	8713	119	None	-173	25	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.1c00692
		DB05381	8713	119	None	-173	25	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.1c00692
		156015793	185038	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	880	23	3	8	9.5	C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21	10.1021/acsmedchemlett.0c00033
		CHEMBL4645867	185038	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	880	23	3	8	9.5	C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21	10.1021/acsmedchemlett.0c00033
		CHEMBL4650701	185038	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	880	23	3	8	9.5	C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21	10.1021/acsmedchemlett.0c00033
		44304091	209730	0	None	-338	3	Human	5.6	pKi	=	5.6	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	432	14	0	5	5.2	CCCCCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OCC)CC2)cc1	10.1016/s0960-894x(02)00309-8
		CHEMBL62949	209730	0	None	-338	3	Human	5.6	pKi	=	5.6	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	432	14	0	5	5.2	CCCCCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OCC)CC2)cc1	10.1016/s0960-894x(02)00309-8
		44304516	172135	0	None	-630	3	Human	4.6	pKi	=	4.6	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	357	8	1	5	1.5	O=C1C[C@H](N2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)CC2)N1	10.1016/s0960-894x(02)00310-4
		CHEMBL423666	172135	0	None	-630	3	Human	4.6	pKi	=	4.6	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	357	8	1	5	1.5	O=C1C[C@H](N2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)CC2)N1	10.1016/s0960-894x(02)00310-4
		18609376	211138	63	None	-	1	Human	4.6	pKi	=	4.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	386	2	0	4	4.7	CC(=O)O[C@]1(C(C)=O)CC[C@H]2[C@@H]3C[C@H](C)C4=CC(=O)CC[C@]4(C)[C@H]3CC[C@@]21C	nan
		6279	211138	63	None	-	1	Human	4.6	pKi	=	4.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	386	2	0	4	4.7	CC(=O)O[C@]1(C(C)=O)CC[C@H]2[C@@H]3C[C@H](C)C4=CC(=O)CC[C@]4(C)[C@H]3CC[C@@]21C	nan
		CHEMBL717	211138	63	None	-	1	Human	4.6	pKi	=	4.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	386	2	0	4	4.7	CC(=O)O[C@]1(C(C)=O)CC[C@H]2[C@@H]3C[C@H](C)C4=CC(=O)CC[C@]4(C)[C@H]3CC[C@@]21C	nan
		44304256	174798	0	None	-1000	3	Human	4.6	pKi	=	4.6	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	360	12	0	4	4.2	CCCCCC(=O)c1ccc(OCCCN2CCN(CCC)CC2)cc1	10.1016/s0960-894x(02)00309-8
		CHEMBL432144	174798	0	None	-1000	3	Human	4.6	pKi	=	4.6	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	360	12	0	4	4.2	CCCCCC(=O)c1ccc(OCCCN2CCN(CCC)CC2)cc1	10.1016/s0960-894x(02)00309-8
		44304032	208266	0	None	-616	3	Human	4.6	pKi	=	4.6	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	413	11	0	6	3.7	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3cnco3)CC2)cc1	10.1016/s0960-894x(02)00309-8
		CHEMBL60509	208266	0	None	-616	3	Human	4.6	pKi	=	4.6	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	413	11	0	6	3.7	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3cnco3)CC2)cc1	10.1016/s0960-894x(02)00309-8
		53324045	63845	0	None	-7	16	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assay	ChEMBL	487	7	1	2	7.3	OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccccc2)c2ccccc2)CC1	10.1016/j.bmcl.2018.10.036
		CHEMBL1644980	63845	0	None	-7	16	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assay	ChEMBL	487	7	1	2	7.3	OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccccc2)c2ccccc2)CC1	10.1016/j.bmcl.2018.10.036
		164614549	191722	0	None	-2	6	Human	7.5	pKi	=	7.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	340	9	4	4	2.2	CCCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1016/j.ejmech.2021.113190
		CHEMBL4853668	191722	0	None	-2	6	Human	7.5	pKi	=	7.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	340	9	4	4	2.2	CCCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1016/j.ejmech.2021.113190
		164619208	192441	0	None	446	4	Human	7.5	pKi	=	7.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	378	6	4	4	2.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccccc1F	10.1016/j.ejmech.2021.113190
		CHEMBL4864852	192441	0	None	446	4	Human	7.5	pKi	=	7.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	378	6	4	4	2.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccccc1F	10.1016/j.ejmech.2021.113190
		2284	9956	33	None	-53	29	Human	5.6	pKi	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	284	4	0	3	4.2	CN(CCCN1c2ccccc2Sc2c1cccc2)C	nan
		4926	9956	33	None	-53	29	Human	5.6	pKi	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	284	4	0	3	4.2	CN(CCCN1c2ccccc2Sc2c1cccc2)C	nan
		7281	9956	33	None	-53	29	Human	5.6	pKi	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	284	4	0	3	4.2	CN(CCCN1c2ccccc2Sc2c1cccc2)C	nan
		CHEMBL564	9956	33	None	-53	29	Human	5.6	pKi	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	284	4	0	3	4.2	CN(CCCN1c2ccccc2Sc2c1cccc2)C	nan
		DB00420	9956	33	None	-53	29	Human	5.6	pKi	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	284	4	0	3	4.2	CN(CCCN1c2ccccc2Sc2c1cccc2)C	nan
		71525681	96503	0	None	-346	6	Human	5.6	pKi	=	5.6	Binding	Displacement of [3H]histamine from human histamine H2 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H2 receptor expressed in HEK cells	ChEMBL	298	3	2	6	1.7	CNC1CN(c2nc(N)nc3cc(C4CCCC4)cnc23)C1	10.1016/j.bmcl.2013.02.091
		CHEMBL2376803	96503	0	None	-346	6	Human	5.6	pKi	=	5.6	Binding	Displacement of [3H]histamine from human histamine H2 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H2 receptor expressed in HEK cells	ChEMBL	298	3	2	6	1.7	CNC1CN(c2nc(N)nc3cc(C4CCCC4)cnc23)C1	10.1016/j.bmcl.2013.02.091
		132060743	169015	0	None	-1	13	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method	ChEMBL	351	3	0	4	3.1	CN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)C3)CC1	10.1016/j.ejmech.2018.02.024
		CHEMBL4163428	169015	0	None	-1	13	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method	ChEMBL	351	3	0	4	3.1	CN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)C3)CC1	10.1016/j.ejmech.2018.02.024
		3191	109635	97	None	-24	25	Human	5.5	pKi	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	469	9	0	3	7.2	CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1	nan
		CHEMBL305660	109635	97	None	-24	25	Human	5.5	pKi	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	469	9	0	3	7.2	CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1	nan
		44335387	115327	0	None	-1023	4	Human	4.5	pKi	=	4.5	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	393	7	0	5	3.8	CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc(C#N)cc3)cc2)CC1	10.1016/s0960-894x(02)00648-0
		CHEMBL320178	115327	0	None	-1023	4	Human	4.5	pKi	=	4.5	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	393	7	0	5	3.8	CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc(C#N)cc3)cc2)CC1	10.1016/s0960-894x(02)00648-0
		44334406	11635	0	None	-75	3	Human	6.5	pKi	=	6.5	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	462	10	1	5	3.8	O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccc(Cl)cc3)C2)cc1)C1CC1	10.1016/s0960-894x(02)00685-6
		CHEMBL104344	11635	0	None	-75	3	Human	6.5	pKi	=	6.5	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	462	10	1	5	3.8	O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccc(Cl)cc3)C2)cc1)C1CC1	10.1016/s0960-894x(02)00685-6
		44334368	115994	0	None	-57	3	Human	6.5	pKi	=	6.5	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	506	10	1	5	3.9	O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccc(Br)cc3)C2)cc1)C1CC1	10.1016/s0960-894x(02)00685-6
		CHEMBL321709	115994	0	None	-57	3	Human	6.5	pKi	=	6.5	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	506	10	1	5	3.9	O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccc(Br)cc3)C2)cc1)C1CC1	10.1016/s0960-894x(02)00685-6
		1204	8713	119	None	-173	25	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acsmedchemlett.0c00033
		1247	8713	119	None	-173	25	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acsmedchemlett.0c00033
		1375	8713	119	None	-173	25	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acsmedchemlett.0c00033
		774	8713	119	None	-173	25	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acsmedchemlett.0c00033
		CHEMBL90	8713	119	None	-173	25	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acsmedchemlett.0c00033
		DB05381	8713	119	None	-173	25	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acsmedchemlett.0c00033
		44304291	209631	0	None	-6606	3	Human	4.5	pKi	=	4.5	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	388	11	0	4	4.0	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)C(C)C)CC2)cc1	10.1016/s0960-894x(02)00309-8
		CHEMBL62527	209631	0	None	-6606	3	Human	4.5	pKi	=	4.5	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	388	11	0	4	4.0	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)C(C)C)CC2)cc1	10.1016/s0960-894x(02)00309-8
		168294767	199798	0	None	-117	20	Human	8.5	pKi	=	8.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	313	8	4	5	0.9	CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
		CHEMBL5207281	199798	0	None	-117	20	Human	8.5	pKi	=	8.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	313	8	4	5	0.9	CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
		CHEMBL5222802	199798	0	None	-117	20	Human	8.5	pKi	=	8.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	313	8	4	5	0.9	CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
		CHEMBL5078202	222315	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1	10.1016/j.bmcl.2021.128388
		CHEMBL5095695	222315	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1	10.1016/j.bmcl.2021.128388
		164627241	193208	0	None	95	4	Human	7.5	pKi	=	7.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	438	6	4	4	3.1	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(Br)cc1	10.1016/j.ejmech.2021.113190
		CHEMBL4876267	193208	0	None	95	4	Human	7.5	pKi	=	7.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	438	6	4	4	3.1	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(Br)cc1	10.1016/j.ejmech.2021.113190
		164618508	192711	0	None	165	4	Human	7.5	pKi	=	7.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	374	6	4	4	2.7	Cc1ccc(C(C)NC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1	10.1016/j.ejmech.2021.113190
		CHEMBL4869194	192711	0	None	165	4	Human	7.5	pKi	=	7.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	374	6	4	4	2.7	Cc1ccc(C(C)NC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1	10.1016/j.ejmech.2021.113190
		10324985	83556	8	None	-223	17	Human	6.5	pKi	=	6.5	Binding	Binding affinity to histamine H2 receptorBinding affinity to histamine H2 receptor	ChEMBL	423	7	0	8	1.7	COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1	10.1021/jm050725j
		CHEMBL199824	83556	8	None	-223	17	Human	6.5	pKi	=	6.5	Binding	Binding affinity to histamine H2 receptorBinding affinity to histamine H2 receptor	ChEMBL	423	7	0	8	1.7	COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1	10.1021/jm050725j
		CHEMBL2068762	83556	8	None	-223	17	Human	6.5	pKi	=	6.5	Binding	Binding affinity to histamine H2 receptorBinding affinity to histamine H2 receptor	ChEMBL	423	7	0	8	1.7	COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1	10.1021/jm050725j
		156010170	185113	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	414	13	3	7	2.3	NCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
		CHEMBL4632998	185113	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	414	13	3	7	2.3	NCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
		CHEMBL4651192	185113	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	414	13	3	7	2.3	NCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
		168277996	199625	0	None	-20	4	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	380	4	4	4	3.3	Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCc2ccccc2)c1	10.1021/acs.jmedchem.1c00692
		CHEMBL5173373	199625	0	None	-20	4	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	380	4	4	4	3.3	Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCc2ccccc2)c1	10.1021/acs.jmedchem.1c00692
		CHEMBL5221736	199625	0	None	-20	4	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	380	4	4	4	3.3	Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCc2ccccc2)c1	10.1021/acs.jmedchem.1c00692
		168278543	199630	0	None	2	4	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	358	4	4	4	1.6	N/C(=N\C(=O)NCc1ccccc1)NCC1CCc2nc(N)sc2C1	10.1021/acs.jmedchem.1c00692
		CHEMBL5184846	199630	0	None	2	4	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	358	4	4	4	1.6	N/C(=N\C(=O)NCc1ccccc1)NCC1CCc2nc(N)sc2C1	10.1021/acs.jmedchem.1c00692
		CHEMBL5221764	199630	0	None	2	4	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	358	4	4	4	1.6	N/C(=N\C(=O)NCc1ccccc1)NCC1CCc2nc(N)sc2C1	10.1021/acs.jmedchem.1c00692
		1599	9120	50	None	-154	16	Human	5.5	pKi	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	476	7	1	3	5.1	Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1	nan
		3955	9120	50	None	-154	16	Human	5.5	pKi	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	476	7	1	3	5.1	Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1	nan
		7215	9120	50	None	-154	16	Human	5.5	pKi	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	476	7	1	3	5.1	Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1	nan
		CHEMBL841	9120	50	None	-154	16	Human	5.5	pKi	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	476	7	1	3	5.1	Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1	nan
		DB00836	9120	50	None	-154	16	Human	5.5	pKi	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	476	7	1	3	5.1	Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1	nan
		73349361	99323	0	None	-3	7	Human	5.5	pKi	=	5.5	Binding	Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	279	4	0	1	3.3	CN(CCc1ccccc1)[C@H]1C2C3CC4C5C3CC2C5C41	10.1016/j.bmc.2013.07.045
		CHEMBL2432058	99323	0	None	-3	7	Human	5.5	pKi	=	5.5	Binding	Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	279	4	0	1	3.3	CN(CCc1ccccc1)[C@H]1C2C3CC4C5C3CC2C5C41	10.1016/j.bmc.2013.07.045
		168294178	199814	0	None	1	4	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	414	5	4	4	4.4	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)C2CCCCC2)cc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5205197	199814	0	None	1	4	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	414	5	4	4	4.4	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)C2CCCCC2)cc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5222887	199814	0	None	1	4	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	414	5	4	4	4.4	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)C2CCCCC2)cc1	10.1021/acs.jmedchem.1c00692
		164609493	191215	0	None	-1	6	Human	7.5	pKi	=	7.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	350	6	4	5	1.9	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccco1	10.1016/j.ejmech.2021.113190
		CHEMBL4846380	191215	0	None	-1	6	Human	7.5	pKi	=	7.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	350	6	4	5	1.9	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccco1	10.1016/j.ejmech.2021.113190
		164614907	191363	0	None	323	4	Human	7.5	pKi	=	7.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	378	6	4	4	2.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(F)cc1	10.1016/j.ejmech.2021.113190
		CHEMBL4848697	191363	0	None	323	4	Human	7.5	pKi	=	7.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	378	6	4	4	2.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(F)cc1	10.1016/j.ejmech.2021.113190
		44334521	114613	0	None	-36	3	Human	4.5	pKi	=	4.5	Binding	Binding affinity towards human Histamine H2 receptor (For compound 11)Binding affinity towards human Histamine H2 receptor (For compound 11)	ChEMBL	262	6	1	4	1.7	CC(=O)c1ccc(OCCCN2CC[C@H](N)C2)cc1	10.1016/s0960-894x(02)00685-6
		CHEMBL319231	114613	0	None	-36	3	Human	4.5	pKi	=	4.5	Binding	Binding affinity towards human Histamine H2 receptor (For compound 11)Binding affinity towards human Histamine H2 receptor (For compound 11)	ChEMBL	262	6	1	4	1.7	CC(=O)c1ccc(OCCCN2CC[C@H](N)C2)cc1	10.1016/s0960-894x(02)00685-6
		168286141	199703	0	None	2	4	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	450	8	4	4	4.8	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)cc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5192993	199703	0	None	2	4	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	450	8	4	4	4.8	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)cc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5222231	199703	0	None	2	4	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	450	8	4	4	4.8	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)cc1	10.1021/acs.jmedchem.1c00692
		50898777	63214	0	None	-29512	8	Human	5.5	pKi	=	5.5	Binding	Binding affinity to Histamine receptor H2Binding affinity to Histamine receptor H2	ChEMBL	441	9	1	6	3.6	COC(=O)CCCCCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1	10.1016/j.bmc.2010.10.011
		CHEMBL1632158	63214	0	None	-29512	8	Human	5.5	pKi	=	5.5	Binding	Binding affinity to Histamine receptor H2Binding affinity to Histamine receptor H2	ChEMBL	441	9	1	6	3.6	COC(=O)CCCCCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1	10.1016/j.bmc.2010.10.011
		11723317	109671	0	None	-100	3	Human	5.5	pKi	=	5.5	Binding	Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors	ChEMBL	316	9	3	2	2.8	S=C(NCCCCCc1c[nH]cn1)NCCc1ccccc1	10.1021/jm00012a025
		CHEMBL305929	109671	0	None	-100	3	Human	5.5	pKi	=	5.5	Binding	Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors	ChEMBL	316	9	3	2	2.8	S=C(NCCCCCc1c[nH]cn1)NCCc1ccccc1	10.1021/jm00012a025
		164610421	192039	0	None	7	2	Human	5.5	pKi	=	5.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	332	5	4	4	2.1	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)Nc1ccccc1	10.1016/j.ejmech.2021.113190
		CHEMBL4858567	192039	0	None	7	2	Human	5.5	pKi	=	5.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	332	5	4	4	2.1	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)Nc1ccccc1	10.1016/j.ejmech.2021.113190
		71525679	96501	0	None	-223	6	Human	5.5	pKi	=	5.5	Binding	Displacement of [3H]histamine from human histamine H2 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H2 receptor expressed in HEK cells	ChEMBL	272	3	2	6	1.0	CCc1cnc2c(N3CC[C@@H](NC)C3)nc(N)nc2c1	10.1016/j.bmcl.2013.02.091
		CHEMBL2376801	96501	0	None	-223	6	Human	5.5	pKi	=	5.5	Binding	Displacement of [3H]histamine from human histamine H2 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H2 receptor expressed in HEK cells	ChEMBL	272	3	2	6	1.0	CCc1cnc2c(N3CC[C@@H](NC)C3)nc(N)nc2c1	10.1016/j.bmcl.2013.02.091
		10420190	213539	0	None	-31	3	Human	4.5	pKi	=	4.5	Binding	Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.	ChEMBL	195	8	2	2	2.3	NCCCCCCCCc1c[nH]cn1	10.1021/jm00002a008
		CHEMBL90063	213539	0	None	-31	3	Human	4.5	pKi	=	4.5	Binding	Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.	ChEMBL	195	8	2	2	2.3	NCCCCCCCCc1c[nH]cn1	10.1021/jm00002a008
		44304558	107796	0	None	-10000	3	Human	4.5	pKi	=	4.5	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	374	11	0	4	3.8	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)CC)CC2)cc1	10.1016/s0960-894x(02)00309-8
		CHEMBL294502	107796	0	None	-10000	3	Human	4.5	pKi	=	4.5	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	374	11	0	4	3.8	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)CC)CC2)cc1	10.1016/s0960-894x(02)00309-8
		44304288	108984	0	None	-14791	3	Human	4.5	pKi	=	4.5	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	386	11	0	4	3.8	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)C3CC3)CC2)cc1	10.1016/s0960-894x(02)00309-8
		CHEMBL302886	108984	0	None	-14791	3	Human	4.5	pKi	=	4.5	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	386	11	0	4	3.8	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)C3CC3)CC2)cc1	10.1016/s0960-894x(02)00309-8
		44304451	109067	0	None	-1862	3	Human	4.5	pKi	=	4.5	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	417	12	1	5	3.3	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](N)C(C)C)CC2)cc1	10.1016/s0960-894x(02)00310-4
		CHEMBL303369	109067	0	None	-1862	3	Human	4.5	pKi	=	4.5	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	417	12	1	5	3.3	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](N)C(C)C)CC2)cc1	10.1016/s0960-894x(02)00310-4
		25128822	194260	0	None	-5888	5	Human	4.5	pKi	=	4.5	Binding	Displacement of [3H]UR-DE257 from human histamine 2 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]UR-DE257 from human histamine 2 receptor expressed in Sf9 cell membranes by liquid scintillation counting	ChEMBL	295	1	1	5	1.6	CN1CCN(c2nc(N)nc3c2CCc2ccccc2-3)CC1	10.1016/j.bmcl.2015.12.035
		CHEMBL494093	194260	0	None	-5888	5	Human	4.5	pKi	=	4.5	Binding	Displacement of [3H]UR-DE257 from human histamine 2 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]UR-DE257 from human histamine 2 receptor expressed in Sf9 cell membranes by liquid scintillation counting	ChEMBL	295	1	1	5	1.6	CN1CCN(c2nc(N)nc3c2CCc2ccccc2-3)CC1	10.1016/j.bmcl.2015.12.035
		44455426	161928	0	None	-44	12	Human	5.5	pKi	=	5.5	Binding	Inhibition of human cloned histamine H2 receptor by competitive binding experimentInhibition of human cloned histamine H2 receptor by competitive binding experiment	ChEMBL	405	9	1	4	4.2	COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(F)cc2)CC1	10.1016/j.bmc.2009.03.021
		CHEMBL402143	161928	0	None	-44	12	Human	5.5	pKi	=	5.5	Binding	Inhibition of human cloned histamine H2 receptor by competitive binding experimentInhibition of human cloned histamine H2 receptor by competitive binding experiment	ChEMBL	405	9	1	4	4.2	COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(F)cc2)CC1	10.1016/j.bmc.2009.03.021
		71456046	90850	0	None	-2089	7	Human	5.5	pKi	=	5.5	Binding	Displacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysisDisplacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysis	ChEMBL	389	6	0	4	4.2	COc1ccccc1N1CCN(Cc2cc(CN(C)C)c3cccccc2-3)CC1	10.1016/j.bmcl.2012.09.064
		CHEMBL2207637	90850	0	None	-2089	7	Human	5.5	pKi	=	5.5	Binding	Displacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysisDisplacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysis	ChEMBL	389	6	0	4	4.2	COc1ccccc1N1CCN(Cc2cc(CN(C)C)c3cccccc2-3)CC1	10.1016/j.bmcl.2012.09.064
		44307779	210338	0	None	-275	4	Human	5.5	pKi	=	5.5	Binding	Compound was tested for its binding affinity towards human H2 receptorCompound was tested for its binding affinity towards human H2 receptor	ChEMBL	332	2	0	2	4.7	C(#Cc1c2c(nc3ccccc13)CCCCC2)CCN1CCCCC1	10.1016/s0960-894x(03)00356-1
		CHEMBL66660	210338	0	None	-275	4	Human	5.5	pKi	=	5.5	Binding	Compound was tested for its binding affinity towards human H2 receptorCompound was tested for its binding affinity towards human H2 receptor	ChEMBL	332	2	0	2	4.7	C(#Cc1c2c(nc3ccccc13)CCCCC2)CCN1CCCCC1	10.1016/s0960-894x(03)00356-1
		156015643	185074	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	1001	28	3	11	9.2	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
		CHEMBL4645213	185074	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	1001	28	3	11	9.2	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
		CHEMBL4650968	185074	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	1001	28	3	11	9.2	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
		CHEMBL5092102	222125	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL		None	None	None		NCCCCCCCCNC(=O)/N=C(\N)NCCCc1c[nH]cn1	10.1016/j.bmcl.2021.128388
		168274129	199588	0	None	-6	4	Human	7.5	pKi	=	7.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	370	12	5	6	1.0	NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
		CHEMBL5176780	199588	0	None	-6	4	Human	7.5	pKi	=	7.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	370	12	5	6	1.0	NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
		CHEMBL5221468	199588	0	None	-6	4	Human	7.5	pKi	=	7.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	370	12	5	6	1.0	NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
		44334212	11401	0	None	-72	3	Human	6.5	pKi	=	6.5	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	456	11	1	5	3.7	CCc1ccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)cc1	10.1016/s0960-894x(02)00685-6
		CHEMBL102925	11401	0	None	-72	3	Human	6.5	pKi	=	6.5	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	456	11	1	5	3.7	CCc1ccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)cc1	10.1016/s0960-894x(02)00685-6
		168273549	199582	0	None	1	4	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	436	6	4	4	4.3	Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5174342	199582	0	None	1	4	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	436	6	4	4	4.3	Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5221438	199582	0	None	1	4	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	436	6	4	4	4.3	Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1	10.1021/acs.jmedchem.1c00692
		44335430	12069	0	None	-144	3	Human	4.5	pKi	=	4.5	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	374	7	0	5	4.0	CCOC(=O)N1CCN(CCCOc2ccc(-c3cccs3)cc2)CC1	10.1016/s0960-894x(02)00648-0
		CHEMBL106602	12069	0	None	-144	3	Human	4.5	pKi	=	4.5	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	374	7	0	5	4.0	CCOC(=O)N1CCN(CCCOc2ccc(-c3cccs3)cc2)CC1	10.1016/s0960-894x(02)00648-0
		44304064	109587	0	None	-1096	3	Human	4.5	pKi	=	4.5	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	451	10	2	6	2.5	N[C@H](Cc1ccc(O)cc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		CHEMBL305371	109587	0	None	-1096	3	Human	4.5	pKi	=	4.5	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	451	10	2	6	2.5	N[C@H](Cc1ccc(O)cc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		164611807	191763	0	None	162	4	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	376	6	4	4	2.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=S)N[C@@H](C)c1ccccc1	10.1016/j.ejmech.2021.113190
		CHEMBL4854278	191763	0	None	162	4	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	376	6	4	4	2.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=S)N[C@@H](C)c1ccccc1	10.1016/j.ejmech.2021.113190
		122442272	145126	0	None	-120	15	Human	5.5	pKi	=	5.5	Binding	Binding affinity to histamine H2 receptor (unknown origin) by radioligand binding assayBinding affinity to histamine H2 receptor (unknown origin) by radioligand binding assay	ChEMBL	239	5	1	2	2.6	C=CCOc1cc(F)c(F)cc1C1CC1CN	10.1021/acs.jmedchem.5b01153
		CHEMBL3769968	145126	0	None	-120	15	Human	5.5	pKi	=	5.5	Binding	Binding affinity to histamine H2 receptor (unknown origin) by radioligand binding assayBinding affinity to histamine H2 receptor (unknown origin) by radioligand binding assay	ChEMBL	239	5	1	2	2.6	C=CCOc1cc(F)c(F)cc1C1CC1CN	10.1021/acs.jmedchem.5b01153
		CHEMBL3771384	145126	0	None	-120	15	Human	5.5	pKi	=	5.5	Binding	Binding affinity to histamine H2 receptor (unknown origin) by radioligand binding assayBinding affinity to histamine H2 receptor (unknown origin) by radioligand binding assay	ChEMBL	239	5	1	2	2.6	C=CCOc1cc(F)c(F)cc1C1CC1CN	10.1021/acs.jmedchem.5b01153
		122442272	145126	0	None	-120	15	Human	5.5	pKi	=	5.5	Binding	Binding affinity to histamine H2 receptor (unknown origin) by radioligand binding assayBinding affinity to histamine H2 receptor (unknown origin) by radioligand binding assay	ChEMBL	239	5	1	2	2.6	C=CCOc1cc(F)c(F)cc1C1CC1CN	10.1021/acs.jmedchem.5b01153
		CHEMBL3769968	145126	0	None	-120	15	Human	5.5	pKi	=	5.5	Binding	Binding affinity to histamine H2 receptor (unknown origin) by radioligand binding assayBinding affinity to histamine H2 receptor (unknown origin) by radioligand binding assay	ChEMBL	239	5	1	2	2.6	C=CCOc1cc(F)c(F)cc1C1CC1CN	10.1021/acs.jmedchem.5b01153
		CHEMBL3771384	145126	0	None	-120	15	Human	5.5	pKi	=	5.5	Binding	Binding affinity to histamine H2 receptor (unknown origin) by radioligand binding assayBinding affinity to histamine H2 receptor (unknown origin) by radioligand binding assay	ChEMBL	239	5	1	2	2.6	C=CCOc1cc(F)c(F)cc1C1CC1CN	10.1021/acs.jmedchem.5b01153
		44335336	11330	0	None	-263	4	Human	4.5	pKi	=	4.5	Binding	Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor	ChEMBL	335	6	1	4	3.4	N#Cc1ccc(-c2ccc(OCCCN3CCC(N)CC3)cc2)cc1	10.1016/s0960-894x(02)00648-0
		CHEMBL102452	11330	0	None	-263	4	Human	4.5	pKi	=	4.5	Binding	Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor	ChEMBL	335	6	1	4	3.4	N#Cc1ccc(-c2ccc(OCCCN3CCC(N)CC3)cc2)cc1	10.1016/s0960-894x(02)00648-0
		168268680	199545	0	None	1	4	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	662	11	8	8	4.8	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5172675	199545	0	None	1	4	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	662	11	8	8	4.8	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5221210	199545	0	None	1	4	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	662	11	8	8	4.8	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1	10.1021/acs.jmedchem.1c00692
		44304445	209767	0	None	-30	3	Human	5.5	pKi	=	5.5	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	531	14	1	6	5.3	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](CC(C)C)NC(=O)OC(C)(C)C)CC2)cc1	10.1016/s0960-894x(02)00310-4
		CHEMBL63112	209767	0	None	-30	3	Human	5.5	pKi	=	5.5	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	531	14	1	6	5.3	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](CC(C)C)NC(=O)OC(C)(C)C)CC2)cc1	10.1016/s0960-894x(02)00310-4
		44304462	209661	0	None	-4897	3	Human	4.5	pKi	=	4.5	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	405	12	2	6	1.7	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](N)CO)CC2)cc1	10.1016/s0960-894x(02)00310-4
		CHEMBL62660	209661	0	None	-4897	3	Human	4.5	pKi	=	4.5	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	405	12	2	6	1.7	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](N)CO)CC2)cc1	10.1016/s0960-894x(02)00310-4
		44304741	209696	0	None	-3388	3	Human	4.5	pKi	=	4.5	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	466	13	1	6	3.3	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](N)Cc3ccncc3)CC2)cc1	10.1016/s0960-894x(02)00310-4
		CHEMBL62808	209696	0	None	-3388	3	Human	4.5	pKi	=	4.5	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	466	13	1	6	3.3	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](N)Cc3ccncc3)CC2)cc1	10.1016/s0960-894x(02)00310-4
		73355417	99314	0	None	1	3	Human	5.5	pKi	=	5.5	Binding	Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	251	3	1	1	2.9	c1ccc(CN[C@H]2C3C4CC5C6C4CC3C6C52)cc1	10.1016/j.bmc.2013.07.045
		CHEMBL2432045	99314	0	None	1	3	Human	5.5	pKi	=	5.5	Binding	Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	251	3	1	1	2.9	c1ccc(CN[C@H]2C3C4CC5C6C4CC3C6C52)cc1	10.1016/j.bmc.2013.07.045
		237	211644	48	None	-3	13	Human	5.5	pKi	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	399	9	1	4	6.0	CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12	nan
		CHEMBL546257	211644	48	None	-3	13	Human	5.5	pKi	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	399	9	1	4	6.0	CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12	nan
		CHEMBL554190	211644	48	None	-3	13	Human	5.5	pKi	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	399	9	1	4	6.0	CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12	nan
		CHEMBL7568	211644	48	None	-3	13	Human	5.5	pKi	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	399	9	1	4	6.0	CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12	nan
		164614841	192053	0	None	223	4	Human	7.5	pKi	=	7.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	388	7	4	4	3.0	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(c1ccccc1)C(C)C	10.1016/j.ejmech.2021.113190
		CHEMBL4858849	192053	0	None	223	4	Human	7.5	pKi	=	7.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	388	7	4	4	3.0	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(c1ccccc1)C(C)C	10.1016/j.ejmech.2021.113190
		44333988	11307	0	None	-93	3	Human	5.5	pKi	=	5.5	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	367	8	1	5	2.6	CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)c3cccnc3)C2)cc1	10.1016/s0960-894x(02)00685-6
		CHEMBL102331	11307	0	None	-93	3	Human	5.5	pKi	=	5.5	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	367	8	1	5	2.6	CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)c3cccnc3)C2)cc1	10.1016/s0960-894x(02)00685-6
		156013896	185019	0	None	-1548	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human recombinant H2R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]UR-DE257 from Gsalphas-coupled human recombinant H2R expressed in baculovirus infected Sf9 insect cell membranes	ChEMBL	401	9	1	2	5.1	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1	10.1021/acs.jmedchem.0c00160
		CHEMBL4635634	185019	0	None	-1548	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human recombinant H2R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]UR-DE257 from Gsalphas-coupled human recombinant H2R expressed in baculovirus infected Sf9 insect cell membranes	ChEMBL	401	9	1	2	5.1	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1	10.1021/acs.jmedchem.0c00160
		CHEMBL4650570	185019	0	None	-1548	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human recombinant H2R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]UR-DE257 from Gsalphas-coupled human recombinant H2R expressed in baculovirus infected Sf9 insect cell membranes	ChEMBL	401	9	1	2	5.1	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1	10.1021/acs.jmedchem.0c00160
		135398737	7745	93	None	-64	90	Human	5.5	pKi	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	nan
		38	7745	93	None	-64	90	Human	5.5	pKi	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	nan
		722	7745	93	None	-64	90	Human	5.5	pKi	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	nan
		CHEMBL42	7745	93	None	-64	90	Human	5.5	pKi	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	nan
		DB00363	7745	93	None	-64	90	Human	5.5	pKi	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	nan
		71455894	90577	0	None	-3	12	Human	5.5	pKi	=	5.5	Binding	Binding affinity to Histamine H2 receptorBinding affinity to Histamine H2 receptor	ChEMBL	325	4	1	4	2.0	COc1ccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1OC	10.1016/j.bmcl.2012.08.046
		CHEMBL2205827	90577	0	None	-3	12	Human	5.5	pKi	=	5.5	Binding	Binding affinity to Histamine H2 receptorBinding affinity to Histamine H2 receptor	ChEMBL	325	4	1	4	2.0	COc1ccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1OC	10.1016/j.bmcl.2012.08.046
		71455894	90577	0	None	-3	12	Human	5.5	pKi	=	5.5	Binding	Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	325	4	1	4	2.0	COc1ccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1OC	10.1016/j.bmc.2013.07.045
		CHEMBL2205827	90577	0	None	-3	12	Human	5.5	pKi	=	5.5	Binding	Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	325	4	1	4	2.0	COc1ccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1OC	10.1016/j.bmc.2013.07.045
		44335407	178623	0	None	-15	3	Human	5.4	pKi	=	5.4	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	452	8	0	5	4.8	CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc(OC(F)(F)F)cc3)cc2)CC1	10.1016/s0960-894x(02)00648-0
		CHEMBL446885	178623	0	None	-15	3	Human	5.4	pKi	=	5.4	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	452	8	0	5	4.8	CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc(OC(F)(F)F)cc3)cc2)CC1	10.1016/s0960-894x(02)00648-0
		26987	7736	33	None	-177	21	Human	6.4	pKi	=	6.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	343	6	0	2	5.1	Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C	nan
		6063	7736	33	None	-177	21	Human	6.4	pKi	=	6.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	343	6	0	2	5.1	Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C	nan
		671	7736	33	None	-177	21	Human	6.4	pKi	=	6.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	343	6	0	2	5.1	Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C	nan
		CHEMBL1626	7736	33	None	-177	21	Human	6.4	pKi	=	6.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	343	6	0	2	5.1	Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C	nan
		DB00283	7736	33	None	-177	21	Human	6.4	pKi	=	6.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	343	6	0	2	5.1	Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C	nan
		155513890	176600	0	None	-177	3	Human	5.4	pKi	=	5.4	Binding	Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells after 90 mins by scintillation counting methodDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells after 90 mins by scintillation counting method	ChEMBL	369	2	2	5	4.1	Clc1ccc(C#Cc2nc(N[C@H]3C[C@H]4CC[C@@H]3C4)c3nc[nH]c3n2)s1	10.1039/C8MD00317C
		CHEMBL4439593	176600	0	None	-177	3	Human	5.4	pKi	=	5.4	Binding	Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells after 90 mins by scintillation counting methodDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells after 90 mins by scintillation counting method	ChEMBL	369	2	2	5	4.1	Clc1ccc(C#Cc2nc(N[C@H]3C[C@H]4CC[C@@H]3C4)c3nc[nH]c3n2)s1	10.1039/C8MD00317C
		126720252	171454	0	None	-12	12	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]-Iodoaminopotentidine from human histamine H2 receptor expressed in HEK293T cell membranes after 90 mins by scintillation counting methodDisplacement of [125I]-Iodoaminopotentidine from human histamine H2 receptor expressed in HEK293T cell membranes after 90 mins by scintillation counting method	ChEMBL	697	15	2	6	9.2	NCCCCCCn1cc(CCCCN2CCC(c3ccc(-c4cc(C(=O)O)cc5cc(-c6ccc(C(F)(F)F)cc6)ccc45)cc3)CC2)nn1	10.1021/acs.jmedchem.8b00168
		CHEMBL4216870	171454	0	None	-12	12	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]-Iodoaminopotentidine from human histamine H2 receptor expressed in HEK293T cell membranes after 90 mins by scintillation counting methodDisplacement of [125I]-Iodoaminopotentidine from human histamine H2 receptor expressed in HEK293T cell membranes after 90 mins by scintillation counting method	ChEMBL	697	15	2	6	9.2	NCCCCCCn1cc(CCCCN2CCC(c3ccc(-c4cc(C(=O)O)cc5cc(-c6ccc(C(F)(F)F)cc6)ccc45)cc3)CC2)nn1	10.1021/acs.jmedchem.8b00168
		164618283	191323	0	None	158	4	Human	7.4	pKi	=	7.4	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	390	7	4	5	2.4	COc1ccc(C(C)NC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1	10.1016/j.ejmech.2021.113190
		CHEMBL4848026	191323	0	None	158	4	Human	7.4	pKi	=	7.4	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	390	7	4	5	2.4	COc1ccc(C(C)NC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1	10.1016/j.ejmech.2021.113190
		44304282	209892	0	None	-12	3	Human	5.4	pKi	=	5.4	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	410	8	0	5	3.8	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)c3cccc(C)c3)cc2)CC1	10.1016/s0960-894x(02)00309-8
		CHEMBL64021	209892	0	None	-12	3	Human	5.4	pKi	=	5.4	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	410	8	0	5	3.8	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)c3cccc(C)c3)cc2)CC1	10.1016/s0960-894x(02)00309-8
		44304383	210082	0	None	-371	3	Human	5.4	pKi	=	5.4	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	418	12	0	5	4.6	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OCC(C)C)CC2)cc1	10.1016/s0960-894x(02)00309-8
		CHEMBL64775	210082	0	None	-371	3	Human	5.4	pKi	=	5.4	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	418	12	0	5	4.6	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OCC(C)C)CC2)cc1	10.1016/s0960-894x(02)00309-8
		44304753	209974	0	None	-4073	3	Human	4.4	pKi	=	4.4	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	466	13	1	6	3.3	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](N)Cc3ccncc3)CC2)cc1	10.1016/s0960-894x(02)00310-4
		CHEMBL64321	209974	0	None	-4073	3	Human	4.4	pKi	=	4.4	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	466	13	1	6	3.3	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](N)Cc3ccncc3)CC2)cc1	10.1016/s0960-894x(02)00310-4
		9818650	210304	0	None	-1513	4	Human	5.4	pKi	=	5.4	Binding	Compound was tested for its binding affinity towards human H2 receptorCompound was tested for its binding affinity towards human H2 receptor	ChEMBL	323	5	1	3	4.4	c1ccc2c(NCCCN3CCCC3)c3c(nc2c1)CCCCC3	10.1016/s0960-894x(03)00356-1
		CHEMBL66388	210304	0	None	-1513	4	Human	5.4	pKi	=	5.4	Binding	Compound was tested for its binding affinity towards human H2 receptorCompound was tested for its binding affinity towards human H2 receptor	ChEMBL	323	5	1	3	4.4	c1ccc2c(NCCCN3CCCC3)c3c(nc2c1)CCCCC3	10.1016/s0960-894x(03)00356-1
		CHEMBL4777443	220825	0	None	-181	14	Human	5.4	pKi	=	5.4	Binding	Selectivity interaction (GPCR panel (PDSP screen)) EUB0000741a HRH2Selectivity interaction (GPCR panel (PDSP screen)) EUB0000741a HRH2	ChEMBL		None	None	None		CC(C)(C)OC(=O)N1CCCC1CN[C@H]1CC[C@@](c2cc(F)ccc2F)(S(=O)(=O)c2ccc(Cl)cc2)CC1	10.6019/CHEMBL5212743
		44334782	12197	0	None	-91	3	Human	6.4	pKi	=	6.4	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	442	10	1	5	3.4	Cc1ccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)cc1	10.1016/s0960-894x(02)00685-6
		CHEMBL107293	12197	0	None	-91	3	Human	6.4	pKi	=	6.4	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	442	10	1	5	3.4	Cc1ccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)cc1	10.1016/s0960-894x(02)00685-6
		168276867	199614	0	None	-1	4	Human	6.4	pKi	=	6.4	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	662	11	8	8	4.8	Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)c1	10.1021/acs.jmedchem.1c00692
		CHEMBL5174278	199614	0	None	-1	4	Human	6.4	pKi	=	6.4	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	662	11	8	8	4.8	Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)c1	10.1021/acs.jmedchem.1c00692
		CHEMBL5221653	199614	0	None	-1	4	Human	6.4	pKi	=	6.4	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	662	11	8	8	4.8	Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)c1	10.1021/acs.jmedchem.1c00692
		44335571	12044	0	None	-1513	4	Human	4.4	pKi	=	4.4	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	322	6	0	4	3.3	N#Cc1ccc(-c2ccc(OCCCN3CCOCC3)cc2)cc1	10.1016/s0960-894x(02)00648-0
		CHEMBL106483	12044	0	None	-1513	4	Human	4.4	pKi	=	4.4	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	322	6	0	4	3.3	N#Cc1ccc(-c2ccc(OCCCN3CCOCC3)cc2)cc1	10.1016/s0960-894x(02)00648-0
		44304450	209646	0	None	-478	3	Human	4.4	pKi	=	4.4	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	417	12	1	5	3.3	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](N)C(C)C)CC2)cc1	10.1016/s0960-894x(02)00310-4
		CHEMBL62592	209646	0	None	-478	3	Human	4.4	pKi	=	4.4	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	417	12	1	5	3.3	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](N)C(C)C)CC2)cc1	10.1016/s0960-894x(02)00310-4
		168283097	199672	0	None	-22	4	Human	6.4	pKi	=	6.4	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	311	9	4	5	0.8	CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)o1	10.1021/acs.jmedchem.1c00692
		CHEMBL5186770	199672	0	None	-22	4	Human	6.4	pKi	=	6.4	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	311	9	4	5	0.8	CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)o1	10.1021/acs.jmedchem.1c00692
		CHEMBL5222043	199672	0	None	-22	4	Human	6.4	pKi	=	6.4	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	311	9	4	5	0.8	CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)o1	10.1021/acs.jmedchem.1c00692
		168284480	199689	0	None	-22	4	Human	6.4	pKi	=	6.4	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	330	6	4	4	1.3	Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCc1ccccc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5197548	199689	0	None	-22	4	Human	6.4	pKi	=	6.4	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	330	6	4	4	1.3	Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCc1ccccc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5222137	199689	0	None	-22	4	Human	6.4	pKi	=	6.4	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	330	6	4	4	1.3	Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCc1ccccc1	10.1021/acs.jmedchem.1c00692
		73346334	99316	0	None	-4	7	Human	5.4	pKi	=	5.4	Binding	Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	265	4	1	1	3.0	c1ccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)cc1	10.1016/j.bmc.2013.07.045
		CHEMBL2432048	99316	0	None	-4	7	Human	5.4	pKi	=	5.4	Binding	Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	265	4	1	1	3.0	c1ccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)cc1	10.1016/j.bmc.2013.07.045
		164608815	191233	0	None	1	6	Human	7.4	pKi	=	7.4	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	380	7	4	4	2.8	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1	10.1016/j.ejmech.2021.113190
		CHEMBL4846638	191233	0	None	1	6	Human	7.4	pKi	=	7.4	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	380	7	4	4	2.8	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1	10.1016/j.ejmech.2021.113190
		4011	89183	49	None	-27	24	Human	6.4	pKi	=	6.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	277	4	1	1	4.2	CNCCCC12CCC(c3ccccc31)c1ccccc12	nan
		CHEMBL21731	89183	49	None	-27	24	Human	6.4	pKi	=	6.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	277	4	1	1	4.2	CNCCCC12CCC(c3ccccc31)c1ccccc12	nan
		44335237	11893	0	None	-144	3	Human	5.4	pKi	=	5.4	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	407	7	0	5	4.1	CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc(C#N)cc3C)cc2)CC1	10.1016/s0960-894x(02)00648-0
		CHEMBL105669	11893	0	None	-144	3	Human	5.4	pKi	=	5.4	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	407	7	0	5	4.1	CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc(C#N)cc3C)cc2)CC1	10.1016/s0960-894x(02)00648-0
		3032915	22267	24	None	-25	7	Human	5.4	pKi	=	5.4	Binding	Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors	ChEMBL	212	5	3	2	1.2	C/N=C(\S)NCCCCc1c[nH]cn1	10.1021/jm00012a025
		CHEMBL12160	22267	24	None	-25	7	Human	5.4	pKi	=	5.4	Binding	Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors	ChEMBL	212	5	3	2	1.2	C/N=C(\S)NCCCCc1c[nH]cn1	10.1021/jm00012a025
		10085839	211281	0	None	-125	3	Human	5.4	pKi	=	5.4	Binding	Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors	ChEMBL	294	7	3	2	2.9	S=C(NCCCCCc1c[nH]cn1)NC1CCCCC1	10.1021/jm00012a025
		CHEMBL72571	211281	0	None	-125	3	Human	5.4	pKi	=	5.4	Binding	Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors	ChEMBL	294	7	3	2	2.9	S=C(NCCCCCc1c[nH]cn1)NC1CCCCC1	10.1021/jm00012a025
		3032915	22267	24	None	-25	7	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	212	5	3	2	1.2	C/N=C(\S)NCCCCc1c[nH]cn1	10.1016/j.bmcl.2010.10.041
		CHEMBL12160	22267	24	None	-25	7	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	212	5	3	2	1.2	C/N=C(\S)NCCCCc1c[nH]cn1	10.1016/j.bmcl.2010.10.041
		164619427	192848	0	None	7	2	Human	5.4	pKi	=	5.4	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	380	5	4	4	3.1	N/C(=N\C(=O)NCCc1ccccc1)Nc1cccc(-c2csc(N)n2)c1	10.1016/j.ejmech.2021.113190
		CHEMBL4871221	192848	0	None	7	2	Human	5.4	pKi	=	5.4	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	380	5	4	4	3.1	N/C(=N\C(=O)NCCc1ccccc1)Nc1cccc(-c2csc(N)n2)c1	10.1016/j.ejmech.2021.113190
		1204	8713	119	None	-173	25	Human	4.4	pKi	=	4.4	Binding	Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm00002a008
		1247	8713	119	None	-173	25	Human	4.4	pKi	=	4.4	Binding	Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm00002a008
		1375	8713	119	None	-173	25	Human	4.4	pKi	=	4.4	Binding	Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm00002a008
		774	8713	119	None	-173	25	Human	4.4	pKi	=	4.4	Binding	Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm00002a008
		CHEMBL90	8713	119	None	-173	25	Human	4.4	pKi	=	4.4	Binding	Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm00002a008
		DB05381	8713	119	None	-173	25	Human	4.4	pKi	=	4.4	Binding	Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm00002a008
		44304387	209707	0	None	-7943	3	Human	4.4	pKi	=	4.4	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	334	7	0	5	2.4	CCOC(=O)N1CCN(CCCOc2ccc(C(C)=O)cc2)CC1	10.1016/s0960-894x(02)00309-8
		CHEMBL62840	209707	0	None	-7943	3	Human	4.4	pKi	=	4.4	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	334	7	0	5	2.4	CCOC(=O)N1CCN(CCCOc2ccc(C(C)=O)cc2)CC1	10.1016/s0960-894x(02)00309-8
		44304312	169566	0	None	-1348	3	Human	4.4	pKi	=	4.4	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	453	10	1	5	2.9	N[C@H](Cc1ccc(F)cc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		CHEMBL417215	169566	0	None	-1348	3	Human	4.4	pKi	=	4.4	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	453	10	1	5	2.9	N[C@H](Cc1ccc(F)cc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		164612037	192156	0	None	-85	20	Human	8.4	pKi	=	8.4	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	326	8	4	4	1.8	CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1016/j.ejmech.2021.113190
		CHEMBL4860528	192156	0	None	-85	20	Human	8.4	pKi	=	8.4	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	326	8	4	4	1.8	CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1016/j.ejmech.2021.113190
		46884734	14744	0	None	-6	2	Human	8.4	pKi	=	8.4	Binding	Inhibition of H2 receptorInhibition of H2 receptor	ChEMBL	341	6	0	4	3.7	COc1nccnc1[C@H](C)C1=C(CCN(C)C)Cc2cc(F)ccc21	10.1016/j.bmcl.2010.07.117
		CHEMBL1090526	14744	0	None	-6	2	Human	8.4	pKi	=	8.4	Binding	Inhibition of H2 receptorInhibition of H2 receptor	ChEMBL	341	6	0	4	3.7	COc1nccnc1[C@H](C)C1=C(CCN(C)C)Cc2cc(F)ccc21	10.1016/j.bmcl.2010.07.117
		168273471	199580	0	None	12	4	Human	8.3	pKi	=	8.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	596	17	8	10	0.7	N/C(=N\C(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
		CHEMBL5173079	199580	0	None	12	4	Human	8.3	pKi	=	8.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	596	17	8	10	0.7	N/C(=N\C(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
		CHEMBL5221433	199580	0	None	12	4	Human	8.3	pKi	=	8.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	596	17	8	10	0.7	N/C(=N\C(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
		71452382	90569	0	None	-12	10	Human	6.4	pKi	=	6.4	Binding	Binding affinity to Histamine H2 receptorBinding affinity to Histamine H2 receptor	ChEMBL	309	4	1	3	2.0	COc1ccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1	10.1016/j.bmcl.2012.08.046
		CHEMBL2205812	90569	0	None	-12	10	Human	6.4	pKi	=	6.4	Binding	Binding affinity to Histamine H2 receptorBinding affinity to Histamine H2 receptor	ChEMBL	309	4	1	3	2.0	COc1ccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1	10.1016/j.bmcl.2012.08.046
		44334035	116822	0	None	-79	3	Human	5.4	pKi	=	5.4	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	476	10	1	7	4.1	O=C(N[C@H]1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)C1)c1csc(-c2cccnc2)n1	10.1016/s0960-894x(02)00685-6
		CHEMBL323517	116822	0	None	-79	3	Human	5.4	pKi	=	5.4	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	476	10	1	7	4.1	O=C(N[C@H]1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)C1)c1csc(-c2cccnc2)n1	10.1016/s0960-894x(02)00685-6
		44334281	11531	0	None	-128	3	Human	4.4	pKi	=	4.4	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	433	9	2	6	2.8	CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)[C@@H](C)NC(=O)OC(C)(C)C)C2)cc1	10.1016/s0960-894x(02)00685-6
		CHEMBL103828	11531	0	None	-128	3	Human	4.4	pKi	=	4.4	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	433	9	2	6	2.8	CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)[C@@H](C)NC(=O)OC(C)(C)C)C2)cc1	10.1016/s0960-894x(02)00685-6
		145980875	173486	0	None	-3	11	Human	6.4	pKi	=	6.4	Binding	Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assay	ChEMBL	443	7	1	2	6.2	OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCCc2ccc(F)cc2)CC1	10.1016/j.bmcl.2018.10.036
		CHEMBL4282702	173486	0	None	-3	11	Human	6.4	pKi	=	6.4	Binding	Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assay	ChEMBL	443	7	1	2	6.2	OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCCc2ccc(F)cc2)CC1	10.1016/j.bmcl.2018.10.036
		1530	8963	50	None	-151	21	Human	5.4	pKi	=	5.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	309	0	0	3	4.0	CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1	nan
		3827	8963	50	None	-151	21	Human	5.4	pKi	=	5.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	309	0	0	3	4.0	CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1	nan
		7206	8963	50	None	-151	21	Human	5.4	pKi	=	5.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	309	0	0	3	4.0	CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1	nan
		CHEMBL534	8963	50	None	-151	21	Human	5.4	pKi	=	5.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	309	0	0	3	4.0	CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1	nan
		DB00920	8963	50	None	-151	21	Human	5.4	pKi	=	5.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	309	0	0	3	4.0	CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1	nan
		CHEMBL5090859	222062	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCCC[n+]1c(C)cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc1C	10.1016/j.bmcl.2021.128388
		44478385	12548	6	None	-70	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [3H]tiotidine from human histamine H2 receptor expressed in Sf9 cellsDisplacement of [3H]tiotidine from human histamine H2 receptor expressed in Sf9 cells	ChEMBL	342	9	3	4	2.5	N#C/N=C(/NCCCCc1c[nH]cn1)NCCSc1ccccc1	10.1021/jm900526h
		CHEMBL1078642	12548	6	None	-70	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [3H]tiotidine from human histamine H2 receptor expressed in Sf9 cellsDisplacement of [3H]tiotidine from human histamine H2 receptor expressed in Sf9 cells	ChEMBL	342	9	3	4	2.5	N#C/N=C(/NCCCCc1c[nH]cn1)NCCSc1ccccc1	10.1021/jm900526h
		44304012	209611	0	None	-21379	3	Human	4.4	pKi	=	4.4	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	389	11	1	5	2.7	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](C)N)CC2)cc1	10.1016/s0960-894x(02)00310-4
		CHEMBL62421	209611	0	None	-21379	3	Human	4.4	pKi	=	4.4	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	389	11	1	5	2.7	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](C)N)CC2)cc1	10.1016/s0960-894x(02)00310-4
		1129	8402	96	None	-1	2	Human	7.4	pKi	=	7.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	nan
		3325	8402	96	None	-1	2	Human	7.4	pKi	=	7.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	nan
		5353622	8402	96	None	-1	2	Human	7.4	pKi	=	7.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	nan
		5702160	8402	96	None	-1	2	Human	7.4	pKi	=	7.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	nan
		7074	8402	96	None	-1	2	Human	7.4	pKi	=	7.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	nan
		CHEMBL902	8402	96	None	-1	2	Human	7.4	pKi	=	7.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	nan
		DB00927	8402	96	None	-1	2	Human	7.4	pKi	=	7.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	nan
		12016525	209694	0	None	-2041	3	Human	4.4	pKi	=	4.4	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	359	8	1	5	1.5	C[C@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		CHEMBL62804	209694	0	None	-2041	3	Human	4.4	pKi	=	4.4	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	359	8	1	5	1.5	C[C@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		71457844	90851	0	None	-2187	7	Human	5.4	pKi	=	5.4	Binding	Displacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysisDisplacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysis	ChEMBL	429	6	0	4	5.1	COc1ccccc1N1CCN(Cc2cc(CN3CCCCC3)c3cccccc2-3)CC1	10.1016/j.bmcl.2012.09.064
		CHEMBL2207638	90851	0	None	-2187	7	Human	5.4	pKi	=	5.4	Binding	Displacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysisDisplacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysis	ChEMBL	429	6	0	4	5.1	COc1ccccc1N1CCN(Cc2cc(CN3CCCCC3)c3cccccc2-3)CC1	10.1016/j.bmcl.2012.09.064
		50878551	97520	61	None	-109	18	Human	5.4	pKi	=	5.4	Binding	Displacement of [3H]Tiotidine from human recombinant histamine H2 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]Tiotidine from human recombinant histamine H2 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis	ChEMBL	270	8	1	2	3.4	C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12	10.1016/j.bmcl.2013.03.066
		CHEMBL2391541	97520	61	None	-109	18	Human	5.4	pKi	=	5.4	Binding	Displacement of [3H]Tiotidine from human recombinant histamine H2 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]Tiotidine from human recombinant histamine H2 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis	ChEMBL	270	8	1	2	3.4	C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12	10.1016/j.bmcl.2013.03.066
		164608941	191162	0	None	75	4	Human	6.4	pKi	=	6.4	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	390	7	4	4	2.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NC[C@@H](C)c1ccccc1	10.1016/j.ejmech.2021.113190
		CHEMBL4845733	191162	0	None	75	4	Human	6.4	pKi	=	6.4	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	390	7	4	4	2.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NC[C@@H](C)c1ccccc1	10.1016/j.ejmech.2021.113190
		50878551	97520	61	None	-109	18	Human	5.4	pKi	=	5.4	Binding	Displacement of [3H]Tiotidine from human recombinant histamine H2 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]Tiotidine from human recombinant histamine H2 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis	ChEMBL	270	8	1	2	3.4	C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12	10.1016/j.bmcl.2013.03.066
		CHEMBL2391541	97520	61	None	-109	18	Human	5.4	pKi	=	5.4	Binding	Displacement of [3H]Tiotidine from human recombinant histamine H2 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]Tiotidine from human recombinant histamine H2 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis	ChEMBL	270	8	1	2	3.4	C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12	10.1016/j.bmcl.2013.03.066
		44304309	175995	0	None	-630	3	Human	4.4	pKi	=	4.4	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	414	8	0	5	3.6	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)c3ccc(F)cc3)cc2)CC1	10.1016/s0960-894x(02)00309-8
		CHEMBL440864	175995	0	None	-630	3	Human	4.4	pKi	=	4.4	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	414	8	0	5	3.6	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)c3ccc(F)cc3)cc2)CC1	10.1016/s0960-894x(02)00309-8
		164627020	193187	0	None	144	4	Human	7.4	pKi	=	7.4	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	422	7	4	4	3.4	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(c1ccccc1)c1ccccc1	10.1016/j.ejmech.2021.113190
		CHEMBL4876025	193187	0	None	144	4	Human	7.4	pKi	=	7.4	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	422	7	4	4	3.4	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(c1ccccc1)c1ccccc1	10.1016/j.ejmech.2021.113190
		53324553	63629	0	None	-6	10	Human	5.4	pKi	=	5.4	Binding	Inhibition of H2 receptorInhibition of H2 receptor	ChEMBL	283	4	1	1	3.1	Fc1cccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)c1	10.1016/j.bmcl.2010.11.075
		CHEMBL1643900	63629	0	None	-6	10	Human	5.4	pKi	=	5.4	Binding	Inhibition of H2 receptorInhibition of H2 receptor	ChEMBL	283	4	1	1	3.1	Fc1cccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)c1	10.1016/j.bmcl.2010.11.075
		53324553	63629	0	None	-6	10	Human	5.4	pKi	=	5.4	Binding	Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	283	4	1	1	3.1	Fc1cccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)c1	10.1016/j.bmc.2013.07.045
		CHEMBL1643900	63629	0	None	-6	10	Human	5.4	pKi	=	5.4	Binding	Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	283	4	1	1	3.1	Fc1cccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)c1	10.1016/j.bmc.2013.07.045
		53325861	63630	0	None	-2	3	Human	5.4	pKi	=	5.4	Binding	Inhibition of H2 receptorInhibition of H2 receptor	ChEMBL	297	4	0	1	3.4	CN(CCc1cccc(F)c1)[C@H]1C2C3CC4C5C3CC2C5C41	10.1016/j.bmcl.2010.11.075
		CHEMBL1643902	63630	0	None	-2	3	Human	5.4	pKi	=	5.4	Binding	Inhibition of H2 receptorInhibition of H2 receptor	ChEMBL	297	4	0	1	3.4	CN(CCc1cccc(F)c1)[C@H]1C2C3CC4C5C3CC2C5C41	10.1016/j.bmcl.2010.11.075
		53325861	63630	0	None	-2	3	Human	5.4	pKi	=	5.4	Binding	Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	297	4	0	1	3.4	CN(CCc1cccc(F)c1)[C@H]1C2C3CC4C5C3CC2C5C41	10.1016/j.bmc.2013.07.045
		CHEMBL1643902	63630	0	None	-2	3	Human	5.4	pKi	=	5.4	Binding	Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	297	4	0	1	3.4	CN(CCc1cccc(F)c1)[C@H]1C2C3CC4C5C3CC2C5C41	10.1016/j.bmc.2013.07.045
		44304449	207278	0	None	-309	3	Human	5.4	pKi	=	5.4	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	531	14	1	6	5.3	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](CC(C)C)NC(=O)OC(C)(C)C)CC2)cc1	10.1016/s0960-894x(02)00310-4
		CHEMBL59870	207278	0	None	-309	3	Human	5.4	pKi	=	5.4	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	531	14	1	6	5.3	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](CC(C)C)NC(=O)OC(C)(C)C)CC2)cc1	10.1016/s0960-894x(02)00310-4
		164626509	193114	0	None	3	2	Human	5.4	pKi	=	5.4	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	358	3	4	4	3.2	N/C(=N\C(=O)NC1CCCCC1)Nc1cccc(-c2csc(N)n2)c1	10.1016/j.ejmech.2021.113190
		CHEMBL4874969	193114	0	None	3	2	Human	5.4	pKi	=	5.4	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	358	3	4	4	3.2	N/C(=N\C(=O)NC1CCCCC1)Nc1cccc(-c2csc(N)n2)c1	10.1016/j.ejmech.2021.113190
		168280339	199644	0	None	-52	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	372	8	3	5	1.1	C[C@@H](NC(=O)/N=C(\N)NCCCn1cc(CN(C)C)nn1)c1ccccc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5188592	199644	0	None	-52	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	372	8	3	5	1.1	C[C@@H](NC(=O)/N=C(\N)NCCCn1cc(CN(C)C)nn1)c1ccccc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5221885	199644	0	None	-52	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	372	8	3	5	1.1	C[C@@H](NC(=O)/N=C(\N)NCCCn1cc(CN(C)C)nn1)c1ccccc1	10.1021/acs.jmedchem.1c00692
		168294166	199793	0	None	1	4	Human	6.3	pKi	=	6.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	360	6	4	4	3.3	CCCCCNC(=O)/N=C(\N)Nc1ccc(-c2sc(N)nc2C)cc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5209081	199793	0	None	1	4	Human	6.3	pKi	=	6.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	360	6	4	4	3.3	CCCCCNC(=O)/N=C(\N)Nc1ccc(-c2sc(N)nc2C)cc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5222775	199793	0	None	1	4	Human	6.3	pKi	=	6.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	360	6	4	4	3.3	CCCCCNC(=O)/N=C(\N)Nc1ccc(-c2sc(N)nc2C)cc1	10.1021/acs.jmedchem.1c00692
		44304014	107562	0	None	-5370	3	Human	4.3	pKi	=	4.3	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	431	10	1	6	2.3	CC(C)(C)OC[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		CHEMBL293033	107562	0	None	-5370	3	Human	4.3	pKi	=	4.3	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	431	10	1	6	2.3	CC(C)(C)OC[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		164622153	192347	0	None	95	4	Human	7.3	pKi	=	7.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	394	6	4	4	3.0	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(Cl)cc1	10.1016/j.ejmech.2021.113190
		CHEMBL4863347	192347	0	None	95	4	Human	7.3	pKi	=	7.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	394	6	4	4	3.0	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(Cl)cc1	10.1016/j.ejmech.2021.113190
		71459761	90855	0	None	-75	7	Human	6.3	pKi	=	6.3	Binding	Displacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysisDisplacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysis	ChEMBL	540	7	0	5	6.1	COc1ccccc1N1CCN(Cc2cc(CN3CCN(c4ccc(Cl)cc4)CC3)c3cccccc2-3)CC1	10.1016/j.bmcl.2012.09.064
		CHEMBL2207642	90855	0	None	-75	7	Human	6.3	pKi	=	6.3	Binding	Displacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysisDisplacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysis	ChEMBL	540	7	0	5	6.1	COc1ccccc1N1CCN(Cc2cc(CN3CCN(c4ccc(Cl)cc4)CC3)c3cccccc2-3)CC1	10.1016/j.bmcl.2012.09.064
		44334556	114044	0	None	-77	3	Human	4.3	pKi	=	4.3	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	449	10	3	7	1.7	CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)[C@H](CO)NC(=O)OC(C)(C)C)C2)cc1	10.1016/s0960-894x(02)00685-6
		CHEMBL316968	114044	0	None	-77	3	Human	4.3	pKi	=	4.3	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	449	10	3	7	1.7	CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)[C@H](CO)NC(=O)OC(C)(C)C)C2)cc1	10.1016/s0960-894x(02)00685-6
		44304377	209556	0	None	-2570	3	Human	4.3	pKi	=	4.3	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	424	11	0	6	3.5	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3cnccn3)CC2)cc1	10.1016/s0960-894x(02)00309-8
		CHEMBL62115	209556	0	None	-2570	3	Human	4.3	pKi	=	4.3	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	424	11	0	6	3.5	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3cnccn3)CC2)cc1	10.1016/s0960-894x(02)00309-8
		44304313	208364	0	None	-2041	3	Human	4.3	pKi	=	4.3	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	441	10	1	6	2.8	N[C@H](Cc1ccsc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		CHEMBL60559	208364	0	None	-2041	3	Human	4.3	pKi	=	4.3	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	441	10	1	6	2.8	N[C@H](Cc1ccsc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		44304277	107724	0	None	-645	3	Human	4.3	pKi	=	4.3	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	401	10	1	5	2.4	CN[C@@H](C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1)C(C)C	10.1016/s0960-894x(02)00310-4
		CHEMBL294087	107724	0	None	-645	3	Human	4.3	pKi	=	4.3	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	401	10	1	5	2.4	CN[C@@H](C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1)C(C)C	10.1016/s0960-894x(02)00310-4
		1231	7724	116	None	-4	8	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation counting	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1021/acs.jmedchem.6b01422
		2756	7724	116	None	-4	8	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation counting	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1021/acs.jmedchem.6b01422
		645	7724	116	None	-4	8	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation counting	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1021/acs.jmedchem.6b01422
		CHEMBL30	7724	116	None	-4	8	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation counting	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1021/acs.jmedchem.6b01422
		DB00501	7724	116	None	-4	8	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation counting	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1021/acs.jmedchem.6b01422
		44467360	131313	0	None	3	2	Human	5.3	pKi	=	5.3	Binding	Inhibition of human histamine H2 receptorInhibition of human histamine H2 receptor	ChEMBL	420	3	2	6	1.5	COc1nc(N2C[C@H]3C(=O)N(C)C(=N)N[C@@]3(c3ccc(F)cc3F)C2)nc(C)c1F	10.1021/acs.jmedchem.5b01995
		CHEMBL3640290	131313	0	None	3	2	Human	5.3	pKi	=	5.3	Binding	Inhibition of human histamine H2 receptorInhibition of human histamine H2 receptor	ChEMBL	420	3	2	6	1.5	COc1nc(N2C[C@H]3C(=O)N(C)C(=N)N[C@@]3(c3ccc(F)cc3F)C2)nc(C)c1F	10.1021/acs.jmedchem.5b01995
		168295528	199810	0	None	-147	20	Human	8.3	pKi	=	8.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	333	6	4	5	0.9	N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
		CHEMBL5206565	199810	0	None	-147	20	Human	8.3	pKi	=	8.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	333	6	4	5	0.9	N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
		CHEMBL5222872	199810	0	None	-147	20	Human	8.3	pKi	=	8.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	333	6	4	5	0.9	N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
		168290815	199752	0	None	-537	6	Human	8.3	pKi	=	8.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	327	9	4	5	1.2	CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
		CHEMBL5200771	199752	0	None	-537	6	Human	8.3	pKi	=	8.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	327	9	4	5	1.2	CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
		CHEMBL5222529	199752	0	None	-537	6	Human	8.3	pKi	=	8.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	327	9	4	5	1.2	CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
		168273640	199584	0	None	-6	6	Human	8.3	pKi	=	8.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	568	15	8	10	-0.1	N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
		CHEMBL5176229	199584	0	None	-6	6	Human	8.3	pKi	=	8.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	568	15	8	10	-0.1	N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
		CHEMBL5221444	199584	0	None	-6	6	Human	8.3	pKi	=	8.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	568	15	8	10	-0.1	N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
		46780481	114308	20	None	-21	53	Human	8.2	pKi	=	8.2	Binding	Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)	ChEMBL	285	0	0	2	4.3	CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1	10.1016/j.bmcl.2013.12.024
		9903970	114308	20	None	-21	53	Human	8.2	pKi	=	8.2	Binding	Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)	ChEMBL	285	0	0	2	4.3	CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1	10.1016/j.bmcl.2013.12.024
		CHEMBL3187365	114308	20	None	-21	53	Human	8.2	pKi	=	8.2	Binding	Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)	ChEMBL	285	0	0	2	4.3	CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1	10.1016/j.bmcl.2013.12.024
		CHEMBL3544974	114308	20	None	-21	53	Human	8.2	pKi	=	8.2	Binding	Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)	ChEMBL	285	0	0	2	4.3	CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1	10.1016/j.bmcl.2013.12.024
		46780481	114308	20	None	-21	53	Human	8.2	pKi	=	8.2	Binding	Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)	ChEMBL	285	0	0	2	4.3	CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1	10.1016/j.bmcl.2013.12.024
		9903970	114308	20	None	-21	53	Human	8.2	pKi	=	8.2	Binding	Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)	ChEMBL	285	0	0	2	4.3	CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1	10.1016/j.bmcl.2013.12.024
		CHEMBL3187365	114308	20	None	-21	53	Human	8.2	pKi	=	8.2	Binding	Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)	ChEMBL	285	0	0	2	4.3	CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1	10.1016/j.bmcl.2013.12.024
		CHEMBL3544974	114308	20	None	-21	53	Human	8.2	pKi	=	8.2	Binding	Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)	ChEMBL	285	0	0	2	4.3	CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1	10.1016/j.bmcl.2013.12.024
		44334395	11733	0	None	-144	3	Human	6.3	pKi	=	6.3	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	446	10	1	5	3.2	O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccc(F)cc3)C2)cc1)C1CC1	10.1016/s0960-894x(02)00685-6
		CHEMBL104808	11733	0	None	-144	3	Human	6.3	pKi	=	6.3	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	446	10	1	5	3.2	O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccc(F)cc3)C2)cc1)C1CC1	10.1016/s0960-894x(02)00685-6
		1204	8713	119	None	-173	25	Human	5.3	pKi	=	5.3	Binding	Binding affinity to histamine H2 receptor (unknown origin)Binding affinity to histamine H2 receptor (unknown origin)	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.5b00516
		1247	8713	119	None	-173	25	Human	5.3	pKi	=	5.3	Binding	Binding affinity to histamine H2 receptor (unknown origin)Binding affinity to histamine H2 receptor (unknown origin)	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.5b00516
		1375	8713	119	None	-173	25	Human	5.3	pKi	=	5.3	Binding	Binding affinity to histamine H2 receptor (unknown origin)Binding affinity to histamine H2 receptor (unknown origin)	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.5b00516
		774	8713	119	None	-173	25	Human	5.3	pKi	=	5.3	Binding	Binding affinity to histamine H2 receptor (unknown origin)Binding affinity to histamine H2 receptor (unknown origin)	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.5b00516
		CHEMBL90	8713	119	None	-173	25	Human	5.3	pKi	=	5.3	Binding	Binding affinity to histamine H2 receptor (unknown origin)Binding affinity to histamine H2 receptor (unknown origin)	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.5b00516
		DB05381	8713	119	None	-173	25	Human	5.3	pKi	=	5.3	Binding	Binding affinity to histamine H2 receptor (unknown origin)Binding affinity to histamine H2 receptor (unknown origin)	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.5b00516
		44334265	116460	0	None	-25	3	Human	5.3	pKi	=	5.3	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	368	8	1	6	2.0	CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)c3cnccn3)C2)cc1	10.1016/s0960-894x(02)00685-6
		CHEMBL322695	116460	0	None	-25	3	Human	5.3	pKi	=	5.3	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	368	8	1	6	2.0	CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)c3cnccn3)C2)cc1	10.1016/s0960-894x(02)00685-6
		44334521	114613	0	None	-36	3	Human	4.3	pKi	=	4.3	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	262	6	1	4	1.7	CC(=O)c1ccc(OCCCN2CC[C@H](N)C2)cc1	10.1016/s0960-894x(02)00685-6
		CHEMBL319231	114613	0	None	-36	3	Human	4.3	pKi	=	4.3	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	262	6	1	4	1.7	CC(=O)c1ccc(OCCCN2CC[C@H](N)C2)cc1	10.1016/s0960-894x(02)00685-6
		1226	8800	20	None	-7	7	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	321	9	4	4	1.2	NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C	10.1016/j.bmcl.2010.10.041
		41376	8800	20	None	-7	7	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	321	9	4	4	1.2	NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C	10.1016/j.bmcl.2010.10.041
		CHEMBL12608	8800	20	None	-7	7	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	321	9	4	4	1.2	NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C	10.1016/j.bmcl.2010.10.041
		10015196	110397	0	None	-251	3	Human	5.3	pKi	=	5.3	Binding	Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors	ChEMBL	254	8	3	2	2.4	CCC/N=C(\S)NCCCCCc1c[nH]cn1	10.1021/jm00012a025
		CHEMBL308717	110397	0	None	-251	3	Human	5.3	pKi	=	5.3	Binding	Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors	ChEMBL	254	8	3	2	2.4	CCC/N=C(\S)NCCCCCc1c[nH]cn1	10.1021/jm00012a025
		44304056	109501	1	None	-5754	3	Human	4.3	pKi	=	4.3	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	401	10	1	5	2.6	CC(C)N[C@H](C)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		CHEMBL304888	109501	1	None	-5754	3	Human	4.3	pKi	=	4.3	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	401	10	1	5	2.6	CC(C)N[C@H](C)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		44304316	209912	0	None	-416	3	Human	4.3	pKi	=	4.3	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	485	8	0	6	3.6	CC(C)(C)OC(=O)N1CCC[C@@H]1C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		CHEMBL64120	209912	0	None	-416	3	Human	4.3	pKi	=	4.3	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	485	8	0	6	3.6	CC(C)(C)OC(=O)N1CCC[C@@H]1C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		1204	8713	119	None	-173	25	Human	4.3	pKi	=	4.3	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2010.10.041
		1247	8713	119	None	-173	25	Human	4.3	pKi	=	4.3	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2010.10.041
		1375	8713	119	None	-173	25	Human	4.3	pKi	=	4.3	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2010.10.041
		774	8713	119	None	-173	25	Human	4.3	pKi	=	4.3	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2010.10.041
		CHEMBL90	8713	119	None	-173	25	Human	4.3	pKi	=	4.3	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2010.10.041
		DB05381	8713	119	None	-173	25	Human	4.3	pKi	=	4.3	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2010.10.041
		132060770	169418	0	None	-8	10	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method	ChEMBL	451	7	0	6	3.5	CCOC(=O)CCN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)CC3)CC1	10.1016/j.ejmech.2018.02.024
		CHEMBL4169689	169418	0	None	-8	10	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method	ChEMBL	451	7	0	6	3.5	CCOC(=O)CCN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)CC3)CC1	10.1016/j.ejmech.2018.02.024
		2812	11551	101	None	-33	34	Human	5.3	pKi	=	5.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	344	4	0	2	5.4	Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1	nan
		CHEMBL104	11551	101	None	-33	34	Human	5.3	pKi	=	5.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	344	4	0	2	5.4	Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1	nan
		164622330	192641	0	None	-2	6	Human	7.3	pKi	=	7.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	360	6	4	4	2.3	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)N[C@@H](C)c1ccccc1	10.1016/j.ejmech.2021.113190
		CHEMBL4867962	192641	0	None	-2	6	Human	7.3	pKi	=	7.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	360	6	4	4	2.3	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)N[C@@H](C)c1ccccc1	10.1016/j.ejmech.2021.113190
		164627774	193344	0	None	1	6	Human	6.3	pKi	=	6.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	344	3	4	4	1.4	N/C(=N\C(=O)NCc1ccccc1)NC1CCc2nc(N)sc2C1	10.1016/j.ejmech.2021.113190
		CHEMBL4878215	193344	0	None	1	6	Human	6.3	pKi	=	6.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	344	3	4	4	1.4	N/C(=N\C(=O)NCc1ccccc1)NC1CCc2nc(N)sc2C1	10.1016/j.ejmech.2021.113190
		71452172	90293	0	None	-1	3	Human	5.3	pKi	=	5.3	Binding	Displacement of [3H]tiotidine from human recombinant histamine H2 receptor after 1.5 hrs by microbeta scintillation counting analysisDisplacement of [3H]tiotidine from human recombinant histamine H2 receptor after 1.5 hrs by microbeta scintillation counting analysis	ChEMBL	274	6	1	5	2.4	c1ccc(OCc2cc(OC[C@@H]3CCCN3)no2)cc1	10.1021/ml3002715
		CHEMBL2203551	90293	0	None	-1	3	Human	5.3	pKi	=	5.3	Binding	Displacement of [3H]tiotidine from human recombinant histamine H2 receptor after 1.5 hrs by microbeta scintillation counting analysisDisplacement of [3H]tiotidine from human recombinant histamine H2 receptor after 1.5 hrs by microbeta scintillation counting analysis	ChEMBL	274	6	1	5	2.4	c1ccc(OCc2cc(OC[C@@H]3CCCN3)no2)cc1	10.1021/ml3002715
		155552683	180945	0	None	-40	4	Human	6.3	pKi	=	6.3	Binding	Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells after 90 mins by scintillation counting methodDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells after 90 mins by scintillation counting method	ChEMBL	379	4	2	5	4.1	Clc1ccc(C#Cc2nc(NCCc3ccccc3)c3nc[nH]c3n2)s1	10.1039/C8MD00317C
		CHEMBL4546937	180945	0	None	-40	4	Human	6.3	pKi	=	6.3	Binding	Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells after 90 mins by scintillation counting methodDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells after 90 mins by scintillation counting method	ChEMBL	379	4	2	5	4.1	Clc1ccc(C#Cc2nc(NCCc3ccccc3)c3nc[nH]c3n2)s1	10.1039/C8MD00317C
		164622256	192495	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	318	4	4	4	2.2	CCCNC(=O)/N=C(\N)Nc1cccc(-c2csc(N)n2)c1	10.1016/j.ejmech.2021.113190
		CHEMBL4865670	192495	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	318	4	4	4	2.2	CCCNC(=O)/N=C(\N)Nc1cccc(-c2csc(N)n2)c1	10.1016/j.ejmech.2021.113190
		145992489	173756	0	None	-1	12	Human	6.3	pKi	=	6.3	Binding	Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assay	ChEMBL	535	7	1	2	7.8	OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC=C(c2ccc(F)cc2)c2ccc(F)cc2)CC1	10.1016/j.bmcl.2018.10.036
		CHEMBL4287623	173756	0	None	-1	12	Human	6.3	pKi	=	6.3	Binding	Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assay	ChEMBL	535	7	1	2	7.8	OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC=C(c2ccc(F)cc2)c2ccc(F)cc2)CC1	10.1016/j.bmcl.2018.10.036
		168290235	199747	0	None	-1737	20	Human	7.3	pKi	=	7.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	315	6	4	3	1.1	C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5201074	199747	0	None	-1737	20	Human	7.3	pKi	=	7.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	315	6	4	3	1.1	C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5222491	199747	0	None	-1737	20	Human	7.3	pKi	=	7.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	315	6	4	3	1.1	C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1	10.1021/acs.jmedchem.1c00692
		71454295	90854	0	None	-660	7	Human	6.3	pKi	=	6.3	Binding	Displacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysisDisplacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysis	ChEMBL	536	8	0	6	5.5	COc1ccccc1N1CCN(Cc2cc(CN3CCN(c4ccccc4OC)CC3)c3cccccc2-3)CC1	10.1016/j.bmcl.2012.09.064
		CHEMBL2207641	90854	0	None	-660	7	Human	6.3	pKi	=	6.3	Binding	Displacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysisDisplacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysis	ChEMBL	536	8	0	6	5.5	COc1ccccc1N1CCN(Cc2cc(CN3CCN(c4ccccc4OC)CC3)c3cccccc2-3)CC1	10.1016/j.bmcl.2012.09.064
		44304329	210006	0	None	-1778	3	Human	4.3	pKi	=	4.3	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	385	8	1	5	1.9	O=C(c1ccc(OCCCN2CCN(C(=O)[C@H]3CCCN3)CC2)cc1)C1CC1	10.1016/s0960-894x(02)00310-4
		CHEMBL64461	210006	0	None	-1778	3	Human	4.3	pKi	=	4.3	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	385	8	1	5	1.9	O=C(c1ccc(OCCCN2CCN(C(=O)[C@H]3CCCN3)CC2)cc1)C1CC1	10.1016/s0960-894x(02)00310-4
		24841480	190678	0	None	-269	20	Human	6.3	pKi	=	6.3	Binding	Antagonist activity at histamine H2 receptor (unknown origin) by PDSP assayAntagonist activity at histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	340	3	0	4	4.5	O=C(OCCN1CCCC1)N1c2ccccc2Sc2ccccc21	10.1016/j.bmcl.2013.04.082
		CHEMBL481153	190678	0	None	-269	20	Human	6.3	pKi	=	6.3	Binding	Antagonist activity at histamine H2 receptor (unknown origin) by PDSP assayAntagonist activity at histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	340	3	0	4	4.5	O=C(OCCN1CCCC1)N1c2ccccc2Sc2ccccc21	10.1016/j.bmcl.2013.04.082
		1231	7724	116	None	-4	8	Human	5.3	pKi	=	5.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	nan
		2756	7724	116	None	-4	8	Human	5.3	pKi	=	5.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	nan
		645	7724	116	None	-4	8	Human	5.3	pKi	=	5.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	nan
		CHEMBL30	7724	116	None	-4	8	Human	5.3	pKi	=	5.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	nan
		DB00501	7724	116	None	-4	8	Human	5.3	pKi	=	5.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	nan
		155558968	181597	0	None	1	3	Human	6.3	pKi	=	6.3	Binding	Binding affinity to human histamine 2 receptor expressed in HEK cells by radioligand binding assayBinding affinity to human histamine 2 receptor expressed in HEK cells by radioligand binding assay	ChEMBL	432	3	2	5	3.2	Cc1cccc(C)c1N1C(=O)[C@H](CC2CNc3ccccc32)NC2(CCN(C)CC2)C1=O	10.1016/j.ejmech.2018.12.048
		CHEMBL4562437	181597	0	None	1	3	Human	6.3	pKi	=	6.3	Binding	Binding affinity to human histamine 2 receptor expressed in HEK cells by radioligand binding assayBinding affinity to human histamine 2 receptor expressed in HEK cells by radioligand binding assay	ChEMBL	432	3	2	5	3.2	Cc1cccc(C)c1N1C(=O)[C@H](CC2CNc3ccccc32)NC2(CCN(C)CC2)C1=O	10.1016/j.ejmech.2018.12.048
		53325242	63844	0	None	-2	17	Human	6.3	pKi	=	6.3	Binding	Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assay	ChEMBL	537	8	1	2	7.9	OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1	10.1016/j.bmcl.2018.10.036
		CHEMBL1644978	63844	0	None	-2	17	Human	6.3	pKi	=	6.3	Binding	Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assay	ChEMBL	537	8	1	2	7.9	OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1	10.1016/j.bmcl.2018.10.036
		162644910	186190	0	None	-50	3	Human	5.3	pKi	=	5.3	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysis	ChEMBL	407	7	0	4	5.0	Clc1cccc(-c2ccc(OCCCN3CCN(c4ccncc4)CC3)cc2)c1	10.1016/j.ejmech.2020.113041
		CHEMBL4740135	186190	0	None	-50	3	Human	5.3	pKi	=	5.3	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysis	ChEMBL	407	7	0	4	5.0	Clc1cccc(-c2ccc(OCCCN3CCN(c4ccncc4)CC3)cc2)c1	10.1016/j.ejmech.2020.113041
		168268716	199541	0	None	1	4	Human	6.3	pKi	=	6.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	372	3	4	4	3.5	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NC2CCCCC2)cc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5170276	199541	0	None	1	4	Human	6.3	pKi	=	6.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	372	3	4	4	3.5	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NC2CCCCC2)cc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5221176	199541	0	None	1	4	Human	6.3	pKi	=	6.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	372	3	4	4	3.5	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NC2CCCCC2)cc1	10.1021/acs.jmedchem.1c00692
		71450707	90853	0	None	-1445	7	Human	5.3	pKi	=	5.3	Binding	Displacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysisDisplacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysis	ChEMBL	444	6	0	5	3.9	COc1ccccc1N1CCN(Cc2cc(CN3CCN(C)CC3)c3cccccc2-3)CC1	10.1016/j.bmcl.2012.09.064
		CHEMBL2207640	90853	0	None	-1445	7	Human	5.3	pKi	=	5.3	Binding	Displacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysisDisplacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysis	ChEMBL	444	6	0	5	3.9	COc1ccccc1N1CCN(Cc2cc(CN3CCN(C)CC3)c3cccccc2-3)CC1	10.1016/j.bmcl.2012.09.064
		155531772	183445	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of 20 nM [3H]UR-DE257 from human H2R expressed in Sf9 cell membranes co-expressing GsalphaS by competition binding assayDisplacement of 20 nM [3H]UR-DE257 from human H2R expressed in Sf9 cell membranes co-expressing GsalphaS by competition binding assay	ChEMBL	334	8	3	6	3.3	Cc1[nH]cnc1CSCCNc1ccnc(NCC(C)(C)C)n1	10.1021/acs.jmedchem.9b01342
		CHEMBL4466349	183445	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of 20 nM [3H]UR-DE257 from human H2R expressed in Sf9 cell membranes co-expressing GsalphaS by competition binding assayDisplacement of 20 nM [3H]UR-DE257 from human H2R expressed in Sf9 cell membranes co-expressing GsalphaS by competition binding assay	ChEMBL	334	8	3	6	3.3	Cc1[nH]cnc1CSCCNc1ccnc(NCC(C)(C)C)n1	10.1021/acs.jmedchem.9b01342
		CHEMBL4598197	183445	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of 20 nM [3H]UR-DE257 from human H2R expressed in Sf9 cell membranes co-expressing GsalphaS by competition binding assayDisplacement of 20 nM [3H]UR-DE257 from human H2R expressed in Sf9 cell membranes co-expressing GsalphaS by competition binding assay	ChEMBL	334	8	3	6	3.3	Cc1[nH]cnc1CSCCNc1ccnc(NCC(C)(C)C)n1	10.1021/acs.jmedchem.9b01342
		CHEMBL5083588	222313	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
		CHEMBL5095633	222313	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
		44335351	11839	0	None	-29	3	Human	5.3	pKi	=	5.3	Binding	Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor	ChEMBL	402	7	0	4	4.6	CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc(Cl)cc3)cc2)CC1	10.1016/s0960-894x(02)00648-0
		CHEMBL105385	11839	0	None	-29	3	Human	5.3	pKi	=	5.3	Binding	Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor	ChEMBL	402	7	0	4	4.6	CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc(Cl)cc3)cc2)CC1	10.1016/s0960-894x(02)00648-0
		168275750	199605	0	None	-87	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	332	6	3	4	1.6	Cc1nnc(CCCN/C(N)=N/C(=O)NCc2ccccc2)s1	10.1021/acs.jmedchem.1c00692
		CHEMBL5175558	199605	0	None	-87	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	332	6	3	4	1.6	Cc1nnc(CCCN/C(N)=N/C(=O)NCc2ccccc2)s1	10.1021/acs.jmedchem.1c00692
		CHEMBL5221581	199605	0	None	-87	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	332	6	3	4	1.6	Cc1nnc(CCCN/C(N)=N/C(=O)NCc2ccccc2)s1	10.1021/acs.jmedchem.1c00692
		44304475	209546	0	None	-10471	3	Human	4.3	pKi	=	4.3	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	348	8	0	5	2.8	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)CC)cc2)CC1	10.1016/s0960-894x(02)00309-8
		CHEMBL62066	209546	0	None	-10471	3	Human	4.3	pKi	=	4.3	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	348	8	0	5	2.8	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)CC)cc2)CC1	10.1016/s0960-894x(02)00309-8
		44335222	170235	0	None	-20	3	Human	4.2	pKi	=	4.2	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	369	7	0	5	3.3	CCOC(=O)N1CCN(CCCOc2ccc(-c3ccncc3)cc2)CC1	10.1016/s0960-894x(02)00648-0
		CHEMBL419912	170235	0	None	-20	3	Human	4.2	pKi	=	4.2	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	369	7	0	5	3.3	CCOC(=O)N1CCN(CCCOc2ccc(-c3ccncc3)cc2)CC1	10.1016/s0960-894x(02)00648-0
		44304357	207389	0	None	-4786	3	Human	4.2	pKi	=	4.2	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	415	9	1	5	3.0	CC(C)(C)C[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		CHEMBL59931	207389	0	None	-4786	3	Human	4.2	pKi	=	4.2	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	415	9	1	5	3.0	CC(C)(C)C[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		137645406	164681	0	None	-75	13	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method	ChEMBL	491	8	0	7	5.4	COc1ccccc1N1CCC2(CCN(CCCSc3nnc(-c4ccccc4)n3C)CC2)CC1	10.1021/acs.jmedchem.9b00412
		CHEMBL4084262	164681	0	None	-75	13	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method	ChEMBL	491	8	0	7	5.4	COc1ccccc1N1CCC2(CCN(CCCSc3nnc(-c4ccccc4)n3C)CC2)CC1	10.1021/acs.jmedchem.9b00412
		168294182	199827	0	None	-3	4	Human	8.2	pKi	=	8.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	314	6	4	2	1.7	C[C@@H](NC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5208722	199827	0	None	-3	4	Human	8.2	pKi	=	8.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	314	6	4	2	1.7	C[C@@H](NC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5222960	199827	0	None	-3	4	Human	8.2	pKi	=	8.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	314	6	4	2	1.7	C[C@@H](NC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1	10.1021/acs.jmedchem.1c00692
		168268853	199564	0	None	-2	6	Human	8.2	pKi	=	8.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	389	8	4	5	1.9	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5180504	199564	0	None	-2	6	Human	8.2	pKi	=	8.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	389	8	4	5	1.9	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5221353	199564	0	None	-2	6	Human	8.2	pKi	=	8.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	389	8	4	5	1.9	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
		164609017	191204	0	None	-1	6	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	416	10	4	4	3.2	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CCCc1ccccc1	10.1016/j.ejmech.2021.113190
		CHEMBL4846201	191204	0	None	-1	6	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	416	10	4	4	3.2	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CCCc1ccccc1	10.1016/j.ejmech.2021.113190
		164610289	191912	0	None	38	4	Human	6.2	pKi	=	6.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	438	7	4	4	3.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NC(c1ccccc1)c1ccccc1	10.1016/j.ejmech.2021.113190
		CHEMBL4856602	191912	0	None	38	4	Human	6.2	pKi	=	6.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	438	7	4	4	3.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NC(c1ccccc1)c1ccccc1	10.1016/j.ejmech.2021.113190
		44304378	170051	0	None	-2951	3	Human	4.2	pKi	=	4.2	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	423	11	0	5	4.1	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3cccnc3)CC2)cc1	10.1016/s0960-894x(02)00309-8
		CHEMBL418658	170051	0	None	-2951	3	Human	4.2	pKi	=	4.2	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	423	11	0	5	4.1	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3cccnc3)CC2)cc1	10.1016/s0960-894x(02)00309-8
		44304348	107378	0	None	-15135	3	Human	4.2	pKi	=	4.2	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	387	10	1	5	2.3	CCC[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		CHEMBL291821	107378	0	None	-15135	3	Human	4.2	pKi	=	4.2	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	387	10	1	5	2.3	CCC[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		44334036	174571	0	None	-154	3	Human	5.2	pKi	=	5.2	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	391	8	1	5	3.0	CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)c3ccc(C#N)cc3)C2)cc1	10.1016/s0960-894x(02)00685-6
		CHEMBL430502	174571	0	None	-154	3	Human	5.2	pKi	=	5.2	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	391	8	1	5	3.0	CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)c3ccc(C#N)cc3)C2)cc1	10.1016/s0960-894x(02)00685-6
		71454294	90852	0	None	-1348	7	Human	5.2	pKi	=	5.2	Binding	Displacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysisDisplacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysis	ChEMBL	431	6	0	5	4.0	COc1ccccc1N1CCN(Cc2cc(CN3CCOCC3)c3cccccc2-3)CC1	10.1016/j.bmcl.2012.09.064
		CHEMBL2207639	90852	0	None	-1348	7	Human	5.2	pKi	=	5.2	Binding	Displacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysisDisplacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysis	ChEMBL	431	6	0	5	4.0	COc1ccccc1N1CCN(Cc2cc(CN3CCOCC3)c3cccccc2-3)CC1	10.1016/j.bmcl.2012.09.064
		71449142	86293	0	None	-104	3	Human	5.2	pKi	=	5.2	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	442	9	0	6	4.2	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)c3ccc(SC)cc3)cc2)CC1	10.1016/s0960-894x(02)00309-8
		CHEMBL2113738	86293	0	None	-104	3	Human	5.2	pKi	=	5.2	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	442	9	0	6	4.2	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)c3ccc(SC)cc3)cc2)CC1	10.1016/s0960-894x(02)00309-8
		44334037	11218	0	None	-112	3	Human	5.2	pKi	=	5.2	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	450	9	1	7	3.7	CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)c3csc(-c4cccnc4)n3)C2)cc1	10.1016/s0960-894x(02)00685-6
		CHEMBL101634	11218	0	None	-112	3	Human	5.2	pKi	=	5.2	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	450	9	1	7	3.7	CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)c3csc(-c4cccnc4)n3)C2)cc1	10.1016/s0960-894x(02)00685-6
		73355415	99308	0	None	-32	13	Human	5.2	pKi	=	5.2	Binding	Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	277	3	1	1	2.1	C1C2C3CC4C2C2C1C3[C@H](NCC13C5C6C7C5C1C7C63)C42	10.1016/j.bmc.2013.07.045
		CHEMBL2432039	99308	0	None	-32	13	Human	5.2	pKi	=	5.2	Binding	Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	277	3	1	1	2.1	C1C2C3CC4C2C2C1C3[C@H](NCC13C5C6C7C5C1C7C63)C42	10.1016/j.bmc.2013.07.045
		CHEMBL5092267	222134	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCC[n+]1c(C)cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc1C	10.1016/j.bmcl.2021.128388
		164611474	192231	0	None	407	4	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	366	6	4	5	2.4	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1cccs1	10.1016/j.ejmech.2021.113190
		CHEMBL4861704	192231	0	None	407	4	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	366	6	4	5	2.4	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1cccs1	10.1016/j.ejmech.2021.113190
		164624107	192501	0	None	-1	6	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	402	9	4	4	2.8	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CCc1ccccc1	10.1016/j.ejmech.2021.113190
		CHEMBL4865765	192501	0	None	-1	6	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	402	9	4	4	2.8	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CCc1ccccc1	10.1016/j.ejmech.2021.113190
		164620678	192798	0	None	177	4	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	374	7	4	4	2.7	CCC(NC(=O)/N=C(\N)NCCCc1sc(N)nc1C)c1ccccc1	10.1016/j.ejmech.2021.113190
		CHEMBL4870510	192798	0	None	177	4	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	374	7	4	4	2.7	CCC(NC(=O)/N=C(\N)NCCCc1sc(N)nc1C)c1ccccc1	10.1016/j.ejmech.2021.113190
		126688	7192	33	None	-1	3	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	157	2	2	4	0.5	NCCc1sc(nc1C)N	10.1016/j.bmcl.2010.10.041
		4025	7192	33	None	-1	3	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	157	2	2	4	0.5	NCCc1sc(nc1C)N	10.1016/j.bmcl.2010.10.041
		CHEMBL293762	7192	33	None	-1	3	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	157	2	2	4	0.5	NCCc1sc(nc1C)N	10.1016/j.bmcl.2010.10.041
		155551348	180736	0	None	1	2	Human	5.2	pKi	=	5.2	Binding	Inhibition of histamine H2 receptor (unknown origin)Inhibition of histamine H2 receptor (unknown origin)	ChEMBL	487	7	1	9	3.7	CCOC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@@H]1OC(C)(C)O[C@@H]12	10.1021/acs.jmedchem.8b01662
		CHEMBL4541409	180736	0	None	1	2	Human	5.2	pKi	=	5.2	Binding	Inhibition of histamine H2 receptor (unknown origin)Inhibition of histamine H2 receptor (unknown origin)	ChEMBL	487	7	1	9	3.7	CCOC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@@H]1OC(C)(C)O[C@@H]12	10.1021/acs.jmedchem.8b01662
		168292954	199776	0	None	-11	6	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	388	8	4	4	2.5	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5202592	199776	0	None	-11	6	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	388	8	4	4	2.5	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5222660	199776	0	None	-11	6	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	388	8	4	4	2.5	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
		162676676	190368	0	None	-323	3	Human	5.2	pKi	=	5.2	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysis	ChEMBL	389	8	0	5	4.5	c1ccc(Oc2ccc(OCCCN3CCN(c4ccncc4)CC3)cc2)cc1	10.1016/j.ejmech.2020.113041
		CHEMBL4800672	190368	0	None	-323	3	Human	5.2	pKi	=	5.2	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysis	ChEMBL	389	8	0	5	4.5	c1ccc(Oc2ccc(OCCCN3CCN(c4ccncc4)CC3)cc2)cc1	10.1016/j.ejmech.2020.113041
		CHEMBL5075713	222308	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL		None	None	None		CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2c[nH]cn2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1016/j.bmcl.2021.128388
		CHEMBL5095559	222308	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL		None	None	None		CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2c[nH]cn2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1016/j.bmcl.2021.128388
		4189	213701	96	None	-36	34	Human	5.2	pKi	=	5.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	414	6	0	3	6.5	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1	nan
		CHEMBL1559	213701	96	None	-36	34	Human	5.2	pKi	=	5.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	414	6	0	3	6.5	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1	nan
		CHEMBL91	213701	96	None	-36	34	Human	5.2	pKi	=	5.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	414	6	0	3	6.5	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1	nan
		130442572	178687	0	None	-144	24	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method	ChEMBL	395	3	0	5	6.0	FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12	10.1021/acs.jmedchem.9b00351
		CHEMBL4469848	178687	0	None	-144	24	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method	ChEMBL	395	3	0	5	6.0	FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12	10.1021/acs.jmedchem.9b00351
		181743	185351	5	None	-338	22	Human	6.2	pKi	=	6.2	Binding	Displacement of [3H]Tiotidine from human histamine H2 receptorDisplacement of [3H]Tiotidine from human histamine H2 receptor	ChEMBL	339	2	0	5	3.2	COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2)OCO4	10.1016/j.bmcl.2009.11.053
		CHEMBL467094	185351	5	None	-338	22	Human	6.2	pKi	=	6.2	Binding	Displacement of [3H]Tiotidine from human histamine H2 receptorDisplacement of [3H]Tiotidine from human histamine H2 receptor	ChEMBL	339	2	0	5	3.2	COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2)OCO4	10.1016/j.bmcl.2009.11.053
		168291233	199758	0	None	-5	4	Human	6.2	pKi	=	6.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	373	8	4	5	1.4	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)o2)cc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5200106	199758	0	None	-5	4	Human	6.2	pKi	=	6.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	373	8	4	5	1.4	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)o2)cc1	10.1021/acs.jmedchem.1c00692
		CHEMBL5222556	199758	0	None	-5	4	Human	6.2	pKi	=	6.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	373	8	4	5	1.4	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)o2)cc1	10.1021/acs.jmedchem.1c00692
		44304031	107448	0	None	-933	3	Human	5.2	pKi	=	5.2	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	452	10	0	6	4.1	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)/C=C/c3ccc(OC)cc3)cc2)CC1	10.1016/s0960-894x(02)00309-8
		CHEMBL292275	107448	0	None	-933	3	Human	5.2	pKi	=	5.2	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	452	10	0	6	4.1	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)/C=C/c3ccc(OC)cc3)cc2)CC1	10.1016/s0960-894x(02)00309-8
		18672441	102170	0	None	-9332	4	Human	4.2	pKi	=	4.2	Binding	Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor	ChEMBL	306	6	0	3	4.1	N#Cc1ccc(-c2ccc(OCCCN3CCCC3)cc2)cc1	10.1016/s0960-894x(02)00648-0
		CHEMBL25688	102170	0	None	-9332	4	Human	4.2	pKi	=	4.2	Binding	Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor	ChEMBL	306	6	0	3	4.1	N#Cc1ccc(-c2ccc(OCCCN3CCCC3)cc2)cc1	10.1016/s0960-894x(02)00648-0
		4601	213526	35	None	-7	17	Human	5.2	pKi	=	5.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	269	6	0	2	3.7	Cc1ccccc1C(OCCN(C)C)c1ccccc1	nan
		CHEMBL1201023	213526	35	None	-7	17	Human	5.2	pKi	=	5.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	269	6	0	2	3.7	Cc1ccccc1C(OCCN(C)C)c1ccccc1	nan
		CHEMBL900	213526	35	None	-7	17	Human	5.2	pKi	=	5.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	269	6	0	2	3.7	Cc1ccccc1C(OCCN(C)C)c1ccccc1	nan
		162664702	188989	0	None	-50	3	Human	5.2	pKi	=	5.2	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysis	ChEMBL	407	7	0	4	5.0	Clc1ccc(-c2ccc(OCCCN3CCN(c4ccncc4)CC3)cc2)cc1	10.1016/j.ejmech.2020.113041
		CHEMBL4783066	188989	0	None	-50	3	Human	5.2	pKi	=	5.2	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysis	ChEMBL	407	7	0	4	5.0	Clc1ccc(-c2ccc(OCCCN3CCN(c4ccncc4)CC3)cc2)cc1	10.1016/j.ejmech.2020.113041
		164611342	191867	0	None	-1	6	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	346	6	4	4	1.8	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCc1ccccc1	10.1016/j.ejmech.2021.113190
		CHEMBL4856005	191867	0	None	-1	6	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	346	6	4	4	1.8	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCc1ccccc1	10.1016/j.ejmech.2021.113190
		164618690	192935	0	None	1	5	Human	6.2	pKi	=	6.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	360	7	4	4	3.4	CCCCCCNC(=O)/N=C(\N)Nc1cccc(-c2csc(N)n2)c1	10.1016/j.ejmech.2021.113190
		CHEMBL4872375	192935	0	None	1	5	Human	6.2	pKi	=	6.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	360	7	4	4	3.4	CCCCCCNC(=O)/N=C(\N)Nc1cccc(-c2csc(N)n2)c1	10.1016/j.ejmech.2021.113190
		127035835	144063	0	None	-4	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [3H]UR-DE257 from human histamine 2 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]UR-DE257 from human histamine 2 receptor expressed in Sf9 cell membranes by liquid scintillation counting	ChEMBL	385	4	1	5	3.6	CN1CCN(c2nc(NCc3ccccc3)nc3c2CCc2ccccc2-3)CC1	10.1016/j.bmcl.2015.12.035
		CHEMBL3752270	144063	0	None	-4	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [3H]UR-DE257 from human histamine 2 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]UR-DE257 from human histamine 2 receptor expressed in Sf9 cell membranes by liquid scintillation counting	ChEMBL	385	4	1	5	3.6	CN1CCN(c2nc(NCc3ccccc3)nc3c2CCc2ccccc2-3)CC1	10.1016/j.bmcl.2015.12.035
		44304079	209405	0	None	-9549	3	Human	4.2	pKi	=	4.2	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	376	9	0	5	3.5	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)CC(C)C)cc2)CC1	10.1016/s0960-894x(02)00309-8
		CHEMBL61231	209405	0	None	-9549	3	Human	4.2	pKi	=	4.2	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	376	9	0	5	3.5	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)CC(C)C)cc2)CC1	10.1016/s0960-894x(02)00309-8
		44335428	11756	0	None	-79	3	Human	4.2	pKi	=	4.2	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	358	7	1	5	2.6	CCOC(=O)N1CCN(CCCOc2ccc(-c3c[nH]cn3)cc2)CC1	10.1016/s0960-894x(02)00648-0
		CHEMBL104947	11756	0	None	-79	3	Human	4.2	pKi	=	4.2	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	358	7	1	5	2.6	CCOC(=O)N1CCN(CCCOc2ccc(-c3c[nH]cn3)cc2)CC1	10.1016/s0960-894x(02)00648-0
		1231	7724	116	None	-4	8	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.bmcl.2013.12.024
		2756	7724	116	None	-4	8	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.bmcl.2013.12.024
		645	7724	116	None	-4	8	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.bmcl.2013.12.024
		CHEMBL30	7724	116	None	-4	8	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.bmcl.2013.12.024
		DB00501	7724	116	None	-4	8	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.bmcl.2013.12.024
		1231	7724	116	None	-4	8	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.bmcl.2013.12.024
		2756	7724	116	None	-4	8	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.bmcl.2013.12.024
		645	7724	116	None	-4	8	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.bmcl.2013.12.024
		CHEMBL30	7724	116	None	-4	8	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.bmcl.2013.12.024
		DB00501	7724	116	None	-4	8	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.bmcl.2013.12.024
		164610892	191977	0	None	1	6	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	394	8	4	4	3.2	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CC1CCCCC1	10.1016/j.ejmech.2021.113190
		CHEMBL4857560	191977	0	None	1	6	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	394	8	4	4	3.2	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CC1CCCCC1	10.1016/j.ejmech.2021.113190
		44334407	115862	0	None	-229	3	Human	6.2	pKi	=	6.2	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	462	10	1	5	3.8	O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3cccc(Cl)c3)C2)cc1)C1CC1	10.1016/s0960-894x(02)00685-6
		CHEMBL321320	115862	0	None	-229	3	Human	6.2	pKi	=	6.2	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	462	10	1	5	3.8	O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3cccc(Cl)c3)C2)cc1)C1CC1	10.1016/s0960-894x(02)00685-6
		44304402	207991	0	None	-426	3	Human	5.2	pKi	=	5.2	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	415	12	0	6	4.5	CCCCCC(=O)c1ccc(OCCCN2CCN(Cc3nccs3)CC2)cc1	10.1016/s0960-894x(02)00309-8
		CHEMBL60360	207991	0	None	-426	3	Human	5.2	pKi	=	5.2	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	415	12	0	6	4.5	CCCCCC(=O)c1ccc(OCCCN2CCN(Cc3nccs3)CC2)cc1	10.1016/s0960-894x(02)00309-8
		1258	6984	12	None	-35481	5	Human	4.2	pKi	=	4.2	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	359	8	1	5	1.5	C[C@H](C(=O)N1CCN(CC1)CCCOc1ccc(cc1)C(=O)C1CC1)N	10.1016/s0960-894x(02)00310-4
		9906860	6984	12	None	-35481	5	Human	4.2	pKi	=	4.2	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	359	8	1	5	1.5	C[C@H](C(=O)N1CCN(CC1)CCCOc1ccc(cc1)C(=O)C1CC1)N	10.1016/s0960-894x(02)00310-4
		CHEMBL302196	6984	12	None	-35481	5	Human	4.2	pKi	=	4.2	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	359	8	1	5	1.5	C[C@H](C(=O)N1CCN(CC1)CCCOc1ccc(cc1)C(=O)C1CC1)N	10.1016/s0960-894x(02)00310-4
		44334042	170268	0	None	-64	3	Human	6.2	pKi	=	6.2	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	453	10	1	6	3.0	N#Cc1ccccc1S(=O)(=O)N[C@H]1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)C1	10.1016/s0960-894x(02)00685-6
		CHEMBL420108	170268	0	None	-64	3	Human	6.2	pKi	=	6.2	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	453	10	1	6	3.0	N#Cc1ccccc1S(=O)(=O)N[C@H]1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)C1	10.1016/s0960-894x(02)00685-6
		44334234	116456	0	None	-707	3	Human	5.2	pKi	=	5.2	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	432	10	1	7	1.8	Cn1cnc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)c1	10.1016/s0960-894x(02)00685-6
		CHEMBL322678	116456	0	None	-707	3	Human	5.2	pKi	=	5.2	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	432	10	1	7	1.8	Cn1cnc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)c1	10.1016/s0960-894x(02)00685-6
		180	7189	56	None	-1412	40	Human	6.1	pKi	=	6.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	nan
		200	7189	56	None	-1412	40	Human	6.1	pKi	=	6.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	nan
		2160	7189	56	None	-1412	40	Human	6.1	pKi	=	6.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	nan
		CHEMBL629	7189	56	None	-1412	40	Human	6.1	pKi	=	6.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	nan
		DB00321	7189	56	None	-1412	40	Human	6.1	pKi	=	6.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	nan
		164611757	191682	0	None	1	6	Human	7.1	pKi	=	7.1	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	402	8	4	4	2.8	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1	10.1016/j.ejmech.2021.113190
		CHEMBL4853107	191682	0	None	1	6	Human	7.1	pKi	=	7.1	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	402	8	4	4	2.8	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1	10.1016/j.ejmech.2021.113190
		44304003	209913	0	None	-2511	3	Human	4.1	pKi	=	4.1	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	384	9	1	6	1.4	N#CC[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		CHEMBL64124	209913	0	None	-2511	3	Human	4.1	pKi	=	4.1	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	384	9	1	6	1.4	N#CC[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		127052294	147080	0	None	-33	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [3H]tiotidine from human histamine H2 receptor expressed in sf9 cell membrane co-expressing Gsalphas incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]tiotidine from human histamine H2 receptor expressed in sf9 cell membrane co-expressing Gsalphas incubated for 60 mins by liquid scintillation counting method	ChEMBL	368	7	3	4	3.1	N#C/N=C(/NCCSc1ccccc1)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1	10.1021/acs.jmedchem.6b00120
		CHEMBL3806079	147080	0	None	-33	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [3H]tiotidine from human histamine H2 receptor expressed in sf9 cell membrane co-expressing Gsalphas incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]tiotidine from human histamine H2 receptor expressed in sf9 cell membrane co-expressing Gsalphas incubated for 60 mins by liquid scintillation counting method	ChEMBL	368	7	3	4	3.1	N#C/N=C(/NCCSc1ccccc1)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1	10.1021/acs.jmedchem.6b00120
		71463063	90576	0	None	-11	8	Human	5.1	pKi	=	5.1	Binding	Binding affinity to Histamine H2 receptorBinding affinity to Histamine H2 receptor	ChEMBL	295	3	1	3	2.0	COc1ccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1	10.1016/j.bmcl.2012.08.046
		CHEMBL2205825	90576	0	None	-11	8	Human	5.1	pKi	=	5.1	Binding	Binding affinity to Histamine H2 receptorBinding affinity to Histamine H2 receptor	ChEMBL	295	3	1	3	2.0	COc1ccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1	10.1016/j.bmcl.2012.08.046
		44334369	11786	0	None	-138	3	Human	6.1	pKi	=	6.1	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	484	10	1	5	4.4	CC(C)(C)c1ccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)cc1	10.1016/s0960-894x(02)00685-6
		CHEMBL105071	11786	0	None	-138	3	Human	6.1	pKi	=	6.1	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	484	10	1	5	4.4	CC(C)(C)c1ccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)cc1	10.1016/s0960-894x(02)00685-6
		127049856	147023	0	None	-25	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [3H]tiotidine from human histamine H2 receptor expressed in sf9 cell membrane co-expressing Gsalphas incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]tiotidine from human histamine H2 receptor expressed in sf9 cell membrane co-expressing Gsalphas incubated for 60 mins by liquid scintillation counting method	ChEMBL	368	7	3	4	3.1	N#C/N=C(/NCCSc1ccccc1)NC[C@H]1CC[C@@H](c2c[nH]cn2)C1	10.1021/acs.jmedchem.6b00120
		CHEMBL3805431	147023	0	None	-25	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [3H]tiotidine from human histamine H2 receptor expressed in sf9 cell membrane co-expressing Gsalphas incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]tiotidine from human histamine H2 receptor expressed in sf9 cell membrane co-expressing Gsalphas incubated for 60 mins by liquid scintillation counting method	ChEMBL	368	7	3	4	3.1	N#C/N=C(/NCCSc1ccccc1)NC[C@H]1CC[C@@H](c2c[nH]cn2)C1	10.1021/acs.jmedchem.6b00120
		9923147	11821	0	None	-1202	4	Human	5.1	pKi	=	5.1	Binding	Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor	ChEMBL	321	6	1	4	3.0	N#Cc1ccc(-c2ccc(OCCCN3CC[C@@H](N)C3)cc2)cc1	10.1016/s0960-894x(02)00648-0
		CHEMBL105267	11821	0	None	-1202	4	Human	5.1	pKi	=	5.1	Binding	Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor	ChEMBL	321	6	1	4	3.0	N#Cc1ccc(-c2ccc(OCCCN3CC[C@@H](N)C3)cc2)cc1	10.1016/s0960-894x(02)00648-0
		71463061	90570	0	None	1	9	Human	6.1	pKi	=	6.1	Binding	Binding affinity to Histamine H2 receptorBinding affinity to Histamine H2 receptor	ChEMBL	339	5	1	4	2.0	COc1cccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)c1OC	10.1016/j.bmcl.2012.08.046
		CHEMBL2205813	90570	0	None	1	9	Human	6.1	pKi	=	6.1	Binding	Binding affinity to Histamine H2 receptorBinding affinity to Histamine H2 receptor	ChEMBL	339	5	1	4	2.0	COc1cccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)c1OC	10.1016/j.bmcl.2012.08.046
		162662563	188825	0	None	-123	3	Human	5.1	pKi	=	5.1	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysis	ChEMBL	391	7	0	4	4.5	Fc1ccc(-c2ccc(OCCCN3CCN(c4ccncc4)CC3)cc2)cc1	10.1016/j.ejmech.2020.113041
		CHEMBL4781093	188825	0	None	-123	3	Human	5.1	pKi	=	5.1	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysis	ChEMBL	391	7	0	4	4.5	Fc1ccc(-c2ccc(OCCCN3CCN(c4ccncc4)CC3)cc2)cc1	10.1016/j.ejmech.2020.113041
		44435200	156454	0	None	-4	4	Human	5.1	pKi	=	5.1	Binding	Antagonist activity at histamine H2 receptor (unknown origin) by PDSP assayAntagonist activity at histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	345	4	0	2	5.8	O=C(CCCc1ccccc1)N1c2ccccc2Sc2ccccc21	10.1016/j.bmcl.2013.04.082
		CHEMBL394755	156454	0	None	-4	4	Human	5.1	pKi	=	5.1	Binding	Antagonist activity at histamine H2 receptor (unknown origin) by PDSP assayAntagonist activity at histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	345	4	0	2	5.8	O=C(CCCc1ccccc1)N1c2ccccc2Sc2ccccc21	10.1016/j.bmcl.2013.04.082
		44335389	11939	0	None	-46	3	Human	5.1	pKi	=	5.1	Binding	Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor	ChEMBL	413	8	0	6	3.8	CCOC(=O)N1CCN(CCCOc2ccc(-c3ccccc3[N+](=O)[O-])cc2)CC1	10.1016/s0960-894x(02)00648-0
		CHEMBL105952	11939	0	None	-46	3	Human	5.1	pKi	=	5.1	Binding	Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor	ChEMBL	413	8	0	6	3.8	CCOC(=O)N1CCN(CCCOc2ccc(-c3ccccc3[N+](=O)[O-])cc2)CC1	10.1016/s0960-894x(02)00648-0
		44304243	209978	0	None	-562	3	Human	5.1	pKi	=	5.1	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	374	13	0	4	4.6	CCCCCC(=O)c1ccc(OCCCN2CCN(CCCC)CC2)cc1	10.1016/s0960-894x(02)00309-8
		CHEMBL64334	209978	0	None	-562	3	Human	5.1	pKi	=	5.1	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	374	13	0	4	4.6	CCCCCC(=O)c1ccc(OCCCN2CCN(CCCC)CC2)cc1	10.1016/s0960-894x(02)00309-8
		156015041	185012	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	1029	30	3	11	10.0	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
		CHEMBL4637356	185012	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	1029	30	3	11	10.0	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
		CHEMBL4650547	185012	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	1029	30	3	11	10.0	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
		164617783	191369	0	None	-1	6	Human	7.1	pKi	=	7.1	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	388	8	4	4	2.8	CCC(CNC(=O)/N=C(\N)NCCCc1sc(N)nc1C)c1ccccc1	10.1016/j.ejmech.2021.113190
		CHEMBL4848815	191369	0	None	-1	6	Human	7.1	pKi	=	7.1	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	388	8	4	4	2.8	CCC(CNC(=O)/N=C(\N)NCCCc1sc(N)nc1C)c1ccccc1	10.1016/j.ejmech.2021.113190
		11393516	11944	0	None	-933	4	Human	5.1	pKi	=	5.1	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	335	6	1	4	3.3	N#Cc1ccc(-c2ccc(OCCCN3CCCNCC3)cc2)cc1	10.1016/s0960-894x(02)00648-0
		CHEMBL105967	11944	0	None	-933	4	Human	5.1	pKi	=	5.1	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	335	6	1	4	3.3	N#Cc1ccc(-c2ccc(OCCCN3CCCNCC3)cc2)cc1	10.1016/s0960-894x(02)00648-0
		75306277	116031	0	None	-39	23	Human	7.1	pKi	=	7.1	Binding	Binding affinity to H2 histamine receptor (unknown origin) by PDSP assayBinding affinity to H2 histamine receptor (unknown origin) by PDSP assay	ChEMBL	308	0	0	3	4.2	CN1CCC2C(C1)c1cccc3c1N2c1ccccc1CS3	10.1039/C2MD00311B
		CHEMBL3217984	116031	0	None	-39	23	Human	7.1	pKi	=	7.1	Binding	Binding affinity to H2 histamine receptor (unknown origin) by PDSP assayBinding affinity to H2 histamine receptor (unknown origin) by PDSP assay	ChEMBL	308	0	0	3	4.2	CN1CCC2C(C1)c1cccc3c1N2c1ccccc1CS3	10.1039/C2MD00311B
		44304088	209166	0	None	-316	3	Human	5.1	pKi	=	5.1	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	402	8	0	5	4.0	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)C3CCCCC3)cc2)CC1	10.1016/s0960-894x(02)00309-8
		CHEMBL61070	209166	0	None	-316	3	Human	5.1	pKi	=	5.1	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	402	8	0	5	4.0	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)C3CCCCC3)cc2)CC1	10.1016/s0960-894x(02)00309-8
		1269	6909	41	None	-269	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	125	2	2	2	0.2	Cc1c(CCN)nc[nH]1	10.1016/j.bmcl.2010.10.041
		37463	6909	41	None	-269	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	125	2	2	2	0.2	Cc1c(CCN)nc[nH]1	10.1016/j.bmcl.2010.10.041
		CHEMBL275443	6909	41	None	-269	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	125	2	2	2	0.2	Cc1c(CCN)nc[nH]1	10.1016/j.bmcl.2010.10.041
		44304090	209729	0	None	-16982	3	Human	4.1	pKi	=	4.1	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	360	8	0	5	2.8	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00309-8
		CHEMBL62948	209729	0	None	-16982	3	Human	4.1	pKi	=	4.1	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	360	8	0	5	2.8	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00309-8
		44304067	208062	0	None	-34673	3	Human	4.1	pKi	=	4.1	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	359	9	1	5	1.4	CNCC(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		CHEMBL60401	208062	0	None	-34673	3	Human	4.1	pKi	=	4.1	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	359	9	1	5	1.4	CNCC(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		168281746	199661	0	None	-676	6	Human	8.1	pKi	=	8.1	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	365	6	4	5	1.6	CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1	10.1021/acs.jmedchem.1c00692
		CHEMBL5184911	199661	0	None	-676	6	Human	8.1	pKi	=	8.1	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	365	6	4	5	1.6	CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1	10.1021/acs.jmedchem.1c00692
		CHEMBL5221974	199661	0	None	-676	6	Human	8.1	pKi	=	8.1	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	365	6	4	5	1.6	CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1	10.1021/acs.jmedchem.1c00692
		75201901	173204	19	None	-588	24	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method	ChEMBL	356	3	0	6	4.9	Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12	10.1021/acs.jmedchem.9b00351
		CHEMBL4277264	173204	19	None	-588	24	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method	ChEMBL	356	3	0	6	4.9	Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12	10.1021/acs.jmedchem.9b00351
		CHEMBL4448899	220715	50	None	-	1	Human	5.1	pKi	=	5.1	Binding	Selectivity interaction (GPCR panel (PDSP screen)) EUB0000307b HRH2Selectivity interaction (GPCR panel (PDSP screen)) EUB0000307b HRH2	ChEMBL		None	None	None		Cc1c(NC(=O)c2cc(C(N)=O)nc3cc(F)ccc23)c(C(F)(F)F)nn1Cc1ccc(C#N)cc1	10.6019/CHEMBL5212743
		21509921	111235	0	None	-7	24	Human	7.1	pKi	=	7.1	Binding	Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)	ChEMBL	288	0	0	2	3.7	CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1	10.1016/j.bmcl.2013.12.024
		CHEMBL3104091	111235	0	None	-7	24	Human	7.1	pKi	=	7.1	Binding	Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)	ChEMBL	288	0	0	2	3.7	CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1	10.1016/j.bmcl.2013.12.024
		21509921	111235	0	None	-7	24	Human	7.1	pKi	=	7.1	Binding	Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)	ChEMBL	288	0	0	2	3.7	CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1	10.1016/j.bmcl.2013.12.024
		CHEMBL3104091	111235	0	None	-7	24	Human	7.1	pKi	=	7.1	Binding	Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)	ChEMBL	288	0	0	2	3.7	CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1	10.1016/j.bmcl.2013.12.024
		44304270	208027	0	None	-512	3	Human	5.1	pKi	=	5.1	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	442	11	0	5	5.0	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3ccc(C)s3)CC2)cc1	10.1016/s0960-894x(02)00309-8
		CHEMBL60383	208027	0	None	-512	3	Human	5.1	pKi	=	5.1	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	442	11	0	5	5.0	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3ccc(C)s3)CC2)cc1	10.1016/s0960-894x(02)00309-8
		130442480	182049	0	None	-100	24	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method	ChEMBL	410	3	0	6	5.7	Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F	10.1021/acs.jmedchem.9b00351
		CHEMBL4572614	182049	0	None	-100	24	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method	ChEMBL	410	3	0	6	5.7	Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F	10.1021/acs.jmedchem.9b00351
		1210	7705	51	None	-446	21	Human	5.1	pKi	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	nan
		1213	7705	51	None	-446	21	Human	5.1	pKi	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	nan
		2725	7705	51	None	-446	21	Human	5.1	pKi	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	nan
		33036	7705	51	None	-446	21	Human	5.1	pKi	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	nan
		4411	7705	51	None	-446	21	Human	5.1	pKi	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	nan
		616	7705	51	None	-446	21	Human	5.1	pKi	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	nan
		6976	7705	51	None	-446	21	Human	5.1	pKi	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	nan
		716121	7705	51	None	-446	21	Human	5.1	pKi	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	nan
		CHEMBL1201353	7705	51	None	-446	21	Human	5.1	pKi	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	nan
		CHEMBL1554789	7705	51	None	-446	21	Human	5.1	pKi	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	nan
		CHEMBL505	7705	51	None	-446	21	Human	5.1	pKi	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	nan
		DB01114	7705	51	None	-446	21	Human	5.1	pKi	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	nan
		DB13679	7705	51	None	-446	21	Human	5.1	pKi	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	nan
		155539605	179624	0	None	-3	6	Human	6.1	pKi	=	6.1	Binding	Binding affinity to human histamine 2 receptor expressed in HEK cells by radioligand binding assayBinding affinity to human histamine 2 receptor expressed in HEK cells by radioligand binding assay	ChEMBL	313	1	0	4	2.1	CC1=NC2(CCN(C)CC2)C(=O)N(c2c(C)cccc2C)C1=O	10.1016/j.ejmech.2018.12.048
		CHEMBL4514672	179624	0	None	-3	6	Human	6.1	pKi	=	6.1	Binding	Binding affinity to human histamine 2 receptor expressed in HEK cells by radioligand binding assayBinding affinity to human histamine 2 receptor expressed in HEK cells by radioligand binding assay	ChEMBL	313	1	0	4	2.1	CC1=NC2(CCN(C)CC2)C(=O)N(c2c(C)cccc2C)C1=O	10.1016/j.ejmech.2018.12.048
		44582705	193775	0	None	-5	13	Human	6.1	pKi	=	6.1	Binding	Inhibition of human cloned histamine H2 receptor by competitive binding experimentInhibition of human cloned histamine H2 receptor by competitive binding experiment	ChEMBL	399	9	0	4	4.5	COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(C)cc2)CC1	10.1016/j.bmc.2009.03.021
		CHEMBL490632	193775	0	None	-5	13	Human	6.1	pKi	=	6.1	Binding	Inhibition of human cloned histamine H2 receptor by competitive binding experimentInhibition of human cloned histamine H2 receptor by competitive binding experiment	ChEMBL	399	9	0	4	4.5	COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(C)cc2)CC1	10.1016/j.bmc.2009.03.021
		145973771	171498	0	None	2	7	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]-Iodoaminopotentidine from human histamine H2 receptor expressed in HEK293T cell membranes after 90 mins by scintillation counting methodDisplacement of [125I]-Iodoaminopotentidine from human histamine H2 receptor expressed in HEK293T cell membranes after 90 mins by scintillation counting method	ChEMBL	797	16	2	7	10.8	CC(C)(C)OC(=O)NCCCCCCn1cc(CCCCN2CCC(c3ccc(-c4cc(C(=O)O)cc5cc(-c6ccc(C(F)(F)F)cc6)ccc45)cc3)CC2)nn1	10.1021/acs.jmedchem.8b00168
		CHEMBL4217398	171498	0	None	2	7	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]-Iodoaminopotentidine from human histamine H2 receptor expressed in HEK293T cell membranes after 90 mins by scintillation counting methodDisplacement of [125I]-Iodoaminopotentidine from human histamine H2 receptor expressed in HEK293T cell membranes after 90 mins by scintillation counting method	ChEMBL	797	16	2	7	10.8	CC(C)(C)OC(=O)NCCCCCCn1cc(CCCCN2CCC(c3ccc(-c4cc(C(=O)O)cc5cc(-c6ccc(C(F)(F)F)cc6)ccc45)cc3)CC2)nn1	10.1021/acs.jmedchem.8b00168
		44335412	114236	0	None	-102	3	Human	5.1	pKi	=	5.1	Binding	Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor	ChEMBL	413	8	0	6	3.8	CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc([N+](=O)[O-])cc3)cc2)CC1	10.1016/s0960-894x(02)00648-0
		CHEMBL318320	114236	0	None	-102	3	Human	5.1	pKi	=	5.1	Binding	Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor	ChEMBL	413	8	0	6	3.8	CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc([N+](=O)[O-])cc3)cc2)CC1	10.1016/s0960-894x(02)00648-0
		44304284	170058	0	None	-208	3	Human	5.1	pKi	=	5.1	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	426	9	0	6	3.5	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)c3ccc(OC)cc3)cc2)CC1	10.1016/s0960-894x(02)00309-8
		CHEMBL418691	170058	0	None	-208	3	Human	5.1	pKi	=	5.1	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	426	9	0	6	3.5	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)c3ccc(OC)cc3)cc2)CC1	10.1016/s0960-894x(02)00309-8
		44304978	174668	0	None	-3890	3	Human	4.1	pKi	=	4.1	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	396	11	0	5	2.8	CCCCCC(=O)c1ccc(OCCCN2CCN(S(C)(=O)=O)CC2)cc1	10.1016/s0960-894x(02)00309-8
		CHEMBL431172	174668	0	None	-3890	3	Human	4.1	pKi	=	4.1	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	396	11	0	5	2.8	CCCCCC(=O)c1ccc(OCCCN2CCN(S(C)(=O)=O)CC2)cc1	10.1016/s0960-894x(02)00309-8
		44304752	209991	0	None	-39810	3	Human	4.1	pKi	=	4.1	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	459	9	1	6	3.1	C[C@@H](NC(=O)OC(C)(C)C)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		CHEMBL64406	209991	0	None	-39810	3	Human	4.1	pKi	=	4.1	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	459	9	1	6	3.1	C[C@@H](NC(=O)OC(C)(C)C)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		11496610	10847	13	None	-2	2	Human	6.1	pKi	=	6.1	Binding	Inhibition of human histamine H2 receptorInhibition of human histamine H2 receptor	ChEMBL	476	4	1	5	5.8	CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C	10.1021/jm801572m
		5582	10847	13	None	-2	2	Human	6.1	pKi	=	6.1	Binding	Inhibition of human histamine H2 receptorInhibition of human histamine H2 receptor	ChEMBL	476	4	1	5	5.8	CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C	10.1021/jm801572m
		CHEMBL474991	10847	13	None	-2	2	Human	6.1	pKi	=	6.1	Binding	Inhibition of human histamine H2 receptorInhibition of human histamine H2 receptor	ChEMBL	476	4	1	5	5.8	CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C	10.1021/jm801572m
		73355421	99327	0	None	-	1	Human	5.1	pKi	=	5.1	Binding	Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	309	3	0	3	3.0	CN(Cc1ccc2c(c1)OCO2)[C@H]1C2C3CC4C5C3CC2C5C41	10.1016/j.bmc.2013.07.045
		CHEMBL2432062	99327	0	None	-	1	Human	5.1	pKi	=	5.1	Binding	Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	309	3	0	3	3.0	CN(Cc1ccc2c(c1)OCO2)[C@H]1C2C3CC4C5C3CC2C5C41	10.1016/j.bmc.2013.07.045
		164620139	192567	0	None	56	4	Human	7.1	pKi	=	7.1	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	436	8	4	4	3.4	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(c1ccccc1)c1ccccc1	10.1016/j.ejmech.2021.113190
		CHEMBL4866734	192567	0	None	56	4	Human	7.1	pKi	=	7.1	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	436	8	4	4	3.4	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(c1ccccc1)c1ccccc1	10.1016/j.ejmech.2021.113190
		11846300	87041	3	None	-1071	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [3H]APT from human histamine H2 receptor transfected in COS7 cellsDisplacement of [3H]APT from human histamine H2 receptor transfected in COS7 cells	ChEMBL	327	0	0	4	3.8	CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1	10.1021/jm051008s
		CHEMBL213912	87041	3	None	-1071	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [3H]APT from human histamine H2 receptor transfected in COS7 cellsDisplacement of [3H]APT from human histamine H2 receptor transfected in COS7 cells	ChEMBL	327	0	0	4	3.8	CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1	10.1021/jm051008s
		137646281	164585	0	None	-1995	17	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method	ChEMBL	423	8	0	7	3.8	COc1ccccc1N1CCN(CCCSc2nnc(-c3ccccc3)n2C)CC1	10.1021/acs.jmedchem.9b00412
		CHEMBL4083252	164585	0	None	-1995	17	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method	ChEMBL	423	8	0	7	3.8	COc1ccccc1N1CCN(CCCSc2nnc(-c3ccccc3)n2C)CC1	10.1021/acs.jmedchem.9b00412
		657255	205863	34	None	-3	15	Human	7.1	pKi	=	7.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	337	12	2	3	5.6	CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1	nan
		CHEMBL588119	205863	34	None	-3	15	Human	7.1	pKi	=	7.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	337	12	2	3	5.6	CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1	nan
		1234	10064	68	None	-2	7	Human	7.1	pKi	=	7.1	Binding	Antagonist activity at histamine H2 receptor (unknown origin) assessed as inhibition constantAntagonist activity at histamine H2 receptor (unknown origin) assessed as inhibition constant	ChEMBL	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	10.1021/acs.jmedchem.0c01901
		3001055	10064	68	None	-2	7	Human	7.1	pKi	=	7.1	Binding	Antagonist activity at histamine H2 receptor (unknown origin) assessed as inhibition constantAntagonist activity at histamine H2 receptor (unknown origin) assessed as inhibition constant	ChEMBL	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	10.1021/acs.jmedchem.0c01901
		CHEMBL512	10064	68	None	-2	7	Human	7.1	pKi	=	7.1	Binding	Antagonist activity at histamine H2 receptor (unknown origin) assessed as inhibition constantAntagonist activity at histamine H2 receptor (unknown origin) assessed as inhibition constant	ChEMBL	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	10.1021/acs.jmedchem.0c01901
		DB00863	10064	68	None	-2	7	Human	7.1	pKi	=	7.1	Binding	Antagonist activity at histamine H2 receptor (unknown origin) assessed as inhibition constantAntagonist activity at histamine H2 receptor (unknown origin) assessed as inhibition constant	ChEMBL	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	10.1021/acs.jmedchem.0c01901
		44304439	109575	0	None	-891	3	Human	5.1	pKi	=	5.1	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	436	12	0	4	4.6	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)Cc3ccccc3)CC2)cc1	10.1016/s0960-894x(02)00309-8
		CHEMBL305338	109575	0	None	-891	3	Human	5.1	pKi	=	5.1	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	436	12	0	4	4.6	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)Cc3ccccc3)CC2)cc1	10.1016/s0960-894x(02)00309-8
		44304332	208123	0	None	-19054	3	Human	4.1	pKi	=	4.1	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	399	9	1	5	2.3	O=C(c1ccc(OCCCN2CCN(C(=O)C[C@H]3CCCN3)CC2)cc1)C1CC1	10.1016/s0960-894x(02)00310-4
		CHEMBL60435	208123	0	None	-19054	3	Human	4.1	pKi	=	4.1	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	399	9	1	5	2.3	O=C(c1ccc(OCCCN2CCN(C(=O)C[C@H]3CCCN3)CC2)cc1)C1CC1	10.1016/s0960-894x(02)00310-4
		44304719	209501	0	None	-19498	3	Human	4.1	pKi	=	4.1	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	425	10	2	6	1.5	N[C@H](Cc1c[nH]cn1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		CHEMBL61792	209501	0	None	-19498	3	Human	4.1	pKi	=	4.1	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	425	10	2	6	1.5	N[C@H](Cc1c[nH]cn1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		44334038	11234	0	None	-316	3	Human	6.1	pKi	=	6.1	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	453	10	1	6	3.0	N#Cc1cccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)c1	10.1016/s0960-894x(02)00685-6
		CHEMBL101748	11234	0	None	-316	3	Human	6.1	pKi	=	6.1	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	453	10	1	6	3.0	N#Cc1cccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)c1	10.1016/s0960-894x(02)00685-6
		10472082	11913	0	None	-13489	4	Human	5.0	pKi	=	5.0	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	334	6	0	3	4.9	C[C@@H]1CC[C@@H](C)N1CCCOc1ccc(-c2ccc(C#N)cc2)cc1	10.1016/s0960-894x(02)00648-0
		CHEMBL105762	11913	0	None	-13489	4	Human	5.0	pKi	=	5.0	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	334	6	0	3	4.9	C[C@@H]1CC[C@@H](C)N1CCCOc1ccc(-c2ccc(C#N)cc2)cc1	10.1016/s0960-894x(02)00648-0
		44335558	116847	0	None	-933	4	Human	5.0	pKi	=	5.0	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	334	6	0	3	4.7	CC1CCN(CCCOc2ccc(-c3ccc(C#N)cc3)cc2)CC1	10.1016/s0960-894x(02)00648-0
		CHEMBL323562	116847	0	None	-933	4	Human	5.0	pKi	=	5.0	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	334	6	0	3	4.7	CC1CCN(CCCOc2ccc(-c3ccc(C#N)cc3)cc2)CC1	10.1016/s0960-894x(02)00648-0
		56963799	81670	0	None	-2290	10	Human	6.0	pKi	=	6.0	Binding	Binding affinity to human recombinant H2 receptorBinding affinity to human recombinant H2 receptor	ChEMBL	378	6	0	5	4.6	C[C@@H]1CCCN1CCc1cc2cc(C(=O)c3ccc([N+](=O)[O-])cc3)ccc2o1	10.1021/jm201690h
		CHEMBL2031737	81670	0	None	-2290	10	Human	6.0	pKi	=	6.0	Binding	Binding affinity to human recombinant H2 receptorBinding affinity to human recombinant H2 receptor	ChEMBL	378	6	0	5	4.6	C[C@@H]1CCCN1CCc1cc2cc(C(=O)c3ccc([N+](=O)[O-])cc3)ccc2o1	10.1021/jm201690h
		1016	10519	78	None	-41	35	Human	5.0	pKi	=	5.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	nan
		2561	10519	78	None	-41	35	Human	5.0	pKi	=	5.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	nan
		2733526	10519	78	None	-41	35	Human	5.0	pKi	=	5.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	nan
		5384	10519	78	None	-41	35	Human	5.0	pKi	=	5.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	nan
		CHEMBL83	10519	78	None	-41	35	Human	5.0	pKi	=	5.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	nan
		DB00675	10519	78	None	-41	35	Human	5.0	pKi	=	5.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	nan
		73213196	111237	4	None	-8	13	Human	6.0	pKi	=	6.0	Binding	Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)	ChEMBL	288	0	0	2	3.9	CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1	10.1016/j.bmcl.2013.12.024
		CHEMBL3104093	111237	4	None	-8	13	Human	6.0	pKi	=	6.0	Binding	Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)	ChEMBL	288	0	0	2	3.9	CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1	10.1016/j.bmcl.2013.12.024
		100	10577	58	None	-46	54	Human	6.0	pKi	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	nan
		2637	10577	58	None	-46	54	Human	6.0	pKi	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	nan
		5452	10577	58	None	-46	54	Human	6.0	pKi	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	nan
		CHEMBL479	10577	58	None	-46	54	Human	6.0	pKi	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	nan
		DB00679	10577	58	None	-46	54	Human	6.0	pKi	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	nan
		73213196	111237	4	None	-8	13	Human	6.0	pKi	=	6.0	Binding	Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)	ChEMBL	288	0	0	2	3.9	CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1	10.1016/j.bmcl.2013.12.024
		CHEMBL3104093	111237	4	None	-8	13	Human	6.0	pKi	=	6.0	Binding	Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)	ChEMBL	288	0	0	2	3.9	CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1	10.1016/j.bmcl.2013.12.024
		162657344	187711	0	None	-1096	3	Human	5.0	pKi	=	5.0	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysis	ChEMBL	388	8	1	5	4.4	c1ccc(Nc2ccc(OCCCN3CCN(c4ccncc4)CC3)cc2)cc1	10.1016/j.ejmech.2020.113041
		CHEMBL4758080	187711	0	None	-1096	3	Human	5.0	pKi	=	5.0	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysis	ChEMBL	388	8	1	5	4.4	c1ccc(Nc2ccc(OCCCN3CCN(c4ccncc4)CC3)cc2)cc1	10.1016/j.ejmech.2020.113041
		71459604	90568	0	None	-1	14	Human	6.0	pKi	=	6.0	Binding	Binding affinity to Histamine H2 receptorBinding affinity to Histamine H2 receptor	ChEMBL	309	4	1	3	2.0	COc1cccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)c1	10.1016/j.bmcl.2012.08.046
		CHEMBL2205811	90568	0	None	-1	14	Human	6.0	pKi	=	6.0	Binding	Binding affinity to Histamine H2 receptorBinding affinity to Histamine H2 receptor	ChEMBL	309	4	1	3	2.0	COc1cccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)c1	10.1016/j.bmcl.2012.08.046
		CHEMBL5088914	222341	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
		CHEMBL5095949	222341	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
		44304223	207168	0	None	-1023	3	Human	5.0	pKi	=	5.0	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	374	12	0	4	4.5	CCCCCC(=O)c1ccc(OCCCN2CCN(CC(C)C)CC2)cc1	10.1016/s0960-894x(02)00309-8
		CHEMBL59798	207168	0	None	-1023	3	Human	5.0	pKi	=	5.0	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	374	12	0	4	4.5	CCCCCC(=O)c1ccc(OCCCN2CCN(CC(C)C)CC2)cc1	10.1016/s0960-894x(02)00309-8
		133	9274	52	None	-141	43	Human	6.0	pKi	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	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	9274	52	None	-141	43	Human	6.0	pKi	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	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	9274	52	None	-141	43	Human	6.0	pKi	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	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	9274	52	None	-141	43	Human	6.0	pKi	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	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	9274	52	None	-141	43	Human	6.0	pKi	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	403	4	1	4	4.1	O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C	nan
		44335172	11869	0	None	-467	3	Human	4.0	pKi	=	4.0	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	374	7	0	5	4.0	CCOC(=O)N1CCN(CCCOc2ccc(-c3ccsc3)cc2)CC1	10.1016/s0960-894x(02)00648-0
		CHEMBL105567	11869	0	None	-467	3	Human	4.0	pKi	=	4.0	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	374	7	0	5	4.0	CCOC(=O)N1CCN(CCCOc2ccc(-c3ccsc3)cc2)CC1	10.1016/s0960-894x(02)00648-0
		44304311	207072	0	None	-16982	3	Human	4.0	pKi	=	4.0	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	442	10	1	7	2.2	N[C@H](Cc1nccs1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		CHEMBL59733	207072	0	None	-16982	3	Human	4.0	pKi	=	4.0	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	442	10	1	7	2.2	N[C@H](Cc1nccs1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
		71450548	90575	0	None	-7	3	Human	5.0	pKi	=	5.0	Binding	Binding affinity to Histamine H2 receptorBinding affinity to Histamine H2 receptor	ChEMBL	295	3	1	3	2.0	COc1cccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)c1	10.1016/j.bmcl.2012.08.046
		CHEMBL2205824	90575	0	None	-7	3	Human	5.0	pKi	=	5.0	Binding	Binding affinity to Histamine H2 receptorBinding affinity to Histamine H2 receptor	ChEMBL	295	3	1	3	2.0	COc1cccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)c1	10.1016/j.bmcl.2012.08.046
		127049855	147006	0	None	-16	4	Human	5.0	pKi	=	5.0	Binding	Displacement of [3H]tiotidine from human histamine H2 receptor expressed in sf9 cell membrane co-expressing Gsalphas incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]tiotidine from human histamine H2 receptor expressed in sf9 cell membrane co-expressing Gsalphas incubated for 60 mins by liquid scintillation counting method	ChEMBL	368	7	3	4	3.1	N#C/N=C(/NCCSc1ccccc1)NC[C@@H]1CC[C@@H](c2c[nH]cn2)C1	10.1021/acs.jmedchem.6b00120
		CHEMBL3805220	147006	0	None	-16	4	Human	5.0	pKi	=	5.0	Binding	Displacement of [3H]tiotidine from human histamine H2 receptor expressed in sf9 cell membrane co-expressing Gsalphas incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]tiotidine from human histamine H2 receptor expressed in sf9 cell membrane co-expressing Gsalphas incubated for 60 mins by liquid scintillation counting method	ChEMBL	368	7	3	4	3.1	N#C/N=C(/NCCSc1ccccc1)NC[C@@H]1CC[C@@H](c2c[nH]cn2)C1	10.1021/acs.jmedchem.6b00120
		132060763	169640	0	None	-3	8	Human	6.0	pKi	=	6.0	Binding	Displacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method	ChEMBL	405	5	0	4	4.1	C=C(C)CN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)CC3)CC1	10.1016/j.ejmech.2018.02.024
		CHEMBL4173095	169640	0	None	-3	8	Human	6.0	pKi	=	6.0	Binding	Displacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method	ChEMBL	405	5	0	4	4.1	C=C(C)CN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)CC3)CC1	10.1016/j.ejmech.2018.02.024
		135	9310	43	None	-39	56	Human	6.0	pKi	=	6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	264	0	0	2	3.1	CN1CCN2C(C1)c1ccccc1Cc1c2cccc1	nan
		1796	9310	43	None	-39	56	Human	6.0	pKi	=	6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	264	0	0	2	3.1	CN1CCN2C(C1)c1ccccc1Cc1c2cccc1	nan
		4184	9310	43	None	-39	56	Human	6.0	pKi	=	6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	264	0	0	2	3.1	CN1CCN2C(C1)c1ccccc1Cc1c2cccc1	nan
		CHEMBL6437	9310	43	None	-39	56	Human	6.0	pKi	=	6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	264	0	0	2	3.1	CN1CCN2C(C1)c1ccccc1Cc1c2cccc1	nan
		DB06148	9310	43	None	-39	56	Human	6.0	pKi	=	6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	264	0	0	2	3.1	CN1CCN2C(C1)c1ccccc1Cc1c2cccc1	nan
		2281	9949	82	None	-	0	Rat	8.6	pIC50	=	8.6	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	Drug Central	334	10	2	3	2.3	CCCN(C(=O)C(NC(=O)c1ccccc1)CCC(=O)O)CCC	None
		4922	9949	82	None	-	0	Rat	8.6	pIC50	=	8.6	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	Drug Central	334	10	2	3	2.3	CCCN(C(=O)C(NC(=O)c1ccccc1)CCC(=O)O)CCC	None
		893	9949	82	None	-	0	Rat	8.6	pIC50	=	8.6	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	Drug Central	334	10	2	3	2.3	CCCN(C(=O)C(NC(=O)c1ccccc1)CCC(=O)O)CCC	None
		CHEMBL316561	9949	82	None	-	0	Rat	8.6	pIC50	=	8.6	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	Drug Central	334	10	2	3	2.3	CCCN(C(=O)C(NC(=O)c1ccccc1)CCC(=O)O)CCC	None
		DB13431	9949	82	None	-	0	Rat	8.6	pIC50	=	8.6	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	Drug Central	334	10	2	3	2.3	CCCN(C(=O)C(NC(=O)c1ccccc1)CCC(=O)O)CCC	None
		1231	7724	116	None	-4	8	Human	8.2	pKd	=	8.2	Binding	NoneNone	Drug Central	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	None
		2756	7724	116	None	-4	8	Human	8.2	pKd	=	8.2	Binding	NoneNone	Drug Central	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	None
		645	7724	116	None	-4	8	Human	8.2	pKd	=	8.2	Binding	NoneNone	Drug Central	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	None
		CHEMBL30	7724	116	None	-4	8	Human	8.2	pKd	=	8.2	Binding	NoneNone	Drug Central	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	None
		DB00501	7724	116	None	-4	8	Human	8.2	pKd	=	8.2	Binding	NoneNone	Drug Central	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	None
		1231	7724	116	None	2	8	Guinea pig	8.2	pKd	=	8.2	Binding	In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.	Drug Central	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	None
		2756	7724	116	None	2	8	Guinea pig	8.2	pKd	=	8.2	Binding	In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.	Drug Central	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	None
		645	7724	116	None	2	8	Guinea pig	8.2	pKd	=	8.2	Binding	In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.	Drug Central	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	None
		CHEMBL30	7724	116	None	2	8	Guinea pig	8.2	pKd	=	8.2	Binding	In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.	Drug Central	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	None
		DB00501	7724	116	None	2	8	Guinea pig	8.2	pKd	=	8.2	Binding	In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.	Drug Central	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	None
		1234	10064	68	None	-2	7	Human	8.2	pKd	=	8.2	Binding	NoneNone	Drug Central	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	None
		3001055	10064	68	None	-2	7	Human	8.2	pKd	=	8.2	Binding	NoneNone	Drug Central	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	None
		CHEMBL512	10064	68	None	-2	7	Human	8.2	pKd	=	8.2	Binding	NoneNone	Drug Central	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	None
		DB00863	10064	68	None	-2	7	Human	8.2	pKd	=	8.2	Binding	NoneNone	Drug Central	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	None
		3033637	224498	0	None	-	1	Human	8.2	pKd	=	8.2	Binding	NoneNone	Drug Central	331	10	2	8	1.3	CNC(NCCSCC1=CSC(CN(C)C)=N1)=C[N+]([O-])=O	None
		1129	8402	96	None	1	2	Guinea pig	8.2	pKd	=	8.2	Binding	In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.	Drug Central	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	None
		3325	8402	96	None	1	2	Guinea pig	8.2	pKd	=	8.2	Binding	In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.	Drug Central	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	None
		5353622	8402	96	None	1	2	Guinea pig	8.2	pKd	=	8.2	Binding	In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.	Drug Central	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	None
		5702160	8402	96	None	1	2	Guinea pig	8.2	pKd	=	8.2	Binding	In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.	Drug Central	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	None
		7074	8402	96	None	1	2	Guinea pig	8.2	pKd	=	8.2	Binding	In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.	Drug Central	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	None
		CHEMBL902	8402	96	None	1	2	Guinea pig	8.2	pKd	=	8.2	Binding	In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.	Drug Central	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	None
		DB00927	8402	96	None	1	2	Guinea pig	8.2	pKd	=	8.2	Binding	In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.	Drug Central	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	None
		1234	10064	68	None	1	7	Guinea pig	8.1	pKd	=	8.1	Binding	Compound was evaluated in vitro inhibitory activity against histamine H2 receptor in isolated Guinea pig right atria.Compound was evaluated in vitro inhibitory activity against histamine H2 receptor in isolated Guinea pig right atria.	Drug Central	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	None
		3001055	10064	68	None	1	7	Guinea pig	8.1	pKd	=	8.1	Binding	Compound was evaluated in vitro inhibitory activity against histamine H2 receptor in isolated Guinea pig right atria.Compound was evaluated in vitro inhibitory activity against histamine H2 receptor in isolated Guinea pig right atria.	Drug Central	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	None
		CHEMBL512	10064	68	None	1	7	Guinea pig	8.1	pKd	=	8.1	Binding	Compound was evaluated in vitro inhibitory activity against histamine H2 receptor in isolated Guinea pig right atria.Compound was evaluated in vitro inhibitory activity against histamine H2 receptor in isolated Guinea pig right atria.	Drug Central	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	None
		DB00863	10064	68	None	1	7	Guinea pig	8.1	pKd	=	8.1	Binding	Compound was evaluated in vitro inhibitory activity against histamine H2 receptor in isolated Guinea pig right atria.Compound was evaluated in vitro inhibitory activity against histamine H2 receptor in isolated Guinea pig right atria.	Drug Central	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	None
		5105	183606	52	None	-	1	Human	8.1	pKd	=	8.1	Binding	NoneNone	Drug Central	348	9	1	5	2.1	CC(=O)OCC(=O)NCCCOc1cccc(CN2CCCCC2)c1	None
		CHEMBL46102	183606	52	None	-	1	Human	8.1	pKd	=	8.1	Binding	NoneNone	Drug Central	348	9	1	5	2.1	CC(=O)OCC(=O)NCCCOc1cccc(CN2CCCCC2)c1	None
		1129	8402	96	None	-1	2	Human	8.1	pKd	=	8.1	Binding	NoneNone	Drug Central	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	None
		3325	8402	96	None	-1	2	Human	8.1	pKd	=	8.1	Binding	NoneNone	Drug Central	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	None
		5353622	8402	96	None	-1	2	Human	8.1	pKd	=	8.1	Binding	NoneNone	Drug Central	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	None
		5702160	8402	96	None	-1	2	Human	8.1	pKd	=	8.1	Binding	NoneNone	Drug Central	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	None
		7074	8402	96	None	-1	2	Human	8.1	pKd	=	8.1	Binding	NoneNone	Drug Central	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	None
		CHEMBL902	8402	96	None	-1	2	Human	8.1	pKd	=	8.1	Binding	NoneNone	Drug Central	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	None
		DB00927	8402	96	None	-1	2	Human	8.1	pKd	=	8.1	Binding	NoneNone	Drug Central	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	None
		1235	10595	36	None	-2	5	Human	8.2	pKd	=	8.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	312	6	4	6	-0.1	N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N	12869657
		3959	10595	36	None	-2	5	Human	8.2	pKd	=	8.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	312	6	4	6	-0.1	N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N	12869657
		50287	10595	36	None	-2	5	Human	8.2	pKd	=	8.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	312	6	4	6	-0.1	N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N	12869657
		CHEMBL269646	10595	36	None	-2	5	Human	8.2	pKd	=	8.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	312	6	4	6	-0.1	N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N	12869657
		None	222930	0	3H-Histamine	-6	3	Guinea pig	9.7	pKi	=	9.7	Binding	NoneNone	PDSP KiDatabase	139	3	2	2	0.6	CC(CC1=CN=CN1)NC	None
		None	222931	0	3H-Histamine	-6	3	Guinea pig	9.7	pKi	=	9.7	Binding	NoneNone	PDSP KiDatabase	139	2	2	2	0.9	CC(C1=CN=CN1)C(C)N	None
		565544	116520	11	3H-Histamine	-1	3	Guinea pig	9.1	pKi	=	9.1	Binding	NoneNone	PDSP KiDatabase	125	2	2	2	0.5	CC(CN)c1cnc[nH]1	None
		CHEMBL322988	116520	11	3H-Histamine	-1	3	Guinea pig	9.1	pKi	=	9.1	Binding	NoneNone	PDSP KiDatabase	125	2	2	2	0.5	CC(CN)c1cnc[nH]1	None
		None	222920	0	3H-Histamine	-8	7	Guinea pig	9.0	pKi	=	9	Binding	NoneNone	PDSP KiDatabase	125	2	2	2	0.3	CC(CC1=CN=CN1)N	None
		1204	8713	119	3H-Histamine	-194	25	Guinea pig	7.0	pKi	=	7	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
		1247	8713	119	3H-Histamine	-194	25	Guinea pig	7.0	pKi	=	7	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
		1375	8713	119	3H-Histamine	-194	25	Guinea pig	7.0	pKi	=	7	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
		774	8713	119	3H-Histamine	-194	25	Guinea pig	7.0	pKi	=	7	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
		CHEMBL90	8713	119	3H-Histamine	-194	25	Guinea pig	7.0	pKi	=	7	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
		DB05381	8713	119	3H-Histamine	-194	25	Guinea pig	7.0	pKi	=	7	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
		202	8290	77	UNDEFINED	-9	33	Guinea pig	6.0	pKi	=	6	Binding	NoneNone	PDSP KiDatabase	297	6	1	3	4.6	CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2	None
		60835	8290	77	UNDEFINED	-9	33	Guinea pig	6.0	pKi	=	6	Binding	NoneNone	PDSP KiDatabase	297	6	1	3	4.6	CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2	None
		972	8290	77	UNDEFINED	-9	33	Guinea pig	6.0	pKi	=	6	Binding	NoneNone	PDSP KiDatabase	297	6	1	3	4.6	CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2	None
		CHEMBL1175	8290	77	UNDEFINED	-9	33	Guinea pig	6.0	pKi	=	6	Binding	NoneNone	PDSP KiDatabase	297	6	1	3	4.6	CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2	None
		DB00476	8290	77	UNDEFINED	-9	33	Guinea pig	6.0	pKi	=	6	Binding	NoneNone	PDSP KiDatabase	297	6	1	3	4.6	CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2	None
		46222048	15756	0	UNDEFINED	-4365	13	Human	6.0	pKi	=	6	Binding	NoneNone	PDSP KiDatabase	260	4	1	2	4.0	CC(C)(C)c1ccc(SCCc2c[nH]cn2)cc1	None
		CHEMBL1098230	15756	0	UNDEFINED	-4365	13	Human	6.0	pKi	=	6	Binding	NoneNone	PDSP KiDatabase	260	4	1	2	4.0	CC(C)(C)c1ccc(SCCc2c[nH]cn2)cc1	None
		5656	209845	87	UNDEFINED	-7	43	Guinea pig	6.0	pKi	=	6	Binding	NoneNone	PDSP KiDatabase	277	5	1	3	3.0	COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1	None
		CHEMBL637	209845	87	UNDEFINED	-7	43	Guinea pig	6.0	pKi	=	6	Binding	NoneNone	PDSP KiDatabase	277	5	1	3	3.0	COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1	None
		54841	209906	52	UNDEFINED	-1	30	Guinea pig	6.0	pKi	=	6	Binding	NoneNone	PDSP KiDatabase	255	6	1	2	3.7	CNCC[C@@H](Oc1ccccc1C)c1ccccc1	None
		CHEMBL641	209906	52	UNDEFINED	-1	30	Guinea pig	6.0	pKi	=	6	Binding	NoneNone	PDSP KiDatabase	255	6	1	2	3.7	CNCC[C@@H](Oc1ccccc1C)c1ccccc1	None
		1269	6909	41	3H-TIOTIDINE	-338	4	Guinea pig	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	125	2	2	2	0.2	Cc1c(CCN)nc[nH]1	None
		37463	6909	41	3H-TIOTIDINE	-338	4	Guinea pig	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	125	2	2	2	0.2	Cc1c(CCN)nc[nH]1	None
		CHEMBL275443	6909	41	3H-TIOTIDINE	-338	4	Guinea pig	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	125	2	2	2	0.2	Cc1c(CCN)nc[nH]1	None
		179	7188	115	3H-TIOTIDINE	-4365	50	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	369	7	2	6	1.3	CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC	None
		2159	7188	115	3H-TIOTIDINE	-4365	50	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	369	7	2	6	1.3	CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC	None
		963	7188	115	3H-TIOTIDINE	-4365	50	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	369	7	2	6	1.3	CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC	None
		CHEMBL243712	7188	115	3H-TIOTIDINE	-4365	50	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	369	7	2	6	1.3	CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC	None
		DB06288	7188	115	3H-TIOTIDINE	-4365	50	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	369	7	2	6	1.3	CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC	None
		242	7258	124	3H-TIOTIDINE	-7244	51	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	447	7	1	4	4.9	O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl	None
		34	7258	124	3H-TIOTIDINE	-7244	51	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	447	7	1	4	4.9	O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl	None
		60795	7258	124	3H-TIOTIDINE	-7244	51	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	447	7	1	4	4.9	O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl	None
		CHEMBL1112	7258	124	3H-TIOTIDINE	-7244	51	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	447	7	1	4	4.9	O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl	None
		DB01238	7258	124	3H-TIOTIDINE	-7244	51	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	447	7	1	4	4.9	O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl	None
		1231	7724	116	3H-Histamine	-4	8	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	None
		2756	7724	116	3H-Histamine	-4	8	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	None
		645	7724	116	3H-Histamine	-4	8	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	None
		CHEMBL30	7724	116	3H-Histamine	-4	8	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	None
		DB00501	7724	116	3H-Histamine	-4	8	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	None
		1248	8206	28	3H-TIOTIDINE	-208	7	Guinea pig	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	161	4	2	3	0.6	CN(CCCSC(=N)N)C	None
		3077	8206	28	3H-TIOTIDINE	-208	7	Guinea pig	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	161	4	2	3	0.6	CN(CCCSC(=N)N)C	None
		90045	8206	28	3H-TIOTIDINE	-208	7	Guinea pig	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	161	4	2	3	0.6	CN(CCCSC(=N)N)C	None
		CHEMBL12344	8206	28	3H-TIOTIDINE	-208	7	Guinea pig	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	161	4	2	3	0.6	CN(CCCSC(=N)N)C	None
		1204	8713	119	3H-TIOTIDINE	-194	25	Guinea pig	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
		1204	8713	119	3H-TIOTIDINE	-173	25	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
		1247	8713	119	3H-TIOTIDINE	-194	25	Guinea pig	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
		1247	8713	119	3H-TIOTIDINE	-173	25	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
		1375	8713	119	3H-TIOTIDINE	-194	25	Guinea pig	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
		1375	8713	119	3H-TIOTIDINE	-173	25	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
		774	8713	119	3H-TIOTIDINE	-194	25	Guinea pig	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
		774	8713	119	3H-TIOTIDINE	-173	25	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
		CHEMBL90	8713	119	3H-TIOTIDINE	-194	25	Guinea pig	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
		CHEMBL90	8713	119	3H-TIOTIDINE	-173	25	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
		DB05381	8713	119	3H-TIOTIDINE	-194	25	Guinea pig	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
		DB05381	8713	119	3H-TIOTIDINE	-173	25	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
		134	9292	24	3H-TIOTIDINE	-8511	67	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	353	4	2	4	1.9	CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO	None
		1775	9292	24	3H-TIOTIDINE	-8511	67	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	353	4	2	4	1.9	CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO	None
		9681	9292	24	3H-TIOTIDINE	-8511	67	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	353	4	2	4	1.9	CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO	None
		CHEMBL1065	9292	24	3H-TIOTIDINE	-8511	67	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	353	4	2	4	1.9	CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO	None
		DB00247	9292	24	3H-TIOTIDINE	-8511	67	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	353	4	2	4	1.9	CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO	None
		15897	9637	0	3H-TIOTIDINE	-354	36	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	203	2	1	1	2.6	CC(Cc1cccc(c1)C(F)(F)F)N	None
		215	9637	0	3H-TIOTIDINE	-354	36	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	203	2	1	1	2.6	CC(Cc1cccc(c1)C(F)(F)F)N	None
		CHEMBL1979333	9637	0	3H-TIOTIDINE	-354	36	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	203	2	1	1	2.6	CC(Cc1cccc(c1)C(F)(F)F)N	None
		2337	10030	77	3H-TIOTIDINE	-1122	62	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	383	5	1	6	2.9	OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2	None
		50	10030	77	3H-TIOTIDINE	-1122	62	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	383	5	1	6	2.9	OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2	None
		5002	10030	77	3H-TIOTIDINE	-1122	62	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	383	5	1	6	2.9	OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2	None
		CHEMBL716	10030	77	3H-TIOTIDINE	-1122	62	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	383	5	1	6	2.9	OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2	None
		DB01224	10030	77	3H-TIOTIDINE	-1122	62	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	383	5	1	6	2.9	OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2	None
		1234	10064	68	3H-Histamine	-2	7	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	None
		3001055	10064	68	3H-Histamine	-2	7	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	None
		CHEMBL512	10064	68	3H-Histamine	-2	7	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	None
		DB00863	10064	68	3H-Histamine	-2	7	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	None
		6917970	10463	61	3H-TIOTIDINE	-2290	33	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	327	2	2	5	2.8	COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O	None
		8370	10463	61	3H-TIOTIDINE	-2290	33	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	327	2	2	5	2.8	COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O	None
		CHEMBL487387	10463	61	3H-TIOTIDINE	-2290	33	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	327	2	2	5	2.8	COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O	None
		1267	10576	49	125I-aminopotentidine	-4168	27	Guinea pig	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	292	2	2	2	2.8	S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1	None
		1267	10576	49	3H-TIOTIDINE	-4168	27	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	292	2	2	2	2.8	S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1	None
		3035905	10576	49	125I-aminopotentidine	-4168	27	Guinea pig	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	292	2	2	2	2.8	S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1	None
		3035905	10576	49	3H-TIOTIDINE	-4168	27	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	292	2	2	2	2.8	S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1	None
		CHEMBL260374	10576	49	125I-aminopotentidine	-4168	27	Guinea pig	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	292	2	2	2	2.8	S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1	None
		CHEMBL260374	10576	49	3H-TIOTIDINE	-4168	27	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	292	2	2	2	2.8	S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1	None
		1235	10595	36	3H-Histamine	-2	5	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	312	6	4	6	-0.1	N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N	None
		3959	10595	36	3H-Histamine	-2	5	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	312	6	4	6	-0.1	N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N	None
		50287	10595	36	3H-Histamine	-2	5	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	312	6	4	6	-0.1	N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N	None
		CHEMBL269646	10595	36	3H-Histamine	-2	5	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	312	6	4	6	-0.1	N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N	None
		2662	18156	131	3H-TIOTIDINE	-41	30	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	381	3	1	4	3.5	Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1	None
		CHEMBL118	18156	131	3H-TIOTIDINE	-41	30	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	381	3	1	4	3.5	Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1	None
		5090	22333	106	3H-TIOTIDINE	-1348	30	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	314	3	0	4	2.6	CS(=O)(=O)c1ccc(C2=C(c3ccccc3)C(=O)OC2)cc1	None
		CHEMBL122	22333	106	3H-TIOTIDINE	-1348	30	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	314	3	0	4	2.6	CS(=O)(=O)c1ccc(C2=C(c3ccccc3)C(=O)OC2)cc1	None
		10297	33885	30	3H-TIOTIDINE	-38	43	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	151	2	2	2	1.1	C[C@H](N)[C@H](O)c1ccccc1	None
		CHEMBL136560	33885	30	3H-TIOTIDINE	-38	43	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	151	2	2	2	1.1	C[C@H](N)[C@H](O)c1ccccc1	None
		156391	53574	99	3H-TIOTIDINE	-1	29	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	230	3	1	2	3.0	COc1ccc2cc([C@H](C)C(=O)O)ccc2c1	None
		CHEMBL1200806	53574	99	3H-TIOTIDINE	-1	29	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	230	3	1	2	3.0	COc1ccc2cc([C@H](C)C(=O)O)ccc2c1	None
		CHEMBL154	53574	99	3H-TIOTIDINE	-1	29	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	230	3	1	2	3.0	COc1ccc2cc([C@H](C)C(=O)O)ccc2c1	None
		10624	77075	19	3H-TIOTIDINE	-776	32	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	284	5	3	3	1.7	CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12	None
		138543650	77075	19	3H-TIOTIDINE	-776	32	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	284	5	3	3	1.7	CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12	None
		CHEMBL194378	77075	19	3H-TIOTIDINE	-776	32	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	284	5	3	3	1.7	CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12	None
		2244	101008	100	3H-TIOTIDINE	-1	27	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	180	2	1	3	1.3	CC(=O)Oc1ccccc1C(=O)O	None
		CHEMBL25	101008	100	3H-TIOTIDINE	-1	27	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	180	2	1	3	1.3	CC(=O)Oc1ccccc1C(=O)O	None
		446220	140299	14	3H-TIOTIDINE	-1778	45	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	303	3	0	5	1.9	COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C	None
		CHEMBL370805	140299	14	3H-TIOTIDINE	-1778	45	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	303	3	0	5	1.9	COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C	None
		44208932	147485	7	UNDEFINED	-89125	37	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	475	5	1	3	6.8	Cc1ccc(Cn2nc(C(=O)NC3C4(C)CCC(C4)C3(C)C)cc2-c2ccc(Cl)c(C)c2)cc1	None
		CHEMBL381689	147485	7	UNDEFINED	-89125	37	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	475	5	1	3	6.8	Cc1ccc(Cn2nc(C(=O)NC3C4(C)CCC(C4)C3(C)C)cc2-c2ccc(Cl)c(C)c2)cc1	None
		1615	174570	24	3H-PYRILAMINE	-26	44	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	193	3	1	3	1.6	CNC(C)Cc1ccc2c(c1)OCO2	None
		1615	174570	24	3H-TIOTIDINE	-26	44	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	193	3	1	3	1.6	CNC(C)Cc1ccc2c(c1)OCO2	None
		CHEMBL43048	174570	24	3H-PYRILAMINE	-26	44	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	193	3	1	3	1.6	CNC(C)Cc1ccc2c(c1)OCO2	None
		CHEMBL43048	174570	24	3H-TIOTIDINE	-26	44	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	193	3	1	3	1.6	CNC(C)Cc1ccc2c(c1)OCO2	None
		12016890	197555	6	3H-TIOTIDINE	-16982	12	Guinea pig	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	318	4	1	3	2.6	NC(=O)c1ccc(F)c2c1CC(N(C1CCC1)C1CCC1)CO2	None
		CHEMBL5183389	197555	6	3H-TIOTIDINE	-16982	12	Guinea pig	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	318	4	1	3	2.6	NC(=O)c1ccc(F)c2c1CC(N(C1CCC1)C1CCC1)CO2	None
		3672	199312	136	3H-TIOTIDINE	-1	27	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	206	4	1	1	3.1	CC(C)Cc1ccc(C(C)C(=O)O)cc1	None
		CHEMBL521	199312	136	3H-TIOTIDINE	-1	27	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	206	4	1	1	3.1	CC(C)Cc1ccc(C(C)C(=O)O)cc1	None
		54676228	200394	112	3H-TIOTIDINE	-1	27	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	331	2	2	5	1.6	CN1C(C(=O)Nc2ccccn2)=C(O)c2ccccc2S1(=O)=O	None
		CHEMBL527	200394	112	3H-TIOTIDINE	-1	27	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	331	2	2	5	1.6	CN1C(C(=O)Nc2ccccn2)=C(O)c2ccccc2S1(=O)=O	None
		4495	203314	92	3H-TIOTIDINE	-1	29	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	308	5	1	5	2.8	CS(=O)(=O)Nc1ccc([N+](=O)[O-])cc1Oc1ccccc1	None
		CHEMBL56367	203314	92	3H-TIOTIDINE	-1	29	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	308	5	1	5	2.8	CS(=O)(=O)Nc1ccc([N+](=O)[O-])cc1Oc1ccccc1	None
		54677470	207330	115	3H-TIOTIDINE	-1	29	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	351	2	2	6	2.0	Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1	None
		CHEMBL1256873	207330	115	3H-TIOTIDINE	-1	29	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	351	2	2	6	2.0	Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1	None
		CHEMBL599	207330	115	3H-TIOTIDINE	-1	29	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	351	2	2	6	2.0	Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1	None
		162265	209053	22	3H-TIOTIDINE	-239	44	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	151	2	2	2	1.1	CC(N)C(O)c1ccccc1	None
		4786	209053	22	3H-TIOTIDINE	-239	44	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	151	2	2	2	1.1	CC(N)C(O)c1ccccc1	None
		CHEMBL61006	209053	22	3H-TIOTIDINE	-239	44	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	151	2	2	2	1.1	CC(N)C(O)c1ccccc1	None
		1973	210262	15	3H-APT	-3	36	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	462	3	1	7	3.9	Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12	None
		CHEMBL1394464	210262	15	3H-APT	-3	36	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	462	3	1	7	3.9	Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12	None
		CHEMBL66089	210262	15	3H-APT	-3	36	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	462	3	1	7	3.9	Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12	None
		3821	211497	17	3H-TIOTIDINE	-1	18	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	237	2	1	2	2.9	CNC1(c2ccccc2Cl)CCCCC1=O	None
		CHEMBL742	211497	17	3H-TIOTIDINE	-1	18	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	237	2	1	2	2.9	CNC1(c2ccccc2Cl)CCCCC1=O	None
		4054	212280	72	3H-TIOTIDINE	-1	36	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	179	0	1	1	2.7	CC12CC3CC(C)(C1)CC(N)(C3)C2	None
		CHEMBL1699	212280	72	3H-TIOTIDINE	-1	36	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	179	0	1	1	2.7	CC12CC3CC(C)(C1)CC(N)(C3)C2	None
		CHEMBL807	212280	72	3H-TIOTIDINE	-1	36	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	179	0	1	1	2.7	CC12CC3CC(C)(C1)CC(N)(C3)C2	None
		119607	212982	113	3H-TIOTIDINE	-97	27	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	314	3	1	4	3.0	Cc1onc(-c2ccccc2)c1-c1ccc(S(N)(=O)=O)cc1	None
		CHEMBL865	212982	113	3H-TIOTIDINE	-97	27	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	314	3	1	4	3.0	Cc1onc(-c2ccccc2)c1-c1ccc(S(N)(=O)=O)cc1	None
		3337	213146	27	3H-TIOTIDINE	-1513	40	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	231	4	1	1	3.2	CCNC(C)Cc1cccc(C(F)(F)F)c1	None
		65801	213146	27	3H-TIOTIDINE	-1513	40	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	231	4	1	1	3.2	CCNC(C)Cc1cccc(C(F)(F)F)c1	None
		66264	213146	27	3H-TIOTIDINE	-1513	40	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	231	4	1	1	3.2	CCNC(C)Cc1cccc(C(F)(F)F)c1	None
		91452	213146	27	3H-TIOTIDINE	-1513	40	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	231	4	1	1	3.2	CCNC(C)Cc1cccc(C(F)(F)F)c1	None
		CHEMBL87493	213146	27	3H-TIOTIDINE	-1513	40	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	231	4	1	1	3.2	CCNC(C)Cc1cccc(C(F)(F)F)c1	None
		11954224	222732	0	3H-TIOTIDINE	-141253	59	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	581	4	3	6	2.0	CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C	None
		None	222772	0	I125- Tiotodine	-1	27	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	329	2	0	4	3.6	CC1=NC=CN1CC2CCC3=C(C2=O)C4=CC=CC=C4N3C.Cl	None
		104911	222798	0	3H-TIOTIDINE	-41686	37	Guinea pig	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	530	7	0	5	5.1	COC1=CC=CC=C1N2CCN(CC2)CCN(C3=CC=CC=N3)C(=O)C4CCCCC4.Cl.Cl.Cl	None
		104911	222798	0	3H-TIOTIDINE	-41686	37	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	530	7	0	5	5.1	COC1=CC=CC=C1N2CCN(CC2)CCN(C3=CC=CC=N3)C(=O)C4CCCCC4.Cl.Cl.Cl	None
		25137849	222958	0	3H-TIOTIDINE	-4	40	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	165	3	2	2	1.3	CC(C(C1=CC=CC=C1)O)NC	None
		71290	222958	0	3H-TIOTIDINE	-4	40	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	165	3	2	2	1.3	CC(C(C1=CC=CC=C1)O)NC	None
		None	223090	0	3H-TIOTIDINE	-1	34	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	240	7	4	6	-0.8	C(C(C(=O)O)N)SSCC(C(=O)O)N	None
		None	223091	0	3H-TIOTIDINE	-1	34	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	149	4	2	3	0.2	CSCCC(C(=O)O)N	None
		None	223092	0	3H-TIOTIDINE	-1	34	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	135	3	3	3	-0.3	C(CS)C(C(=O)O)N	None
		None	223093	0	3H-TIOTIDINE	-1	34	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	121	2	3	3	-0.7	C(C(C(=O)O)N)S	None
		None	223094	0	3H-TIOTIDINE	-1	29	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	117	0	1	3	-0.0	C1CSC(=O)C1N	None
		None	223095	0	3H-TIOTIDINE	-1	40	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	153	3	3	3	-1.4	C(C(C(=O)O)N)S(=O)O	None
		None	223096	0	3H-TIOTIDINE	-1	39	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	169	3	3	4	-1.7	C(C(C(=O)O)N)S(=O)(=O)O	None
		None	223104	0	3H-TIOTIDINE	-13	40	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	149	2	1	2	1.2	CC(C(=O)C1=CC=CC=C1)N	None
		1576	223105	0	3H-TIOTIDINE	-16	40	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	163	3	1	2	1.5	CC(C(=O)C1=CC=CC=C1)NC	None
		135269	223168	0	3H-TIOTIDINE	-1	29	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	222	5	1	3	2.5	CCCCC(=O)OC1=CC=CC=C1C(=O)O	None
		23681059	223169	0	3H-TIOTIDINE	-1	28	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	230	3	1	2	3.0	CC(C1=CC2=C(C=C1)C=C(C=C2)OC)C(=O)O	None
		5018304	223170	0	3H-TIOTIDINE	-1	28	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	317	4	1	3	0.0	C1=CC=C(C(=C1)CC(=O)[O-])NC2=C(C=CC=C2Cl)Cl.[Na+]	None
		84003	223171	0	3H-TIOTIDINE	-1	27	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	376	6	5	7	-0.0	C1CN2C(=CC=C2C(=O)C3=CC=CC=C3)C1C(=O)O.C(C(CO)(CO)N)O	None
		123619	223172	0	3H-TIOTIDINE	-1412	27	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	358	3	0	4	4.2	CC1=NC=C(C=C1)C2=NC=C(C=C2C3=CC=C(C=C3)S(=O)(=O)C)Cl	None
		119828	223173	0	3H-TIOTIDINE	-1	29	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	370	5	1	5	3.5	CCC(=O)NS(=O)(=O)C1=CC=C(C=C1)C2=C(ON=C2C3=CC=CC=C3)C	None
		None	223174	0	3H-TIOTIDINE	-7	28	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	517	8	2	5	5.2	CC1=C(C2=C(N1C(=O)C3=CC=C(C=C3)Cl)C=CC(=C2)OC)CC(=O)NCCC4=CC=C(C=C4)NC(=O)C	None
		None	223229	0	Functional	-660	28	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	322	5	2	3	4.1	CC(CC1=CNC2=C1C=C(C=C2)OCC3=CC=CS3)N.Cl	None
		None	223229	0	UNDEFINED	-660	28	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	322	5	2	3	4.1	CC(CC1=CNC2=C1C=C(C=C2)OCC3=CC=CS3)N.Cl	None
		None	223268	0	3H-TIOTIDINE	-4570	26	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	347	6	0	3	5.0	CC(=O)N(CC1=CC=CC=C1OC)C2=CC=CC=C2OC3=CC=CC=C3	None
		None	223272	0	125I-aminopotentidine	-10471285	17	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	372	2	1	3	4.4	CC(C)(C)C1=CC=C(C=C1)NC(=O)N2CCN(CC2)C3=C(C=CC=N3)Cl	None
		None	223273	0	125I-aminopotentidine	-1	13	Guinea pig	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	399	7	4	5	1.8	CN(C)CC(C1=CC=C(C=C1)O)C2(CCCCC2)O.C(CC(=O)O)C(=O)O.O	None
		None	223858	0	UNDEFINED	-3467	5	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	463	4	1	4	3.7	C1C(C(=NN1C(=NS(=O)(=O)C2=CC=C(C=C2)C#N)N)C3=CC=C(C=C3)Cl)C4=CC=CC=C4	None
		1353	8692	93	3H-TIOTIDINE	-131	85	Human	6.0	pKi	=	6	Binding	NoneNone	PDSP KiDatabase	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	None
		3559	8692	93	3H-TIOTIDINE	-131	85	Human	6.0	pKi	=	6	Binding	NoneNone	PDSP KiDatabase	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	None
		86	8692	93	3H-TIOTIDINE	-131	85	Human	6.0	pKi	=	6	Binding	NoneNone	PDSP KiDatabase	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	None
		CHEMBL54	8692	93	3H-TIOTIDINE	-131	85	Human	6.0	pKi	=	6	Binding	NoneNone	PDSP KiDatabase	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	None
		DB00502	8692	93	3H-TIOTIDINE	-131	85	Human	6.0	pKi	=	6	Binding	NoneNone	PDSP KiDatabase	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	None
		1129	8402	96	3H-TIOTIDINE	1	2	Guinea pig	7.9	pKi	=	7.9	Binding	NoneNone	PDSP KiDatabase	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	None
		3325	8402	96	3H-TIOTIDINE	1	2	Guinea pig	7.9	pKi	=	7.9	Binding	NoneNone	PDSP KiDatabase	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	None
		5353622	8402	96	3H-TIOTIDINE	1	2	Guinea pig	7.9	pKi	=	7.9	Binding	NoneNone	PDSP KiDatabase	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	None
		5702160	8402	96	3H-TIOTIDINE	1	2	Guinea pig	7.9	pKi	=	7.9	Binding	NoneNone	PDSP KiDatabase	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	None
		7074	8402	96	3H-TIOTIDINE	1	2	Guinea pig	7.9	pKi	=	7.9	Binding	NoneNone	PDSP KiDatabase	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	None
		CHEMBL902	8402	96	3H-TIOTIDINE	1	2	Guinea pig	7.9	pKi	=	7.9	Binding	NoneNone	PDSP KiDatabase	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	None
		DB00927	8402	96	3H-TIOTIDINE	1	2	Guinea pig	7.9	pKi	=	7.9	Binding	NoneNone	PDSP KiDatabase	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	None
		2389	10104	118	3H-TIOTIDINE	-288	66	Human	6.9	pKi	=	6.9	Binding	NoneNone	PDSP KiDatabase	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	None
		5073	10104	118	3H-TIOTIDINE	-288	66	Human	6.9	pKi	=	6.9	Binding	NoneNone	PDSP KiDatabase	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	None
		96	10104	118	3H-TIOTIDINE	-288	66	Human	6.9	pKi	=	6.9	Binding	NoneNone	PDSP KiDatabase	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	None
		CHEMBL85	10104	118	3H-TIOTIDINE	-288	66	Human	6.9	pKi	=	6.9	Binding	NoneNone	PDSP KiDatabase	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	None
		DB00734	10104	118	3H-TIOTIDINE	-288	66	Human	6.9	pKi	=	6.9	Binding	NoneNone	PDSP KiDatabase	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	None
		115237	62359	119	3H-TIOTIDINE	-123	54	Human	6.9	pKi	=	6.9	Binding	NoneNone	PDSP KiDatabase	426	4	1	7	3.1	Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O	None
		CHEMBL1621	62359	119	3H-TIOTIDINE	-123	54	Human	6.9	pKi	=	6.9	Binding	NoneNone	PDSP KiDatabase	426	4	1	7	3.1	Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O	None
		100	10577	58	3H-TIOTIDINE	-46	54	Human	6.9	pKi	=	6.9	Binding	NoneNone	PDSP KiDatabase	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	None
		2637	10577	58	3H-TIOTIDINE	-46	54	Human	6.9	pKi	=	6.9	Binding	NoneNone	PDSP KiDatabase	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	None
		5452	10577	58	3H-TIOTIDINE	-46	54	Human	6.9	pKi	=	6.9	Binding	NoneNone	PDSP KiDatabase	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	None
		CHEMBL479	10577	58	3H-TIOTIDINE	-46	54	Human	6.9	pKi	=	6.9	Binding	NoneNone	PDSP KiDatabase	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	None
		DB00679	10577	58	3H-TIOTIDINE	-46	54	Human	6.9	pKi	=	6.9	Binding	NoneNone	PDSP KiDatabase	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	None
		1204	8713	119	3H-Histamine	-173	25	Human	7.8	pKi	=	7.8	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
		1247	8713	119	3H-Histamine	-173	25	Human	7.8	pKi	=	7.8	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
		1375	8713	119	3H-Histamine	-173	25	Human	7.8	pKi	=	7.8	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
		774	8713	119	3H-Histamine	-173	25	Human	7.8	pKi	=	7.8	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
		CHEMBL90	8713	119	3H-Histamine	-173	25	Human	7.8	pKi	=	7.8	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
		DB05381	8713	119	3H-Histamine	-173	25	Human	7.8	pKi	=	7.8	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
		1235	10595	36	125I-iodoaminopotentidine	-2	5	Human	7.8	pKi	=	7.8	Binding	NoneNone	PDSP KiDatabase	312	6	4	6	-0.1	N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N	None
		3959	10595	36	125I-iodoaminopotentidine	-2	5	Human	7.8	pKi	=	7.8	Binding	NoneNone	PDSP KiDatabase	312	6	4	6	-0.1	N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N	None
		50287	10595	36	125I-iodoaminopotentidine	-2	5	Human	7.8	pKi	=	7.8	Binding	NoneNone	PDSP KiDatabase	312	6	4	6	-0.1	N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N	None
		CHEMBL269646	10595	36	125I-iodoaminopotentidine	-2	5	Human	7.8	pKi	=	7.8	Binding	NoneNone	PDSP KiDatabase	312	6	4	6	-0.1	N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N	None
		135398737	7745	93	3H-TIOTIDINE	-64	90	Human	6.8	pKi	=	6.8	Binding	NoneNone	PDSP KiDatabase	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	None
		38	7745	93	3H-TIOTIDINE	-64	90	Human	6.8	pKi	=	6.8	Binding	NoneNone	PDSP KiDatabase	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	None
		722	7745	93	3H-TIOTIDINE	-64	90	Human	6.8	pKi	=	6.8	Binding	NoneNone	PDSP KiDatabase	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	None
		CHEMBL42	7745	93	3H-TIOTIDINE	-64	90	Human	6.8	pKi	=	6.8	Binding	NoneNone	PDSP KiDatabase	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	None
		DB00363	7745	93	3H-TIOTIDINE	-64	90	Human	6.8	pKi	=	6.8	Binding	NoneNone	PDSP KiDatabase	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	None
		1204	8713	119	3H-TIOTIDINE	-316	25	Rat	7.8	pKi	=	7.8	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
		1247	8713	119	3H-TIOTIDINE	-316	25	Rat	7.8	pKi	=	7.8	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
		1375	8713	119	3H-TIOTIDINE	-316	25	Rat	7.8	pKi	=	7.8	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
		774	8713	119	3H-TIOTIDINE	-316	25	Rat	7.8	pKi	=	7.8	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
		CHEMBL90	8713	119	3H-TIOTIDINE	-316	25	Rat	7.8	pKi	=	7.8	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
		DB05381	8713	119	3H-TIOTIDINE	-316	25	Rat	7.8	pKi	=	7.8	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
		2726	7706	68	3H-TIOTIDINE	-85	72	Human	6.8	pKi	=	6.8	Binding	NoneNone	PDSP KiDatabase	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	None
		621	7706	68	3H-TIOTIDINE	-85	72	Human	6.8	pKi	=	6.8	Binding	NoneNone	PDSP KiDatabase	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	None
		83	7706	68	3H-TIOTIDINE	-85	72	Human	6.8	pKi	=	6.8	Binding	NoneNone	PDSP KiDatabase	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	None
		CHEMBL71	7706	68	3H-TIOTIDINE	-85	72	Human	6.8	pKi	=	6.8	Binding	NoneNone	PDSP KiDatabase	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	None
		DB00477	7706	68	3H-TIOTIDINE	-85	72	Human	6.8	pKi	=	6.8	Binding	NoneNone	PDSP KiDatabase	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	None
		46780481	114308	20	3H-TIOTIDINE	-21	53	Human	8.6	pKi	=	8.6	Binding	NoneNone	PDSP KiDatabase	285	0	0	2	4.3	CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1	None
		9903970	114308	20	3H-TIOTIDINE	-21	53	Human	8.6	pKi	=	8.6	Binding	NoneNone	PDSP KiDatabase	285	0	0	2	4.3	CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1	None
		CHEMBL3187365	114308	20	3H-TIOTIDINE	-21	53	Human	8.6	pKi	=	8.6	Binding	NoneNone	PDSP KiDatabase	285	0	0	2	4.3	CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1	None
		CHEMBL3544974	114308	20	3H-TIOTIDINE	-21	53	Human	8.6	pKi	=	8.6	Binding	NoneNone	PDSP KiDatabase	285	0	0	2	4.3	CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1	None
		1613	9127	53	3H-TIOTIDINE	-10	44	Human	6.7	pKi	=	6.7	Binding	NoneNone	PDSP KiDatabase	327	0	0	4	3.8	CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2	None
		205	9127	53	3H-TIOTIDINE	-10	44	Human	6.7	pKi	=	6.7	Binding	NoneNone	PDSP KiDatabase	327	0	0	4	3.8	CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2	None
		3964	9127	53	3H-TIOTIDINE	-10	44	Human	6.7	pKi	=	6.7	Binding	NoneNone	PDSP KiDatabase	327	0	0	4	3.8	CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2	None
		CHEMBL831	9127	53	3H-TIOTIDINE	-10	44	Human	6.7	pKi	=	6.7	Binding	NoneNone	PDSP KiDatabase	327	0	0	4	3.8	CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2	None
		DB00408	9127	53	3H-TIOTIDINE	-10	44	Human	6.7	pKi	=	6.7	Binding	NoneNone	PDSP KiDatabase	327	0	0	4	3.8	CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2	None
		21830793	98610	10	3H-8-OH-DPAT	-14125	46	Bovine	5.7	pKi	=	5.7	Binding	NoneNone	PDSP KiDatabase	373	7	0	8	0.6	COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1	None
		CHEMBL2413154	98610	10	3H-8-OH-DPAT	-14125	46	Bovine	5.7	pKi	=	5.7	Binding	NoneNone	PDSP KiDatabase	373	7	0	8	0.6	COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1	None
		None	223033	0	125I-aminopotentidine	-1905	20	Guinea pig	5.6	pKi	=	5.6	Binding	NoneNone	PDSP KiDatabase	416	9	3	4	2.8	C1=CC(=CC=C1CCNC(N)SCCCC2=CN=CN2)I	None
		1226	8800	20	3H-Histamine	-7	7	Human	7.6	pKi	=	7.6	Binding	NoneNone	PDSP KiDatabase	321	9	4	4	1.2	NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C	None
		41376	8800	20	3H-Histamine	-7	7	Human	7.6	pKi	=	7.6	Binding	NoneNone	PDSP KiDatabase	321	9	4	4	1.2	NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C	None
		CHEMBL12608	8800	20	3H-Histamine	-7	7	Human	7.6	pKi	=	7.6	Binding	NoneNone	PDSP KiDatabase	321	9	4	4	1.2	NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C	None
		1248	8206	28	125I-iodoaminopotentidine	-123	7	Human	4.6	pKi	=	4.6	Binding	NoneNone	PDSP KiDatabase	161	4	2	3	0.6	CN(CCCSC(=N)N)C	None
		3077	8206	28	125I-iodoaminopotentidine	-123	7	Human	4.6	pKi	=	4.6	Binding	NoneNone	PDSP KiDatabase	161	4	2	3	0.6	CN(CCCSC(=N)N)C	None
		90045	8206	28	125I-iodoaminopotentidine	-123	7	Human	4.6	pKi	=	4.6	Binding	NoneNone	PDSP KiDatabase	161	4	2	3	0.6	CN(CCCSC(=N)N)C	None
		CHEMBL12344	8206	28	125I-iodoaminopotentidine	-123	7	Human	4.6	pKi	=	4.6	Binding	NoneNone	PDSP KiDatabase	161	4	2	3	0.6	CN(CCCSC(=N)N)C	None
		119570	9933	96	3H-TIOTIDINE	-169	39	Human	5.6	pKi	=	5.6	Binding	NoneNone	PDSP KiDatabase	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	None
		2233	9933	96	3H-TIOTIDINE	-169	39	Human	5.6	pKi	=	5.6	Binding	NoneNone	PDSP KiDatabase	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	None
		953	9933	96	3H-TIOTIDINE	-169	39	Human	5.6	pKi	=	5.6	Binding	NoneNone	PDSP KiDatabase	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	None
		CHEMBL301265	9933	96	3H-TIOTIDINE	-169	39	Human	5.6	pKi	=	5.6	Binding	NoneNone	PDSP KiDatabase	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	None
		DB00413	9933	96	3H-TIOTIDINE	-169	39	Human	5.6	pKi	=	5.6	Binding	NoneNone	PDSP KiDatabase	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	None
		3032915	22267	24	3H-TIOTIDINE	-51	7	Guinea pig	5.5	pKi	=	5.5	Binding	NoneNone	PDSP KiDatabase	212	5	3	2	1.2	C/N=C(\S)NCCCCc1c[nH]cn1	None
		CHEMBL12160	22267	24	3H-TIOTIDINE	-51	7	Guinea pig	5.5	pKi	=	5.5	Binding	NoneNone	PDSP KiDatabase	212	5	3	2	1.2	C/N=C(\S)NCCCCc1c[nH]cn1	None
		1248	8206	28	3H-Histamine	-123	7	Human	6.5	pKi	=	6.5	Binding	NoneNone	PDSP KiDatabase	161	4	2	3	0.6	CN(CCCSC(=N)N)C	None
		3077	8206	28	3H-Histamine	-123	7	Human	6.5	pKi	=	6.5	Binding	NoneNone	PDSP KiDatabase	161	4	2	3	0.6	CN(CCCSC(=N)N)C	None
		90045	8206	28	3H-Histamine	-123	7	Human	6.5	pKi	=	6.5	Binding	NoneNone	PDSP KiDatabase	161	4	2	3	0.6	CN(CCCSC(=N)N)C	None
		CHEMBL12344	8206	28	3H-Histamine	-123	7	Human	6.5	pKi	=	6.5	Binding	NoneNone	PDSP KiDatabase	161	4	2	3	0.6	CN(CCCSC(=N)N)C	None
		213	10625	55	3H-TIOTIDINE	-12	43	Human	5.5	pKi	=	5.5	Binding	NoneNone	PDSP KiDatabase	371	5	0	6	2.4	Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2	None
		2717	10625	55	3H-TIOTIDINE	-12	43	Human	5.5	pKi	=	5.5	Binding	NoneNone	PDSP KiDatabase	371	5	0	6	2.4	Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2	None
		5533	10625	55	3H-TIOTIDINE	-12	43	Human	5.5	pKi	=	5.5	Binding	NoneNone	PDSP KiDatabase	371	5	0	6	2.4	Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2	None
		CHEMBL621	10625	55	3H-TIOTIDINE	-12	43	Human	5.5	pKi	=	5.5	Binding	NoneNone	PDSP KiDatabase	371	5	0	6	2.4	Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2	None
		DB00656	10625	55	3H-TIOTIDINE	-12	43	Human	5.5	pKi	=	5.5	Binding	NoneNone	PDSP KiDatabase	371	5	0	6	2.4	Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2	None
		1235	10595	36	3H-TIOTIDINE	-1	5	Guinea pig	7.5	pKi	=	7.5	Binding	NoneNone	PDSP KiDatabase	312	6	4	6	-0.1	N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N	None
		3959	10595	36	3H-TIOTIDINE	-1	5	Guinea pig	7.5	pKi	=	7.5	Binding	NoneNone	PDSP KiDatabase	312	6	4	6	-0.1	N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N	None
		50287	10595	36	3H-TIOTIDINE	-1	5	Guinea pig	7.5	pKi	=	7.5	Binding	NoneNone	PDSP KiDatabase	312	6	4	6	-0.1	N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N	None
		CHEMBL269646	10595	36	3H-TIOTIDINE	-1	5	Guinea pig	7.5	pKi	=	7.5	Binding	NoneNone	PDSP KiDatabase	312	6	4	6	-0.1	N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N	None
		135409468	8816	69	3H-TIOTIDINE	-123	39	Human	6.5	pKi	=	6.5	Binding	NoneNone	PDSP KiDatabase	312	1	2	4	1.7	Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1	None
		333	8816	69	3H-TIOTIDINE	-123	39	Human	6.5	pKi	=	6.5	Binding	NoneNone	PDSP KiDatabase	312	1	2	4	1.7	Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1	None
		CHEMBL845	8816	69	3H-TIOTIDINE	-123	39	Human	6.5	pKi	=	6.5	Binding	NoneNone	PDSP KiDatabase	312	1	2	4	1.7	Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1	None
		2865	10915	73	3H-TIOTIDINE	-281	53	Human	5.5	pKi	=	5.5	Binding	NoneNone	PDSP KiDatabase	412	4	1	5	3.8	O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2	None
		59	10915	73	3H-TIOTIDINE	-281	53	Human	5.5	pKi	=	5.5	Binding	NoneNone	PDSP KiDatabase	412	4	1	5	3.8	O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2	None
		60854	10915	73	3H-TIOTIDINE	-281	53	Human	5.5	pKi	=	5.5	Binding	NoneNone	PDSP KiDatabase	412	4	1	5	3.8	O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2	None
		CHEMBL708	10915	73	3H-TIOTIDINE	-281	53	Human	5.5	pKi	=	5.5	Binding	NoneNone	PDSP KiDatabase	412	4	1	5	3.8	O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2	None
		DB00246	10915	73	3H-TIOTIDINE	-281	53	Human	5.5	pKi	=	5.5	Binding	NoneNone	PDSP KiDatabase	412	4	1	5	3.8	O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2	None
		62865	8057	0	3H-Cimetidine	-128	15	Guinea pig	6.5	pKi	=	6.5	Binding	NoneNone	PDSP KiDatabase	323	4	0	4	4.4	N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1	None
		746	8057	0	3H-Cimetidine	-128	15	Guinea pig	6.5	pKi	=	6.5	Binding	NoneNone	PDSP KiDatabase	323	4	0	4	4.4	N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1	None
		84	8057	0	3H-Cimetidine	-128	15	Guinea pig	6.5	pKi	=	6.5	Binding	NoneNone	PDSP KiDatabase	323	4	0	4	4.4	N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1	None
		CHEMBL2104153	8057	0	3H-Cimetidine	-128	15	Guinea pig	6.5	pKi	=	6.5	Binding	NoneNone	PDSP KiDatabase	323	4	0	4	4.4	N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1	None
		DB09000	8057	0	3H-Cimetidine	-128	15	Guinea pig	6.5	pKi	=	6.5	Binding	NoneNone	PDSP KiDatabase	323	4	0	4	4.4	N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1	None
		3032915	22267	24	3H-Histamine	-25	7	Human	7.4	pKi	=	7.4	Binding	NoneNone	PDSP KiDatabase	212	5	3	2	1.2	C/N=C(\S)NCCCCc1c[nH]cn1	None
		CHEMBL12160	22267	24	3H-Histamine	-25	7	Human	7.4	pKi	=	7.4	Binding	NoneNone	PDSP KiDatabase	212	5	3	2	1.2	C/N=C(\S)NCCCCc1c[nH]cn1	None
		1234	10064	68	3H-TIOTIDINE	1	7	Guinea pig	6.4	pKi	=	6.4	Binding	NoneNone	PDSP KiDatabase	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	None
		3001055	10064	68	3H-TIOTIDINE	1	7	Guinea pig	6.4	pKi	=	6.4	Binding	NoneNone	PDSP KiDatabase	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	None
		CHEMBL512	10064	68	3H-TIOTIDINE	1	7	Guinea pig	6.4	pKi	=	6.4	Binding	NoneNone	PDSP KiDatabase	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	None
		DB00863	10064	68	3H-TIOTIDINE	1	7	Guinea pig	6.4	pKi	=	6.4	Binding	NoneNone	PDSP KiDatabase	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	None
		3032915	22267	24	125I-iodoaminopotentidine	-25	7	Human	5.4	pKi	=	5.4	Binding	NoneNone	PDSP KiDatabase	212	5	3	2	1.2	C/N=C(\S)NCCCCc1c[nH]cn1	None
		CHEMBL12160	22267	24	125I-iodoaminopotentidine	-25	7	Human	5.4	pKi	=	5.4	Binding	NoneNone	PDSP KiDatabase	212	5	3	2	1.2	C/N=C(\S)NCCCCc1c[nH]cn1	None
		1204	8713	119	None	-173	25	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	Drug Central	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
		1247	8713	119	None	-173	25	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	Drug Central	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
		1375	8713	119	None	-173	25	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	Drug Central	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
		774	8713	119	None	-173	25	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	Drug Central	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
		CHEMBL90	8713	119	None	-173	25	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	Drug Central	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
		DB05381	8713	119	None	-173	25	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	Drug Central	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
		18609376	211138	63	None	-	1	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	386	2	0	4	4.7	CC(=O)O[C@]1(C(C)=O)CC[C@H]2[C@@H]3C[C@H](C)C4=CC(=O)CC[C@]4(C)[C@H]3CC[C@@]21C	None
		6279	211138	63	None	-	1	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	386	2	0	4	4.7	CC(=O)O[C@]1(C(C)=O)CC[C@H]2[C@@H]3C[C@H](C)C4=CC(=O)CC[C@]4(C)[C@H]3CC[C@@]21C	None
		CHEMBL717	211138	63	None	-	1	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	386	2	0	4	4.7	CC(=O)O[C@]1(C(C)=O)CC[C@H]2[C@@H]3C[C@H](C)C4=CC(=O)CC[C@]4(C)[C@H]3CC[C@@]21C	None
		3823	56995	42	None	-66	11	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	530	7	0	7	4.2	CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1	None
		76973198	56995	42	None	-66	11	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	530	7	0	7	4.2	CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1	None
		CHEMBL157101	56995	42	None	-66	11	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	530	7	0	7	4.2	CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1	None
		104903	63118	17	None	-5	6	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	624	6	0	8	5.5	C[C@@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)C3=CC[C@]2(C)[C@H]1C(=O)CN1CCN(c2cc(N3CCCC3)nc(N3CCCC3)n2)CC1	None
		CHEMBL1630578	63118	17	None	-5	6	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	624	6	0	8	5.5	C[C@@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)C3=CC[C@]2(C)[C@H]1C(=O)CN1CCN(c2cc(N3CCCC3)nc(N3CCCC3)n2)CC1	None
		5048	9907	64	None	-114	7	Human	8.3	pKi	=	8.3	Binding	NoneNone	Drug Central	295	8	0	2	4.2	Clc1ccc(cc1)CCCOCCCN1CCCCC1	None
		8924	9907	64	None	-114	7	Human	8.3	pKi	=	8.3	Binding	NoneNone	Drug Central	295	8	0	2	4.2	Clc1ccc(cc1)CCCOCCCN1CCCCC1	None
		9948102	9907	64	None	-114	7	Human	8.3	pKi	=	8.3	Binding	NoneNone	Drug Central	295	8	0	2	4.2	Clc1ccc(cc1)CCCOCCCN1CCCCC1	None
		CHEMBL462605	9907	64	None	-114	7	Human	8.3	pKi	=	8.3	Binding	NoneNone	Drug Central	295	8	0	2	4.2	Clc1ccc(cc1)CCCOCCCN1CCCCC1	None
		DB11642	9907	64	None	-114	7	Human	8.3	pKi	=	8.3	Binding	NoneNone	Drug Central	295	8	0	2	4.2	Clc1ccc(cc1)CCCOCCCN1CCCCC1	None
		176	7186	66	None	-6	31	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	None
		2157	7186	66	None	-6	31	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	None
		2566	7186	66	None	-6	31	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	None
		CHEMBL633	7186	66	None	-6	31	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	None
		DB01118	7186	66	None	-6	31	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	None
		11954259	222758	0	3H-TIOTIDINE	-1348	43	Human	6.4	pKi	=	6.4	Binding	NoneNone	PDSP KiDatabase	443	5	0	5	3.5	CN1CCN(CC1)CCC=C2C3=CC=CC=C3SC4=C2C=C(C=C4)S(=O)(=O)N(C)C	None
		135398745	9688	112	3H-TIOTIDINE	-9	65	Human	7.4	pKi	=	7.4	Binding	NoneNone	PDSP KiDatabase	312	1	1	5	1.7	CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C	None
		47	9688	112	3H-TIOTIDINE	-9	65	Human	7.4	pKi	=	7.4	Binding	NoneNone	PDSP KiDatabase	312	1	1	5	1.7	CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C	None
		CHEMBL715	9688	112	3H-TIOTIDINE	-9	65	Human	7.4	pKi	=	7.4	Binding	NoneNone	PDSP KiDatabase	312	1	1	5	1.7	CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C	None
		DB00334	9688	112	3H-TIOTIDINE	-9	65	Human	7.4	pKi	=	7.4	Binding	NoneNone	PDSP KiDatabase	312	1	1	5	1.7	CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C	None
		1231	7724	116	3H-TIOTIDINE	2	8	Guinea pig	6.3	pKi	=	6.3	Binding	NoneNone	PDSP KiDatabase	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	None
		2756	7724	116	3H-TIOTIDINE	2	8	Guinea pig	6.3	pKi	=	6.3	Binding	NoneNone	PDSP KiDatabase	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	None
		645	7724	116	3H-TIOTIDINE	2	8	Guinea pig	6.3	pKi	=	6.3	Binding	NoneNone	PDSP KiDatabase	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	None
		CHEMBL30	7724	116	3H-TIOTIDINE	2	8	Guinea pig	6.3	pKi	=	6.3	Binding	NoneNone	PDSP KiDatabase	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	None
		DB00501	7724	116	3H-TIOTIDINE	2	8	Guinea pig	6.3	pKi	=	6.3	Binding	NoneNone	PDSP KiDatabase	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	None
		1016	10519	78	None	-41	35	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	None
		2561	10519	78	None	-41	35	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	None
		2733526	10519	78	None	-41	35	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	None
		5384	10519	78	None	-41	35	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	None
		CHEMBL83	10519	78	None	-41	35	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	None
		DB00675	10519	78	None	-41	35	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	None
		1210	7705	51	None	-446	21	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	None
		1213	7705	51	None	-446	21	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	None
		2725	7705	51	None	-446	21	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	None
		33036	7705	51	None	-446	21	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	None
		4411	7705	51	None	-446	21	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	None
		616	7705	51	None	-446	21	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	None
		6976	7705	51	None	-446	21	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	None
		716121	7705	51	None	-446	21	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	None
		CHEMBL1201353	7705	51	None	-446	21	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	None
		CHEMBL1554789	7705	51	None	-446	21	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	None
		CHEMBL505	7705	51	None	-446	21	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	None
		DB01114	7705	51	None	-446	21	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	None
		DB13679	7705	51	None	-446	21	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	None
		4601	213526	35	None	-7	17	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	269	6	0	2	3.7	Cc1ccccc1C(OCCN(C)C)c1ccccc1	None
		CHEMBL1201023	213526	35	None	-7	17	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	269	6	0	2	3.7	Cc1ccccc1C(OCCN(C)C)c1ccccc1	None
		CHEMBL900	213526	35	None	-7	17	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	269	6	0	2	3.7	Cc1ccccc1C(OCCN(C)C)c1ccccc1	None
		4189	213701	96	None	-36	34	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	414	6	0	3	6.5	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1	None
		CHEMBL1559	213701	96	None	-36	34	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	414	6	0	3	6.5	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1	None
		CHEMBL91	213701	96	None	-36	34	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	414	6	0	3	6.5	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1	None
		2812	11551	101	None	-33	34	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	344	4	0	2	5.4	Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1	None
		CHEMBL104	11551	101	None	-33	34	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	344	4	0	2	5.4	Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1	None
		1530	8963	50	None	-151	21	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	309	0	0	3	4.0	CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1	None
		3827	8963	50	None	-151	21	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	309	0	0	3	4.0	CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1	None
		7206	8963	50	None	-151	21	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	309	0	0	3	4.0	CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1	None
		CHEMBL534	8963	50	None	-151	21	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	309	0	0	3	4.0	CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1	None
		DB00920	8963	50	None	-151	21	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	309	0	0	3	4.0	CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1	None
		237	211644	48	None	-3	13	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	399	9	1	4	6.0	CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12	None
		CHEMBL546257	211644	48	None	-3	13	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	399	9	1	4	6.0	CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12	None
		CHEMBL554190	211644	48	None	-3	13	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	399	9	1	4	6.0	CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12	None
		CHEMBL7568	211644	48	None	-3	13	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	399	9	1	4	6.0	CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12	None
		2865	10915	73	None	-281	53	Human	8.3	pKi	=	8.3	Binding	NoneNone	Drug Central	412	4	1	5	3.8	O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2	None
		59	10915	73	None	-281	53	Human	8.3	pKi	=	8.3	Binding	NoneNone	Drug Central	412	4	1	5	3.8	O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2	None
		60854	10915	73	None	-281	53	Human	8.3	pKi	=	8.3	Binding	NoneNone	Drug Central	412	4	1	5	3.8	O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2	None
		CHEMBL708	10915	73	None	-281	53	Human	8.3	pKi	=	8.3	Binding	NoneNone	Drug Central	412	4	1	5	3.8	O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2	None
		DB00246	10915	73	None	-281	53	Human	8.3	pKi	=	8.3	Binding	NoneNone	Drug Central	412	4	1	5	3.8	O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2	None
		213	10625	55	None	-12	43	Human	8.3	pKi	=	8.3	Binding	NoneNone	Drug Central	371	5	0	6	2.4	Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2	None
		2717	10625	55	None	-12	43	Human	8.3	pKi	=	8.3	Binding	NoneNone	Drug Central	371	5	0	6	2.4	Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2	None
		5533	10625	55	None	-12	43	Human	8.3	pKi	=	8.3	Binding	NoneNone	Drug Central	371	5	0	6	2.4	Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2	None
		CHEMBL621	10625	55	None	-12	43	Human	8.3	pKi	=	8.3	Binding	NoneNone	Drug Central	371	5	0	6	2.4	Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2	None
		DB00656	10625	55	None	-12	43	Human	8.3	pKi	=	8.3	Binding	NoneNone	Drug Central	371	5	0	6	2.4	Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2	None
		1599	9120	50	None	-154	16	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	476	7	1	3	5.1	Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1	None
		3955	9120	50	None	-154	16	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	476	7	1	3	5.1	Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1	None
		7215	9120	50	None	-154	16	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	476	7	1	3	5.1	Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1	None
		CHEMBL841	9120	50	None	-154	16	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	476	7	1	3	5.1	Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1	None
		DB00836	9120	50	None	-154	16	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	476	7	1	3	5.1	Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1	None
		3191	109635	97	None	-24	25	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	469	9	0	3	7.2	CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1	None
		CHEMBL305660	109635	97	None	-24	25	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	469	9	0	3	7.2	CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1	None
		2284	9956	33	None	-53	29	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	284	4	0	3	4.2	CN(CCCN1c2ccccc2Sc2c1cccc2)C	None
		4926	9956	33	None	-53	29	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	284	4	0	3	4.2	CN(CCCN1c2ccccc2Sc2c1cccc2)C	None
		7281	9956	33	None	-53	29	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	284	4	0	3	4.2	CN(CCCN1c2ccccc2Sc2c1cccc2)C	None
		CHEMBL564	9956	33	None	-53	29	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	284	4	0	3	4.2	CN(CCCN1c2ccccc2Sc2c1cccc2)C	None
		DB00420	9956	33	None	-53	29	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	284	4	0	3	4.2	CN(CCCN1c2ccccc2Sc2c1cccc2)C	None
		2520	210787	70	None	-20	12	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	454	13	0	6	5.1	COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC	None
		CHEMBL1280	210787	70	None	-20	12	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	454	13	0	6	5.1	COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC	None
		CHEMBL6966	210787	70	None	-20	12	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	454	13	0	6	5.1	COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC	None
		1971	9641	38	None	-22	30	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	263	3	1	1	3.8	CNCCC=C1c2ccccc2CCc2c1cccc2	None
		2404	9641	38	None	-22	30	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	263	3	1	1	3.8	CNCCC=C1c2ccccc2CCc2c1cccc2	None
		4543	9641	38	None	-22	30	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	263	3	1	1	3.8	CNCCC=C1c2ccccc2CCc2c1cccc2	None
		CHEMBL445	9641	38	None	-22	30	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	263	3	1	1	3.8	CNCCC=C1c2ccccc2CCc2c1cccc2	None
		DB00540	9641	38	None	-22	30	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	263	3	1	1	3.8	CNCCC=C1c2ccccc2CCc2c1cccc2	None
		2398	7741	62	None	-13	29	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	314	4	0	2	4.5	CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C	None
		2801	7741	62	None	-13	29	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	314	4	0	2	4.5	CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C	None
		701	7741	62	None	-13	29	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	314	4	0	2	4.5	CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C	None
		CHEMBL415	7741	62	None	-13	29	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	314	4	0	2	4.5	CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C	None
		DB01242	7741	62	None	-13	29	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	314	4	0	2	4.5	CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C	None
		5291	214216	120	None	-1	2	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	493	7	2	7	4.6	Cc1ccc(NC(=O)c2ccc(CN3CCN(C)CC3)cc2)cc1Nc1nccc(-c2cccnc2)n1	None
		CHEMBL941	214216	120	None	-1	2	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	493	7	2	7	4.6	Cc1ccc(NC(=O)c2ccc(CN3CCN(C)CC3)cc2)cc1Nc1nccc(-c2cccnc2)n1	None
		1225	8253	26	None	-20	22	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	279	3	0	2	4.0	CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C	None
		3958	8253	26	None	-20	22	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	279	3	0	2	4.0	CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C	None
		667477	8253	26	None	-20	22	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	279	3	0	2	4.0	CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C	None
		CHEMBL860	8253	26	None	-20	22	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	279	3	0	2	4.0	CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C	None
		DB01142	8253	26	None	-20	22	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	279	3	0	2	4.0	CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C	None
		2247	7293	81	None	-56	42	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	None
		249	7293	81	None	-56	42	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	None
		2603	7293	81	None	-56	42	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	None
		CHEMBL296419	7293	81	None	-56	42	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	None
		DB00637	7293	81	None	-56	42	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	None
		3042	8196	35	None	-53	15	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	309	7	0	3	4.4	CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC	None
		355	8196	35	None	-53	15	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	309	7	0	3	4.4	CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC	None
		868	8196	35	None	-53	15	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	309	7	0	3	4.4	CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC	None
		CHEMBL1123	8196	35	None	-53	15	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	309	7	0	3	4.4	CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC	None
		DB00804	8196	35	None	-53	15	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	309	7	0	3	4.4	CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC	None
		3198	212292	76	None	-19	34	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	380	6	0	3	5.8	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1	None
		CHEMBL1201049	212292	76	None	-19	34	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	380	6	0	3	5.8	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1	None
		CHEMBL808	212292	76	None	-19	34	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	380	6	0	3	5.8	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1	None
		57469	25638	125	None	-1	3	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	240	2	1	4	2.8	CC(C)Cn1cnc2c(N)nc3ccccc3c21	None
		CHEMBL1282	25638	125	None	-1	3	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	240	2	1	4	2.8	CC(C)Cn1cnc2c(N)nc3ccccc3c21	None
		1231	7724	116	None	-2	8	Rat	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	None
		2756	7724	116	None	-2	8	Rat	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	None
		645	7724	116	None	-2	8	Rat	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	None
		CHEMBL30	7724	116	None	-2	8	Rat	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	None
		DB00501	7724	116	None	-2	8	Rat	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	None
		1201549	7384	24	None	-74	20	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	307	4	0	2	4.4	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1	None
		333	7384	24	None	-74	20	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	307	4	0	2	4.4	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1	None
		7601	7384	24	None	-74	20	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	307	4	0	2	4.4	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1	None
		CHEMBL1201203	7384	24	None	-74	20	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	307	4	0	2	4.4	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1	None
		CHEMBL438151	7384	24	None	-74	20	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	307	4	0	2	4.4	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1	None
		DB00245	7384	24	None	-74	20	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	307	4	0	2	4.4	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1	None
		2286	9957	51	None	-26	30	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	None
		4927	9957	51	None	-26	30	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	None
		7282	9957	51	None	-26	30	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	None
		CHEMBL643	9957	51	None	-26	30	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	None
		DB01069	9957	51	None	-26	30	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	None
		11057	182928	23	None	-2	20	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	372	4	0	2	4.5	CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1	None
		3468	182928	23	None	-2	20	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	372	4	0	2	4.5	CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1	None
		CHEMBL459265	182928	23	None	-2	20	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	372	4	0	2	4.5	CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1	None
		CHEMBL64894	182928	23	None	-2	20	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	372	4	0	2	4.5	CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1	None
		124087	8171	114	None	-29	15	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	310	0	1	2	4.0	Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1	None
		7157	8171	114	None	-29	15	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	310	0	1	2	4.0	Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1	None
		814	8171	114	None	-29	15	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	310	0	1	2	4.0	Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1	None
		CHEMBL1172	8171	114	None	-29	15	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	310	0	1	2	4.0	Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1	None
		DB00967	8171	114	None	-29	15	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	310	0	1	2	4.0	Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1	None
		1588	9105	27	None	-223	44	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	338	3	2	2	2.8	CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC	None
		28864	9105	27	None	-223	44	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	338	3	2	2	2.8	CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC	None
		43	9105	27	None	-223	44	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	338	3	2	2	2.8	CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC	None
		CHEMBL157138	9105	27	None	-223	44	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	338	3	2	2	2.8	CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC	None
		DB00589	9105	27	None	-223	44	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	338	3	2	2	2.8	CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC	None
		103	10925	61	3H-TIOTIDINE	-46	53	Human	6.3	pKi	=	6.3	Binding	NoneNone	PDSP KiDatabase	331	4	0	3	4.9	CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C	None
		2875	10925	61	3H-TIOTIDINE	-46	53	Human	6.3	pKi	=	6.3	Binding	NoneNone	PDSP KiDatabase	331	4	0	3	4.9	CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C	None
		5736	10925	61	3H-TIOTIDINE	-46	53	Human	6.3	pKi	=	6.3	Binding	NoneNone	PDSP KiDatabase	331	4	0	3	4.9	CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C	None
		CHEMBL285802	10925	61	3H-TIOTIDINE	-46	53	Human	6.3	pKi	=	6.3	Binding	NoneNone	PDSP KiDatabase	331	4	0	3	4.9	CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C	None
		DB09225	10925	61	3H-TIOTIDINE	-46	53	Human	6.3	pKi	=	6.3	Binding	NoneNone	PDSP KiDatabase	331	4	0	3	4.9	CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C	None
		1226	8800	20	125I-iodoaminopotentidine	-7	7	Human	6.3	pKi	=	6.3	Binding	NoneNone	PDSP KiDatabase	321	9	4	4	1.2	NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C	None
		41376	8800	20	125I-iodoaminopotentidine	-7	7	Human	6.3	pKi	=	6.3	Binding	NoneNone	PDSP KiDatabase	321	9	4	4	1.2	NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C	None
		CHEMBL12608	8800	20	125I-iodoaminopotentidine	-7	7	Human	6.3	pKi	=	6.3	Binding	NoneNone	PDSP KiDatabase	321	9	4	4	1.2	NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C	None
		1204	8713	119	125I-iodoaminopotentidine	-173	25	Human	4.3	pKi	=	4.3	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
		1247	8713	119	125I-iodoaminopotentidine	-173	25	Human	4.3	pKi	=	4.3	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
		1375	8713	119	125I-iodoaminopotentidine	-173	25	Human	4.3	pKi	=	4.3	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
		774	8713	119	125I-iodoaminopotentidine	-173	25	Human	4.3	pKi	=	4.3	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
		CHEMBL90	8713	119	125I-iodoaminopotentidine	-173	25	Human	4.3	pKi	=	4.3	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
		DB05381	8713	119	125I-iodoaminopotentidine	-173	25	Human	4.3	pKi	=	4.3	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
		1233	9293	0	3H-TIOTIDINE	3	4	Guinea pig	6.3	pKi	=	6.3	Binding	NoneNone	PDSP KiDatabase	244	5	3	3	1.0	CNC(=S)NCCSCc1nc[nH]c1C	None
		1548992	9293	0	3H-TIOTIDINE	3	4	Guinea pig	6.3	pKi	=	6.3	Binding	NoneNone	PDSP KiDatabase	244	5	3	3	1.0	CNC(=S)NCCSCc1nc[nH]c1C	None
		CHEMBL275446	9293	0	3H-TIOTIDINE	3	4	Guinea pig	6.3	pKi	=	6.3	Binding	NoneNone	PDSP KiDatabase	244	5	3	3	1.0	CNC(=S)NCCSCc1nc[nH]c1C	None
		DB08805	9293	0	3H-TIOTIDINE	3	4	Guinea pig	6.3	pKi	=	6.3	Binding	NoneNone	PDSP KiDatabase	244	5	3	3	1.0	CNC(=S)NCCSCc1nc[nH]c1C	None
		1212	8443	50	3H-TIOTIDINE	-323	65	Human	6.3	pKi	=	6.3	Binding	NoneNone	PDSP KiDatabase	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	None
		204	8443	50	3H-TIOTIDINE	-323	65	Human	6.3	pKi	=	6.3	Binding	NoneNone	PDSP KiDatabase	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	None
		3372	8443	50	3H-TIOTIDINE	-323	65	Human	6.3	pKi	=	6.3	Binding	NoneNone	PDSP KiDatabase	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	None
		CHEMBL726	8443	50	3H-TIOTIDINE	-323	65	Human	6.3	pKi	=	6.3	Binding	NoneNone	PDSP KiDatabase	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	None
		DB00623	8443	50	3H-TIOTIDINE	-323	65	Human	6.3	pKi	=	6.3	Binding	NoneNone	PDSP KiDatabase	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	None
		1223	7740	41	3H-TIOTIDINE	-32359	11	Human	5.2	pKi	=	5.2	Binding	NoneNone	PDSP KiDatabase	308	6	2	3	3.2	Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N	None
		2790	7740	41	3H-TIOTIDINE	-32359	11	Human	5.2	pKi	=	5.2	Binding	NoneNone	PDSP KiDatabase	308	6	2	3	3.2	Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N	None
		CHEMBL14690	7740	41	3H-TIOTIDINE	-32359	11	Human	5.2	pKi	=	5.2	Binding	NoneNone	PDSP KiDatabase	308	6	2	3	3.2	Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N	None
		135	9310	43	None	-39	56	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	264	0	0	2	3.1	CN1CCN2C(C1)c1ccccc1Cc1c2cccc1	None
		1796	9310	43	None	-39	56	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	264	0	0	2	3.1	CN1CCN2C(C1)c1ccccc1Cc1c2cccc1	None
		4184	9310	43	None	-39	56	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	264	0	0	2	3.1	CN1CCN2C(C1)c1ccccc1Cc1c2cccc1	None
		CHEMBL6437	9310	43	None	-39	56	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	264	0	0	2	3.1	CN1CCN2C(C1)c1ccccc1Cc1c2cccc1	None
		DB06148	9310	43	None	-39	56	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	264	0	0	2	3.1	CN1CCN2C(C1)c1ccccc1Cc1c2cccc1	None
		33630	185736	99	None	-13	28	Human	8.2	pKi	=	8.2	Binding	Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assay	Drug Central	523	7	1	2	7.5	OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1	None
		CHEMBL47050	185736	99	None	-13	28	Human	8.2	pKi	=	8.2	Binding	Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assay	Drug Central	523	7	1	2	7.5	OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1	None
		1353	8692	93	None	-131	85	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	None
		3559	8692	93	None	-131	85	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	None
		86	8692	93	None	-131	85	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	None
		CHEMBL54	8692	93	None	-131	85	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	None
		DB00502	8692	93	None	-131	85	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	None
		133	9274	52	None	-141	43	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	403	4	1	4	4.1	O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C	None
		1723	9274	52	None	-141	43	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	403	4	1	4	4.1	O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C	None
		28693	9274	52	None	-141	43	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	403	4	1	4	4.1	O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C	None
		CHEMBL19215	9274	52	None	-141	43	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	403	4	1	4	4.1	O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C	None
		DB13520	9274	52	None	-141	43	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	403	4	1	4	4.1	O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C	None
		1234	10064	68	None	-1	7	Rat	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	None
		3001055	10064	68	None	-1	7	Rat	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	None
		CHEMBL512	10064	68	None	-1	7	Rat	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	None
		DB00863	10064	68	None	-1	7	Rat	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	None
		1212	8443	50	None	-323	65	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	None
		204	8443	50	None	-323	65	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	None
		3372	8443	50	None	-323	65	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	None
		CHEMBL726	8443	50	None	-323	65	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	None
		DB00623	8443	50	None	-323	65	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	None
		3389	224490	0	None	-1	26	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	549	12	0	6	6.8	CCCCCCC(=O)OCCN1CCN(CCCN2C3=CC=CC=C3SC3=C2C=C(C=C3)C(F)(F)F)CC1	None
		103	10925	61	None	-46	53	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	331	4	0	3	4.9	CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C	None
		2875	10925	61	None	-46	53	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	331	4	0	3	4.9	CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C	None
		5736	10925	61	None	-46	53	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	331	4	0	3	4.9	CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C	None
		CHEMBL285802	10925	61	None	-46	53	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	331	4	0	3	4.9	CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C	None
		DB09225	10925	61	None	-46	53	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	331	4	0	3	4.9	CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C	None
		212	10578	47	None	-6	25	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	443	5	0	5	3.5	CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C	None
		2639	10578	47	None	-6	25	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	443	5	0	5	3.5	CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C	None
		941651	10578	47	None	-6	25	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	443	5	0	5	3.5	CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C	None
		CHEMBL1201	10578	47	None	-6	25	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	443	5	0	5	3.5	CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C	None
		DB01623	10578	47	None	-6	25	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	443	5	0	5	3.5	CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C	None
		4011	89183	49	None	-27	24	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	277	4	1	1	4.2	CNCCCC12CCC(c3ccccc31)c1ccccc12	None
		CHEMBL21731	89183	49	None	-27	24	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	277	4	1	1	4.2	CNCCCC12CCC(c3ccccc31)c1ccccc12	None
		26987	7736	33	None	-177	21	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	343	6	0	2	5.1	Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C	None
		6063	7736	33	None	-177	21	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	343	6	0	2	5.1	Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C	None
		671	7736	33	None	-177	21	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	343	6	0	2	5.1	Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C	None
		CHEMBL1626	7736	33	None	-177	21	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	343	6	0	2	5.1	Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C	None
		DB00283	7736	33	None	-177	21	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	343	6	0	2	5.1	Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C	None
		1613	9127	53	None	-10	44	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	327	0	0	4	3.8	CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2	None
		205	9127	53	None	-10	44	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	327	0	0	4	3.8	CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2	None
		3964	9127	53	None	-10	44	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	327	0	0	4	3.8	CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2	None
		CHEMBL831	9127	53	None	-10	44	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	327	0	0	4	3.8	CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2	None
		DB00408	9127	53	None	-10	44	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	327	0	0	4	3.8	CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2	None
		277	8083	62	None	-43	50	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	287	0	0	1	4.7	CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1	None
		2913	8083	62	None	-43	50	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	287	0	0	1	4.7	CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1	None
		765	8083	62	None	-43	50	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	287	0	0	1	4.7	CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1	None
		CHEMBL516	8083	62	None	-43	50	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	287	0	0	1	4.7	CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1	None
		DB00434	8083	62	None	-43	50	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	287	0	0	1	4.7	CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1	None
		4806	10780	88	None	-5	13	Human	8.2	pKi	=	8.2	Binding	Binding affinity to human histamine H2 receptorBinding affinity to human histamine H2 receptor	Drug Central	298	3	1	3	3.9	Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1	None
		7351	10780	88	None	-5	13	Human	8.2	pKi	=	8.2	Binding	Binding affinity to human histamine H2 receptorBinding affinity to human histamine H2 receptor	Drug Central	298	3	1	3	3.9	Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1	None
		9966051	10780	88	None	-5	13	Human	8.2	pKi	=	8.2	Binding	Binding affinity to human histamine H2 receptorBinding affinity to human histamine H2 receptor	Drug Central	298	3	1	3	3.9	Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1	None
		CHEMBL2104993	10780	88	None	-5	13	Human	8.2	pKi	=	8.2	Binding	Binding affinity to human histamine H2 receptorBinding affinity to human histamine H2 receptor	Drug Central	298	3	1	3	3.9	Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1	None
		DB09068	10780	88	None	-5	13	Human	8.2	pKi	=	8.2	Binding	Binding affinity to human histamine H2 receptorBinding affinity to human histamine H2 receptor	Drug Central	298	3	1	3	3.9	Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1	None
		2726	7706	68	None	-85	72	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	None
		621	7706	68	None	-85	72	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	None
		83	7706	68	None	-85	72	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	None
		CHEMBL71	7706	68	None	-85	72	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	None
		DB00477	7706	68	None	-85	72	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	None
		135398737	7745	93	None	-64	90	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	None
		38	7745	93	None	-64	90	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	None
		722	7745	93	None	-64	90	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	None
		CHEMBL42	7745	93	None	-64	90	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	None
		DB00363	7745	93	None	-64	90	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	None
		100	10577	58	None	-46	54	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	None
		2637	10577	58	None	-46	54	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	None
		5452	10577	58	None	-46	54	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	None
		CHEMBL479	10577	58	None	-46	54	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	None
		DB00679	10577	58	None	-46	54	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	None
		2389	10104	118	None	-288	66	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	None
		5073	10104	118	None	-288	66	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	None
		96	10104	118	None	-288	66	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	None
		CHEMBL85	10104	118	None	-288	66	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	None
		DB00734	10104	118	None	-288	66	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	None
		115237	62359	119	None	-123	54	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	426	4	1	7	3.1	Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O	None
		CHEMBL1621	62359	119	None	-123	54	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	426	4	1	7	3.1	Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O	None
		1226	8800	20	3H-TIOTIDINE	-3	7	Guinea pig	7.2	pKi	=	7.2	Binding	NoneNone	PDSP KiDatabase	321	9	4	4	1.2	NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C	None
		41376	8800	20	3H-TIOTIDINE	-3	7	Guinea pig	7.2	pKi	=	7.2	Binding	NoneNone	PDSP KiDatabase	321	9	4	4	1.2	NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C	None
		CHEMBL12608	8800	20	3H-TIOTIDINE	-3	7	Guinea pig	7.2	pKi	=	7.2	Binding	NoneNone	PDSP KiDatabase	321	9	4	4	1.2	NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C	None
		1231	7724	116	125I-iodoaminopotentidine	-4	8	Human	6.2	pKi	=	6.2	Binding	NoneNone	PDSP KiDatabase	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	None
		2756	7724	116	125I-iodoaminopotentidine	-4	8	Human	6.2	pKi	=	6.2	Binding	NoneNone	PDSP KiDatabase	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	None
		645	7724	116	125I-iodoaminopotentidine	-4	8	Human	6.2	pKi	=	6.2	Binding	NoneNone	PDSP KiDatabase	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	None
		CHEMBL30	7724	116	125I-iodoaminopotentidine	-4	8	Human	6.2	pKi	=	6.2	Binding	NoneNone	PDSP KiDatabase	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	None
		DB00501	7724	116	125I-iodoaminopotentidine	-4	8	Human	6.2	pKi	=	6.2	Binding	NoneNone	PDSP KiDatabase	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	None
		657255	205863	34	None	-3	15	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	337	12	2	3	5.6	CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1	None
		CHEMBL588119	205863	34	None	-3	15	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	337	12	2	3	5.6	CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1	None
		135398745	9688	112	None	-9	65	Human	8.1	pKi	=	8.1	Binding	NoneNone	Drug Central	312	1	1	5	1.7	CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C	None
		47	9688	112	None	-9	65	Human	8.1	pKi	=	8.1	Binding	NoneNone	Drug Central	312	1	1	5	1.7	CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C	None
		CHEMBL715	9688	112	None	-9	65	Human	8.1	pKi	=	8.1	Binding	NoneNone	Drug Central	312	1	1	5	1.7	CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C	None
		DB00334	9688	112	None	-9	65	Human	8.1	pKi	=	8.1	Binding	NoneNone	Drug Central	312	1	1	5	1.7	CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C	None
		1234	10064	68	125I-iodoaminopotentidine	-2	7	Human	7.1	pKi	=	7.1	Binding	NoneNone	PDSP KiDatabase	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	None
		3001055	10064	68	125I-iodoaminopotentidine	-2	7	Human	7.1	pKi	=	7.1	Binding	NoneNone	PDSP KiDatabase	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	None
		CHEMBL512	10064	68	125I-iodoaminopotentidine	-2	7	Human	7.1	pKi	=	7.1	Binding	NoneNone	PDSP KiDatabase	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	None
		DB00863	10064	68	125I-iodoaminopotentidine	-2	7	Human	7.1	pKi	=	7.1	Binding	NoneNone	PDSP KiDatabase	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	None
		5048	9907	64	None	-114	7	Human	5.0	pKi	=	5.0	Binding	UnclassifiedUnclassified	Guide to Pharmacology	295	8	0	2	4.2	Clc1ccc(cc1)CCCOCCCN1CCCCC1	26084539
		8924	9907	64	None	-114	7	Human	5.0	pKi	=	5.0	Binding	UnclassifiedUnclassified	Guide to Pharmacology	295	8	0	2	4.2	Clc1ccc(cc1)CCCOCCCN1CCCCC1	26084539
		9948102	9907	64	None	-114	7	Human	5.0	pKi	=	5.0	Binding	UnclassifiedUnclassified	Guide to Pharmacology	295	8	0	2	4.2	Clc1ccc(cc1)CCCOCCCN1CCCCC1	26084539
		CHEMBL462605	9907	64	None	-114	7	Human	5.0	pKi	=	5.0	Binding	UnclassifiedUnclassified	Guide to Pharmacology	295	8	0	2	4.2	Clc1ccc(cc1)CCCOCCCN1CCCCC1	26084539
		DB11642	9907	64	None	-114	7	Human	5.0	pKi	=	5.0	Binding	UnclassifiedUnclassified	Guide to Pharmacology	295	8	0	2	4.2	Clc1ccc(cc1)CCCOCCCN1CCCCC1	26084539
		1231	7724	116	None	-2	8	Rat	5.9	pKi	=	5.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	9384502
		2756	7724	116	None	-2	8	Rat	5.9	pKi	=	5.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	9384502
		645	7724	116	None	-2	8	Rat	5.9	pKi	=	5.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	9384502
		CHEMBL30	7724	116	None	-2	8	Rat	5.9	pKi	=	5.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	9384502
		DB00501	7724	116	None	-2	8	Rat	5.9	pKi	=	5.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	9384502
		1234	10064	68	None	-1	7	Rat	6.2	pKi	=	6.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	9384502
		3001055	10064	68	None	-1	7	Rat	6.2	pKi	=	6.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	9384502
		CHEMBL512	10064	68	None	-1	7	Rat	6.2	pKi	=	6.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	9384502
		DB00863	10064	68	None	-1	7	Rat	6.2	pKi	=	6.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	9384502
		1231	7724	116	None	-4	8	Human	6.9	pKi	=	6.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	23466604
		2756	7724	116	None	-4	8	Human	6.9	pKi	=	6.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	23466604
		645	7724	116	None	-4	8	Human	6.9	pKi	=	6.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	23466604
		CHEMBL30	7724	116	None	-4	8	Human	6.9	pKi	=	6.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	23466604
		DB00501	7724	116	None	-4	8	Human	6.9	pKi	=	6.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	23466604
		1234	10064	68	None	-2	7	Human	7.1	pKi	=	7.1	Binding	UnclassifiedUnclassified	Guide to Pharmacology	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	7921611
		3001055	10064	68	None	-2	7	Human	7.1	pKi	=	7.1	Binding	UnclassifiedUnclassified	Guide to Pharmacology	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	7921611
		CHEMBL512	10064	68	None	-2	7	Human	7.1	pKi	=	7.1	Binding	UnclassifiedUnclassified	Guide to Pharmacology	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	7921611
		DB00863	10064	68	None	-2	7	Human	7.1	pKi	=	7.1	Binding	UnclassifiedUnclassified	Guide to Pharmacology	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	7921611
		1235	10595	36	None	1	5	Rat	7.5	pKi	=	7.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	312	6	4	6	-0.1	N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N	9384502
		3959	10595	36	None	1	5	Rat	7.5	pKi	=	7.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	312	6	4	6	-0.1	N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N	9384502
		50287	10595	36	None	1	5	Rat	7.5	pKi	=	7.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	312	6	4	6	-0.1	N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N	9384502
		CHEMBL269646	10595	36	None	1	5	Rat	7.5	pKi	=	7.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	312	6	4	6	-0.1	N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N	9384502
		1265	7729	60	None	-17782	8	Human	5.0	pKi	>	5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	270	7	1	3	3.0	O=C(c1ccc(cc1)OCCCc1[nH]cnc1)C1CC1	26084539
		6422124	7729	60	None	-17782	8	Human	5.0	pKi	>	5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	270	7	1	3	3.0	O=C(c1ccc(cc1)OCCCc1[nH]cnc1)C1CC1	26084539
		CHEMBL14638	7729	60	None	-17782	8	Human	5.0	pKi	>	5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	270	7	1	3	3.0	O=C(c1ccc(cc1)OCCCc1[nH]cnc1)C1CC1	26084539
		441082	7946	48	None	-2137	8	Human	5.0	pKi	>	5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	356	1	0	2	4.8	CN([C@H]1CC[C@]2(C(=CC[C@@H]3[C@@H]2CC[C@]24[C@H]3CC[C@@H]4[C@@H](N(C2)C)C)C1)C)C	26084539
		8981	7946	48	None	-2137	8	Human	5.0	pKi	>	5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	356	1	0	2	4.8	CN([C@H]1CC[C@]2(C(=CC[C@@H]3[C@@H]2CC[C@]24[C@H]3CC[C@@H]4[C@@H](N(C2)C)C)C1)C)C	26084539
		CHEMBL191703	7946	48	None	-2137	8	Human	5.0	pKi	>	5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	356	1	0	2	4.8	CN([C@H]1CC[C@]2(C(=CC[C@@H]3[C@@H]2CC[C@]24[C@H]3CC[C@@H]4[C@@H](N(C2)C)C)C1)C)C	26084539
		11697697	9325	24	None	-6309	6	Human	5.0	pKi	>	5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	431	6	0	5	4.6	Cc1nc2cccc(c2c(=O)n1c1ccc(cc1)OCCCN1CCCC1)C(F)(F)F	26084539
		7346	9325	24	None	-6309	6	Human	5.0	pKi	>	5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	431	6	0	5	4.6	Cc1nc2cccc(c2c(=O)n1c1ccc(cc1)OCCCN1CCCC1)C(F)(F)F	26084539
		CHEMBL476323	9325	24	None	-6309	6	Human	5.0	pKi	>	5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	431	6	0	5	4.6	Cc1nc2cccc(c2c(=O)n1c1ccc(cc1)OCCCN1CCCC1)C(F)(F)F	26084539
		DB11910	9325	24	None	-6309	6	Human	5.0	pKi	>	5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	431	6	0	5	4.6	Cc1nc2cccc(c2c(=O)n1c1ccc(cc1)OCCCN1CCCC1)C(F)(F)F	26084539
		117072554	8804	0	None	-1000	4	Human	5.3	pKi	>	5.3	Binding	UnclassifiedUnclassified	Guide to Pharmacology	450	5	2	6	2.3	CN1CCN(CC1)C1=CC(=NC(N1)N)c1ccc2c(c1)CN(CC2)C(=O)CCC1CCCC1	26084539
		8982	8804	0	None	-1000	4	Human	5.3	pKi	>	5.3	Binding	UnclassifiedUnclassified	Guide to Pharmacology	450	5	2	6	2.3	CN1CCN(CC1)C1=CC(=NC(N1)N)c1ccc2c(c1)CN(CC2)C(=O)CCC1CCCC1	26084539
		24994634	8923	31	None	-194	7	Human	6.0	pKi	>	6	Binding	UnclassifiedUnclassified	Guide to Pharmacology	221	2	2	5	0.7	N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C	26084539
		8984	8923	31	None	-194	7	Human	6.0	pKi	>	6	Binding	UnclassifiedUnclassified	Guide to Pharmacology	221	2	2	5	0.7	N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C	26084539
		CHEMBL3236549	8923	31	None	-194	7	Human	6.0	pKi	>	6	Binding	UnclassifiedUnclassified	Guide to Pharmacology	221	2	2	5	0.7	N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C	26084539
		45257132	10454	10	None	-83	4	Human	6.0	pKi	>	6	Binding	UnclassifiedUnclassified	Guide to Pharmacology	366	4	2	6	2.7	CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N	26084539
		8983	10454	10	None	-83	4	Human	6.0	pKi	>	6	Binding	UnclassifiedUnclassified	Guide to Pharmacology	366	4	2	6	2.7	CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N	26084539
		CHEMBL595180	10454	10	None	-83	4	Human	6.0	pKi	>	6	Binding	UnclassifiedUnclassified	Guide to Pharmacology	366	4	2	6	2.7	CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N	26084539
		119570	9933	96	None	-169	39	Human	8.3	pKi	None	8.3	Binding	NoneNone	Drug Central	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	None
		2233	9933	96	None	-169	39	Human	8.3	pKi	None	8.3	Binding	NoneNone	Drug Central	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	None
		953	9933	96	None	-169	39	Human	8.3	pKi	None	8.3	Binding	NoneNone	Drug Central	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	None
		CHEMBL301265	9933	96	None	-169	39	Human	8.3	pKi	None	8.3	Binding	NoneNone	Drug Central	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	None
		DB00413	9933	96	None	-169	39	Human	8.3	pKi	None	8.3	Binding	NoneNone	Drug Central	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	None
		1204	8713	119	None	-316	25	Rat	3.8	pKi	None	3.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	111	2	2	2	-0.1	NCCc1cnc[nH]1	9384502
		1247	8713	119	None	-316	25	Rat	3.8	pKi	None	3.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	111	2	2	2	-0.1	NCCc1cnc[nH]1	9384502
		1375	8713	119	None	-316	25	Rat	3.8	pKi	None	3.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	111	2	2	2	-0.1	NCCc1cnc[nH]1	9384502
		774	8713	119	None	-316	25	Rat	3.8	pKi	None	3.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	111	2	2	2	-0.1	NCCc1cnc[nH]1	9384502
		CHEMBL90	8713	119	None	-316	25	Rat	3.8	pKi	None	3.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	111	2	2	2	-0.1	NCCc1cnc[nH]1	9384502
		DB05381	8713	119	None	-316	25	Rat	3.8	pKi	None	3.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	111	2	2	2	-0.1	NCCc1cnc[nH]1	9384502
		1218	7017	52	None	-3548	4	Human	5.2	pKi	None	5.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	330	4	0	3	5.0	N#Cc1ccc(cc1)c1ccc2c(c1)cc(o2)CCN1CCC[C@H]1C	15608078
		9818903	7017	52	None	-3548	4	Human	5.2	pKi	None	5.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	330	4	0	3	5.0	N#Cc1ccc(cc1)c1ccc2c(c1)cc(o2)CCN1CCC[C@H]1C	15608078
		CHEMBL351231	7017	52	None	-3548	4	Human	5.2	pKi	None	5.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	330	4	0	3	5.0	N#Cc1ccc(cc1)c1ccc2c(c1)cc(o2)CCN1CCC[C@H]1C	15608078
		1223	7740	41	None	-32359	11	Human	5.2	pKi	None	5.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	308	6	2	3	3.2	Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N	12606603
		2790	7740	41	None	-32359	11	Human	5.2	pKi	None	5.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	308	6	2	3	3.2	Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N	12606603
		CHEMBL14690	7740	41	None	-32359	11	Human	5.2	pKi	None	5.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	308	6	2	3	3.2	Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N	12606603
		1229	7530	0	None	-63	6	Rat	5.5	pKi	None	5.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	262	5	3	2	2.0	CNC(=S)NCCCCc1cccc2c1cn[nH]2	8692899
		5311293	7530	0	None	-63	6	Rat	5.5	pKi	None	5.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	262	5	3	2	2.0	CNC(=S)NCCCCc1cccc2c1cn[nH]2	8692899
		1233	9293	0	None	-3	4	Rat	5.8	pKi	None	5.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	244	5	3	3	1.0	CNC(=S)NCCSCc1nc[nH]c1C	9384502
		1548992	9293	0	None	-3	4	Rat	5.8	pKi	None	5.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	244	5	3	3	1.0	CNC(=S)NCCSCc1nc[nH]c1C	9384502
		CHEMBL275446	9293	0	None	-3	4	Rat	5.8	pKi	None	5.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	244	5	3	3	1.0	CNC(=S)NCCSCc1nc[nH]c1C	9384502
		DB08805	9293	0	None	-3	4	Rat	5.8	pKi	None	5.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	244	5	3	3	1.0	CNC(=S)NCCSCc1nc[nH]c1C	9384502
		1200	10735	2	None	4	3	Human	6.0	pKi	None	6	Binding	UnclassifiedUnclassified	Guide to Pharmacology	335	8	4	5	0.7	O=C(NC(=NCCCc1cnc[nH]1)N)CSCc1nc[nH]c1C	16394198
		25149519	10735	2	None	4	3	Human	6.0	pKi	None	6	Binding	UnclassifiedUnclassified	Guide to Pharmacology	335	8	4	5	0.7	O=C(NC(=NCCCc1cnc[nH]1)N)CSCc1nc[nH]c1C	16394198
		CHEMBL513056	10735	2	None	4	3	Human	6.0	pKi	None	6	Binding	UnclassifiedUnclassified	Guide to Pharmacology	335	8	4	5	0.7	O=C(NC(=NCCCc1cnc[nH]1)N)CSCc1nc[nH]c1C	16394198
		1199	9750	0	None	37	3	Human	7.0	pKi	None	7	Binding	UnclassifiedUnclassified	Guide to Pharmacology	394	8	3	4	2.5	NC(=NCCCc1[nH]cnc1)NC(=O)CC(c1ccccn1)c1ccc(cc1)F	16394198
		25149244	9750	0	None	37	3	Human	7.0	pKi	None	7	Binding	UnclassifiedUnclassified	Guide to Pharmacology	394	8	3	4	2.5	NC(=NCCCc1[nH]cnc1)NC(=O)CC(c1ccccn1)c1ccc(cc1)F	16394198
		CHEMBL472273	9750	0	None	37	3	Human	7.0	pKi	None	7	Binding	UnclassifiedUnclassified	Guide to Pharmacology	394	8	3	4	2.5	NC(=NCCCc1[nH]cnc1)NC(=O)CC(c1ccccn1)c1ccc(cc1)F	16394198
		1221	7263	9	None	-2	3	Human	7.2	pKi	None	7.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	380	9	3	3	3.0	NC(=NCCCc1[nH]cnc1)NCCC(c1ccccn1)c1ccc(cc1)F	16394198
		65895	7263	9	None	-2	3	Human	7.2	pKi	None	7.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	380	9	3	3	3.0	NC(=NCCCc1[nH]cnc1)NCCC(c1ccccn1)c1ccc(cc1)F	16394198
		CHEMBL293802	7263	9	None	-2	3	Human	7.2	pKi	None	7.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	380	9	3	3	3.0	NC(=NCCCc1[nH]cnc1)NCCC(c1ccccn1)c1ccc(cc1)F	16394198
		1226	8800	20	None	-7	7	Human	7.2	pKi	None	7.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	321	9	4	4	1.2	NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C	16394198
		41376	8800	20	None	-7	7	Human	7.2	pKi	None	7.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	321	9	4	4	1.2	NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C	16394198
		CHEMBL12608	8800	20	None	-7	7	Human	7.2	pKi	None	7.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	321	9	4	4	1.2	NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C	16394198
		1232	8837	6	None	-	1	Rat	9.2	pKi	None	9.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	603	11	4	6	3.1	N#CNC(=NCCCOc1cccc(c1)CN1CCCCC1)NCCNC(=O)c1ccc(c(c1)I)N	9384502
		181461	8837	6	None	-	1	Rat	9.2	pKi	None	9.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	603	11	4	6	3.1	N#CNC(=NCCCOc1cccc(c1)CN1CCCCC1)NCCNC(=O)c1ccc(c(c1)I)N	9384502
		CHEMBL72193	8837	6	None	-	1	Rat	9.2	pKi	None	9.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	603	11	4	6	3.1	N#CNC(=NCCCOc1cccc(c1)CN1CCCCC1)NCCNC(=O)c1ccc(c(c1)I)N	9384502

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Ligand source activities (1 row/activity)