GPCRdb

Ligand source activities (1 row/activity)

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Ligands (move mouse cursor over ligand name to see structure)					Receptor	Activity									Chemical information
Sel. page	Common name	GPCRdb ID	Reference ligand	Vendors	Species	Assay Type	Activity Type	Activity Relation	Activity Value	p-value (-log)	Fold selectivity	Tested GPCRs	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI
	2274	3173	None	38	Human	Functional	pAC50	=	6.0	6.0	-10	36	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	373	4	0	4	4.6	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2	10.1038/s41467-023-40064-9
	4917	3173	None	38	Human	Functional	pAC50	=	6.0	6.0	-10	36	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	373	4	0	4	4.6	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2	10.1038/s41467-023-40064-9
	4917.0	3173	None	38	Human	Functional	pAC50	=	6.0	6.0	-10	36	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	373	4	0	4	4.6	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2	10.1038/s41467-023-40064-9
	7279	3173	None	38	Human	Functional	pAC50	=	6.0	6.0	-10	36	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	373	4	0	4	4.6	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2	10.1038/s41467-023-40064-9
	CHEMBL728	3173	None	38	Human	Functional	pAC50	=	6.0	6.0	-10	36	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	373	4	0	4	4.6	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2	10.1038/s41467-023-40064-9
	DB00433	3173	None	38	Human	Functional	pAC50	=	6.0	6.0	-10	36	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	373	4	0	4	4.6	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2	10.1038/s41467-023-40064-9
	2470	3653	None	40	Human	Functional	pAC50	=	5.9	5.9	-38018	23	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	395	6	1	4	3.2	Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1	10.1038/s41467-023-40064-9
	3300	3653	None	40	Human	Functional	pAC50	=	5.9	5.9	-38018	23	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	395	6	1	4	3.2	Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1	10.1038/s41467-023-40064-9
	5265	3653	None	40	Human	Functional	pAC50	=	5.9	5.9	-38018	23	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	395	6	1	4	3.2	Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1	10.1038/s41467-023-40064-9
	99	3653	None	40	Human	Functional	pAC50	=	5.9	5.9	-38018	23	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	395	6	1	4	3.2	Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1	10.1038/s41467-023-40064-9
	CHEMBL267930	3653	None	40	Human	Functional	pAC50	=	5.9	5.9	-38018	23	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	395	6	1	4	3.2	Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1	10.1038/s41467-023-40064-9
	3081361	93987	None	66	Human	Functional	pAC50	=	5.9	5.9	1	14	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	474	5	1	5	4.4	COc1cc2/c(=N/c3ccc(Br)cc3F)nc[nH]c2cc1OCC1CCN(C)CC1	10.1038/s41467-023-40064-9
	CHEMBL24828	93987	None	66	Human	Functional	pAC50	=	5.9	5.9	1	14	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	474	5	1	5	4.4	COc1cc2/c(=N/c3ccc(Br)cc3F)nc[nH]c2cc1OCC1CCN(C)CC1	10.1038/s41467-023-40064-9
	214	3860	None	43	Human	Functional	pAC50	=	5.7	5.7	-31	28	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	407	4	0	4	4.9	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
	2740	3860	None	43	Human	Functional	pAC50	=	5.7	5.7	-31	28	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	407	4	0	4	4.9	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
	5566	3860	None	43	Human	Functional	pAC50	=	5.7	5.7	-31	28	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	407	4	0	4	4.9	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
	5566.0	3860	None	43	Human	Functional	pAC50	=	5.7	5.7	-31	28	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	407	4	0	4	4.9	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
	66064	3860	None	43	Human	Functional	pAC50	=	5.7	5.7	-31	28	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	407	4	0	4	4.9	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
	CHEMBL422	3860	None	43	Human	Functional	pAC50	=	5.7	5.7	-31	28	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	407	4	0	4	4.9	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
	DB00831	3860	None	43	Human	Functional	pAC50	=	5.7	5.7	-31	28	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	407	4	0	4	4.9	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
	242	470	None	70	Human	Functional	pAC50	=	5.7	5.7	-97	33	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	447	7	1	4	4.9	O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl	10.1038/s41467-023-40064-9
	34	470	None	70	Human	Functional	pAC50	=	5.7	5.7	-97	33	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	447	7	1	4	4.9	O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl	10.1038/s41467-023-40064-9
	60795	470	None	70	Human	Functional	pAC50	=	5.7	5.7	-97	33	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	447	7	1	4	4.9	O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl	10.1038/s41467-023-40064-9
	60795.0	470	None	70	Human	Functional	pAC50	=	5.7	5.7	-97	33	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	447	7	1	4	4.9	O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl	10.1038/s41467-023-40064-9
	CHEMBL1112	470	None	70	Human	Functional	pAC50	=	5.7	5.7	-97	33	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	447	7	1	4	4.9	O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl	10.1038/s41467-023-40064-9
	DB01238	470	None	70	Human	Functional	pAC50	=	5.7	5.7	-97	33	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	447	7	1	4	4.9	O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl	10.1038/s41467-023-40064-9
	2393	3334	None	46	Human	Functional	pAC50	=	4.7	4.7	-891	8	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	269	5	1	4	1.9	CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C	10.1038/s41467-023-40064-9
	5078	3334	None	46	Human	Functional	pAC50	=	4.7	4.7	-891	8	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	269	5	1	4	1.9	CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C	10.1038/s41467-023-40064-9
	5078.0	3334	None	46	Human	Functional	pAC50	=	4.7	4.7	-891	8	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	269	5	1	4	1.9	CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C	10.1038/s41467-023-40064-9
	51	3334	None	46	Human	Functional	pAC50	=	4.7	4.7	-891	8	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	269	5	1	4	1.9	CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C	10.1038/s41467-023-40064-9
	CHEMBL905	3334	None	46	Human	Functional	pAC50	=	4.7	4.7	-891	8	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	269	5	1	4	1.9	CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C	10.1038/s41467-023-40064-9
	DB00953	3334	None	46	Human	Functional	pAC50	=	4.7	4.7	-891	8	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	269	5	1	4	1.9	CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C	10.1038/s41467-023-40064-9
	3547	141460	None	43	Human	Functional	pAC50	=	4.7	4.7	-3	8	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	291	2	1	4	1.2	O=S(=O)(c1cccc2cnccc12)N1CCCNCC1	10.1038/s41467-023-40064-9
	CHEMBL38380	141460	None	43	Human	Functional	pAC50	=	4.7	4.7	-3	8	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	291	2	1	4	1.2	O=S(=O)(c1cccc2cnccc12)N1CCCNCC1	10.1038/s41467-023-40064-9
	CHEMBL541388	141460	None	43	Human	Functional	pAC50	=	4.7	4.7	-3	8	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	291	2	1	4	1.2	O=S(=O)(c1cccc2cnccc12)N1CCCNCC1	10.1038/s41467-023-40064-9
	71398	106495	None	32	Human	Functional	pAC50	=	4.6	4.6	-3235	14	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	302	5	4	4	3.6	C[C@@H](Cc1ccc(O)c(O)c1)[C@H](C)Cc1ccc(O)c(O)c1	10.1038/s41467-023-40064-9
	CHEMBL313972	106495	None	32	Human	Functional	pAC50	=	4.6	4.6	-3235	14	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	302	5	4	4	3.6	C[C@@H](Cc1ccc(O)c(O)c1)[C@H](C)Cc1ccc(O)c(O)c1	10.1038/s41467-023-40064-9
	68617	207985	None	33	Human	Functional	pAC50	=	4.6	4.6	-66	30	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	305	2	1	1	5.2	CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21	10.1038/s41467-023-40064-9
	CHEMBL1709	207985	None	33	Human	Functional	pAC50	=	4.6	4.6	-66	30	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	305	2	1	1	5.2	CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21	10.1038/s41467-023-40064-9
	CHEMBL809	207985	None	33	Human	Functional	pAC50	=	4.6	4.6	-66	30	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	305	2	1	1	5.2	CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21	10.1038/s41467-023-40064-9
	367	3824	None	10	Human	Functional	pAC50	=	6.6	6.6	-1548	8	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	392	4	1	6	2.3	O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3	10.1038/s41467-023-40064-9
	5487427	3824	None	10	Human	Functional	pAC50	=	6.6	6.6	-1548	8	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	392	4	1	6	2.3	O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3	10.1038/s41467-023-40064-9
	5487427.0	3824	None	10	Human	Functional	pAC50	=	6.6	6.6	-1548	8	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	392	4	1	6	2.3	O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3	10.1038/s41467-023-40064-9
	8592	3824	None	10	Human	Functional	pAC50	=	6.6	6.6	-1548	8	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	392	4	1	6	2.3	O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3	10.1038/s41467-023-40064-9
	CHEMBL1900528	3824	None	10	Human	Functional	pAC50	=	6.6	6.6	-1548	8	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	392	4	1	6	2.3	O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3	10.1038/s41467-023-40064-9
	CHEMBL3305968	3824	None	10	Human	Functional	pAC50	=	6.6	6.6	-1548	8	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	392	4	1	6	2.3	O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3	10.1038/s41467-023-40064-9
	CHEMBL4650755	3824	None	10	Human	Functional	pAC50	=	6.6	6.6	-1548	8	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	392	4	1	6	2.3	O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3	10.1038/s41467-023-40064-9
	DB01409	3824	None	10	Human	Functional	pAC50	=	6.6	6.6	-1548	8	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	392	4	1	6	2.3	O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3	10.1038/s41467-023-40064-9
	168871	89164	None	10	Human	Functional	pAC50	=	4.6	4.6	-1949	13	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	563	4	3	6	2.1	CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C[C@@H]4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12	10.1038/s41467-023-40064-9
	CHEMBL2365712	89164	None	10	Human	Functional	pAC50	=	4.6	4.6	-1949	13	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	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
	2771	197264	None	50	Human	Functional	pAC50	=	5.6	5.6	-25	16	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	324	5	0	3	3.8	CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21	10.1038/s41467-023-40064-9
	CHEMBL1200781	197264	None	50	Human	Functional	pAC50	=	5.6	5.6	-25	16	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	324	5	0	3	3.8	CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21	10.1038/s41467-023-40064-9
	CHEMBL549	197264	None	50	Human	Functional	pAC50	=	5.6	5.6	-25	16	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	324	5	0	3	3.8	CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21	10.1038/s41467-023-40064-9
	191	403	None	60	Human	Functional	pAC50	=	6.5	6.5	-21	36	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	313	0	1	4	3.4	Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1	10.1038/s41467-023-40064-9
	201	403	None	60	Human	Functional	pAC50	=	6.5	6.5	-21	36	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	313	0	1	4	3.4	Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1	10.1038/s41467-023-40064-9
	2170	403	None	60	Human	Functional	pAC50	=	6.5	6.5	-21	36	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	313	0	1	4	3.4	Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1	10.1038/s41467-023-40064-9
	2170.0	403	None	60	Human	Functional	pAC50	=	6.5	6.5	-21	36	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	313	0	1	4	3.4	Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1	10.1038/s41467-023-40064-9
	CHEMBL1113	403	None	60	Human	Functional	pAC50	=	6.5	6.5	-21	36	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	313	0	1	4	3.4	Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1	10.1038/s41467-023-40064-9
	DB00543	403	None	60	Human	Functional	pAC50	=	6.5	6.5	-21	36	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	313	0	1	4	3.4	Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1	10.1038/s41467-023-40064-9
	1400	1957	None	46	Human	Functional	pAC50	=	6.4	6.4	1	16	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	374	8	1	4	3.1	OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1	10.1038/s41467-023-40064-9
	3658	1957	None	46	Human	Functional	pAC50	=	6.4	6.4	1	16	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	374	8	1	4	3.1	OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1	10.1038/s41467-023-40064-9
	3658.0	1957	None	46	Human	Functional	pAC50	=	6.4	6.4	1	16	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	374	8	1	4	3.1	OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1	10.1038/s41467-023-40064-9
	7199	1957	None	46	Human	Functional	pAC50	=	6.4	6.4	1	16	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	374	8	1	4	3.1	OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1	10.1038/s41467-023-40064-9
	91513	1957	None	46	Human	Functional	pAC50	=	6.4	6.4	1	16	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	374	8	1	4	3.1	OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1	10.1038/s41467-023-40064-9
	CHEMBL896	1957	None	46	Human	Functional	pAC50	=	6.4	6.4	1	16	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	374	8	1	4	3.1	OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1	10.1038/s41467-023-40064-9
	DB00557	1957	None	46	Human	Functional	pAC50	=	6.4	6.4	1	16	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	374	8	1	4	3.1	OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1	10.1038/s41467-023-40064-9
	146570	43468	None	43	Human	Functional	pAC50	=	5.3	5.3	1	7	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	324	5	0	3	3.8	CN(C)CCC[C@@]1(c2ccc(F)cc2)OCc2cc(C#N)ccc21	10.1038/s41467-023-40064-9
	CHEMBL1508	43468	None	43	Human	Functional	pAC50	=	5.3	5.3	1	7	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	324	5	0	3	3.8	CN(C)CCC[C@@]1(c2ccc(F)cc2)OCc2cc(C#N)ccc21	10.1038/s41467-023-40064-9
	1210	918	None	42	Human	Functional	pAC50	=	7.3	7.3	-2	22	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	1213	918	None	42	Human	Functional	pAC50	=	7.3	7.3	-2	22	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	2725	918	None	42	Human	Functional	pAC50	=	7.3	7.3	-2	22	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	33036	918	None	42	Human	Functional	pAC50	=	7.3	7.3	-2	22	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	33036.0	918	None	42	Human	Functional	pAC50	=	7.3	7.3	-2	22	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	4411	918	None	42	Human	Functional	pAC50	=	7.3	7.3	-2	22	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	616	918	None	42	Human	Functional	pAC50	=	7.3	7.3	-2	22	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	6976	918	None	42	Human	Functional	pAC50	=	7.3	7.3	-2	22	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	716121	918	None	42	Human	Functional	pAC50	=	7.3	7.3	-2	22	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	CHEMBL1201353	918	None	42	Human	Functional	pAC50	=	7.3	7.3	-2	22	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	CHEMBL1554789	918	None	42	Human	Functional	pAC50	=	7.3	7.3	-2	22	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	CHEMBL505	918	None	42	Human	Functional	pAC50	=	7.3	7.3	-2	22	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	DB01114	918	None	42	Human	Functional	pAC50	=	7.3	7.3	-2	22	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	DB13679	918	None	42	Human	Functional	pAC50	=	7.3	7.3	-2	22	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	100	3805	None	44	Human	Functional	pAC50	=	6.2	6.2	-33	38	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	10.1038/s41467-023-40064-9
	2637	3805	None	44	Human	Functional	pAC50	=	6.2	6.2	-33	38	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	10.1038/s41467-023-40064-9
	5452	3805	None	44	Human	Functional	pAC50	=	6.2	6.2	-33	38	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	10.1038/s41467-023-40064-9
	CHEMBL479	3805	None	44	Human	Functional	pAC50	=	6.2	6.2	-33	38	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	10.1038/s41467-023-40064-9
	DB00679	3805	None	44	Human	Functional	pAC50	=	6.2	6.2	-33	38	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	10.1038/s41467-023-40064-9
	16351	102785	None	36	Human	Functional	pAC50	=	6.2	6.2	-18	17	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	343	0	0	4	4.1	CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1	10.1038/s41467-023-40064-9
	16351.0	102785	None	36	Human	Functional	pAC50	=	6.2	6.2	-18	17	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	343	0	0	4	4.1	CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1	10.1038/s41467-023-40064-9
	CHEMBL304902	102785	None	36	Human	Functional	pAC50	=	6.2	6.2	-18	17	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	343	0	0	4	4.1	CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1	10.1038/s41467-023-40064-9
	DB13256	102785	None	36	Human	Functional	pAC50	=	6.2	6.2	-18	17	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	343	0	0	4	4.1	CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1	10.1038/s41467-023-40064-9
	213	3853	None	34	Human	Functional	pAC50	=	6.2	6.2	-21	21	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	371	5	0	6	2.4	Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2	10.1038/s41467-023-40064-9
	2717	3853	None	34	Human	Functional	pAC50	=	6.2	6.2	-21	21	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	371	5	0	6	2.4	Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2	10.1038/s41467-023-40064-9
	5533	3853	None	34	Human	Functional	pAC50	=	6.2	6.2	-21	21	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	371	5	0	6	2.4	Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2	10.1038/s41467-023-40064-9
	5533.0	3853	None	34	Human	Functional	pAC50	=	6.2	6.2	-21	21	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	371	5	0	6	2.4	Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2	10.1038/s41467-023-40064-9
	CHEMBL621	3853	None	34	Human	Functional	pAC50	=	6.2	6.2	-21	21	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	371	5	0	6	2.4	Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2	10.1038/s41467-023-40064-9
	DB00656	3853	None	34	Human	Functional	pAC50	=	6.2	6.2	-21	21	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	371	5	0	6	2.4	Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2	10.1038/s41467-023-40064-9
	4640	78295	None	23	Human	Functional	pAC50	=	6.2	6.2	-9	11	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	379	6	1	4	3.9	COc1cc2[nH]c(C)c(CCN3CCN(c4ccccc4)CC3)c2cc1OC	10.1038/s41467-023-40064-9
	CHEMBL2107011	78295	None	23	Human	Functional	pAC50	=	6.2	6.2	-9	11	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	379	6	1	4	3.9	COc1cc2[nH]c(C)c(CCN3CCN(c4ccccc4)CC3)c2cc1OC	10.1038/s41467-023-40064-9
	19861	209982	None	33	Human	Functional	pAC50	=	7.2	7.2	3	10	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	290	0	0	2	3.7	CN1CCC(=C2c3ccccc3CCc3cccnc32)CC1	10.1038/s41467-023-40064-9
	19861.0	209982	None	33	Human	Functional	pAC50	=	7.2	7.2	3	10	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	290	0	0	2	3.7	CN1CCC(=C2c3ccccc3CCc3cccnc32)CC1	10.1038/s41467-023-40064-9
	CHEMBL946	209982	None	33	Human	Functional	pAC50	=	7.2	7.2	3	10	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	290	0	0	2	3.7	CN1CCC(=C2c3ccccc3CCc3cccnc32)CC1	10.1038/s41467-023-40064-9
	DB00719	209982	None	33	Human	Functional	pAC50	=	7.2	7.2	3	10	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	290	0	0	2	3.7	CN1CCC(=C2c3ccccc3CCc3cccnc32)CC1	10.1038/s41467-023-40064-9
	2220	3134	None	58	Human	Functional	pAC50	=	7.2	7.2	-6	17	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	295	0	0	2	4.4	CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1	10.1038/s41467-023-40064-9
	27400	3134	None	58	Human	Functional	pAC50	=	7.2	7.2	-6	17	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	295	0	0	2	4.4	CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1	10.1038/s41467-023-40064-9
	27400.0	3134	None	58	Human	Functional	pAC50	=	7.2	7.2	-6	17	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	295	0	0	2	4.4	CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1	10.1038/s41467-023-40064-9
	93	3134	None	58	Human	Functional	pAC50	=	7.2	7.2	-6	17	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	295	0	0	2	4.4	CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1	10.1038/s41467-023-40064-9
	CHEMBL294951	3134	None	58	Human	Functional	pAC50	=	7.2	7.2	-6	17	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	295	0	0	2	4.4	CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1	10.1038/s41467-023-40064-9
	DB06153	3134	None	58	Human	Functional	pAC50	=	7.2	7.2	-6	17	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	295	0	0	2	4.4	CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1	10.1038/s41467-023-40064-9
	1385580	29284	None	49	Human	Functional	pAC50	=	6.2	6.2	-18	19	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	426	7	1	4	4.1	O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1	10.1038/s41467-023-40064-9
	4615	29284	None	49	Human	Functional	pAC50	=	6.2	6.2	-18	19	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	426	7	1	4	4.1	O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1	10.1038/s41467-023-40064-9
	4615.0	29284	None	49	Human	Functional	pAC50	=	6.2	6.2	-18	19	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	426	7	1	4	4.1	O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1	10.1038/s41467-023-40064-9
	CHEMBL13828	29284	None	49	Human	Functional	pAC50	=	6.2	6.2	-18	19	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	426	7	1	4	4.1	O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1	10.1038/s41467-023-40064-9
	DB12877	29284	None	49	Human	Functional	pAC50	=	6.2	6.2	-18	19	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	426	7	1	4	4.1	O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1	10.1038/s41467-023-40064-9
	2470	3653	None	40	Human	Functional	pAC50	=	5.2	5.2	-38018	23	Agonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	395	6	1	4	3.2	Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1	10.1038/s41467-023-40064-9
	3300	3653	None	40	Human	Functional	pAC50	=	5.2	5.2	-38018	23	Agonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	395	6	1	4	3.2	Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1	10.1038/s41467-023-40064-9
	5265	3653	None	40	Human	Functional	pAC50	=	5.2	5.2	-38018	23	Agonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	395	6	1	4	3.2	Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1	10.1038/s41467-023-40064-9
	99	3653	None	40	Human	Functional	pAC50	=	5.2	5.2	-38018	23	Agonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	395	6	1	4	3.2	Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1	10.1038/s41467-023-40064-9
	CHEMBL267930	3653	None	40	Human	Functional	pAC50	=	5.2	5.2	-38018	23	Agonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	395	6	1	4	3.2	Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1	10.1038/s41467-023-40064-9
	2601	3780	None	25	Human	Functional	pAC50	=	5.1	5.1	-1288	17	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	340	3	2	2	2.9	CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC	10.1038/s41467-023-40064-9
	443951	3780	None	25	Human	Functional	pAC50	=	5.1	5.1	-1288	17	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	340	3	2	2	2.9	CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC	10.1038/s41467-023-40064-9
	56	3780	None	25	Human	Functional	pAC50	=	5.1	5.1	-1288	17	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	340	3	2	2	2.9	CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC	10.1038/s41467-023-40064-9
	CHEMBL73151	3780	None	25	Human	Functional	pAC50	=	5.1	5.1	-1288	17	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	340	3	2	2	2.9	CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC	10.1038/s41467-023-40064-9
	DB13399	3780	None	25	Human	Functional	pAC50	=	5.1	5.1	-1288	17	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	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
	2218	15289	None	20	Human	Functional	pAC50	=	5.1	5.1	-3	12	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	322	8	0	2	4.4	CCN(CC)CCCN(c1ccccc1)C1Cc2ccccc2C1	10.1038/s41467-023-40064-9
	CHEMBL1213033	15289	None	20	Human	Functional	pAC50	=	5.1	5.1	-3	12	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	322	8	0	2	4.4	CCN(CC)CCCN(c1ccccc1)C1Cc2ccccc2C1	10.1038/s41467-023-40064-9
	21722	17999	None	26	Human	Functional	pAC50	=	6.1	6.1	-1	21	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	284	4	0	2	4.3	CN(C)CCCn1c2c(c3ccccc31)CCCCCC2	10.1038/s41467-023-40064-9
	CHEMBL126224	17999	None	26	Human	Functional	pAC50	=	6.1	6.1	-1	21	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	284	4	0	2	4.3	CN(C)CCCn1c2c(c3ccccc31)CCCCCC2	10.1038/s41467-023-40064-9
	2247	505	None	55	Human	Functional	pAC50	=	6.0	6.0	-4	42	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	10.1038/s41467-023-40064-9
	249	505	None	55	Human	Functional	pAC50	=	6.0	6.0	-4	42	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	10.1038/s41467-023-40064-9
	2603	505	None	55	Human	Functional	pAC50	=	6.0	6.0	-4	42	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	10.1038/s41467-023-40064-9
	CHEMBL296419	505	None	55	Human	Functional	pAC50	=	6.0	6.0	-4	42	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	10.1038/s41467-023-40064-9
	DB00637	505	None	55	Human	Functional	pAC50	=	6.0	6.0	-4	42	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	10.1038/s41467-023-40064-9
	2333	142422	None	66	Human	Functional	pAC50	=	5.0	5.0	-7	14	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	422	3	1	3	5.5	CCc1oc2ccccc2c1C(=O)c1cc(Br)c(O)c(Br)c1	10.1038/s41467-023-40064-9
	CHEMBL388590	142422	None	66	Human	Functional	pAC50	=	5.0	5.0	-7	14	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	422	3	1	3	5.5	CCc1oc2ccccc2c1C(=O)c1cc(Br)c(O)c(Br)c1	10.1038/s41467-023-40064-9
	10042467	1426	None	1	Guinea pig	Functional	pEC50	=	6.9	6.9	-1	2	Effective concentration for agonism activity in Endothelium-Denuded guinea pig aortic segmentEffective concentration for agonism activity in Endothelium-Denuded guinea pig aortic segment	ChEMBL	333	8	1	2	4.3	CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C	10.1021/jm991056a
	1203	1426	None	1	Guinea pig	Functional	pEC50	=	6.9	6.9	-1	2	Effective concentration for agonism activity in Endothelium-Denuded guinea pig aortic segmentEffective concentration for agonism activity in Endothelium-Denuded guinea pig aortic segment	ChEMBL	333	8	1	2	4.3	CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C	10.1021/jm991056a
	CHEMBL11553	1426	None	1	Guinea pig	Functional	pEC50	=	6.9	6.9	-1	2	Effective concentration for agonism activity in Endothelium-Denuded guinea pig aortic segmentEffective concentration for agonism activity in Endothelium-Denuded guinea pig aortic segment	ChEMBL	333	8	1	2	4.3	CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C	10.1021/jm991056a
	10689833	12770	None	0	Rat	Functional	pEC50	=	5.9	5.9	-4	2	Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619	ChEMBL	359	8	1	2	4.8	c1ccc(C(CCc2nc(CCN3CCCC3)c[nH]2)c2ccccc2)cc1	10.1021/jm991056a
	CHEMBL11879	12770	None	0	Rat	Functional	pEC50	=	5.9	5.9	-4	2	Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619	ChEMBL	359	8	1	2	4.8	c1ccc(C(CCc2nc(CCN3CCCC3)c[nH]2)c2ccccc2)cc1	10.1021/jm991056a
	11791817	98356	None	0	Guinea pig	Functional	pEC50	=	6.8	6.8	-1	2	Effective concentration for agonist activity in guinea pig ileum whole segmentEffective concentration for agonist activity in guinea pig ileum whole segment	ChEMBL	345	9	2	2	4.5	c1ccc(C(CCc2nc(CCNC3CC3)c[nH]2)c2ccccc2)cc1	10.1021/jm991056a
	CHEMBL274831	98356	None	0	Guinea pig	Functional	pEC50	=	6.8	6.8	-1	2	Effective concentration for agonist activity in guinea pig ileum whole segmentEffective concentration for agonist activity in guinea pig ileum whole segment	ChEMBL	345	9	2	2	4.5	c1ccc(C(CCc2nc(CCNC3CC3)c[nH]2)c2ccccc2)cc1	10.1021/jm991056a
	10403687	2511	None	2	Rat	Functional	pEC50	=	6.8	6.8	-1	2	Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619	ChEMBL	319	8	2	2	3.9	CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm991056a
	1205	2511	None	2	Rat	Functional	pEC50	=	6.8	6.8	-1	2	Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619	ChEMBL	319	8	2	2	3.9	CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm991056a
	CHEMBL275035	2511	None	2	Rat	Functional	pEC50	=	6.8	6.8	-1	2	Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619	ChEMBL	319	8	2	2	3.9	CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm991056a
	1269	121	None	34	Human	Functional	pEC50	=	4.8	4.8	-354	6	Agonist activity at human histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase assayAgonist activity at human histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase assay	ChEMBL	125	2	2	2	0.2	Cc1c(CCN)nc[nH]1	10.1021/jm900526h
	37463	121	None	34	Human	Functional	pEC50	=	4.8	4.8	-354	6	Agonist activity at human histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase assayAgonist activity at human histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase assay	ChEMBL	125	2	2	2	0.2	Cc1c(CCN)nc[nH]1	10.1021/jm900526h
	CHEMBL275443	121	None	34	Human	Functional	pEC50	=	4.8	4.8	-354	6	Agonist activity at human histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase assayAgonist activity at human histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase assay	ChEMBL	125	2	2	2	0.2	Cc1c(CCN)nc[nH]1	10.1021/jm900526h
	126688	404	None	24	Human	Functional	pEC50	=	4.8	4.8	-57	2	Agonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay	ChEMBL	157	2	2	4	0.5	NCCc1sc(nc1C)N	10.1016/j.bmcl.2010.10.041
	4025	404	None	24	Human	Functional	pEC50	=	4.8	4.8	-57	2	Agonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay	ChEMBL	157	2	2	4	0.5	NCCc1sc(nc1C)N	10.1016/j.bmcl.2010.10.041
	CHEMBL293762	404	None	24	Human	Functional	pEC50	=	4.8	4.8	-57	2	Agonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay	ChEMBL	157	2	2	4	0.5	NCCc1sc(nc1C)N	10.1016/j.bmcl.2010.10.041
	11617365	74301	None	0	Guinea pig	Functional	pEC50	=	5.8	5.8	-	1	Agonist activity at histamine H1 receptor in guinea pig ileumAgonist activity at histamine H1 receptor in guinea pig ileum	ChEMBL	319	7	2	3	3.3	NCCc1c[nH]c(C(=O)CC(c2ccccc2)c2ccccc2)n1	10.1016/j.bmcl.2005.10.030
	CHEMBL202371	74301	None	0	Guinea pig	Functional	pEC50	=	5.8	5.8	-	1	Agonist activity at histamine H1 receptor in guinea pig ileumAgonist activity at histamine H1 receptor in guinea pig ileum	ChEMBL	319	7	2	3	3.3	NCCc1c[nH]c(C(=O)CC(c2ccccc2)c2ccccc2)n1	10.1016/j.bmcl.2005.10.030
	10042467	1426	None	1	Rat	Functional	pEC50	=	6.8	6.8	1	2	Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619	ChEMBL	333	8	1	2	4.3	CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C	10.1021/jm991056a
	1203	1426	None	1	Rat	Functional	pEC50	=	6.8	6.8	1	2	Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619	ChEMBL	333	8	1	2	4.3	CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C	10.1021/jm991056a
	CHEMBL11553	1426	None	1	Rat	Functional	pEC50	=	6.8	6.8	1	2	Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619	ChEMBL	333	8	1	2	4.3	CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C	10.1021/jm991056a
	10447834	1933	None	1	Guinea pig	Functional	pEC50	=	6.7	6.7	2	3	Effective concentration for agonist activity in guinea pig ileum whole segmentEffective concentration for agonist activity in guinea pig ileum whole segment	ChEMBL	305	7	2	2	3.7	NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm991056a
	4026	1933	None	1	Guinea pig	Functional	pEC50	=	6.7	6.7	2	3	Effective concentration for agonist activity in guinea pig ileum whole segmentEffective concentration for agonist activity in guinea pig ileum whole segment	ChEMBL	305	7	2	2	3.7	NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm991056a
	CHEMBL275507	1933	None	1	Guinea pig	Functional	pEC50	=	6.7	6.7	2	3	Effective concentration for agonist activity in guinea pig ileum whole segmentEffective concentration for agonist activity in guinea pig ileum whole segment	ChEMBL	305	7	2	2	3.7	NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm991056a
	1204	1932	None	74	Human	Functional	pEC50	=	6.7	6.7	-13	11	Agonist activity at human histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase assayAgonist activity at human histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm900526h
	1247	1932	None	74	Human	Functional	pEC50	=	6.7	6.7	-13	11	Agonist activity at human histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase assayAgonist activity at human histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm900526h
	1375	1932	None	74	Human	Functional	pEC50	=	6.7	6.7	-13	11	Agonist activity at human histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase assayAgonist activity at human histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm900526h
	774	1932	None	74	Human	Functional	pEC50	=	6.7	6.7	-13	11	Agonist activity at human histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase assayAgonist activity at human histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm900526h
	774.0	1932	None	74	Human	Functional	pEC50	=	6.7	6.7	-13	11	Agonist activity at human histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase assayAgonist activity at human histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm900526h
	CHEMBL90	1932	None	74	Human	Functional	pEC50	=	6.7	6.7	-13	11	Agonist activity at human histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase assayAgonist activity at human histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm900526h
	DB05381	1932	None	74	Human	Functional	pEC50	=	6.7	6.7	-13	11	Agonist activity at human histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase assayAgonist activity at human histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm900526h
	10447834	1933	None	1	Guinea pig	Functional	pEC50	=	5.7	5.7	2	3	Effective concentration for agonism activity in Endothelium-Denuded guinea pig aortic segmentEffective concentration for agonism activity in Endothelium-Denuded guinea pig aortic segment	ChEMBL	305	7	2	2	3.7	NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm991056a
	4026	1933	None	1	Guinea pig	Functional	pEC50	=	5.7	5.7	2	3	Effective concentration for agonism activity in Endothelium-Denuded guinea pig aortic segmentEffective concentration for agonism activity in Endothelium-Denuded guinea pig aortic segment	ChEMBL	305	7	2	2	3.7	NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm991056a
	CHEMBL275507	1933	None	1	Guinea pig	Functional	pEC50	=	5.7	5.7	2	3	Effective concentration for agonism activity in Endothelium-Denuded guinea pig aortic segmentEffective concentration for agonism activity in Endothelium-Denuded guinea pig aortic segment	ChEMBL	305	7	2	2	3.7	NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm991056a
	1204	1932	None	74	Guinea pig	Functional	pEC50	=	6.7	6.7	-10	11	Agonist activity at histamine H1 receptor in guinea pig ileumAgonist activity at histamine H1 receptor in guinea pig ileum	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2005.10.030
	1247	1932	None	74	Guinea pig	Functional	pEC50	=	6.7	6.7	-10	11	Agonist activity at histamine H1 receptor in guinea pig ileumAgonist activity at histamine H1 receptor in guinea pig ileum	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2005.10.030
	1375	1932	None	74	Guinea pig	Functional	pEC50	=	6.7	6.7	-10	11	Agonist activity at histamine H1 receptor in guinea pig ileumAgonist activity at histamine H1 receptor in guinea pig ileum	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2005.10.030
	774	1932	None	74	Guinea pig	Functional	pEC50	=	6.7	6.7	-10	11	Agonist activity at histamine H1 receptor in guinea pig ileumAgonist activity at histamine H1 receptor in guinea pig ileum	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2005.10.030
	774.0	1932	None	74	Guinea pig	Functional	pEC50	=	6.7	6.7	-10	11	Agonist activity at histamine H1 receptor in guinea pig ileumAgonist activity at histamine H1 receptor in guinea pig ileum	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2005.10.030
	CHEMBL90	1932	None	74	Guinea pig	Functional	pEC50	=	6.7	6.7	-10	11	Agonist activity at histamine H1 receptor in guinea pig ileumAgonist activity at histamine H1 receptor in guinea pig ileum	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2005.10.030
	DB05381	1932	None	74	Guinea pig	Functional	pEC50	=	6.7	6.7	-10	11	Agonist activity at histamine H1 receptor in guinea pig ileumAgonist activity at histamine H1 receptor in guinea pig ileum	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2005.10.030
	1194	45	None	1	Human	Functional	pEC50	=	6.7	6.7	50	2	Agonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay	ChEMBL	265	3	2	2	2.3	NCCc1cnc([nH]1)c1cccc(c1)Br	10.1016/j.bmcl.2010.10.041
	23786499	45	None	1	Human	Functional	pEC50	=	6.7	6.7	50	2	Agonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay	ChEMBL	265	3	2	2	2.3	NCCc1cnc([nH]1)c1cccc(c1)Br	10.1016/j.bmcl.2010.10.041
	CHEMBL26116	45	None	1	Human	Functional	pEC50	=	6.7	6.7	50	2	Agonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay	ChEMBL	265	3	2	2	2.3	NCCc1cnc([nH]1)c1cccc(c1)Br	10.1016/j.bmcl.2010.10.041
	1204	1932	None	74	Human	Functional	pEC50	=	6.7	6.7	-13	11	Agonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2010.10.041
	1247	1932	None	74	Human	Functional	pEC50	=	6.7	6.7	-13	11	Agonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2010.10.041
	1375	1932	None	74	Human	Functional	pEC50	=	6.7	6.7	-13	11	Agonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2010.10.041
	774	1932	None	74	Human	Functional	pEC50	=	6.7	6.7	-13	11	Agonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2010.10.041
	774.0	1932	None	74	Human	Functional	pEC50	=	6.7	6.7	-13	11	Agonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2010.10.041
	CHEMBL90	1932	None	74	Human	Functional	pEC50	=	6.7	6.7	-13	11	Agonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2010.10.041
	DB05381	1932	None	74	Human	Functional	pEC50	=	6.7	6.7	-13	11	Agonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2010.10.041
	11791817	98356	None	0	Guinea pig	Functional	pEC50	=	5.6	5.6	-1	2	Effective concentration for agonism activity in endothelium-denuded guinea pig aortic segmentEffective concentration for agonism activity in endothelium-denuded guinea pig aortic segment	ChEMBL	345	9	2	2	4.5	c1ccc(C(CCc2nc(CCNC3CC3)c[nH]2)c2ccccc2)cc1	10.1021/jm991056a
	CHEMBL274831	98356	None	0	Guinea pig	Functional	pEC50	=	5.6	5.6	-1	2	Effective concentration for agonism activity in endothelium-denuded guinea pig aortic segmentEffective concentration for agonism activity in endothelium-denuded guinea pig aortic segment	ChEMBL	345	9	2	2	4.5	c1ccc(C(CCc2nc(CCNC3CC3)c[nH]2)c2ccccc2)cc1	10.1021/jm991056a
	5310982	93665	None	1	Human	Functional	pEC50	=	6.6	6.6	3	2	Agonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay	ChEMBL	255	3	2	2	2.6	NCCc1c[nH]c(-c2cccc(C(F)(F)F)c2)n1	10.1016/j.bmcl.2010.10.041
	CHEMBL24665	93665	None	1	Human	Functional	pEC50	=	6.6	6.6	3	2	Agonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay	ChEMBL	255	3	2	2	2.6	NCCc1c[nH]c(-c2cccc(C(F)(F)F)c2)n1	10.1016/j.bmcl.2010.10.041
	44267376	10223	None	0	Guinea pig	Functional	pEC50	=	5.6	5.6	-	1	Effective concentration for agonist activity in guinea pig ileum whole segmentEffective concentration for agonist activity in guinea pig ileum whole segment	ChEMBL	277	5	2	2	3.1	NCCc1c[nH]c(C(c2ccccc2)c2ccccc2)n1	10.1021/jm991056a
	CHEMBL11603	10223	None	0	Guinea pig	Functional	pEC50	=	5.6	5.6	-	1	Effective concentration for agonist activity in guinea pig ileum whole segmentEffective concentration for agonist activity in guinea pig ileum whole segment	ChEMBL	277	5	2	2	3.1	NCCc1c[nH]c(C(c2ccccc2)c2ccccc2)n1	10.1021/jm991056a
	10689833	12770	None	0	Guinea pig	Functional	pEC50	=	6.5	6.5	4	2	Effective concentration for agonist activity in guinea pig ileum whole segmentEffective concentration for agonist activity in guinea pig ileum whole segment	ChEMBL	359	8	1	2	4.8	c1ccc(C(CCc2nc(CCN3CCCC3)c[nH]2)c2ccccc2)cc1	10.1021/jm991056a
	CHEMBL11879	12770	None	0	Guinea pig	Functional	pEC50	=	6.5	6.5	4	2	Effective concentration for agonist activity in guinea pig ileum whole segmentEffective concentration for agonist activity in guinea pig ileum whole segment	ChEMBL	359	8	1	2	4.8	c1ccc(C(CCc2nc(CCN3CCCC3)c[nH]2)c2ccccc2)cc1	10.1021/jm991056a
	10688111	10042	None	1	Guinea pig	Functional	pEC50	=	6.5	6.5	2	2	Effective concentration for agonist activity in guinea pig ileum whole segmentEffective concentration for agonist activity in guinea pig ileum whole segment	ChEMBL	333	9	2	2	4.3	CCNCCc1c[nH]c(CCC(c2ccccc2)c2ccccc2)n1	10.1021/jm991056a
	CHEMBL11515	10042	None	1	Guinea pig	Functional	pEC50	=	6.5	6.5	2	2	Effective concentration for agonist activity in guinea pig ileum whole segmentEffective concentration for agonist activity in guinea pig ileum whole segment	ChEMBL	333	9	2	2	4.3	CCNCCc1c[nH]c(CCC(c2ccccc2)c2ccccc2)n1	10.1021/jm991056a
	10447834	1933	None	1	Guinea pig	Functional	pEC50	=	6.5	6.5	2	3	Effective concentration for agonism activity in Endothelium-Denuded guinea pig aortic segmentEffective concentration for agonism activity in Endothelium-Denuded guinea pig aortic segment	ChEMBL	305	7	2	2	3.7	NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm991056a
	4026	1933	None	1	Guinea pig	Functional	pEC50	=	6.5	6.5	2	3	Effective concentration for agonism activity in Endothelium-Denuded guinea pig aortic segmentEffective concentration for agonism activity in Endothelium-Denuded guinea pig aortic segment	ChEMBL	305	7	2	2	3.7	NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm991056a
	CHEMBL275507	1933	None	1	Guinea pig	Functional	pEC50	=	6.5	6.5	2	3	Effective concentration for agonism activity in Endothelium-Denuded guinea pig aortic segmentEffective concentration for agonism activity in Endothelium-Denuded guinea pig aortic segment	ChEMBL	305	7	2	2	3.7	NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm991056a
	11791817	98356	None	0	Rat	Functional	pEC50	=	6.5	6.5	1	2	Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619	ChEMBL	345	9	2	2	4.5	c1ccc(C(CCc2nc(CCNC3CC3)c[nH]2)c2ccccc2)cc1	10.1021/jm991056a
	CHEMBL274831	98356	None	0	Rat	Functional	pEC50	=	6.5	6.5	1	2	Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619	ChEMBL	345	9	2	2	4.5	c1ccc(C(CCc2nc(CCNC3CC3)c[nH]2)c2ccccc2)cc1	10.1021/jm991056a
	10685002	10162	None	0	Guinea pig	Functional	pEC50	=	4.4	4.4	-	1	Effective concentration for agonist activity in guinea pig ileum whole segmentEffective concentration for agonist activity in guinea pig ileum whole segment	ChEMBL	291	6	2	2	3.3	NCCc1c[nH]c(CC(c2ccccc2)c2ccccc2)n1	10.1021/jm991056a
	CHEMBL11584	10162	None	0	Guinea pig	Functional	pEC50	=	4.4	4.4	-	1	Effective concentration for agonist activity in guinea pig ileum whole segmentEffective concentration for agonist activity in guinea pig ileum whole segment	ChEMBL	291	6	2	2	3.3	NCCc1c[nH]c(CC(c2ccccc2)c2ccccc2)n1	10.1021/jm991056a
	1204	1932	None	74	Human	Functional	pEC50	=	7.4	7.4	-13	11	Agonist activity at human H1 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H1 receptor expressed in 293-EBNA cells by luciferase reporter gene assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm0603318
	1247	1932	None	74	Human	Functional	pEC50	=	7.4	7.4	-13	11	Agonist activity at human H1 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H1 receptor expressed in 293-EBNA cells by luciferase reporter gene assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm0603318
	1375	1932	None	74	Human	Functional	pEC50	=	7.4	7.4	-13	11	Agonist activity at human H1 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H1 receptor expressed in 293-EBNA cells by luciferase reporter gene assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm0603318
	774	1932	None	74	Human	Functional	pEC50	=	7.4	7.4	-13	11	Agonist activity at human H1 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H1 receptor expressed in 293-EBNA cells by luciferase reporter gene assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm0603318
	774.0	1932	None	74	Human	Functional	pEC50	=	7.4	7.4	-13	11	Agonist activity at human H1 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H1 receptor expressed in 293-EBNA cells by luciferase reporter gene assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm0603318
	CHEMBL90	1932	None	74	Human	Functional	pEC50	=	7.4	7.4	-13	11	Agonist activity at human H1 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H1 receptor expressed in 293-EBNA cells by luciferase reporter gene assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm0603318
	DB05381	1932	None	74	Human	Functional	pEC50	=	7.4	7.4	-13	11	Agonist activity at human H1 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H1 receptor expressed in 293-EBNA cells by luciferase reporter gene assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm0603318
	10403687	2511	None	2	Guinea pig	Functional	pEC50	=	6.3	6.3	1	2	Effective concentration for agonism activity in endothelium-denuded guinea pig aortic segmentEffective concentration for agonism activity in endothelium-denuded guinea pig aortic segment	ChEMBL	319	8	2	2	3.9	CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm991056a
	1205	2511	None	2	Guinea pig	Functional	pEC50	=	6.3	6.3	1	2	Effective concentration for agonism activity in endothelium-denuded guinea pig aortic segmentEffective concentration for agonism activity in endothelium-denuded guinea pig aortic segment	ChEMBL	319	8	2	2	3.9	CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm991056a
	CHEMBL275035	2511	None	2	Guinea pig	Functional	pEC50	=	6.3	6.3	1	2	Effective concentration for agonism activity in endothelium-denuded guinea pig aortic segmentEffective concentration for agonism activity in endothelium-denuded guinea pig aortic segment	ChEMBL	319	8	2	2	3.9	CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm991056a
	10403687	2511	None	2	Guinea pig	Functional	pEC50	=	7.2	7.2	1	2	Effective concentration for agonist activity in guinea pig ileum whole segmentEffective concentration for agonist activity in guinea pig ileum whole segment	ChEMBL	319	8	2	2	3.9	CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm991056a
	1205	2511	None	2	Guinea pig	Functional	pEC50	=	7.2	7.2	1	2	Effective concentration for agonist activity in guinea pig ileum whole segmentEffective concentration for agonist activity in guinea pig ileum whole segment	ChEMBL	319	8	2	2	3.9	CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm991056a
	CHEMBL275035	2511	None	2	Guinea pig	Functional	pEC50	=	7.2	7.2	1	2	Effective concentration for agonist activity in guinea pig ileum whole segmentEffective concentration for agonist activity in guinea pig ileum whole segment	ChEMBL	319	8	2	2	3.9	CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm991056a
	11846300	80297	None	3	Human	Functional	pEC50	=	8.2	8.2	2	2	Activity at human histamine H1 receptor transfected in COS7 cells by NF-kappaB luciferase reporter assayActivity at human histamine H1 receptor transfected in COS7 cells by NF-kappaB luciferase reporter assay	ChEMBL	327	0	0	4	3.8	CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1	10.1021/jm051008s
	CHEMBL213912	80297	None	3	Human	Functional	pEC50	=	8.2	8.2	2	2	Activity at human histamine H1 receptor transfected in COS7 cells by NF-kappaB luciferase reporter assayActivity at human histamine H1 receptor transfected in COS7 cells by NF-kappaB luciferase reporter assay	ChEMBL	327	0	0	4	3.8	CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1	10.1021/jm051008s
	10688111	10042	None	1	Rat	Functional	pEC50	=	6.2	6.2	-2	2	Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619	ChEMBL	333	9	2	2	4.3	CCNCCc1c[nH]c(CCC(c2ccccc2)c2ccccc2)n1	10.1021/jm991056a
	CHEMBL11515	10042	None	1	Rat	Functional	pEC50	=	6.2	6.2	-2	2	Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619	ChEMBL	333	9	2	2	4.3	CCNCCc1c[nH]c(CCC(c2ccccc2)c2ccccc2)n1	10.1021/jm991056a
	10403687	2511	None	2	Guinea pig	Functional	pEC50	=	7.1	7.1	1	2	Effective concentration for agonism activity in Endothelium-Denuded guinea pig aortic segmentEffective concentration for agonism activity in Endothelium-Denuded guinea pig aortic segment	ChEMBL	319	8	2	2	3.9	CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm991056a
	1205	2511	None	2	Guinea pig	Functional	pEC50	=	7.1	7.1	1	2	Effective concentration for agonism activity in Endothelium-Denuded guinea pig aortic segmentEffective concentration for agonism activity in Endothelium-Denuded guinea pig aortic segment	ChEMBL	319	8	2	2	3.9	CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm991056a
	CHEMBL275035	2511	None	2	Guinea pig	Functional	pEC50	=	7.1	7.1	1	2	Effective concentration for agonism activity in Endothelium-Denuded guinea pig aortic segmentEffective concentration for agonism activity in Endothelium-Denuded guinea pig aortic segment	ChEMBL	319	8	2	2	3.9	CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm991056a
	91613	17994	None	20	Human	Functional	pEC50	=	6.1	6.1	5	2	Agonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay	ChEMBL	125	2	2	2	0.2	Cc1ncc(CCN)[nH]1	10.1016/j.bmcl.2010.10.041
	CHEMBL12620	17994	None	20	Human	Functional	pEC50	=	6.1	6.1	5	2	Agonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay	ChEMBL	125	2	2	2	0.2	Cc1ncc(CCN)[nH]1	10.1016/j.bmcl.2010.10.041
	10042467	1426	None	1	Guinea pig	Functional	pEC50	=	7.1	7.1	-1	2	Effective concentration for agonist activity in guinea pig ileum whole segmentEffective concentration for agonist activity in guinea pig ileum whole segment	ChEMBL	333	8	1	2	4.3	CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C	10.1021/jm991056a
	1203	1426	None	1	Guinea pig	Functional	pEC50	=	7.1	7.1	-1	2	Effective concentration for agonist activity in guinea pig ileum whole segmentEffective concentration for agonist activity in guinea pig ileum whole segment	ChEMBL	333	8	1	2	4.3	CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C	10.1021/jm991056a
	CHEMBL11553	1426	None	1	Guinea pig	Functional	pEC50	=	7.1	7.1	-1	2	Effective concentration for agonist activity in guinea pig ileum whole segmentEffective concentration for agonist activity in guinea pig ileum whole segment	ChEMBL	333	8	1	2	4.3	CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C	10.1021/jm991056a
	10042467	1426	None	1	Guinea pig	Functional	pEC50	=	6.1	6.1	-1	2	Effective concentration for agonism activity in endothelium-denuded guinea pig aortic segmentEffective concentration for agonism activity in endothelium-denuded guinea pig aortic segment	ChEMBL	333	8	1	2	4.3	CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C	10.1021/jm991056a
	1203	1426	None	1	Guinea pig	Functional	pEC50	=	6.1	6.1	-1	2	Effective concentration for agonism activity in endothelium-denuded guinea pig aortic segmentEffective concentration for agonism activity in endothelium-denuded guinea pig aortic segment	ChEMBL	333	8	1	2	4.3	CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C	10.1021/jm991056a
	CHEMBL11553	1426	None	1	Guinea pig	Functional	pEC50	=	6.1	6.1	-1	2	Effective concentration for agonism activity in endothelium-denuded guinea pig aortic segmentEffective concentration for agonism activity in endothelium-denuded guinea pig aortic segment	ChEMBL	333	8	1	2	4.3	CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C	10.1021/jm991056a
	10447834	1933	None	1	Rat	Functional	pEC50	=	6.1	6.1	-2	3	Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619	ChEMBL	305	7	2	2	3.7	NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm991056a
	4026	1933	None	1	Rat	Functional	pEC50	=	6.1	6.1	-2	3	Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619	ChEMBL	305	7	2	2	3.7	NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm991056a
	CHEMBL275507	1933	None	1	Rat	Functional	pEC50	=	6.1	6.1	-2	3	Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619	ChEMBL	305	7	2	2	3.7	NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm991056a
	11976	920	None	44	Human	Functional	pIC50	=	9	9.0	-9	16	Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay	ChEMBL	315	3	0	2	5.2	CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl	10.1021/jm300671m
	667467	920	None	44	Human	Functional	pIC50	=	9	9.0	-9	16	Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay	ChEMBL	315	3	0	2	5.2	CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl	10.1021/jm300671m
	667467.0	920	None	44	Human	Functional	pIC50	=	9	9.0	-9	16	Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay	ChEMBL	315	3	0	2	5.2	CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl	10.1021/jm300671m
	CHEMBL908	920	None	44	Human	Functional	pIC50	=	9	9.0	-9	16	Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay	ChEMBL	315	3	0	2	5.2	CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl	10.1021/jm300671m
	DB01239	920	None	44	Human	Functional	pIC50	=	9	9.0	-9	16	Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay	ChEMBL	315	3	0	2	5.2	CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl	10.1021/jm300671m
	13623342	64368	None	0	Guinea pig	Functional	pIC50	=	8	8.0	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	286	5	0	5	1.9	C=COCCn1c(N2CCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	CHEMBL18123	64368	None	0	Guinea pig	Functional	pIC50	=	8	8.0	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	286	5	0	5	1.9	C=COCCn1c(N2CCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	3071006	65036	None	0	Guinea pig	Functional	pIC50	=	8	8.0	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	314	6	0	5	2.4	C=CCOCCn1c(N2CCCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	CHEMBL18233	65036	None	0	Guinea pig	Functional	pIC50	=	8	8.0	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	314	6	0	5	2.4	C=CCOCCn1c(N2CCCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	13623366	66735	None	0	Guinea pig	Functional	pIC50	=	8	8.0	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	330	7	0	5	3.0	CCCCOCCn1c(N2CCCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	CHEMBL18561	66735	None	0	Guinea pig	Functional	pIC50	=	8	8.0	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	330	7	0	5	3.0	CCCCOCCn1c(N2CCCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	3071004	167863	None	4	Guinea pig	Functional	pIC50	=	8	8.0	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	288	5	0	5	1.8	CCOCCn1c(N2CCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	CHEMBL430338	167863	None	4	Guinea pig	Functional	pIC50	=	8	8.0	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	288	5	0	5	1.8	CCOCCn1c(N2CCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	1227	2489	None	32	Human	Functional	pIC50	=	8	8.0	2	14	Inverse agonist activity at human wild-type histamine H1 receptor assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assayInverse agonist activity at human wild-type histamine H1 receptor assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assay	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1038/nchembio714
	2331	2489	None	32	Human	Functional	pIC50	=	8	8.0	2	14	Inverse agonist activity at human wild-type histamine H1 receptor assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assayInverse agonist activity at human wild-type histamine H1 receptor assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assay	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1038/nchembio714
	3957	2489	None	32	Human	Functional	pIC50	=	8	8.0	2	14	Inverse agonist activity at human wild-type histamine H1 receptor assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assayInverse agonist activity at human wild-type histamine H1 receptor assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assay	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1038/nchembio714
	4992	2489	None	32	Human	Functional	pIC50	=	8	8.0	2	14	Inverse agonist activity at human wild-type histamine H1 receptor assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assayInverse agonist activity at human wild-type histamine H1 receptor assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assay	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1038/nchembio714
	4992.0	2489	None	32	Human	Functional	pIC50	=	8	8.0	2	14	Inverse agonist activity at human wild-type histamine H1 receptor assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assayInverse agonist activity at human wild-type histamine H1 receptor assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assay	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1038/nchembio714
	CHEMBL511	2489	None	32	Human	Functional	pIC50	=	8	8.0	2	14	Inverse agonist activity at human wild-type histamine H1 receptor assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assayInverse agonist activity at human wild-type histamine H1 receptor assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assay	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1038/nchembio714
	DB06691	2489	None	32	Human	Functional	pIC50	=	8	8.0	2	14	Inverse agonist activity at human wild-type histamine H1 receptor assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assayInverse agonist activity at human wild-type histamine H1 receptor assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assay	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1038/nchembio714
	44458944	99114	None	0	Guinea pig	Functional	pIC50	=	8.0	8.0	-	1	In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileumIn vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum	ChEMBL	337	3	0	1	5.5	c1ccc(CN2CCC3C(=C(c4ccccc4)c4ccccc43)C2)cc1	10.1016/s0960-894x(00)00199-2
	CHEMBL280432	99114	None	0	Guinea pig	Functional	pIC50	=	8.0	8.0	-	1	In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileumIn vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum	ChEMBL	337	3	0	1	5.5	c1ccc(CN2CCC3C(=C(c4ccccc4)c4ccccc43)C2)cc1	10.1016/s0960-894x(00)00199-2
	44224259	62743	None	4	Human	Functional	pIC50	=	7	7.0	30	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay	ChEMBL	291	3	0	3	3.3	CN1CCc2c(c3ccccc3n2CCc2cccnc2)C1	10.1016/j.bmcl.2009.04.128
	CHEMBL1783959	62743	None	4	Human	Functional	pIC50	=	7	7.0	30	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay	ChEMBL	291	3	0	3	3.3	CN1CCc2c(c3ccccc3n2CCc2cccnc2)C1	10.1016/j.bmcl.2009.04.128
	3529324	210813	None	1	Guinea pig	Functional	pIC50	=	6	6.0	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	306	6	0	3	3.3	CC(C)c1ccc(C2SCC(=O)N2CCCN(C)C)cc1	10.1021/jm00093a025
	CHEMBL1202934	210813	None	1	Guinea pig	Functional	pIC50	=	6	6.0	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	306	6	0	3	3.3	CC(C)c1ccc(C2SCC(=O)N2CCCN(C)C)cc1	10.1021/jm00093a025
	CHEMBL99417	210813	None	1	Guinea pig	Functional	pIC50	=	6	6.0	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	306	6	0	3	3.3	CC(C)c1ccc(C2SCC(=O)N2CCCN(C)C)cc1	10.1021/jm00093a025
	44126329	62738	None	5	Human	Functional	pIC50	=	5	5.0	-2	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assay	ChEMBL	305	3	0	3	3.6	Cc1ccc2c(c1)c1c(n2CCc2ccccn2)CCN(C)C1	10.1016/j.bmcl.2009.04.128
	CHEMBL1783954	62738	None	5	Human	Functional	pIC50	=	5	5.0	-2	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assay	ChEMBL	305	3	0	3	3.6	Cc1ccc2c(c1)c1c(n2CCc2ccccn2)CCN(C)C1	10.1016/j.bmcl.2009.04.128
	153996	112731	None	0	Human	Functional	pIC50	=	5	5.0	-57	6	Compound was evaluated for the antagonistic activity against H1 receptorCompound was evaluated for the antagonistic activity against H1 receptor	ChEMBL	639	10	1	6	5.7	COc1cc(C(=O)N2CC[C@](CCN3CCC(C(N)=O)(c4ccccc4)CC3)(c3ccc(Cl)c(Cl)c3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10097-X
	CHEMBL330366	112731	None	0	Human	Functional	pIC50	=	5	5.0	-57	6	Compound was evaluated for the antagonistic activity against H1 receptorCompound was evaluated for the antagonistic activity against H1 receptor	ChEMBL	639	10	1	6	5.7	COc1cc(C(=O)N2CC[C@](CCN3CCC(C(N)=O)(c4ccccc4)CC3)(c3ccc(Cl)c(Cl)c3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10097-X
	CHEMBL539021	112731	None	0	Human	Functional	pIC50	=	5	5.0	-57	6	Compound was evaluated for the antagonistic activity against H1 receptorCompound was evaluated for the antagonistic activity against H1 receptor	ChEMBL	639	10	1	6	5.7	COc1cc(C(=O)N2CC[C@](CCN3CCC(C(N)=O)(c4ccccc4)CC3)(c3ccc(Cl)c(Cl)c3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10097-X
	44126270	201607	None	5	Human	Functional	pIC50	=	7.0	7.0	10	2	Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge	ChEMBL	320	4	0	3	3.9	COc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1	10.1016/j.bmcl.2009.11.037
	CHEMBL589389	201607	None	5	Human	Functional	pIC50	=	7.0	7.0	10	2	Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge	ChEMBL	320	4	0	3	3.9	COc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1	10.1016/j.bmcl.2009.11.037
	3071008	98803	None	0	Guinea pig	Functional	pIC50	=	8.0	8.0	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	274	5	1	5	1.5	CCOCCn1c(N2CCNCC2)nc2ccccc21	10.1021/jm00157a010
	CHEMBL278053	98803	None	0	Guinea pig	Functional	pIC50	=	8.0	8.0	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	274	5	1	5	1.5	CCOCCn1c(N2CCNCC2)nc2ccccc21	10.1021/jm00157a010
	54585846	62747	None	4	Human	Functional	pIC50	=	7.0	7.0	38	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay	ChEMBL	323	3	0	3	3.7	Cc1ccc(CCn2c3c(c4cc(F)ccc42)CN(C)CC3)cn1	10.1016/j.bmcl.2009.04.128
	CHEMBL1783963	62747	None	4	Human	Functional	pIC50	=	7.0	7.0	38	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay	ChEMBL	323	3	0	3	3.7	Cc1ccc(CCn2c3c(c4cc(F)ccc42)CN(C)CC3)cn1	10.1016/j.bmcl.2009.04.128
	44126269	203941	None	4	Human	Functional	pIC50	=	7.0	7.0	2	2	Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge	ChEMBL	318	3	0	2	4.5	Cc1ccc(CCn2c3c(c4cc(C)ccc42)CN(C)CC3)cc1	10.1016/j.bmcl.2009.11.037
	CHEMBL605081	203941	None	4	Human	Functional	pIC50	=	7.0	7.0	2	2	Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge	ChEMBL	318	3	0	2	4.5	Cc1ccc(CCn2c3c(c4cc(C)ccc42)CN(C)CC3)cc1	10.1016/j.bmcl.2009.11.037
	1210	918	None	42	Guinea pig	Functional	pIC50	=	7.9	7.9	2	22	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1021/jm00157a010
	1213	918	None	42	Guinea pig	Functional	pIC50	=	7.9	7.9	2	22	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1021/jm00157a010
	2725	918	None	42	Guinea pig	Functional	pIC50	=	7.9	7.9	2	22	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1021/jm00157a010
	33036	918	None	42	Guinea pig	Functional	pIC50	=	7.9	7.9	2	22	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1021/jm00157a010
	33036.0	918	None	42	Guinea pig	Functional	pIC50	=	7.9	7.9	2	22	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1021/jm00157a010
	4411	918	None	42	Guinea pig	Functional	pIC50	=	7.9	7.9	2	22	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1021/jm00157a010
	616	918	None	42	Guinea pig	Functional	pIC50	=	7.9	7.9	2	22	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1021/jm00157a010
	6976	918	None	42	Guinea pig	Functional	pIC50	=	7.9	7.9	2	22	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1021/jm00157a010
	716121	918	None	42	Guinea pig	Functional	pIC50	=	7.9	7.9	2	22	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1021/jm00157a010
	CHEMBL1201353	918	None	42	Guinea pig	Functional	pIC50	=	7.9	7.9	2	22	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1021/jm00157a010
	CHEMBL1554789	918	None	42	Guinea pig	Functional	pIC50	=	7.9	7.9	2	22	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1021/jm00157a010
	CHEMBL505	918	None	42	Guinea pig	Functional	pIC50	=	7.9	7.9	2	22	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1021/jm00157a010
	DB01114	918	None	42	Guinea pig	Functional	pIC50	=	7.9	7.9	2	22	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1021/jm00157a010
	DB13679	918	None	42	Guinea pig	Functional	pIC50	=	7.9	7.9	2	22	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1021/jm00157a010
	3071000	98709	None	0	Guinea pig	Functional	pIC50	=	7.9	7.9	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	298	5	0	5	1.4	C#CCOCCn1c(N2CCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	CHEMBL277311	98709	None	0	Guinea pig	Functional	pIC50	=	7.9	7.9	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	298	5	0	5	1.4	C#CCOCCn1c(N2CCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	54582939	62741	None	5	Human	Functional	pIC50	=	6.9	6.9	8	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay	ChEMBL	369	3	0	3	4.0	CN1CCc2c(c3cc(Br)ccc3n2CCc2ccccn2)C1	10.1016/j.bmcl.2009.04.128
	CHEMBL1783957	62741	None	5	Human	Functional	pIC50	=	6.9	6.9	8	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay	ChEMBL	369	3	0	3	4.0	CN1CCc2c(c3cc(Br)ccc3n2CCc2ccccn2)C1	10.1016/j.bmcl.2009.04.128
	54579957	62748	None	4	Human	Functional	pIC50	=	6.9	6.9	36	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay	ChEMBL	291	3	0	3	3.3	CN1CCc2c(c3ccccc3n2CCc2ccncc2)C1	10.1016/j.bmcl.2009.04.128
	CHEMBL1783964	62748	None	4	Human	Functional	pIC50	=	6.9	6.9	36	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay	ChEMBL	291	3	0	3	3.3	CN1CCc2c(c3ccccc3n2CCc2ccncc2)C1	10.1016/j.bmcl.2009.04.128
	54580942	62751	None	7	Human	Functional	pIC50	=	6.9	6.9	13	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay	ChEMBL	309	3	0	3	3.4	CN1CCc2c(c3cc(F)ccc3n2CCc2ccncc2)C1	10.1016/j.bmcl.2009.04.128
	CHEMBL1783967	62751	None	7	Human	Functional	pIC50	=	6.9	6.9	13	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay	ChEMBL	309	3	0	3	3.4	CN1CCc2c(c3cc(F)ccc3n2CCc2ccncc2)C1	10.1016/j.bmcl.2009.04.128
	4440380	4256	None	1	Guinea pig	Functional	pIC50	=	5.9	5.9	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	278	5	0	3	2.5	Cc1ccc(C2SCC(=O)N2CCCN(C)C)cc1	10.1021/jm00093a025
	CHEMBL100487	4256	None	1	Guinea pig	Functional	pIC50	=	5.9	5.9	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	278	5	0	3	2.5	Cc1ccc(C2SCC(=O)N2CCCN(C)C)cc1	10.1021/jm00093a025
	CHEMBL1202938	4256	None	1	Guinea pig	Functional	pIC50	=	5.9	5.9	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	278	5	0	3	2.5	Cc1ccc(C2SCC(=O)N2CCCN(C)C)cc1	10.1021/jm00093a025
	10234086	111697	None	0	Human	Functional	pIC50	=	5.9	5.9	-6	2	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	744	13	0	10	6.7	COC(=O)c1ccc(Cn2c(C(=O)C3CCN(CCC4(c5ccccc5)CCN(C(=O)c5cc(OC)c(OC)c(OC)c5)C4)CC3)nc3ccccc32)cc1	10.1016/S0960-894X(97)10097-X
	CHEMBL328511	111697	None	0	Human	Functional	pIC50	=	5.9	5.9	-6	2	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	744	13	0	10	6.7	COC(=O)c1ccc(Cn2c(C(=O)C3CCN(CCC4(c5ccccc5)CCN(C(=O)c5cc(OC)c(OC)c(OC)c5)C4)CC3)nc3ccccc32)cc1	10.1016/S0960-894X(97)10097-X
	10190770	210474	None	0	Human	Functional	pIC50	=	6.9	6.9	-1	2	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	772	12	0	8	8.3	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc(Cl)c(Cl)c3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10097-X
	CHEMBL330430	210474	None	0	Human	Functional	pIC50	=	6.9	6.9	-1	2	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	772	12	0	8	8.3	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc(Cl)c(Cl)c3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10097-X
	CHEMBL97357	210474	None	0	Human	Functional	pIC50	=	6.9	6.9	-1	2	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	772	12	0	8	8.3	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc(Cl)c(Cl)c3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10097-X
	54585848	62754	None	5	Human	Functional	pIC50	=	5.9	5.9	5	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay	ChEMBL	316	3	0	4	3.1	CN1CCc2c(c3cc(C#N)ccc3n2CCc2ccccn2)C1	10.1016/j.bmcl.2009.04.128
	CHEMBL1783971	62754	None	5	Human	Functional	pIC50	=	5.9	5.9	5	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay	ChEMBL	316	3	0	4	3.1	CN1CCc2c(c3cc(C#N)ccc3n2CCc2ccccn2)C1	10.1016/j.bmcl.2009.04.128
	13623354	99034	None	0	Guinea pig	Functional	pIC50	=	7.9	7.9	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	274	4	0	5	1.4	COCCn1c(N2CCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	CHEMBL279872	99034	None	0	Guinea pig	Functional	pIC50	=	7.9	7.9	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	274	4	0	5	1.4	COCCn1c(N2CCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	46225000	201571	None	4	Human	Functional	pIC50	=	6.9	6.9	9	2	Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as reduction of histamine-induced intracellular calcium spike at phase 2 treated 20 to 30 seconds after histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as reduction of histamine-induced intracellular calcium spike at phase 2 treated 20 to 30 seconds after histamine challenge	ChEMBL	308	3	0	2	4.0	CN1CCc2c(c3cc(F)ccc3n2CCc2ccccc2)C1	10.1016/j.bmcl.2009.11.037
	CHEMBL589148	201571	None	4	Human	Functional	pIC50	=	6.9	6.9	9	2	Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as reduction of histamine-induced intracellular calcium spike at phase 2 treated 20 to 30 seconds after histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as reduction of histamine-induced intracellular calcium spike at phase 2 treated 20 to 30 seconds after histamine challenge	ChEMBL	308	3	0	2	4.0	CN1CCc2c(c3cc(F)ccc3n2CCc2ccccc2)C1	10.1016/j.bmcl.2009.11.037
	13623347	61074	None	0	Guinea pig	Functional	pIC50	=	5.9	5.9	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	286	4	0	4	3.1	CCCC(C)n1c(N2CCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	CHEMBL17635	61074	None	0	Guinea pig	Functional	pIC50	=	5.9	5.9	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	286	4	0	4	3.1	CCCC(C)n1c(N2CCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	13623346	98999	None	0	Guinea pig	Functional	pIC50	=	5.9	5.9	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	286	4	0	4	2.8	CC(C)CCn1c(N2CCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	CHEMBL279621	98999	None	0	Guinea pig	Functional	pIC50	=	5.9	5.9	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	286	4	0	4	2.8	CC(C)CCn1c(N2CCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	42631003	202074	None	10	Human	Functional	pIC50	=	6.8	6.8	2	2	Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as reduction of histamine-induced intracellular calcium spike at phase 2 treated 20 to 30 seconds after histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as reduction of histamine-induced intracellular calcium spike at phase 2 treated 20 to 30 seconds after histamine challenge	ChEMBL	304	3	0	2	4.2	Cc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1	10.1016/j.bmcl.2009.11.037
	CHEMBL592752	202074	None	10	Human	Functional	pIC50	=	6.8	6.8	2	2	Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as reduction of histamine-induced intracellular calcium spike at phase 2 treated 20 to 30 seconds after histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as reduction of histamine-induced intracellular calcium spike at phase 2 treated 20 to 30 seconds after histamine challenge	ChEMBL	304	3	0	2	4.2	Cc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1	10.1016/j.bmcl.2009.11.037
	13623371	65226	None	0	Guinea pig	Functional	pIC50	=	7.8	7.8	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	378	7	0	5	3.8	CCOCCn1c(N2CCCN(Cc3ccccc3)CC2)nc2ccccc21	10.1021/jm00157a010
	CHEMBL18255	65226	None	0	Guinea pig	Functional	pIC50	=	7.8	7.8	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	378	7	0	5	3.8	CCOCCn1c(N2CCCN(Cc3ccccc3)CC2)nc2ccccc21	10.1021/jm00157a010
	13623360	98862	None	0	Guinea pig	Functional	pIC50	=	7.8	7.8	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	330	8	0	5	3.0	CCCCN1CCN(c2nc3ccccc3n2CCOCC)CC1	10.1021/jm00157a010
	CHEMBL278504	98862	None	0	Guinea pig	Functional	pIC50	=	7.8	7.8	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	330	8	0	5	3.0	CCCCN1CCN(c2nc3ccccc3n2CCOCC)CC1	10.1021/jm00157a010
	13623338	63368	None	0	Guinea pig	Functional	pIC50	=	6.8	6.8	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	314	7	0	4	3.8	CCCCCCCn1c(N2CCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	CHEMBL17946	63368	None	0	Guinea pig	Functional	pIC50	=	6.8	6.8	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	314	7	0	4	3.8	CCCCCCCn1c(N2CCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	46224879	204004	None	3	Human	Functional	pIC50	=	6.8	6.8	-1	2	Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as reduction of histamine-induced intracellular calcium spike at phase 2 treated 20 to 30 seconds after histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as reduction of histamine-induced intracellular calcium spike at phase 2 treated 20 to 30 seconds after histamine challenge	ChEMBL	302	2	0	2	4.6	Cc1ccc2c(c1)c1c(n2/C=C\c2ccccc2)CCN(C)C1	10.1016/j.bmcl.2009.11.037
	CHEMBL605405	204004	None	3	Human	Functional	pIC50	=	6.8	6.8	-1	2	Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as reduction of histamine-induced intracellular calcium spike at phase 2 treated 20 to 30 seconds after histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as reduction of histamine-induced intracellular calcium spike at phase 2 treated 20 to 30 seconds after histamine challenge	ChEMBL	302	2	0	2	4.6	Cc1ccc2c(c1)c1c(n2/C=C\c2ccccc2)CCN(C)C1	10.1016/j.bmcl.2009.11.037
	9832306	112787	None	0	Human	Functional	pIC50	=	6.8	6.8	2	2	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	806	17	0	10	8.2	CCOc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc(OC)c(OC)c3)C2)cc(OCC)c1OCC	10.1016/S0960-894X(97)10097-X
	CHEMBL330367	112787	None	0	Human	Functional	pIC50	=	6.8	6.8	2	2	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	806	17	0	10	8.2	CCOc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc(OC)c(OC)c3)C2)cc(OCC)c1OCC	10.1016/S0960-894X(97)10097-X
	CHEMBL330462	112787	None	0	Human	Functional	pIC50	=	6.8	6.8	2	2	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	806	17	0	10	8.2	CCOc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc(OC)c(OC)c3)C2)cc(OCC)c1OCC	10.1016/S0960-894X(97)10097-X
	197033	201608	None	42	Human	Functional	pIC50	=	6.8	6.8	1	2	Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge	ChEMBL	319	3	0	3	3.9	Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1	10.1016/j.bmcl.2009.11.037
	CHEMBL589390	201608	None	42	Human	Functional	pIC50	=	6.8	6.8	1	2	Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge	ChEMBL	319	3	0	3	3.9	Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1	10.1016/j.bmcl.2009.11.037
	1227	2489	None	32	Human	Functional	pIC50	=	6.8	6.8	2	14	Inverse agonist activity at human wild-type histamine H1 receptor N7.45L mutant assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assayInverse agonist activity at human wild-type histamine H1 receptor N7.45L mutant assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assay	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1038/nchembio714
	2331	2489	None	32	Human	Functional	pIC50	=	6.8	6.8	2	14	Inverse agonist activity at human wild-type histamine H1 receptor N7.45L mutant assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assayInverse agonist activity at human wild-type histamine H1 receptor N7.45L mutant assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assay	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1038/nchembio714
	3957	2489	None	32	Human	Functional	pIC50	=	6.8	6.8	2	14	Inverse agonist activity at human wild-type histamine H1 receptor N7.45L mutant assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assayInverse agonist activity at human wild-type histamine H1 receptor N7.45L mutant assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assay	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1038/nchembio714
	4992	2489	None	32	Human	Functional	pIC50	=	6.8	6.8	2	14	Inverse agonist activity at human wild-type histamine H1 receptor N7.45L mutant assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assayInverse agonist activity at human wild-type histamine H1 receptor N7.45L mutant assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assay	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1038/nchembio714
	4992.0	2489	None	32	Human	Functional	pIC50	=	6.8	6.8	2	14	Inverse agonist activity at human wild-type histamine H1 receptor N7.45L mutant assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assayInverse agonist activity at human wild-type histamine H1 receptor N7.45L mutant assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assay	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1038/nchembio714
	CHEMBL511	2489	None	32	Human	Functional	pIC50	=	6.8	6.8	2	14	Inverse agonist activity at human wild-type histamine H1 receptor N7.45L mutant assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assayInverse agonist activity at human wild-type histamine H1 receptor N7.45L mutant assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assay	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1038/nchembio714
	DB06691	2489	None	32	Human	Functional	pIC50	=	6.8	6.8	2	14	Inverse agonist activity at human wild-type histamine H1 receptor N7.45L mutant assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assayInverse agonist activity at human wild-type histamine H1 receptor N7.45L mutant assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assay	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1038/nchembio714
	197033	201608	None	42	Human	Functional	pIC50	=	5.8	5.8	1	2	Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as reduction of histamine-induced intracellular calcium spike at phase 2 treated 20 to 30 seconds after histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as reduction of histamine-induced intracellular calcium spike at phase 2 treated 20 to 30 seconds after histamine challenge	ChEMBL	319	3	0	3	3.9	Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1	10.1016/j.bmcl.2009.11.037
	CHEMBL589390	201608	None	42	Human	Functional	pIC50	=	5.8	5.8	1	2	Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as reduction of histamine-induced intracellular calcium spike at phase 2 treated 20 to 30 seconds after histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as reduction of histamine-induced intracellular calcium spike at phase 2 treated 20 to 30 seconds after histamine challenge	ChEMBL	319	3	0	3	3.9	Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1	10.1016/j.bmcl.2009.11.037
	197033	201608	None	42	Human	Functional	pIC50	=	5.8	5.8	1	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assay	ChEMBL	319	3	0	3	3.9	Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1	10.1016/j.bmcl.2009.04.128
	CHEMBL589390	201608	None	42	Human	Functional	pIC50	=	5.8	5.8	1	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assay	ChEMBL	319	3	0	3	3.9	Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1	10.1016/j.bmcl.2009.04.128
	54582940	62742	None	4	Human	Functional	pIC50	=	5.8	5.8	1	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assay	ChEMBL	359	3	0	3	4.3	CN1CCc2c(c3cc(C(F)(F)F)ccc3n2CCc2ccccn2)C1	10.1016/j.bmcl.2009.04.128
	CHEMBL1783958	62742	None	4	Human	Functional	pIC50	=	5.8	5.8	1	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assay	ChEMBL	359	3	0	3	4.3	CN1CCc2c(c3cc(C(F)(F)F)ccc3n2CCc2ccccn2)C1	10.1016/j.bmcl.2009.04.128
	13623367	60399	None	0	Guinea pig	Functional	pIC50	=	7.8	7.8	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	316	6	0	5	2.6	CCOCCn1c(N2CCCN(CC)CC2)nc2ccccc21	10.1021/jm00157a010
	CHEMBL17474	60399	None	0	Guinea pig	Functional	pIC50	=	7.8	7.8	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	316	6	0	5	2.6	CCOCCn1c(N2CCCN(CC)CC2)nc2ccccc21	10.1021/jm00157a010
	13623359	64583	None	0	Guinea pig	Functional	pIC50	=	7.8	7.8	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	316	7	0	5	2.6	CCCN1CCN(c2nc3ccccc3n2CCOCC)CC1	10.1021/jm00157a010
	CHEMBL18151	64583	None	0	Guinea pig	Functional	pIC50	=	7.8	7.8	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	316	7	0	5	2.6	CCCN1CCN(c2nc3ccccc3n2CCOCC)CC1	10.1021/jm00157a010
	3071032	65060	None	0	Guinea pig	Functional	pIC50	=	7.8	7.8	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	316	6	0	5	2.6	CCCOCCn1c(N2CCCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	CHEMBL18234	65060	None	0	Guinea pig	Functional	pIC50	=	7.8	7.8	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	316	6	0	5	2.6	CCCOCCn1c(N2CCCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	621659	62749	None	8	Human	Functional	pIC50	=	6.8	6.8	-2	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay	ChEMBL	305	3	0	3	3.6	Cc1ccc2c(c1)c1c(n2CCc2ccncc2)CCN(C)C1	10.1016/j.bmcl.2009.04.128
	CHEMBL1783965	62749	None	8	Human	Functional	pIC50	=	6.8	6.8	-2	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay	ChEMBL	305	3	0	3	3.6	Cc1ccc2c(c1)c1c(n2CCc2ccncc2)CCN(C)C1	10.1016/j.bmcl.2009.04.128
	197033	201608	None	42	Human	Functional	pIC50	=	6.8	6.8	1	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay	ChEMBL	319	3	0	3	3.9	Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1	10.1016/j.bmcl.2009.04.128
	CHEMBL589390	201608	None	42	Human	Functional	pIC50	=	6.8	6.8	1	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay	ChEMBL	319	3	0	3	3.9	Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1	10.1016/j.bmcl.2009.04.128
	44458903	90680	None	0	Guinea pig	Functional	pIC50	=	7.8	7.8	-	1	In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileumIn vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum	ChEMBL	275	2	0	1	4.3	CCN1CCC2=C(C1)C(c1ccccc1)c1ccccc12	10.1016/s0960-894x(00)00199-2
	CHEMBL23897	90680	None	0	Guinea pig	Functional	pIC50	=	7.8	7.8	-	1	In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileumIn vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum	ChEMBL	275	2	0	1	4.3	CCN1CCC2=C(C1)C(c1ccccc1)c1ccccc12	10.1016/s0960-894x(00)00199-2
	2773189	59759	None	1	Guinea pig	Functional	pIC50	=	7.8	7.8	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	306	3	0	4	2.8	CN1CCN(c2nc3ccccc3n2Cc2ccccc2)CC1	10.1021/jm00157a010
	CHEMBL17246	59759	None	1	Guinea pig	Functional	pIC50	=	7.8	7.8	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	306	3	0	4	2.8	CN1CCN(c2nc3ccccc3n2Cc2ccccc2)CC1	10.1021/jm00157a010
	3071002	63037	None	0	Guinea pig	Functional	pIC50	=	7.8	7.8	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	300	6	0	5	2.0	C=CCOCCn1c(N2CCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	CHEMBL17876	63037	None	0	Guinea pig	Functional	pIC50	=	7.8	7.8	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	300	6	0	5	2.0	C=CCOCCn1c(N2CCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	145990794	166896	None	0	Human	Functional	pIC50	=	6.8	6.8	-28	6	Antagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay	ChEMBL	437	6	0	5	3.8	O=C1[C@H]2[C@@H]3CC[C@@H](C3)[C@H]2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1	10.1016/j.ejmech.2017.12.099
	CHEMBL4284346	166896	None	0	Human	Functional	pIC50	=	6.8	6.8	-28	6	Antagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay	ChEMBL	437	6	0	5	3.8	O=C1[C@H]2[C@@H]3CC[C@@H](C3)[C@H]2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1	10.1016/j.ejmech.2017.12.099
	4919	208692	None	16	Human	Functional	pIC50	=	4.8	4.8	-263	5	Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay	ChEMBL	287	5	1	2	3.9	OC(CCN1CCCC1)(c1ccccc1)C1CCCCC1	10.1021/jm300671m
	4919.0	208692	None	16	Human	Functional	pIC50	=	4.8	4.8	-263	5	Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay	ChEMBL	287	5	1	2	3.9	OC(CCN1CCCC1)(c1ccccc1)C1CCCCC1	10.1021/jm300671m
	CHEMBL86715	208692	None	16	Human	Functional	pIC50	=	4.8	4.8	-263	5	Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay	ChEMBL	287	5	1	2	3.9	OC(CCN1CCCC1)(c1ccccc1)C1CCCCC1	10.1021/jm300671m
	DB00387	208692	None	16	Human	Functional	pIC50	=	4.8	4.8	-263	5	Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay	ChEMBL	287	5	1	2	3.9	OC(CCN1CCCC1)(c1ccccc1)C1CCCCC1	10.1021/jm300671m
	13623352	60026	None	0	Guinea pig	Functional	pIC50	=	7.8	7.8	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	288	5	0	5	2.2	CCCOCn1c(N2CCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	CHEMBL17349	60026	None	0	Guinea pig	Functional	pIC50	=	7.8	7.8	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	288	5	0	5	2.2	CCCOCn1c(N2CCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	3071010	63940	None	0	Guinea pig	Functional	pIC50	=	7.8	7.8	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	302	6	0	5	2.2	CCOCCn1c(N2CCN(CC)CC2)nc2ccccc21	10.1021/jm00157a010
	CHEMBL18060	63940	None	0	Guinea pig	Functional	pIC50	=	7.8	7.8	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	302	6	0	5	2.2	CCOCCn1c(N2CCN(CC)CC2)nc2ccccc21	10.1021/jm00157a010
	46224877	203157	None	4	Human	Functional	pIC50	=	6.7	6.7	74	2	Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as reduction of histamine-induced intracellular calcium spike at phase 2 treated 20 to 30 seconds after histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as reduction of histamine-induced intracellular calcium spike at phase 2 treated 20 to 30 seconds after histamine challenge	ChEMBL	288	2	0	2	4.3	CN1CCc2c(c3ccccc3n2/C=C\c2ccccc2)C1	10.1016/j.bmcl.2009.11.037
	CHEMBL599913	203157	None	4	Human	Functional	pIC50	=	6.7	6.7	74	2	Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as reduction of histamine-induced intracellular calcium spike at phase 2 treated 20 to 30 seconds after histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as reduction of histamine-induced intracellular calcium spike at phase 2 treated 20 to 30 seconds after histamine challenge	ChEMBL	288	2	0	2	4.3	CN1CCc2c(c3ccccc3n2/C=C\c2ccccc2)C1	10.1016/j.bmcl.2009.11.037
	54586812	62737	None	4	Human	Functional	pIC50	=	5.7	5.7	12	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay	ChEMBL	291	3	0	3	3.3	CN1CCc2c(c3ccccc3n2CCc2ccccn2)C1	10.1016/j.bmcl.2009.04.128
	CHEMBL1783953	62737	None	4	Human	Functional	pIC50	=	5.7	5.7	12	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay	ChEMBL	291	3	0	3	3.3	CN1CCc2c(c3ccccc3n2CCc2ccccn2)C1	10.1016/j.bmcl.2009.04.128
	13623336	60516	None	0	Guinea pig	Functional	pIC50	=	7.7	7.7	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	286	5	0	4	3.0	CCCCCn1c(N2CCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	CHEMBL17555	60516	None	0	Guinea pig	Functional	pIC50	=	7.7	7.7	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	286	5	0	4	3.0	CCCCCn1c(N2CCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	13623350	63132	None	0	Guinea pig	Functional	pIC50	=	7.7	7.7	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	304	5	0	5	2.5	CCSCCn1c(N2CCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	CHEMBL17893	63132	None	0	Guinea pig	Functional	pIC50	=	7.7	7.7	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	304	5	0	5	2.5	CCSCCn1c(N2CCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	145983928	166507	None	0	Human	Functional	pIC50	=	6.7	6.7	-53	6	Antagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay	ChEMBL	435	6	0	5	3.6	O=C1[C@H]2[C@@H]3C=C[C@@H](C3)[C@H]2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1	10.1016/j.ejmech.2017.12.099
	CHEMBL4277101	166507	None	0	Human	Functional	pIC50	=	6.7	6.7	-53	6	Antagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay	ChEMBL	435	6	0	5	3.6	O=C1[C@H]2[C@@H]3C=C[C@@H](C3)[C@H]2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1	10.1016/j.ejmech.2017.12.099
	3071014	98138	None	0	Guinea pig	Functional	pIC50	=	7.7	7.7	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	302	6	0	5	2.2	CCCOCCn1c(N2CCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	CHEMBL273320	98138	None	0	Guinea pig	Functional	pIC50	=	7.7	7.7	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	302	6	0	5	2.2	CCCOCCn1c(N2CCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	126624	210749	None	5	Guinea pig	Functional	pIC50	=	4.7	4.7	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	264	5	0	3	2.2	CN(C)CCCN1C(=O)CSC1c1ccccc1	10.1021/jm00093a025
	CHEMBL1202936	210749	None	5	Guinea pig	Functional	pIC50	=	4.7	4.7	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	264	5	0	3	2.2	CN(C)CCCN1C(=O)CSC1c1ccccc1	10.1021/jm00093a025
	CHEMBL98989	210749	None	5	Guinea pig	Functional	pIC50	=	4.7	4.7	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	264	5	0	3	2.2	CN(C)CCCN1C(=O)CSC1c1ccccc1	10.1021/jm00093a025
	10123138	108582	None	0	Human	Functional	pIC50	=	6.7	6.7	-1	2	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	748	12	0	10	6.7	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc4c(c3)OCO4)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10097-X
	CHEMBL317524	108582	None	0	Human	Functional	pIC50	=	6.7	6.7	-1	2	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	748	12	0	10	6.7	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc4c(c3)OCO4)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10097-X
	CHEMBL320002	108582	None	0	Human	Functional	pIC50	=	6.7	6.7	-1	2	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	748	12	0	10	6.7	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc4c(c3)OCO4)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10097-X
	2861271	4255	None	7	Guinea pig	Functional	pIC50	=	4.7	4.7	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	298	5	0	3	2.9	CN(C)CCCN1C(=O)CSC1c1ccc(Cl)cc1	10.1021/jm00093a025
	CHEMBL100486	4255	None	7	Guinea pig	Functional	pIC50	=	4.7	4.7	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	298	5	0	3	2.9	CN(C)CCCN1C(=O)CSC1c1ccc(Cl)cc1	10.1021/jm00093a025
	46224878	201925	None	0	Human	Functional	pIC50	=	5.7	5.7	2	2	Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as reduction of histamine-induced intracellular calcium spike at phase 2 treated 20 to 30 seconds after histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as reduction of histamine-induced intracellular calcium spike at phase 2 treated 20 to 30 seconds after histamine challenge	ChEMBL	290	2	0	2	4.0	CN1CCC2C(C1)c1ccccc1N2/C=C/c1ccccc1	10.1016/j.bmcl.2009.11.037
	CHEMBL591568	201925	None	0	Human	Functional	pIC50	=	5.7	5.7	2	2	Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as reduction of histamine-induced intracellular calcium spike at phase 2 treated 20 to 30 seconds after histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as reduction of histamine-induced intracellular calcium spike at phase 2 treated 20 to 30 seconds after histamine challenge	ChEMBL	290	2	0	2	4.0	CN1CCC2C(C1)c1ccccc1N2/C=C/c1ccccc1	10.1016/j.bmcl.2009.11.037
	54585847	62752	None	5	Human	Functional	pIC50	=	6.7	6.7	29	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay	ChEMBL	359	3	0	3	4.3	CN1CCc2c(c3cc(C(F)(F)F)ccc3n2CCc2ccncc2)C1	10.1016/j.bmcl.2009.04.128
	CHEMBL1783968	62752	None	5	Human	Functional	pIC50	=	6.7	6.7	29	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay	ChEMBL	359	3	0	3	4.3	CN1CCc2c(c3cc(C(F)(F)F)ccc3n2CCc2ccncc2)C1	10.1016/j.bmcl.2009.04.128
	198539	99285	None	1	Guinea pig	Functional	pIC50	=	6.7	6.7	-	1	In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileumIn vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum	ChEMBL	259	1	0	1	3.8	CN1CC=C2C(=C(c3ccccc3)c3ccccc32)C1	10.1016/s0960-894x(00)00199-2
	CHEMBL281638	99285	None	1	Guinea pig	Functional	pIC50	=	6.7	6.7	-	1	In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileumIn vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum	ChEMBL	259	1	0	1	3.8	CN1CC=C2C(=C(c3ccccc3)c3ccccc32)C1	10.1016/s0960-894x(00)00199-2
	2860026	108432	None	5	Guinea pig	Functional	pIC50	=	5.7	5.7	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	298	5	0	3	2.9	CN(C)CCCN1C(=O)CSC1c1cccc(Cl)c1	10.1021/jm00093a025
	CHEMBL319829	108432	None	5	Guinea pig	Functional	pIC50	=	5.7	5.7	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	298	5	0	3	2.9	CN(C)CCCN1C(=O)CSC1c1cccc(Cl)c1	10.1021/jm00093a025
	7430452	99532	None	0	Guinea pig	Functional	pIC50	=	7.6	7.6	-	1	In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileumIn vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum	ChEMBL	309	4	1	3	3.1	CCN1CC[C@@](O)(c2ccccc2)[C@H](C(=O)c2ccccc2)C1	10.1016/s0960-894x(00)00199-2
	CHEMBL283169	99532	None	0	Guinea pig	Functional	pIC50	=	7.6	7.6	-	1	In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileumIn vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum	ChEMBL	309	4	1	3	3.1	CCN1CC[C@@](O)(c2ccccc2)[C@H](C(=O)c2ccccc2)C1	10.1016/s0960-894x(00)00199-2
	2861590	107316	None	5	Guinea pig	Functional	pIC50	=	5.6	5.6	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	342	5	0	3	3.0	CN(C)CCCN1C(=O)CSC1c1ccc(Br)cc1	10.1021/jm00093a025
	CHEMBL1202937	107316	None	5	Guinea pig	Functional	pIC50	=	5.6	5.6	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	342	5	0	3	3.0	CN(C)CCCN1C(=O)CSC1c1ccc(Br)cc1	10.1021/jm00093a025
	CHEMBL316951	107316	None	5	Guinea pig	Functional	pIC50	=	5.6	5.6	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	342	5	0	3	3.0	CN(C)CCCN1C(=O)CSC1c1ccc(Br)cc1	10.1021/jm00093a025
	10212223	210599	None	0	Human	Functional	pIC50	=	6.6	6.6	-2	2	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	704	12	0	8	7.0	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccccc3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10097-X
	CHEMBL431458	210599	None	0	Human	Functional	pIC50	=	6.6	6.6	-2	2	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	704	12	0	8	7.0	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccccc3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10097-X
	CHEMBL98079	210599	None	0	Human	Functional	pIC50	=	6.6	6.6	-2	2	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	704	12	0	8	7.0	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccccc3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10097-X
	10190056	111501	None	0	Human	Functional	pIC50	=	6.6	6.6	1	2	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	674	11	0	7	7.0	COc1ccc(C2(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)CCN(C(=O)c3ccccc3)C2)cc1OC	10.1016/S0960-894X(97)10097-X
	CHEMBL327497	111501	None	0	Human	Functional	pIC50	=	6.6	6.6	1	2	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	674	11	0	7	7.0	COc1ccc(C2(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)CCN(C(=O)c3ccccc3)C2)cc1OC	10.1016/S0960-894X(97)10097-X
	13623341	62140	None	0	Guinea pig	Functional	pIC50	=	6.6	6.6	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	320	4	0	4	3.0	CN1CCN(c2nc3ccccc3n2CCc2ccccc2)CC1	10.1021/jm00157a010
	CHEMBL17763	62140	None	0	Guinea pig	Functional	pIC50	=	6.6	6.6	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	320	4	0	4	3.0	CN1CCN(c2nc3ccccc3n2CCc2ccccc2)CC1	10.1021/jm00157a010
	2872050	210685	None	2	Guinea pig	Functional	pIC50	=	4.6	4.6	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	282	5	0	3	2.4	CN(C)CCCN1C(=O)CSC1c1ccc(F)cc1	10.1021/jm00093a025
	CHEMBL1202939	210685	None	2	Guinea pig	Functional	pIC50	=	4.6	4.6	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	282	5	0	3	2.4	CN(C)CCCN1C(=O)CSC1c1ccc(F)cc1	10.1021/jm00093a025
	CHEMBL98605	210685	None	2	Guinea pig	Functional	pIC50	=	4.6	4.6	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	282	5	0	3	2.4	CN(C)CCCN1C(=O)CSC1c1ccc(F)cc1	10.1021/jm00093a025
	2284	3182	None	26	Human	Functional	pIC50	=	5.6	5.6	-3	34	Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay	ChEMBL	284	4	0	3	4.2	CN(CCCN1c2ccccc2Sc2c1cccc2)C	10.1021/jm300671m
	4926	3182	None	26	Human	Functional	pIC50	=	5.6	5.6	-3	34	Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay	ChEMBL	284	4	0	3	4.2	CN(CCCN1c2ccccc2Sc2c1cccc2)C	10.1021/jm300671m
	7281	3182	None	26	Human	Functional	pIC50	=	5.6	5.6	-3	34	Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay	ChEMBL	284	4	0	3	4.2	CN(CCCN1c2ccccc2Sc2c1cccc2)C	10.1021/jm300671m
	CHEMBL564	3182	None	26	Human	Functional	pIC50	=	5.6	5.6	-3	34	Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay	ChEMBL	284	4	0	3	4.2	CN(CCCN1c2ccccc2Sc2c1cccc2)C	10.1021/jm300671m
	DB00420	3182	None	26	Human	Functional	pIC50	=	5.6	5.6	-3	34	Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay	ChEMBL	284	4	0	3	4.2	CN(CCCN1c2ccccc2Sc2c1cccc2)C	10.1021/jm300671m
	9984168	98342	None	10	Guinea pig	Functional	pIC50	=	7.6	7.6	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	288	5	1	5	1.9	CCOCCn1c(N2CCCNCC2)nc2ccccc21	10.1021/jm00157a010
	CHEMBL274747	98342	None	10	Guinea pig	Functional	pIC50	=	7.6	7.6	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	288	5	1	5	1.9	CCOCCn1c(N2CCCNCC2)nc2ccccc21	10.1021/jm00157a010
	14984033	210637	None	0	Guinea pig	Functional	pIC50	=	4.6	4.6	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	294	6	0	4	2.2	COc1cccc(C2SCC(=O)N2CCCN(C)C)c1	10.1021/jm00093a025
	CHEMBL1202941	210637	None	0	Guinea pig	Functional	pIC50	=	4.6	4.6	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	294	6	0	4	2.2	COc1cccc(C2SCC(=O)N2CCCN(C)C)c1	10.1021/jm00093a025
	CHEMBL98334	210637	None	0	Guinea pig	Functional	pIC50	=	4.6	4.6	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	294	6	0	4	2.2	COc1cccc(C2SCC(=O)N2CCCN(C)C)c1	10.1021/jm00093a025
	145993117	167017	None	0	Human	Functional	pIC50	=	6.6	6.6	-204	6	Antagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay	ChEMBL	427	7	0	5	4.4	CCC1(C)CC(=O)N(CCCCN2CCN(c3cccc4sccc34)CC2)C(=O)C1	10.1016/j.ejmech.2017.12.099
	CHEMBL4286717	167017	None	0	Human	Functional	pIC50	=	6.6	6.6	-204	6	Antagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay	ChEMBL	427	7	0	5	4.4	CCC1(C)CC(=O)N(CCCCN2CCN(c3cccc4sccc34)CC2)C(=O)C1	10.1016/j.ejmech.2017.12.099
	708981	88826	None	0	Guinea pig	Functional	pIC50	=	7.6	7.6	-	1	In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileumIn vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum	ChEMBL	295	3	1	3	2.7	CN1CC[C@@](O)(c2ccccc2)[C@H](C(=O)c2ccccc2)C1	10.1016/s0960-894x(00)00199-2
	CHEMBL23638	88826	None	0	Guinea pig	Functional	pIC50	=	7.6	7.6	-	1	In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileumIn vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum	ChEMBL	295	3	1	3	2.7	CN1CC[C@@](O)(c2ccccc2)[C@H](C(=O)c2ccccc2)C1	10.1016/s0960-894x(00)00199-2
	13623337	98856	None	0	Guinea pig	Functional	pIC50	=	7.6	7.6	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	300	6	0	4	3.4	CCCCCCn1c(N2CCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	CHEMBL278457	98856	None	0	Guinea pig	Functional	pIC50	=	7.6	7.6	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	300	6	0	4	3.4	CCCCCCn1c(N2CCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	15585276	61986	None	0	Guinea pig	Functional	pIC50	=	7.6	7.6	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	364	7	0	5	3.4	CCOCCn1c(N2CCN(Cc3ccccc3)CC2)nc2ccccc21	10.1021/jm00157a010
	CHEMBL17742	61986	None	0	Guinea pig	Functional	pIC50	=	7.6	7.6	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	364	7	0	5	3.4	CCOCCn1c(N2CCN(Cc3ccccc3)CC2)nc2ccccc21	10.1021/jm00157a010
	54582000	62756	None	4	Human	Functional	pIC50	=	5.6	5.6	-	1	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay	ChEMBL	388	4	0	4	4.0	Cc1ccc2c(c1)c1c(n2CCc2cccnc2)CCN(C2CCN(C)CC2)C1	10.1016/j.bmcl.2009.04.128
	CHEMBL1783974	62756	None	4	Human	Functional	pIC50	=	5.6	5.6	-	1	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay	ChEMBL	388	4	0	4	4.0	Cc1ccc2c(c1)c1c(n2CCc2cccnc2)CCN(C2CCN(C)CC2)C1	10.1016/j.bmcl.2009.04.128
	162910	84655	None	2	Guinea pig	Functional	pIC50	=	7.6	7.6	-	1	In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileumIn vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum	ChEMBL	261	1	0	1	3.9	CN1CCC2C(=C(c3ccccc3)c3ccccc32)C1	10.1016/s0960-894x(00)00199-2
	CHEMBL22215	84655	None	2	Guinea pig	Functional	pIC50	=	7.6	7.6	-	1	In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileumIn vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum	ChEMBL	261	1	0	1	3.9	CN1CCC2C(=C(c3ccccc3)c3ccccc32)C1	10.1016/s0960-894x(00)00199-2
	15542879	112887	None	0	Human	Functional	pIC50	=	6.5	6.5	-2	2	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	687	12	0	9	6.3	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccncc4)CC3)(c3ccccc3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10097-X
	CHEMBL330719	112887	None	0	Human	Functional	pIC50	=	6.5	6.5	-2	2	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	687	12	0	9	6.3	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccncc4)CC3)(c3ccccc3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10097-X
	13623357	63399	None	0	Guinea pig	Functional	pIC50	=	6.5	6.5	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	287	5	1	5	1.4	CCNCCn1c(N2CCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	CHEMBL17959	63399	None	0	Guinea pig	Functional	pIC50	=	6.5	6.5	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	287	5	1	5	1.4	CCNCCn1c(N2CCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	10168749	210080	None	0	Human	Functional	pIC50	=	6.5	6.5	-3	2	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	676	12	0	9	6.5	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccco4)CC3)(c3ccccc3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10097-X
	CHEMBL95127	210080	None	0	Human	Functional	pIC50	=	6.5	6.5	-3	2	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	676	12	0	9	6.5	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccco4)CC3)(c3ccccc3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10097-X
	1227	2489	None	32	Human	Functional	pIC50	=	8.5	8.5	2	14	Antagonist activity at human recombinant H1 receptor assessed as inhibition of histamine-induced intracellular Ca2+ releaseAntagonist activity at human recombinant H1 receptor assessed as inhibition of histamine-induced intracellular Ca2+ release	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1021/jm401895u
	2331	2489	None	32	Human	Functional	pIC50	=	8.5	8.5	2	14	Antagonist activity at human recombinant H1 receptor assessed as inhibition of histamine-induced intracellular Ca2+ releaseAntagonist activity at human recombinant H1 receptor assessed as inhibition of histamine-induced intracellular Ca2+ release	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1021/jm401895u
	3957	2489	None	32	Human	Functional	pIC50	=	8.5	8.5	2	14	Antagonist activity at human recombinant H1 receptor assessed as inhibition of histamine-induced intracellular Ca2+ releaseAntagonist activity at human recombinant H1 receptor assessed as inhibition of histamine-induced intracellular Ca2+ release	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1021/jm401895u
	4992	2489	None	32	Human	Functional	pIC50	=	8.5	8.5	2	14	Antagonist activity at human recombinant H1 receptor assessed as inhibition of histamine-induced intracellular Ca2+ releaseAntagonist activity at human recombinant H1 receptor assessed as inhibition of histamine-induced intracellular Ca2+ release	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1021/jm401895u
	4992.0	2489	None	32	Human	Functional	pIC50	=	8.5	8.5	2	14	Antagonist activity at human recombinant H1 receptor assessed as inhibition of histamine-induced intracellular Ca2+ releaseAntagonist activity at human recombinant H1 receptor assessed as inhibition of histamine-induced intracellular Ca2+ release	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1021/jm401895u
	CHEMBL511	2489	None	32	Human	Functional	pIC50	=	8.5	8.5	2	14	Antagonist activity at human recombinant H1 receptor assessed as inhibition of histamine-induced intracellular Ca2+ releaseAntagonist activity at human recombinant H1 receptor assessed as inhibition of histamine-induced intracellular Ca2+ release	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1021/jm401895u
	DB06691	2489	None	32	Human	Functional	pIC50	=	8.5	8.5	2	14	Antagonist activity at human recombinant H1 receptor assessed as inhibition of histamine-induced intracellular Ca2+ releaseAntagonist activity at human recombinant H1 receptor assessed as inhibition of histamine-induced intracellular Ca2+ release	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1021/jm401895u
	44126326	202075	None	6	Human	Functional	pIC50	=	7.5	7.5	32	2	Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge	ChEMBL	322	3	0	2	4.3	Cc1ccc2c(c1)c1c(n2CCc2ccc(F)cc2)CCN(C)C1	10.1016/j.bmcl.2009.11.037
	CHEMBL592753	202075	None	6	Human	Functional	pIC50	=	7.5	7.5	32	2	Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge	ChEMBL	322	3	0	2	4.3	Cc1ccc2c(c1)c1c(n2CCc2ccc(F)cc2)CCN(C)C1	10.1016/j.bmcl.2009.11.037
	13623361	64666	None	0	Guinea pig	Functional	pIC50	=	7.5	7.5	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	344	9	0	5	3.4	CCCCCN1CCN(c2nc3ccccc3n2CCOCC)CC1	10.1021/jm00157a010
	CHEMBL18181	64666	None	0	Guinea pig	Functional	pIC50	=	7.5	7.5	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	344	9	0	5	3.4	CCCCCN1CCN(c2nc3ccccc3n2CCOCC)CC1	10.1021/jm00157a010
	145993493	167453	None	0	Human	Functional	pIC50	=	6.5	6.5	-38	6	Antagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay	ChEMBL	439	6	0	5	4.5	O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1	10.1016/j.ejmech.2017.12.099
	CHEMBL4294617	167453	None	0	Human	Functional	pIC50	=	6.5	6.5	-38	6	Antagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay	ChEMBL	439	6	0	5	4.5	O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1	10.1016/j.ejmech.2017.12.099
	9918576	209796	None	0	Human	Functional	pIC50	=	6.5	6.5	-2	3	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	764	14	0	10	7.0	COc1ccc(C2(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)CCN(C(=O)c3cc(OC)c(OC)c(OC)c3)C2)cc1OC	10.1016/S0960-894X(97)10097-X
	CHEMBL93556	209796	None	0	Human	Functional	pIC50	=	6.5	6.5	-2	3	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	764	14	0	10	7.0	COc1ccc(C2(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)CCN(C(=O)c3cc(OC)c(OC)c(OC)c3)C2)cc1OC	10.1016/S0960-894X(97)10097-X
	44126328	203562	None	4	Human	Functional	pIC50	=	7.5	7.5	74	2	Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge	ChEMBL	322	3	0	2	4.3	Cc1ccc(CCn2c3c(c4cc(F)ccc42)CN(C)CC3)cc1	10.1016/j.bmcl.2009.11.037
	CHEMBL603049	203562	None	4	Human	Functional	pIC50	=	7.5	7.5	74	2	Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge	ChEMBL	322	3	0	2	4.3	Cc1ccc(CCn2c3c(c4cc(F)ccc42)CN(C)CC3)cc1	10.1016/j.bmcl.2009.11.037
	13623363	99090	None	0	Guinea pig	Functional	pIC50	=	7.5	7.5	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	378	8	0	5	3.4	CCOCCn1c(N2CCN(CCc3ccccc3)CC2)nc2ccccc21	10.1021/jm00157a010
	CHEMBL280255	99090	None	0	Guinea pig	Functional	pIC50	=	7.5	7.5	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	378	8	0	5	3.4	CCOCCn1c(N2CCN(CCc3ccccc3)CC2)nc2ccccc21	10.1021/jm00157a010
	14984031	210832	None	0	Guinea pig	Functional	pIC50	=	5.5	5.5	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	282	5	0	3	2.4	CN(C)CCCN1C(=O)CSC1c1cccc(F)c1	10.1021/jm00093a025
	CHEMBL1202933	210832	None	0	Guinea pig	Functional	pIC50	=	5.5	5.5	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	282	5	0	3	2.4	CN(C)CCCN1C(=O)CSC1c1cccc(F)c1	10.1021/jm00093a025
	CHEMBL99529	210832	None	0	Guinea pig	Functional	pIC50	=	5.5	5.5	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	282	5	0	3	2.4	CN(C)CCCN1C(=O)CSC1c1cccc(F)c1	10.1021/jm00093a025
	44126330	62744	None	4	Human	Functional	pIC50	=	5.5	5.5	-2	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assay	ChEMBL	305	3	0	3	3.6	Cc1ccc2c(c1)c1c(n2CCc2cccnc2)CCN(C)C1	10.1016/j.bmcl.2009.04.128
	CHEMBL1783960	62744	None	4	Human	Functional	pIC50	=	5.5	5.5	-2	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assay	ChEMBL	305	3	0	3	3.6	Cc1ccc2c(c1)c1c(n2CCc2cccnc2)CCN(C)C1	10.1016/j.bmcl.2009.04.128
	46225027	201573	None	4	Human	Functional	pIC50	=	7.5	7.5	74	2	Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge	ChEMBL	338	4	0	3	4.0	COc1ccc(CCn2c3c(c4cc(F)ccc42)CN(C)CC3)cc1	10.1016/j.bmcl.2009.11.037
	CHEMBL589150	201573	None	4	Human	Functional	pIC50	=	7.5	7.5	74	2	Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge	ChEMBL	338	4	0	3	4.0	COc1ccc(CCn2c3c(c4cc(F)ccc42)CN(C)CC3)cc1	10.1016/j.bmcl.2009.11.037
	54583938	62753	None	0	Human	Functional	pIC50	=	6.5	6.5	1	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay	ChEMBL	306	3	0	4	3.0	Cc1ccc2c(c1)c1c(n2CCc2cnccn2)CCN(C)C1	10.1016/j.bmcl.2009.04.128
	CHEMBL1783970	62753	None	0	Human	Functional	pIC50	=	6.5	6.5	1	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay	ChEMBL	306	3	0	4	3.0	Cc1ccc2c(c1)c1c(n2CCc2cnccn2)CCN(C)C1	10.1016/j.bmcl.2009.04.128
	2773179	98771	None	1	Guinea pig	Functional	pIC50	=	6.5	6.5	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	230	1	0	4	1.3	CN1CCN(c2nc3ccccc3n2C)CC1	10.1021/jm00157a010
	CHEMBL277749	98771	None	1	Guinea pig	Functional	pIC50	=	6.5	6.5	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	230	1	0	4	1.3	CN1CCN(c2nc3ccccc3n2C)CC1	10.1021/jm00157a010
	46224877	203157	None	4	Human	Functional	pIC50	=	7.5	7.5	74	2	Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge	ChEMBL	288	2	0	2	4.3	CN1CCc2c(c3ccccc3n2/C=C\c2ccccc2)C1	10.1016/j.bmcl.2009.11.037
	CHEMBL599913	203157	None	4	Human	Functional	pIC50	=	7.5	7.5	74	2	Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge	ChEMBL	288	2	0	2	4.3	CN1CCc2c(c3ccccc3n2/C=C\c2ccccc2)C1	10.1016/j.bmcl.2009.11.037
	1227	2489	None	32	Guinea pig	Functional	pIC50	=	7.5	7.5	-2	14	In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileumIn vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1016/s0960-894x(00)00199-2
	2331	2489	None	32	Guinea pig	Functional	pIC50	=	7.5	7.5	-2	14	In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileumIn vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1016/s0960-894x(00)00199-2
	3957	2489	None	32	Guinea pig	Functional	pIC50	=	7.5	7.5	-2	14	In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileumIn vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1016/s0960-894x(00)00199-2
	4992	2489	None	32	Guinea pig	Functional	pIC50	=	7.5	7.5	-2	14	In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileumIn vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1016/s0960-894x(00)00199-2
	4992.0	2489	None	32	Guinea pig	Functional	pIC50	=	7.5	7.5	-2	14	In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileumIn vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1016/s0960-894x(00)00199-2
	CHEMBL511	2489	None	32	Guinea pig	Functional	pIC50	=	7.5	7.5	-2	14	In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileumIn vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1016/s0960-894x(00)00199-2
	DB06691	2489	None	32	Guinea pig	Functional	pIC50	=	7.5	7.5	-2	14	In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileumIn vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1016/s0960-894x(00)00199-2
	10123040	161189	None	0	Human	Functional	pIC50	=	5.5	5.5	-7	2	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	730	13	1	9	6.6	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(C(=O)O)cc4)CC3)(c3ccccc3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10097-X
	CHEMBL411691	161189	None	0	Human	Functional	pIC50	=	5.5	5.5	-7	2	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	730	13	1	9	6.6	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(C(=O)O)cc4)CC3)(c3ccccc3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10097-X
	CHEMBL537027	161189	None	0	Human	Functional	pIC50	=	5.5	5.5	-7	2	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	730	13	1	9	6.6	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(C(=O)O)cc4)CC3)(c3ccccc3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10097-X
	46224878	201925	None	0	Human	Functional	pIC50	=	6.5	6.5	2	2	Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge	ChEMBL	290	2	0	2	4.0	CN1CCC2C(C1)c1ccccc1N2/C=C/c1ccccc1	10.1016/j.bmcl.2009.11.037
	CHEMBL591568	201925	None	0	Human	Functional	pIC50	=	6.5	6.5	2	2	Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge	ChEMBL	290	2	0	2	4.0	CN1CCC2C(C1)c1ccccc1N2/C=C/c1ccccc1	10.1016/j.bmcl.2009.11.037
	46225002	201950	None	4	Human	Functional	pIC50	=	7.5	7.5	602	2	Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge	ChEMBL	376	3	0	2	5.0	CN1CCc2c(c3cc(F)ccc3n2CCc2ccc(C(F)(F)F)cc2)C1	10.1016/j.bmcl.2009.11.037
	CHEMBL591803	201950	None	4	Human	Functional	pIC50	=	7.5	7.5	602	2	Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge	ChEMBL	376	3	0	2	5.0	CN1CCc2c(c3cc(F)ccc3n2CCc2ccc(C(F)(F)F)cc2)C1	10.1016/j.bmcl.2009.11.037
	11291	98850	None	21	Guinea pig	Functional	pIC50	=	7.4	7.4	223	3	In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileumIn vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum	ChEMBL	261	1	0	1	3.9	CN1CCC2=C(C1)C(c1ccccc1)c1ccccc12	10.1016/s0960-894x(00)00199-2
	11291.0	98850	None	21	Guinea pig	Functional	pIC50	=	7.4	7.4	223	3	In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileumIn vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum	ChEMBL	261	1	0	1	3.9	CN1CCC2=C(C1)C(c1ccccc1)c1ccccc12	10.1016/s0960-894x(00)00199-2
	CHEMBL278398	98850	None	21	Guinea pig	Functional	pIC50	=	7.4	7.4	223	3	In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileumIn vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum	ChEMBL	261	1	0	1	3.9	CN1CCC2=C(C1)C(c1ccccc1)c1ccccc12	10.1016/s0960-894x(00)00199-2
	DB01619	98850	None	21	Guinea pig	Functional	pIC50	=	7.4	7.4	223	3	In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileumIn vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum	ChEMBL	261	1	0	1	3.9	CN1CCC2=C(C1)C(c1ccccc1)c1ccccc12	10.1016/s0960-894x(00)00199-2
	10233656	210310	None	0	Human	Functional	pIC50	=	6.4	6.4	-3	2	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	687	12	0	9	6.3	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccccn4)CC3)(c3ccccc3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10097-X
	CHEMBL96442	210310	None	0	Human	Functional	pIC50	=	6.4	6.4	-3	2	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	687	12	0	9	6.3	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccccn4)CC3)(c3ccccc3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10097-X
	13623343	98554	None	0	Guinea pig	Functional	pIC50	=	7.4	7.4	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	316	7	0	5	2.6	CCCCOCCn1c(N2CCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	CHEMBL276070	98554	None	0	Guinea pig	Functional	pIC50	=	7.4	7.4	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	316	7	0	5	2.6	CCCCOCCn1c(N2CCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	13623334	63944	None	0	Guinea pig	Functional	pIC50	=	6.4	6.4	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	258	3	0	4	2.2	CCCn1c(N2CCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	CHEMBL18062	63944	None	0	Guinea pig	Functional	pIC50	=	6.4	6.4	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	258	3	0	4	2.2	CCCn1c(N2CCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	10122529	109612	None	0	Human	Functional	pIC50	=	6.4	6.4	-3	2	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	668	14	0	9	5.9	CCOCCn1c(C(=O)C2CCN(CCC3(c4ccccc4)CCN(C(=O)c4cc(OC)c(OC)c(OC)c4)C3)CC2)nc2ccccc21	10.1016/S0960-894X(97)10097-X
	CHEMBL322194	109612	None	0	Human	Functional	pIC50	=	6.4	6.4	-3	2	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	668	14	0	9	5.9	CCOCCn1c(C(=O)C2CCN(CCC3(c4ccccc4)CCN(C(=O)c4cc(OC)c(OC)c(OC)c4)C3)CC2)nc2ccccc21	10.1016/S0960-894X(97)10097-X
	54581997	62750	None	5	Human	Functional	pIC50	=	6.4	6.4	11	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay	ChEMBL	321	4	0	4	3.3	COc1ccc2c(c1)c1c(n2CCc2ccncc2)CCN(C)C1	10.1016/j.bmcl.2009.04.128
	CHEMBL1783966	62750	None	5	Human	Functional	pIC50	=	6.4	6.4	11	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay	ChEMBL	321	4	0	4	3.3	COc1ccc2c(c1)c1c(n2CCc2ccncc2)CCN(C)C1	10.1016/j.bmcl.2009.04.128
	621659	62749	None	8	Human	Functional	pIC50	=	5.4	5.4	-2	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assay	ChEMBL	305	3	0	3	3.6	Cc1ccc2c(c1)c1c(n2CCc2ccncc2)CCN(C)C1	10.1016/j.bmcl.2009.04.128
	CHEMBL1783965	62749	None	8	Human	Functional	pIC50	=	5.4	5.4	-2	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assay	ChEMBL	305	3	0	3	3.6	Cc1ccc2c(c1)c1c(n2CCc2ccncc2)CCN(C)C1	10.1016/j.bmcl.2009.04.128
	10123040	161189	None	0	Human	Functional	pIC50	=	8.4	8.4	-7	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	730	13	1	9	6.6	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(C(=O)O)cc4)CC3)(c3ccccc3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10098-1
	CHEMBL411691	161189	None	0	Human	Functional	pIC50	=	8.4	8.4	-7	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	730	13	1	9	6.6	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(C(=O)O)cc4)CC3)(c3ccccc3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10098-1
	CHEMBL537027	161189	None	0	Human	Functional	pIC50	=	8.4	8.4	-7	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	730	13	1	9	6.6	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(C(=O)O)cc4)CC3)(c3ccccc3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10098-1
	10212725	98222	None	0	Human	Functional	pIC50	=	8.3	8.3	1	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	790	15	1	11	6.6	COc1ccc(C2(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(C(=O)O)cc4)CC3)CCN(C(=O)c3cc(OC)c(OC)c(OC)c3)C2)cc1OC	10.1016/S0960-894X(97)10098-1
	CHEMBL273915	98222	None	0	Human	Functional	pIC50	=	8.3	8.3	1	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	790	15	1	11	6.6	COc1ccc(C2(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(C(=O)O)cc4)CC3)CCN(C(=O)c3cc(OC)c(OC)c(OC)c3)C2)cc1OC	10.1016/S0960-894X(97)10098-1
	46225000	201571	None	4	Human	Functional	pIC50	=	7.4	7.4	9	2	Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge	ChEMBL	308	3	0	2	4.0	CN1CCc2c(c3cc(F)ccc3n2CCc2ccccc2)C1	10.1016/j.bmcl.2009.11.037
	CHEMBL589148	201571	None	4	Human	Functional	pIC50	=	7.4	7.4	9	2	Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge	ChEMBL	308	3	0	2	4.0	CN1CCc2c(c3cc(F)ccc3n2CCc2ccccc2)C1	10.1016/j.bmcl.2009.11.037
	42631003	202074	None	10	Human	Functional	pIC50	=	7.4	7.4	2	2	Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge	ChEMBL	304	3	0	2	4.2	Cc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1	10.1016/j.bmcl.2009.11.037
	CHEMBL592752	202074	None	10	Human	Functional	pIC50	=	7.4	7.4	2	2	Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge	ChEMBL	304	3	0	2	4.2	Cc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1	10.1016/j.bmcl.2009.11.037
	14984030	107386	None	0	Guinea pig	Functional	pIC50	=	4.4	4.4	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	279	5	1	4	1.8	CN(C)CCCN1C(=O)CSC1c1ccc(N)cc1	10.1021/jm00093a025
	CHEMBL1202935	107386	None	0	Guinea pig	Functional	pIC50	=	4.4	4.4	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	279	5	1	4	1.8	CN(C)CCCN1C(=O)CSC1c1ccc(N)cc1	10.1021/jm00093a025
	CHEMBL317518	107386	None	0	Guinea pig	Functional	pIC50	=	4.4	4.4	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	279	5	1	4	1.8	CN(C)CCCN1C(=O)CSC1c1ccc(N)cc1	10.1021/jm00093a025
	44224259	62743	None	4	Human	Functional	pIC50	=	6.4	6.4	30	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assay	ChEMBL	291	3	0	3	3.3	CN1CCc2c(c3ccccc3n2CCc2cccnc2)C1	10.1016/j.bmcl.2009.04.128
	CHEMBL1783959	62743	None	4	Human	Functional	pIC50	=	6.4	6.4	30	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assay	ChEMBL	291	3	0	3	3.3	CN1CCc2c(c3ccccc3n2CCc2cccnc2)C1	10.1016/j.bmcl.2009.04.128
	13623358	98792	None	0	Guinea pig	Functional	pIC50	=	6.4	6.4	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	260	3	1	5	0.8	CN1CCN(c2nc3ccccc3n2CCO)CC1	10.1021/jm00157a010
	CHEMBL277956	98792	None	0	Guinea pig	Functional	pIC50	=	6.4	6.4	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	260	3	1	5	0.8	CN1CCN(c2nc3ccccc3n2CCO)CC1	10.1021/jm00157a010
	15542881	112654	None	0	Human	Functional	pIC50	=	6.4	6.4	-3	2	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	687	12	0	9	6.3	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4cccnc4)CC3)(c3ccccc3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10097-X
	CHEMBL330172	112654	None	0	Human	Functional	pIC50	=	6.4	6.4	-3	2	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	687	12	0	9	6.3	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4cccnc4)CC3)(c3ccccc3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10097-X
	145966333	164155	None	0	Human	Functional	pIC50	=	6.4	6.4	-346	6	Antagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assay	ChEMBL	424	8	1	6	3.6	CNC(=O)c1cc(OCCCCN2CCN(c3cccc4sccc34)CC2)ccn1	10.1016/j.bmcl.2018.01.038
	CHEMBL4209188	164155	None	0	Human	Functional	pIC50	=	6.4	6.4	-346	6	Antagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assay	ChEMBL	424	8	1	6	3.6	CNC(=O)c1cc(OCCCCN2CCN(c3cccc4sccc34)CC2)ccn1	10.1016/j.bmcl.2018.01.038
	13623355	64365	None	0	Guinea pig	Functional	pIC50	=	7.4	7.4	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	304	6	1	6	0.8	CN1CCN(c2nc3ccccc3n2CCOCCO)CC1	10.1021/jm00157a010
	CHEMBL18122	64365	None	0	Guinea pig	Functional	pIC50	=	7.4	7.4	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	304	6	1	6	0.8	CN1CCN(c2nc3ccccc3n2CCOCCO)CC1	10.1021/jm00157a010
	242	470	None	70	Human	Functional	pIC50	=	6.4	6.4	-97	33	Antagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay	ChEMBL	447	7	1	4	4.9	O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl	10.1016/j.ejmech.2017.12.099
	34	470	None	70	Human	Functional	pIC50	=	6.4	6.4	-97	33	Antagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay	ChEMBL	447	7	1	4	4.9	O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl	10.1016/j.ejmech.2017.12.099
	60795	470	None	70	Human	Functional	pIC50	=	6.4	6.4	-97	33	Antagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay	ChEMBL	447	7	1	4	4.9	O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl	10.1016/j.ejmech.2017.12.099
	60795.0	470	None	70	Human	Functional	pIC50	=	6.4	6.4	-97	33	Antagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay	ChEMBL	447	7	1	4	4.9	O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl	10.1016/j.ejmech.2017.12.099
	CHEMBL1112	470	None	70	Human	Functional	pIC50	=	6.4	6.4	-97	33	Antagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay	ChEMBL	447	7	1	4	4.9	O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl	10.1016/j.ejmech.2017.12.099
	DB01238	470	None	70	Human	Functional	pIC50	=	6.4	6.4	-97	33	Antagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay	ChEMBL	447	7	1	4	4.9	O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl	10.1016/j.ejmech.2017.12.099
	242	470	None	70	Human	Functional	pIC50	=	6.4	6.4	-97	33	Antagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assay	ChEMBL	447	7	1	4	4.9	O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl	10.1016/j.bmcl.2018.01.038
	34	470	None	70	Human	Functional	pIC50	=	6.4	6.4	-97	33	Antagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assay	ChEMBL	447	7	1	4	4.9	O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl	10.1016/j.bmcl.2018.01.038
	60795	470	None	70	Human	Functional	pIC50	=	6.4	6.4	-97	33	Antagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assay	ChEMBL	447	7	1	4	4.9	O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl	10.1016/j.bmcl.2018.01.038
	60795.0	470	None	70	Human	Functional	pIC50	=	6.4	6.4	-97	33	Antagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assay	ChEMBL	447	7	1	4	4.9	O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl	10.1016/j.bmcl.2018.01.038
	CHEMBL1112	470	None	70	Human	Functional	pIC50	=	6.4	6.4	-97	33	Antagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assay	ChEMBL	447	7	1	4	4.9	O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl	10.1016/j.bmcl.2018.01.038
	DB01238	470	None	70	Human	Functional	pIC50	=	6.4	6.4	-97	33	Antagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assay	ChEMBL	447	7	1	4	4.9	O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl	10.1016/j.bmcl.2018.01.038
	13623339	63315	None	0	Guinea pig	Functional	pIC50	=	5.4	5.4	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	356	10	0	4	4.9	CCCCCCCCCCn1c(N2CCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	CHEMBL17931	63315	None	0	Guinea pig	Functional	pIC50	=	5.4	5.4	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	356	10	0	4	4.9	CCCCCCCCCCn1c(N2CCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	13623356	62512	None	0	Guinea pig	Functional	pIC50	=	6.4	6.4	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	350	6	0	5	3.0	CN1CCN(c2nc3ccccc3n2CCOCc2ccccc2)CC1	10.1021/jm00157a010
	CHEMBL17808	62512	None	0	Guinea pig	Functional	pIC50	=	6.4	6.4	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	350	6	0	5	3.0	CN1CCN(c2nc3ccccc3n2CCOCc2ccccc2)CC1	10.1021/jm00157a010
	10283825	96746	None	0	Human	Functional	pIC50	=	6.4	6.4	-1	2	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	740	12	0	8	7.3	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc(F)cc3F)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10097-X
	CHEMBL264007	96746	None	0	Human	Functional	pIC50	=	6.4	6.4	-1	2	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	740	12	0	8	7.3	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc(F)cc3F)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10097-X
	10147107	210079	None	0	Human	Functional	pIC50	=	6.4	6.4	-3	2	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	755	12	0	9	7.6	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccccn4)CC3)(c3ccc(Cl)c(Cl)c3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10097-X
	CHEMBL431850	210079	None	0	Human	Functional	pIC50	=	6.4	6.4	-3	2	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	755	12	0	9	7.6	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccccn4)CC3)(c3ccc(Cl)c(Cl)c3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10097-X
	CHEMBL95125	210079	None	0	Human	Functional	pIC50	=	6.4	6.4	-3	2	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	755	12	0	9	7.6	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccccn4)CC3)(c3ccc(Cl)c(Cl)c3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10097-X
	145964299	164227	None	0	Human	Functional	pIC50	=	5.4	5.4	-489	6	Antagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assay	ChEMBL	426	8	1	6	3.8	CNC(=O)c1cc(OCCCCN2CCC(c3noc4cc(F)ccc34)CC2)ccn1	10.1016/j.bmcl.2018.01.038
	CHEMBL4210030	164227	None	0	Human	Functional	pIC50	=	5.4	5.4	-489	6	Antagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assay	ChEMBL	426	8	1	6	3.8	CNC(=O)c1cc(OCCCCN2CCC(c3noc4cc(F)ccc34)CC2)ccn1	10.1016/j.bmcl.2018.01.038
	44327909	112421	None	0	Human	Functional	pIC50	=	6.4	6.4	-37	2	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	706	14	0	10	6.5	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4CCOc4ccco4)CC3)(c3ccccc3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10097-X
	CHEMBL329450	112421	None	0	Human	Functional	pIC50	=	6.4	6.4	-37	2	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	706	14	0	10	6.5	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4CCOc4ccco4)CC3)(c3ccccc3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10097-X
	101616	15772	None	19	Human	Functional	pIC50	=	4.4	4.4	-3	2	Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay	ChEMBL	337	6	1	3	4.2	CN1[C@H](C[C@H](O)c2ccccc2)CCC[C@@H]1CC(=O)c1ccccc1	10.1021/jm300671m
	CHEMBL122270	15772	None	19	Human	Functional	pIC50	=	4.4	4.4	-3	2	Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay	ChEMBL	337	6	1	3	4.2	CN1[C@H](C[C@H](O)c2ccccc2)CCC[C@@H]1CC(=O)c1ccccc1	10.1021/jm300671m
	2389	3331	None	72	Human	Functional	pIC50	=	6.3	6.3	-234	29	Antagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay	ChEMBL	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	10.1016/j.ejmech.2017.12.099
	5073	3331	None	72	Human	Functional	pIC50	=	6.3	6.3	-234	29	Antagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay	ChEMBL	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	10.1016/j.ejmech.2017.12.099
	5073.0	3331	None	72	Human	Functional	pIC50	=	6.3	6.3	-234	29	Antagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay	ChEMBL	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	10.1016/j.ejmech.2017.12.099
	96	3331	None	72	Human	Functional	pIC50	=	6.3	6.3	-234	29	Antagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay	ChEMBL	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	10.1016/j.ejmech.2017.12.099
	CHEMBL85	3331	None	72	Human	Functional	pIC50	=	6.3	6.3	-234	29	Antagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay	ChEMBL	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	10.1016/j.ejmech.2017.12.099
	DB00734	3331	None	72	Human	Functional	pIC50	=	6.3	6.3	-234	29	Antagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay	ChEMBL	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	10.1016/j.ejmech.2017.12.099
	2389	3331	None	72	Human	Functional	pIC50	=	6.3	6.3	-234	29	Antagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assay	ChEMBL	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	10.1016/j.bmcl.2018.01.038
	5073	3331	None	72	Human	Functional	pIC50	=	6.3	6.3	-234	29	Antagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assay	ChEMBL	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	10.1016/j.bmcl.2018.01.038
	5073.0	3331	None	72	Human	Functional	pIC50	=	6.3	6.3	-234	29	Antagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assay	ChEMBL	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	10.1016/j.bmcl.2018.01.038
	96	3331	None	72	Human	Functional	pIC50	=	6.3	6.3	-234	29	Antagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assay	ChEMBL	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	10.1016/j.bmcl.2018.01.038
	CHEMBL85	3331	None	72	Human	Functional	pIC50	=	6.3	6.3	-234	29	Antagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assay	ChEMBL	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	10.1016/j.bmcl.2018.01.038
	DB00734	3331	None	72	Human	Functional	pIC50	=	6.3	6.3	-234	29	Antagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assay	ChEMBL	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	10.1016/j.bmcl.2018.01.038
	1227	2489	None	32	Human	Functional	pIC50	=	7.3	7.3	2	14	Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1021/jm300671m
	2331	2489	None	32	Human	Functional	pIC50	=	7.3	7.3	2	14	Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1021/jm300671m
	3957	2489	None	32	Human	Functional	pIC50	=	7.3	7.3	2	14	Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1021/jm300671m
	4992	2489	None	32	Human	Functional	pIC50	=	7.3	7.3	2	14	Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1021/jm300671m
	4992.0	2489	None	32	Human	Functional	pIC50	=	7.3	7.3	2	14	Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1021/jm300671m
	CHEMBL511	2489	None	32	Human	Functional	pIC50	=	7.3	7.3	2	14	Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1021/jm300671m
	DB06691	2489	None	32	Human	Functional	pIC50	=	7.3	7.3	2	14	Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1021/jm300671m
	75201901	166520	None	21	Human	Functional	pIC50	=	5.3	5.3	-208	4	Antagonist activity at histamine H1 receptor (unknown origin)Antagonist activity at histamine H1 receptor (unknown origin)	ChEMBL	356	3	0	6	4.9	Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12	10.1021/acs.jmedchem.8b01622
	CHEMBL4277264	166520	None	21	Human	Functional	pIC50	=	5.3	5.3	-208	4	Antagonist activity at histamine H1 receptor (unknown origin)Antagonist activity at histamine H1 receptor (unknown origin)	ChEMBL	356	3	0	6	4.9	Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12	10.1021/acs.jmedchem.8b01622
	54582938	62739	None	5	Human	Functional	pIC50	=	5.3	5.3	1	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay	ChEMBL	321	4	0	4	3.3	COc1ccc2c(c1)c1c(n2CCc2ccccn2)CCN(C)C1	10.1016/j.bmcl.2009.04.128
	CHEMBL1783955	62739	None	5	Human	Functional	pIC50	=	5.3	5.3	1	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay	ChEMBL	321	4	0	4	3.3	COc1ccc2c(c1)c1c(n2CCc2ccccn2)CCN(C)C1	10.1016/j.bmcl.2009.04.128
	54580942	62751	None	7	Human	Functional	pIC50	=	6.3	6.3	13	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assay	ChEMBL	309	3	0	3	3.4	CN1CCc2c(c3cc(F)ccc3n2CCc2ccncc2)C1	10.1016/j.bmcl.2009.04.128
	CHEMBL1783967	62751	None	7	Human	Functional	pIC50	=	6.3	6.3	13	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assay	ChEMBL	309	3	0	3	3.4	CN1CCc2c(c3cc(F)ccc3n2CCc2ccncc2)C1	10.1016/j.bmcl.2009.04.128
	10315027	98983	None	0	Guinea pig	Functional	pIC50	=	6.3	6.3	-	1	In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileumIn vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum	ChEMBL	337	3	0	1	5.5	c1ccc(CN2CCC3=C(C2)C(c2ccccc2)c2ccccc23)cc1	10.1016/s0960-894x(00)00199-2
	CHEMBL279454	98983	None	0	Guinea pig	Functional	pIC50	=	6.3	6.3	-	1	In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileumIn vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum	ChEMBL	337	3	0	1	5.5	c1ccc(CN2CCC3=C(C2)C(c2ccccc2)c2ccccc23)cc1	10.1016/s0960-894x(00)00199-2
	15542673	210023	None	0	Human	Functional	pIC50	=	6.3	6.3	-1	2	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	772	12	0	8	8.0	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc(C(F)(F)F)cc3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10097-X
	CHEMBL94834	210023	None	0	Human	Functional	pIC50	=	6.3	6.3	-1	2	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	772	12	0	8	8.0	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc(C(F)(F)F)cc3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10097-X
	10305888	210014	None	0	Human	Functional	pIC50	=	8.3	8.3	1	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	750	14	1	9	7.0	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4CCCC(=O)O)CC3)(c3ccc(Cl)c(Cl)c3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10098-1
	CHEMBL94788	210014	None	0	Human	Functional	pIC50	=	8.3	8.3	1	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	750	14	1	9	7.0	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4CCCC(=O)O)CC3)(c3ccc(Cl)c(Cl)c3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10098-1
	44328321	167891	None	0	Human	Functional	pIC50	=	8.3	8.3	1	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	788	17	1	10	7.4	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4CCCCOc4ccccc4C(=O)O)CC3)(c3ccccc3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10098-1
	CHEMBL430471	167891	None	0	Human	Functional	pIC50	=	8.3	8.3	1	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	788	17	1	10	7.4	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4CCCCOc4ccccc4C(=O)O)CC3)(c3ccccc3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10098-1
	10305069	210309	None	0	Human	Functional	pIC50	=	8.2	8.2	1	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	656	12	1	9	5.4	COc1ccc(C2(CCN3CCC(C(=O)c4nc5ccccc5[nH]4)CC3)CCN(C(=O)c3cc(OC)c(OC)c(OC)c3)C2)cc1OC	10.1016/S0960-894X(97)10098-1
	CHEMBL96441	210309	None	0	Human	Functional	pIC50	=	8.2	8.2	1	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	656	12	1	9	5.4	COc1ccc(C2(CCN3CCC(C(=O)c4nc5ccccc5[nH]4)CC3)CCN(C(=O)c3cc(OC)c(OC)c(OC)c3)C2)cc1OC	10.1016/S0960-894X(97)10098-1
	10234086	111697	None	0	Human	Functional	pIC50	=	8.2	8.2	-6	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	744	13	0	10	6.7	COC(=O)c1ccc(Cn2c(C(=O)C3CCN(CCC4(c5ccccc5)CCN(C(=O)c5cc(OC)c(OC)c(OC)c5)C4)CC3)nc3ccccc32)cc1	10.1016/S0960-894X(97)10098-1
	CHEMBL328511	111697	None	0	Human	Functional	pIC50	=	8.2	8.2	-6	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	744	13	0	10	6.7	COC(=O)c1ccc(Cn2c(C(=O)C3CCN(CCC4(c5ccccc5)CCN(C(=O)c5cc(OC)c(OC)c(OC)c5)C4)CC3)nc3ccccc32)cc1	10.1016/S0960-894X(97)10098-1
	13623335	98855	None	0	Guinea pig	Functional	pIC50	=	7.3	7.3	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	272	4	0	4	2.6	CCCCn1c(N2CCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	CHEMBL278456	98855	None	0	Guinea pig	Functional	pIC50	=	7.3	7.3	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	272	4	0	4	2.6	CCCCn1c(N2CCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	10121390	112802	None	0	Human	Functional	pIC50	=	6.3	6.3	-3	2	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	596	10	1	7	5.4	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5[nH]4)CC3)(c3ccccc3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10097-X
	CHEMBL330499	112802	None	0	Human	Functional	pIC50	=	6.3	6.3	-3	2	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	596	10	1	7	5.4	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5[nH]4)CC3)(c3ccccc3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10097-X
	10190413	209788	None	0	Human	Functional	pIC50	=	6.3	6.3	-3	2	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	717	13	0	10	6.3	COc1ccc(C2(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccccn4)CC3)CCN(C(=O)c3cc(OC)c(OC)c(OC)c3)C2)cc1	10.1016/S0960-894X(97)10097-X
	CHEMBL410270	209788	None	0	Human	Functional	pIC50	=	6.3	6.3	-3	2	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	717	13	0	10	6.3	COc1ccc(C2(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccccn4)CC3)CCN(C(=O)c3cc(OC)c(OC)c(OC)c3)C2)cc1	10.1016/S0960-894X(97)10097-X
	CHEMBL93519	209788	None	0	Human	Functional	pIC50	=	6.3	6.3	-3	2	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	717	13	0	10	6.3	COc1ccc(C2(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccccn4)CC3)CCN(C(=O)c3cc(OC)c(OC)c(OC)c3)C2)cc1	10.1016/S0960-894X(97)10097-X
	54579957	62748	None	4	Human	Functional	pIC50	=	6.3	6.3	36	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assay	ChEMBL	291	3	0	3	3.3	CN1CCc2c(c3ccccc3n2CCc2ccncc2)C1	10.1016/j.bmcl.2009.04.128
	CHEMBL1783964	62748	None	4	Human	Functional	pIC50	=	6.3	6.3	36	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assay	ChEMBL	291	3	0	3	3.3	CN1CCc2c(c3ccccc3n2CCc2ccncc2)C1	10.1016/j.bmcl.2009.04.128
	44126329	62738	None	5	Human	Functional	pIC50	=	6.3	6.3	-2	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay	ChEMBL	305	3	0	3	3.6	Cc1ccc2c(c1)c1c(n2CCc2ccccn2)CCN(C)C1	10.1016/j.bmcl.2009.04.128
	CHEMBL1783954	62738	None	5	Human	Functional	pIC50	=	6.3	6.3	-2	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay	ChEMBL	305	3	0	3	3.6	Cc1ccc2c(c1)c1c(n2CCc2ccccn2)CCN(C)C1	10.1016/j.bmcl.2009.04.128
	44126330	62744	None	4	Human	Functional	pIC50	=	6.3	6.3	-2	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay	ChEMBL	305	3	0	3	3.6	Cc1ccc2c(c1)c1c(n2CCc2cccnc2)CCN(C)C1	10.1016/j.bmcl.2009.04.128
	CHEMBL1783960	62744	None	4	Human	Functional	pIC50	=	6.3	6.3	-2	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay	ChEMBL	305	3	0	3	3.6	Cc1ccc2c(c1)c1c(n2CCc2cccnc2)CCN(C)C1	10.1016/j.bmcl.2009.04.128
	13623348	59059	None	0	Guinea pig	Functional	pIC50	=	6.3	6.3	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	300	5	0	4	3.2	CCCC(C)Cn1c(N2CCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	CHEMBL16939	59059	None	0	Guinea pig	Functional	pIC50	=	6.3	6.3	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	300	5	0	4	3.2	CCCC(C)Cn1c(N2CCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	10423703	107351	None	0	Guinea pig	Functional	pIC50	=	5.3	5.3	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	278	5	0	3	2.5	Cc1cccc(C2SCC(=O)N2CCCN(C)C)c1	10.1021/jm00093a025
	CHEMBL1202942	107351	None	0	Guinea pig	Functional	pIC50	=	5.3	5.3	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	278	5	0	3	2.5	Cc1cccc(C2SCC(=O)N2CCCN(C)C)c1	10.1021/jm00093a025
	CHEMBL317171	107351	None	0	Guinea pig	Functional	pIC50	=	5.3	5.3	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	278	5	0	3	2.5	Cc1cccc(C2SCC(=O)N2CCCN(C)C)c1	10.1021/jm00093a025
	10300214	84233	None	0	Human	Functional	pIC50	=	5.3	5.3	-	1	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	492	9	2	5	5.0	O=C(Nc1ccccc1OCC(O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)C1CCC1	10.1016/j.bmcl.2012.09.113
	CHEMBL2208416	84233	None	0	Human	Functional	pIC50	=	5.3	5.3	-	1	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	492	9	2	5	5.0	O=C(Nc1ccccc1OCC(O)CN1CCC(Oc2ccc(Cl)c(Cl)c2)CC1)C1CCC1	10.1016/j.bmcl.2012.09.113
	15830914	98960	None	0	Guinea pig	Functional	pIC50	=	7.3	7.3	-	1	In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileumIn vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum	ChEMBL	245	1	1	1	3.5	C1=C2C(=C(c3ccccc3)c3ccccc32)CNC1	10.1016/s0960-894x(00)00199-2
	CHEMBL279297	98960	None	0	Guinea pig	Functional	pIC50	=	7.3	7.3	-	1	In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileumIn vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum	ChEMBL	245	1	1	1	3.5	C1=C2C(=C(c3ccccc3)c3ccccc32)CNC1	10.1016/s0960-894x(00)00199-2
	13623351	61176	None	0	Guinea pig	Functional	pIC50	=	6.3	6.3	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	318	6	0	5	2.9	CCSCCCn1c(N2CCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	CHEMBL17655	61176	None	0	Guinea pig	Functional	pIC50	=	6.3	6.3	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	318	6	0	5	2.9	CCSCCCn1c(N2CCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	54582940	62742	None	4	Human	Functional	pIC50	=	6.3	6.3	1	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay	ChEMBL	359	3	0	3	4.3	CN1CCc2c(c3cc(C(F)(F)F)ccc3n2CCc2ccccn2)C1	10.1016/j.bmcl.2009.04.128
	CHEMBL1783958	62742	None	4	Human	Functional	pIC50	=	6.3	6.3	1	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay	ChEMBL	359	3	0	3	4.3	CN1CCc2c(c3cc(C(F)(F)F)ccc3n2CCc2ccccn2)C1	10.1016/j.bmcl.2009.04.128
	2600	3779	None	53	Human	Functional	pIC50	=	6.3	6.3	4	32	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	471	8	2	3	6.4	OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O	10.1016/S0960-894X(97)10097-X
	2608	3779	None	53	Human	Functional	pIC50	=	6.3	6.3	4	32	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	471	8	2	3	6.4	OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O	10.1016/S0960-894X(97)10097-X
	5405	3779	None	53	Human	Functional	pIC50	=	6.3	6.3	4	32	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	471	8	2	3	6.4	OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O	10.1016/S0960-894X(97)10097-X
	CHEMBL17157	3779	None	53	Human	Functional	pIC50	=	6.3	6.3	4	32	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	471	8	2	3	6.4	OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O	10.1016/S0960-894X(97)10097-X
	DB00342	3779	None	53	Human	Functional	pIC50	=	6.3	6.3	4	32	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	471	8	2	3	6.4	OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O	10.1016/S0960-894X(97)10097-X
	10917690	210064	None	1	Human	Functional	pIC50	=	7.2	7.2	-3	4	Compound was evaluated for the antagonistic activity against H1 receptorCompound was evaluated for the antagonistic activity against H1 receptor	ChEMBL	471	8	0	5	5.4	COc1ccc(CCN2CCC(C(=O)c3nc4ccccc4n3Cc3ccc(F)cc3)CC2)cc1	10.1016/S0960-894X(97)10097-X
	CHEMBL95051	210064	None	1	Human	Functional	pIC50	=	7.2	7.2	-3	4	Compound was evaluated for the antagonistic activity against H1 receptorCompound was evaluated for the antagonistic activity against H1 receptor	ChEMBL	471	8	0	5	5.4	COc1ccc(CCN2CCC(C(=O)c3nc4ccccc4n3Cc3ccc(F)cc3)CC2)cc1	10.1016/S0960-894X(97)10097-X
	44328320	210060	None	0	Human	Functional	pIC50	=	8.2	8.2	1	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	802	17	0	11	7.5	COC(=O)c1ccccc1OCCCCn1c(C(=O)C2CCN(CCC3(c4ccccc4)CCN(C(=O)c4cc(OC)c(OC)c(OC)c4)C3)CC2)nc2ccccc21	10.1016/S0960-894X(97)10098-1
	CHEMBL95029	210060	None	0	Human	Functional	pIC50	=	8.2	8.2	1	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	802	17	0	11	7.5	COC(=O)c1ccccc1OCCCCn1c(C(=O)C2CCN(CCC3(c4ccccc4)CCN(C(=O)c4cc(OC)c(OC)c(OC)c4)C3)CC2)nc2ccccc21	10.1016/S0960-894X(97)10098-1
	10147218	107522	None	0	Human	Functional	pIC50	=	8.2	8.2	1	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	778	15	0	10	7.5	CCOC(=O)CCCn1c(C(=O)C2CCN(CCC3(c4ccc(Cl)c(Cl)c4)CCN(C(=O)c4cc(OC)c(OC)c(OC)c4)C3)CC2)nc2ccccc21	10.1016/S0960-894X(97)10098-1
	CHEMBL318369	107522	None	0	Human	Functional	pIC50	=	8.2	8.2	1	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	778	15	0	10	7.5	CCOC(=O)CCCn1c(C(=O)C2CCN(CCC3(c4ccc(Cl)c(Cl)c4)CCN(C(=O)c4cc(OC)c(OC)c(OC)c4)C3)CC2)nc2ccccc21	10.1016/S0960-894X(97)10098-1
	10169609	210104	None	0	Human	Functional	pIC50	=	8.2	8.2	1	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	804	15	0	12	6.7	COC(=O)c1ccc(Cn2c(C(=O)C3CCN(CCC4(c5ccc(OC)c(OC)c5)CCN(C(=O)c5cc(OC)c(OC)c(OC)c5)C4)CC3)nc3ccccc32)cc1	10.1016/S0960-894X(97)10098-1
	CHEMBL95243	210104	None	0	Human	Functional	pIC50	=	8.2	8.2	1	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	804	15	0	12	6.7	COC(=O)c1ccc(Cn2c(C(=O)C3CCN(CCC4(c5ccc(OC)c(OC)c5)CCN(C(=O)c5cc(OC)c(OC)c(OC)c5)C4)CC3)nc3ccccc32)cc1	10.1016/S0960-894X(97)10098-1
	3219	202251	None	48	Guinea pig	Functional	pIC50	=	8.2	8.2	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	302	5	0	5	2.2	CCOCCn1c(N2CCCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	3219.0	202251	None	48	Guinea pig	Functional	pIC50	=	8.2	8.2	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	302	5	0	5	2.2	CCOCCn1c(N2CCCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	CHEMBL594	202251	None	48	Guinea pig	Functional	pIC50	=	8.2	8.2	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	302	5	0	5	2.2	CCOCCn1c(N2CCCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	DB01084	202251	None	48	Guinea pig	Functional	pIC50	=	8.2	8.2	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	302	5	0	5	2.2	CCOCCn1c(N2CCCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	44328188	111589	None	0	Human	Functional	pIC50	=	8.2	8.2	1	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	728	16	0	11	5.9	CCOCCn1c(C(=O)C2CCN(CCC3(c4ccc(OC)c(OC)c4)CCN(C(=O)c4cc(OC)c(OC)c(OC)c4)C3)CC2)nc2ccccc21	10.1016/S0960-894X(97)10098-1
	CHEMBL327888	111589	None	0	Human	Functional	pIC50	=	8.2	8.2	1	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	728	16	0	11	5.9	CCOCCn1c(C(=O)C2CCN(CCC3(c4ccc(OC)c(OC)c4)CCN(C(=O)c4cc(OC)c(OC)c(OC)c4)C3)CC2)nc2ccccc21	10.1016/S0960-894X(97)10098-1
	15542880	209965	None	0	Human	Functional	pIC50	=	8.2	8.2	1	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	705	12	0	9	6.4	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccccn4)CC3)(c3ccc(F)cc3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10098-1
	CHEMBL94480	209965	None	0	Human	Functional	pIC50	=	8.2	8.2	1	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	705	12	0	9	6.4	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccccn4)CC3)(c3ccc(F)cc3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10098-1
	10284042	210445	None	0	Human	Functional	pIC50	=	8.2	8.2	1	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	777	13	0	10	6.5	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4CCN4CCOCC4)CC3)(c3ccc(Cl)c(Cl)c3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10098-1
	CHEMBL97240	210445	None	0	Human	Functional	pIC50	=	8.2	8.2	1	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	777	13	0	10	6.5	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4CCN4CCOCC4)CC3)(c3ccc(Cl)c(Cl)c3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10098-1
	10121390	112802	None	0	Human	Functional	pIC50	=	8.2	8.2	-3	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	596	10	1	7	5.4	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5[nH]4)CC3)(c3ccccc3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10098-1
	CHEMBL330499	112802	None	0	Human	Functional	pIC50	=	8.2	8.2	-3	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	596	10	1	7	5.4	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5[nH]4)CC3)(c3ccccc3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10098-1
	10190413	209788	None	0	Human	Functional	pIC50	=	8.2	8.2	-3	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	717	13	0	10	6.3	COc1ccc(C2(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccccn4)CC3)CCN(C(=O)c3cc(OC)c(OC)c(OC)c3)C2)cc1	10.1016/S0960-894X(97)10098-1
	CHEMBL410270	209788	None	0	Human	Functional	pIC50	=	8.2	8.2	-3	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	717	13	0	10	6.3	COc1ccc(C2(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccccn4)CC3)CCN(C(=O)c3cc(OC)c(OC)c(OC)c3)C2)cc1	10.1016/S0960-894X(97)10098-1
	CHEMBL93519	209788	None	0	Human	Functional	pIC50	=	8.2	8.2	-3	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	717	13	0	10	6.3	COc1ccc(C2(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccccn4)CC3)CCN(C(=O)c3cc(OC)c(OC)c(OC)c3)C2)cc1	10.1016/S0960-894X(97)10098-1
	15542673	210023	None	0	Human	Functional	pIC50	=	8.2	8.2	-1	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	772	12	0	8	8.0	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc(C(F)(F)F)cc3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10098-1
	CHEMBL94834	210023	None	0	Human	Functional	pIC50	=	8.2	8.2	-1	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	772	12	0	8	8.0	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc(C(F)(F)F)cc3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10098-1
	15542869	210068	None	0	Human	Functional	pIC50	=	8.2	8.2	1	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	720	15	0	10	6.6	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4CCOCc4ccco4)CC3)(c3ccccc3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10098-1
	CHEMBL95076	210068	None	0	Human	Functional	pIC50	=	8.2	8.2	1	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	720	15	0	10	6.6	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4CCOCc4ccco4)CC3)(c3ccccc3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10098-1
	10283825	96746	None	0	Human	Functional	pIC50	=	8.2	8.2	-1	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	740	12	0	8	7.3	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc(F)cc3F)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10098-1
	CHEMBL264007	96746	None	0	Human	Functional	pIC50	=	8.2	8.2	-1	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	740	12	0	8	7.3	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc(F)cc3F)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10098-1
	10147107	210079	None	0	Human	Functional	pIC50	=	8.2	8.2	-3	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	755	12	0	9	7.6	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccccn4)CC3)(c3ccc(Cl)c(Cl)c3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10098-1
	CHEMBL431850	210079	None	0	Human	Functional	pIC50	=	8.2	8.2	-3	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	755	12	0	9	7.6	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccccn4)CC3)(c3ccc(Cl)c(Cl)c3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10098-1
	CHEMBL95125	210079	None	0	Human	Functional	pIC50	=	8.2	8.2	-3	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	755	12	0	9	7.6	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccccn4)CC3)(c3ccc(Cl)c(Cl)c3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10098-1
	15542881	112654	None	0	Human	Functional	pIC50	=	8.2	8.2	-3	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	687	12	0	9	6.3	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4cccnc4)CC3)(c3ccccc3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10098-1
	CHEMBL330172	112654	None	0	Human	Functional	pIC50	=	8.2	8.2	-3	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	687	12	0	9	6.3	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4cccnc4)CC3)(c3ccccc3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10098-1
	15542679	108583	None	0	Human	Functional	pIC50	=	8.2	8.2	1	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	664	10	1	7	6.7	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5[nH]4)CC3)(c3ccc(Cl)c(Cl)c3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10098-1
	CHEMBL320003	108583	None	0	Human	Functional	pIC50	=	8.2	8.2	1	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	664	10	1	7	6.7	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5[nH]4)CC3)(c3ccc(Cl)c(Cl)c3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10098-1
	10122529	109612	None	0	Human	Functional	pIC50	=	8.2	8.2	-3	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	668	14	0	9	5.9	CCOCCn1c(C(=O)C2CCN(CCC3(c4ccccc4)CCN(C(=O)c4cc(OC)c(OC)c(OC)c4)C3)CC2)nc2ccccc21	10.1016/S0960-894X(97)10098-1
	CHEMBL322194	109612	None	0	Human	Functional	pIC50	=	8.2	8.2	-3	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	668	14	0	9	5.9	CCOCCn1c(C(=O)C2CCN(CCC3(c4ccccc4)CCN(C(=O)c4cc(OC)c(OC)c(OC)c4)C3)CC2)nc2ccccc21	10.1016/S0960-894X(97)10098-1
	10233656	210310	None	0	Human	Functional	pIC50	=	8.2	8.2	-3	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	687	12	0	9	6.3	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccccn4)CC3)(c3ccccc3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10098-1
	CHEMBL96442	210310	None	0	Human	Functional	pIC50	=	8.2	8.2	-3	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	687	12	0	9	6.3	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccccn4)CC3)(c3ccccc3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10098-1
	18333241	210252	None	0	Human	Functional	pIC50	=	8.2	8.2	1	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	736	14	0	9	7.2	CCOCCn1c(C(=O)C2CCN(CCC3(c4ccc(Cl)c(Cl)c4)CCN(C(=O)c4cc(OC)c(OC)c(OC)c4)C3)CC2)nc2ccccc21	10.1016/S0960-894X(97)10098-1
	CHEMBL96141	210252	None	0	Human	Functional	pIC50	=	8.2	8.2	1	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	736	14	0	9	7.2	CCOCCn1c(C(=O)C2CCN(CCC3(c4ccc(Cl)c(Cl)c4)CCN(C(=O)c4cc(OC)c(OC)c(OC)c4)C3)CC2)nc2ccccc21	10.1016/S0960-894X(97)10098-1
	9918576	209796	None	0	Human	Functional	pIC50	=	8.2	8.2	-2	3	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	764	14	0	10	7.0	COc1ccc(C2(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)CCN(C(=O)c3cc(OC)c(OC)c(OC)c3)C2)cc1OC	10.1016/S0960-894X(97)10098-1
	CHEMBL93556	209796	None	0	Human	Functional	pIC50	=	8.2	8.2	-2	3	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	764	14	0	10	7.0	COc1ccc(C2(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)CCN(C(=O)c3cc(OC)c(OC)c(OC)c3)C2)cc1OC	10.1016/S0960-894X(97)10098-1
	10168749	210080	None	0	Human	Functional	pIC50	=	8.2	8.2	-3	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	676	12	0	9	6.5	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccco4)CC3)(c3ccccc3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10098-1
	CHEMBL95127	210080	None	0	Human	Functional	pIC50	=	8.2	8.2	-3	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	676	12	0	9	6.5	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccco4)CC3)(c3ccccc3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10098-1
	15542879	112887	None	0	Human	Functional	pIC50	=	8.2	8.2	-2	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	687	12	0	9	6.3	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccncc4)CC3)(c3ccccc3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10098-1
	CHEMBL330719	112887	None	0	Human	Functional	pIC50	=	8.2	8.2	-2	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	687	12	0	9	6.3	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccncc4)CC3)(c3ccccc3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10098-1
	10190770	210474	None	0	Human	Functional	pIC50	=	8.2	8.2	-1	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	772	12	0	8	8.3	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc(Cl)c(Cl)c3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10098-1
	CHEMBL330430	210474	None	0	Human	Functional	pIC50	=	8.2	8.2	-1	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	772	12	0	8	8.3	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc(Cl)c(Cl)c3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10098-1
	CHEMBL97357	210474	None	0	Human	Functional	pIC50	=	8.2	8.2	-1	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	772	12	0	8	8.3	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc(Cl)c(Cl)c3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10098-1
	10190638	210001	None	0	Human	Functional	pIC50	=	8.2	8.2	-1	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	748	12	0	10	6.7	COc1ccc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc4c(c3)OCO4)C2)c(OC)c1OC	10.1016/S0960-894X(97)10098-1
	CHEMBL94726	210001	None	0	Human	Functional	pIC50	=	8.2	8.2	-1	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	748	12	0	10	6.7	COc1ccc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc4c(c3)OCO4)C2)c(OC)c1OC	10.1016/S0960-894X(97)10098-1
	10283765	108143	None	0	Human	Functional	pIC50	=	8.2	8.2	1	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	730	12	0	8	7.4	CC(C)Oc1cccc(CC(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc4c(c3)OCO4)C2)c1	10.1016/S0960-894X(97)10098-1
	CHEMBL319535	108143	None	0	Human	Functional	pIC50	=	8.2	8.2	1	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	730	12	0	8	7.4	CC(C)Oc1cccc(CC(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc4c(c3)OCO4)C2)c1	10.1016/S0960-894X(97)10098-1
	18333379	210034	None	0	Human	Functional	pIC50	=	8.2	8.2	1	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	686	15	0	9	5.9	CCOCCn1c(C(=O)C2CCN(CCC3(c4ccc(F)cc4)CCN(Cc4cc(OC)c(OC)c(OC)c4)C3=O)CC2)nc2ccccc21	10.1016/S0960-894X(97)10098-1
	CHEMBL94906	210034	None	0	Human	Functional	pIC50	=	8.2	8.2	1	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	686	15	0	9	5.9	CCOCCn1c(C(=O)C2CCN(CCC3(c4ccc(F)cc4)CCN(Cc4cc(OC)c(OC)c(OC)c4)C3=O)CC2)nc2ccccc21	10.1016/S0960-894X(97)10098-1
	10190056	111501	None	0	Human	Functional	pIC50	=	8.2	8.2	1	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	674	11	0	7	7.0	COc1ccc(C2(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)CCN(C(=O)c3ccccc3)C2)cc1OC	10.1016/S0960-894X(97)10098-1
	CHEMBL327497	111501	None	0	Human	Functional	pIC50	=	8.2	8.2	1	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	674	11	0	7	7.0	COc1ccc(C2(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)CCN(C(=O)c3ccccc3)C2)cc1OC	10.1016/S0960-894X(97)10098-1
	10212223	210599	None	0	Human	Functional	pIC50	=	8.2	8.2	-2	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	704	12	0	8	7.0	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccccc3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10098-1
	CHEMBL431458	210599	None	0	Human	Functional	pIC50	=	8.2	8.2	-2	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	704	12	0	8	7.0	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccccc3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10098-1
	CHEMBL98079	210599	None	0	Human	Functional	pIC50	=	8.2	8.2	-2	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	704	12	0	8	7.0	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccccc3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10098-1
	15542874	112232	None	0	Human	Functional	pIC50	=	8.2	8.2	1	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	786	12	0	8	8.7	COc1cc(C(=O)N2CCCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc(Cl)c(Cl)c3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10098-1
	CHEMBL329055	112232	None	0	Human	Functional	pIC50	=	8.2	8.2	1	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	786	12	0	8	8.7	COc1cc(C(=O)N2CCCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc(Cl)c(Cl)c3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10098-1
	10123138	108582	None	0	Human	Functional	pIC50	=	8.2	8.2	-1	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	748	12	0	10	6.7	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc4c(c3)OCO4)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10098-1
	CHEMBL317524	108582	None	0	Human	Functional	pIC50	=	8.2	8.2	-1	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	748	12	0	10	6.7	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc4c(c3)OCO4)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10098-1
	CHEMBL320002	108582	None	0	Human	Functional	pIC50	=	8.2	8.2	-1	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	748	12	0	10	6.7	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc4c(c3)OCO4)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10098-1
	9832306	112787	None	0	Human	Functional	pIC50	=	8.2	8.2	2	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	806	17	0	10	8.2	CCOc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc(OC)c(OC)c3)C2)cc(OCC)c1OCC	10.1016/S0960-894X(97)10098-1
	CHEMBL330367	112787	None	0	Human	Functional	pIC50	=	8.2	8.2	2	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	806	17	0	10	8.2	CCOc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc(OC)c(OC)c3)C2)cc(OCC)c1OCC	10.1016/S0960-894X(97)10098-1
	CHEMBL330462	112787	None	0	Human	Functional	pIC50	=	8.2	8.2	2	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	806	17	0	10	8.2	CCOc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4Cc4ccc(F)cc4)CC3)(c3ccc(OC)c(OC)c3)C2)cc(OCC)c1OCC	10.1016/S0960-894X(97)10098-1
	15542871	210314	None	0	Human	Functional	pIC50	=	8.2	8.2	-1	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	726	9	0	7	8.0	O=C(c1nc2ccccc2n1Cc1ccc(F)cc1)C1CCN(CCC2(c3ccc4c(c3)OCO4)CCN(C(=O)c3ccc(Cl)cc3Cl)C2)CC1	10.1016/S0960-894X(97)10098-1
	CHEMBL96466	210314	None	0	Human	Functional	pIC50	=	8.2	8.2	-1	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	726	9	0	7	8.0	O=C(c1nc2ccccc2n1Cc1ccc(F)cc1)C1CCN(CCC2(c3ccc4c(c3)OCO4)CCN(C(=O)c3ccc(Cl)cc3Cl)C2)CC1	10.1016/S0960-894X(97)10098-1
	3071016	98631	None	0	Guinea pig	Functional	pIC50	=	8.2	8.2	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	336	5	0	5	2.9	CN1CCN(c2nc3ccccc3n2CCOc2ccccc2)CC1	10.1021/jm00157a010
	CHEMBL276735	98631	None	0	Guinea pig	Functional	pIC50	=	8.2	8.2	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	336	5	0	5	2.9	CN1CCN(c2nc3ccccc3n2CCOc2ccccc2)CC1	10.1021/jm00157a010
	14984032	210800	None	0	Guinea pig	Functional	pIC50	=	4.2	4.2	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	342	5	0	3	3.0	CN(C)CCCN1C(=O)CSC1c1cccc(Br)c1	10.1021/jm00093a025
	CHEMBL1202932	210800	None	0	Guinea pig	Functional	pIC50	=	4.2	4.2	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	342	5	0	3	3.0	CN(C)CCCN1C(=O)CSC1c1cccc(Br)c1	10.1021/jm00093a025
	CHEMBL99350	210800	None	0	Guinea pig	Functional	pIC50	=	4.2	4.2	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	342	5	0	3	3.0	CN(C)CCCN1C(=O)CSC1c1cccc(Br)c1	10.1021/jm00093a025
	54579956	62740	None	4	Human	Functional	pIC50	=	6.2	6.2	3	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assay	ChEMBL	309	3	0	3	3.4	CN1CCc2c(c3cc(F)ccc3n2CCc2ccccn2)C1	10.1016/j.bmcl.2009.04.128
	CHEMBL1783956	62740	None	4	Human	Functional	pIC50	=	6.2	6.2	3	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assay	ChEMBL	309	3	0	3	3.4	CN1CCc2c(c3cc(F)ccc3n2CCc2ccccn2)C1	10.1016/j.bmcl.2009.04.128
	54586813	62745	None	4	Human	Functional	pIC50	=	6.2	6.2	-	1	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay	ChEMBL	309	3	0	3	3.4	CN1CCc2c(c3cc(F)ccc3n2CCc2cccnc2)C1	10.1016/j.bmcl.2009.04.128
	CHEMBL1783961	62745	None	4	Human	Functional	pIC50	=	6.2	6.2	-	1	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay	ChEMBL	309	3	0	3	3.4	CN1CCc2c(c3cc(F)ccc3n2CCc2cccnc2)C1	10.1016/j.bmcl.2009.04.128
	44126325	201570	None	4	Human	Functional	pIC50	=	7.2	7.2	10	2	Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge	ChEMBL	334	4	0	3	4.2	COc1ccc(CCn2c3c(c4cc(C)ccc42)CN(C)CC3)cc1	10.1016/j.bmcl.2009.11.037
	CHEMBL589147	201570	None	4	Human	Functional	pIC50	=	7.2	7.2	10	2	Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge	ChEMBL	334	4	0	3	4.2	COc1ccc(CCn2c3c(c4cc(C)ccc42)CN(C)CC3)cc1	10.1016/j.bmcl.2009.11.037
	44126272	201606	None	4	Human	Functional	pIC50	=	7.2	7.2	14	2	Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge	ChEMBL	358	3	0	2	4.9	CN1CCc2c(c3cc(C(F)(F)F)ccc3n2CCc2ccccc2)C1	10.1016/j.bmcl.2009.11.037
	CHEMBL589388	201606	None	4	Human	Functional	pIC50	=	7.2	7.2	14	2	Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge	ChEMBL	358	3	0	2	4.9	CN1CCc2c(c3cc(C(F)(F)F)ccc3n2CCc2ccccc2)C1	10.1016/j.bmcl.2009.11.037
	13623349	98636	None	0	Guinea pig	Functional	pIC50	=	7.2	7.2	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	304	5	0	5	2.9	CCCSCn1c(N2CCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	CHEMBL276774	98636	None	0	Guinea pig	Functional	pIC50	=	7.2	7.2	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	304	5	0	5	2.9	CCCSCn1c(N2CCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	16082828	80291	None	0	Human	Functional	pIC50	=	5.2	5.2	-398	3	Antagonist activity at human H1 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assayAntagonist activity at human H1 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assay	ChEMBL	275	6	2	2	3.3	Clc1ccc(CNCC[C@@H]2C[C@H]2c2c[nH]cn2)cc1	10.1021/jm0603318
	CHEMBL213886	80291	None	0	Human	Functional	pIC50	=	5.2	5.2	-398	3	Antagonist activity at human H1 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assayAntagonist activity at human H1 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assay	ChEMBL	275	6	2	2	3.3	Clc1ccc(CNCC[C@@H]2C[C@H]2c2c[nH]cn2)cc1	10.1021/jm0603318
	10917690	210064	None	1	Human	Functional	pIC50	=	8.1	8.1	-3	4	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	471	8	0	5	5.4	COc1ccc(CCN2CCC(C(=O)c3nc4ccccc4n3Cc3ccc(F)cc3)CC2)cc1	10.1016/S0960-894X(97)10098-1
	CHEMBL95051	210064	None	1	Human	Functional	pIC50	=	8.1	8.1	-3	4	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	471	8	0	5	5.4	COc1ccc(CCN2CCC(C(=O)c3nc4ccccc4n3Cc3ccc(F)cc3)CC2)cc1	10.1016/S0960-894X(97)10098-1
	44328187	210598	None	0	Human	Functional	pIC50	=	8.1	8.1	-1	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	456	7	0	5	5.6	COc1ccc(CCN2CCC(=Nc3nc4ccccc4n3Cc3ccc(F)cc3)CC2)cc1	10.1016/S0960-894X(97)10098-1
	CHEMBL98076	210598	None	0	Human	Functional	pIC50	=	8.1	8.1	-1	2	Antagonistic activity against histamine H1 receptorAntagonistic activity against histamine H1 receptor	ChEMBL	456	7	0	5	5.6	COc1ccc(CCN2CCC(=Nc3nc4ccccc4n3Cc3ccc(F)cc3)CC2)cc1	10.1016/S0960-894X(97)10098-1
	13623370	98444	None	0	Guinea pig	Functional	pIC50	=	8.1	8.1	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	358	9	0	5	3.8	CCCCCN1CCCN(c2nc3ccccc3n2CCOCC)CC1	10.1021/jm00157a010
	CHEMBL275383	98444	None	0	Guinea pig	Functional	pIC50	=	8.1	8.1	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	358	9	0	5	3.8	CCCCCN1CCCN(c2nc3ccccc3n2CCOCC)CC1	10.1021/jm00157a010
	46224879	204004	None	3	Human	Functional	pIC50	=	7.2	7.2	-1	2	Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge	ChEMBL	302	2	0	2	4.6	Cc1ccc2c(c1)c1c(n2/C=C\c2ccccc2)CCN(C)C1	10.1016/j.bmcl.2009.11.037
	CHEMBL605405	204004	None	3	Human	Functional	pIC50	=	7.2	7.2	-1	2	Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge	ChEMBL	302	2	0	2	4.6	Cc1ccc2c(c1)c1c(n2/C=C\c2ccccc2)CCN(C)C1	10.1016/j.bmcl.2009.11.037
	54581998	62755	None	2	Human	Functional	pIC50	=	5.1	5.1	5	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay	ChEMBL	368	4	0	4	4.3	CN1CCc2c(c3cc(-c4cccnc4)ccc3n2CCc2ccccn2)C1	10.1016/j.bmcl.2009.04.128
	CHEMBL1783972	62755	None	2	Human	Functional	pIC50	=	5.1	5.1	5	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay	ChEMBL	368	4	0	4	4.3	CN1CCc2c(c3cc(-c4cccnc4)ccc3n2CCc2ccccn2)C1	10.1016/j.bmcl.2009.04.128
	54585846	62747	None	4	Human	Functional	pIC50	=	6.1	6.1	38	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assay	ChEMBL	323	3	0	3	3.7	Cc1ccc(CCn2c3c(c4cc(F)ccc42)CN(C)CC3)cn1	10.1016/j.bmcl.2009.04.128
	CHEMBL1783963	62747	None	4	Human	Functional	pIC50	=	6.1	6.1	38	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assay	ChEMBL	323	3	0	3	3.7	Cc1ccc(CCn2c3c(c4cc(F)ccc42)CN(C)CC3)cn1	10.1016/j.bmcl.2009.04.128
	54583939	62757	None	4	Human	Functional	pIC50	=	5.1	5.1	-	1	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay	ChEMBL	388	4	0	4	4.0	Cc1ccc2c(c1)c1c(n2CCc2ccncc2)CCN(C2CCN(C)CC2)C1	10.1016/j.bmcl.2009.04.128
	CHEMBL1783975	62757	None	4	Human	Functional	pIC50	=	5.1	5.1	-	1	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay	ChEMBL	388	4	0	4	4.0	Cc1ccc2c(c1)c1c(n2CCc2ccncc2)CCN(C2CCN(C)CC2)C1	10.1016/j.bmcl.2009.04.128
	13623340	59058	None	0	Guinea pig	Functional	pIC50	=	6.1	6.1	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	292	2	0	4	2.8	CN1CCN(c2nc3ccccc3n2-c2ccccc2)CC1	10.1021/jm00157a010
	CHEMBL16938	59058	None	0	Guinea pig	Functional	pIC50	=	6.1	6.1	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	292	2	0	4	2.8	CN1CCN(c2nc3ccccc3n2-c2ccccc2)CC1	10.1021/jm00157a010
	54583938	62753	None	0	Human	Functional	pIC50	=	5.1	5.1	1	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assay	ChEMBL	306	3	0	4	3.0	Cc1ccc2c(c1)c1c(n2CCc2cnccn2)CCN(C)C1	10.1016/j.bmcl.2009.04.128
	CHEMBL1783970	62753	None	0	Human	Functional	pIC50	=	5.1	5.1	1	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assay	ChEMBL	306	3	0	4	3.0	Cc1ccc2c(c1)c1c(n2CCc2cnccn2)CCN(C)C1	10.1016/j.bmcl.2009.04.128
	13623369	62413	None	0	Guinea pig	Functional	pIC50	=	8.1	8.1	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	344	8	0	5	3.4	CCCCN1CCCN(c2nc3ccccc3n2CCOCC)CC1	10.1021/jm00157a010
	CHEMBL17795	62413	None	0	Guinea pig	Functional	pIC50	=	8.1	8.1	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	344	8	0	5	3.4	CCCCN1CCCN(c2nc3ccccc3n2CCOCC)CC1	10.1021/jm00157a010
	13623368	162340	None	0	Guinea pig	Functional	pIC50	=	8.1	8.1	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	330	7	0	5	3.0	CCCN1CCCN(c2nc3ccccc3n2CCOCC)CC1	10.1021/jm00157a010
	CHEMBL416357	162340	None	0	Guinea pig	Functional	pIC50	=	8.1	8.1	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	330	7	0	5	3.0	CCCN1CCCN(c2nc3ccccc3n2CCOCC)CC1	10.1021/jm00157a010
	13623362	98136	None	0	Guinea pig	Functional	pIC50	=	8.1	8.1	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	358	10	0	5	3.8	CCCCCCN1CCN(c2nc3ccccc3n2CCOCC)CC1	10.1021/jm00157a010
	CHEMBL273315	98136	None	0	Guinea pig	Functional	pIC50	=	8.1	8.1	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	358	10	0	5	3.8	CCCCCCN1CCN(c2nc3ccccc3n2CCOCC)CC1	10.1021/jm00157a010
	16082831	80377	None	0	Human	Functional	pIC50	=	5.1	5.1	-1000	3	Antagonist activity at human H1 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assayAntagonist activity at human H1 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assay	ChEMBL	275	6	2	2	3.3	Clc1ccc(CNCC[C@H]2C[C@@H]2c2c[nH]cn2)cc1	10.1021/jm0603318
	CHEMBL214311	80377	None	0	Human	Functional	pIC50	=	5.1	5.1	-1000	3	Antagonist activity at human H1 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assayAntagonist activity at human H1 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assay	ChEMBL	275	6	2	2	3.3	Clc1ccc(CNCC[C@H]2C[C@@H]2c2c[nH]cn2)cc1	10.1021/jm0603318
	13623353	60518	None	0	Guinea pig	Functional	pIC50	=	6.1	6.1	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	288	5	0	5	1.8	COCCCn1c(N2CCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	CHEMBL17556	60518	None	0	Guinea pig	Functional	pIC50	=	6.1	6.1	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	288	5	0	5	1.8	COCCCn1c(N2CCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	11976	920	None	44	Human	Functional	pIC50	=	6.1	6.1	-9	16	Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay	ChEMBL	315	3	0	2	5.2	CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl	10.1021/jm300671m
	667467	920	None	44	Human	Functional	pIC50	=	6.1	6.1	-9	16	Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay	ChEMBL	315	3	0	2	5.2	CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl	10.1021/jm300671m
	667467.0	920	None	44	Human	Functional	pIC50	=	6.1	6.1	-9	16	Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay	ChEMBL	315	3	0	2	5.2	CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl	10.1021/jm300671m
	CHEMBL908	920	None	44	Human	Functional	pIC50	=	6.1	6.1	-9	16	Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay	ChEMBL	315	3	0	2	5.2	CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl	10.1021/jm300671m
	DB01239	920	None	44	Human	Functional	pIC50	=	6.1	6.1	-9	16	Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay	ChEMBL	315	3	0	2	5.2	CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl	10.1021/jm300671m
	3071012	163385	None	0	Guinea pig	Functional	pIC50	=	8.0	8.0	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	350	5	0	5	3.3	CN1CCCN(c2nc3ccccc3n2CCOc2ccccc2)CC1	10.1021/jm00157a010
	CHEMBL418731	163385	None	0	Guinea pig	Functional	pIC50	=	8.0	8.0	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	350	5	0	5	3.3	CN1CCCN(c2nc3ccccc3n2CCOc2ccccc2)CC1	10.1021/jm00157a010
	3070998	99035	None	0	Guinea pig	Functional	pIC50	=	8	8.0	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	312	5	0	5	1.8	C#CCOCCn1c(N2CCCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	CHEMBL279875	99035	None	0	Guinea pig	Functional	pIC50	=	8	8.0	-	1	In vitro inhibition of histamine-induced contractions in guinea pig ileumIn vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	312	5	0	5	1.8	C#CCOCCn1c(N2CCCN(C)CC2)nc2ccccc21	10.1021/jm00157a010
	145963961	164498	None	0	Human	Functional	pIC50	=	6.0	6.0	-416	6	Antagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assay	ChEMBL	425	8	1	7	3.0	CNC(=O)c1cc(OCCCCN2CCN(c3nsc4ccccc34)CC2)ccn1	10.1016/j.bmcl.2018.01.038
	CHEMBL4213342	164498	None	0	Human	Functional	pIC50	=	6.0	6.0	-416	6	Antagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assay	ChEMBL	425	8	1	7	3.0	CNC(=O)c1cc(OCCCCN2CCN(c3nsc4ccccc34)CC2)ccn1	10.1016/j.bmcl.2018.01.038
	54586812	62737	None	4	Human	Functional	pIC50	=	6.0	6.0	12	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assay	ChEMBL	291	3	0	3	3.3	CN1CCc2c(c3ccccc3n2CCc2ccccn2)C1	10.1016/j.bmcl.2009.04.128
	CHEMBL1783953	62737	None	4	Human	Functional	pIC50	=	6.0	6.0	12	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assay	ChEMBL	291	3	0	3	3.3	CN1CCc2c(c3ccccc3n2CCc2ccccn2)C1	10.1016/j.bmcl.2009.04.128
	54586813	62745	None	4	Human	Functional	pIC50	=	6.0	6.0	-	1	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assay	ChEMBL	309	3	0	3	3.4	CN1CCc2c(c3cc(F)ccc3n2CCc2cccnc2)C1	10.1016/j.bmcl.2009.04.128
	CHEMBL1783961	62745	None	4	Human	Functional	pIC50	=	6.0	6.0	-	1	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium flow during phase-II compound dosed after histamine addition by Fura-2 based fluorometric assay	ChEMBL	309	3	0	3	3.4	CN1CCc2c(c3cc(F)ccc3n2CCc2cccnc2)C1	10.1016/j.bmcl.2009.04.128
	54579956	62740	None	4	Human	Functional	pIC50	=	6.0	6.0	3	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay	ChEMBL	309	3	0	3	3.4	CN1CCc2c(c3cc(F)ccc3n2CCc2ccccn2)C1	10.1016/j.bmcl.2009.04.128
	CHEMBL1783956	62740	None	4	Human	Functional	pIC50	=	6.0	6.0	3	2	Antagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assayAntagonist activity at human histamine H1 receptor in SK-N-SH cells assessed as inhibition of histamine-induced calcium level increase during phase-1 compound incubated before histamine addition by Fura-2 based fluorometric assay	ChEMBL	309	3	0	3	3.4	CN1CCc2c(c3cc(F)ccc3n2CCc2ccccn2)C1	10.1016/j.bmcl.2009.04.128
	10212645	13294	None	0	Human	Functional	pIC50	=	5.0	5.0	-346	2	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	774	16	1	10	7.0	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4CCCOc4ccccc4C(=O)O)CC3)(c3ccccc3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10097-X
	CHEMBL1191766	13294	None	0	Human	Functional	pIC50	=	5.0	5.0	-346	2	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	774	16	1	10	7.0	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4CCCOc4ccccc4C(=O)O)CC3)(c3ccccc3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10097-X
	CHEMBL542908	13294	None	0	Human	Functional	pIC50	=	5.0	5.0	-346	2	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	774	16	1	10	7.0	COc1cc(C(=O)N2CCC(CCN3CCC(C(=O)c4nc5ccccc5n4CCCOc4ccccc4C(=O)O)CC3)(c3ccccc3)C2)cc(OC)c1OC	10.1016/S0960-894X(97)10097-X
	4601	209205	None	27	Human	Functional	pIC50	=	4.0	4.0	-549	19	Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay	ChEMBL	269	6	0	2	3.7	Cc1ccccc1C(OCCN(C)C)c1ccccc1	10.1021/jm300671m
	4601.0	209205	None	27	Human	Functional	pIC50	=	4.0	4.0	-549	19	Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay	ChEMBL	269	6	0	2	3.7	Cc1ccccc1C(OCCN(C)C)c1ccccc1	10.1021/jm300671m
	CHEMBL1201023	209205	None	27	Human	Functional	pIC50	=	4.0	4.0	-549	19	Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay	ChEMBL	269	6	0	2	3.7	Cc1ccccc1C(OCCN(C)C)c1ccccc1	10.1021/jm300671m
	CHEMBL900	209205	None	27	Human	Functional	pIC50	=	4.0	4.0	-549	19	Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay	ChEMBL	269	6	0	2	3.7	Cc1ccccc1C(OCCN(C)C)c1ccccc1	10.1021/jm300671m
	DB01173	209205	None	27	Human	Functional	pIC50	=	4.0	4.0	-549	19	Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assayAntagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay	ChEMBL	269	6	0	2	3.7	Cc1ccccc1C(OCCN(C)C)c1ccccc1	10.1021/jm300671m
	44126327	204110	None	4	Human	Functional	pIC50	=	7.0	7.0	41	2	Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge	ChEMBL	372	3	0	2	5.2	Cc1ccc2c(c1)c1c(n2CCc2ccc(C(F)(F)F)cc2)CCN(C)C1	10.1016/j.bmcl.2009.11.037
	CHEMBL606036	204110	None	4	Human	Functional	pIC50	=	7.0	7.0	41	2	Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challengeAntagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge	ChEMBL	372	3	0	2	5.2	Cc1ccc2c(c1)c1c(n2CCc2ccc(C(F)(F)F)cc2)CCN(C)C1	10.1016/j.bmcl.2009.11.037
	10190842	107280	None	0	Human	Functional	pIC50	=	6	6.0	-63	2	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	788	16	0	11	7.1	COC(=O)c1ccccc1OCCCn1c(C(=O)C2CCN(CCC3(c4ccccc4)CCN(C(=O)c4cc(OC)c(OC)c(OC)c4)C3)CC2)nc2ccccc21	10.1016/S0960-894X(97)10097-X
	CHEMBL316705	107280	None	0	Human	Functional	pIC50	=	6	6.0	-63	2	Antagonism of the human histamine H1 receptorAntagonism of the human histamine H1 receptor	ChEMBL	788	16	0	11	7.1	COC(=O)c1ccccc1OCCCn1c(C(=O)C2CCN(CCC3(c4ccccc4)CCN(C(=O)c4cc(OC)c(OC)c(OC)c4)C3)CC2)nc2ccccc21	10.1016/S0960-894X(97)10097-X
	71461781	80500	None	0	Human	Functional	pKd	=	10.4	10.4	-	0	Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay	ChEMBL	409	7	0	4	4.9	CCCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O	10.1016/j.bmc.2012.08.032
	CHEMBL2146802	80500	None	0	Human	Functional	pKd	=	10.4	10.4	-	0	Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay	ChEMBL	409	7	0	4	4.9	CCCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O	10.1016/j.bmc.2012.08.032
	15254720	61321	None	0	Human	Functional	pKd	=	10	10.0	-	0	Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay	ChEMBL	367	4	0	4	3.7	CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O	10.1016/j.bmc.2012.08.032
	CHEMBL1767136	61321	None	0	Human	Functional	pKd	=	10	10.0	-	0	Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay	ChEMBL	367	4	0	4	3.7	CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O	10.1016/j.bmc.2012.08.032
	71461782	80504	None	0	Human	Functional	pKd	=	10	10.0	-	0	Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay	ChEMBL	410	7	0	5	4.3	CCCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cnccc2c1=O	10.1016/j.bmc.2012.08.032
	CHEMBL2146806	80504	None	0	Human	Functional	pKd	=	10	10.0	-	0	Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay	ChEMBL	410	7	0	5	4.3	CCCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cnccc2c1=O	10.1016/j.bmc.2012.08.032
	2267	559	None	45	Human	Functional	pKd	=	9.7	9.7	32	14	Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay	ChEMBL	381	3	0	4	4.3	CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2	10.1016/j.bmc.2012.08.032
	2267.0	559	None	45	Human	Functional	pKd	=	9.7	9.7	32	14	Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay	ChEMBL	381	3	0	4	4.3	CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2	10.1016/j.bmc.2012.08.032
	271	559	None	45	Human	Functional	pKd	=	9.7	9.7	32	14	Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay	ChEMBL	381	3	0	4	4.3	CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2	10.1016/j.bmc.2012.08.032
	7121	559	None	45	Human	Functional	pKd	=	9.7	9.7	32	14	Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay	ChEMBL	381	3	0	4	4.3	CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2	10.1016/j.bmc.2012.08.032
	CHEMBL639	559	None	45	Human	Functional	pKd	=	9.7	9.7	32	14	Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay	ChEMBL	381	3	0	4	4.3	CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2	10.1016/j.bmc.2012.08.032
	DB00972	559	None	45	Human	Functional	pKd	=	9.7	9.7	32	14	Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay	ChEMBL	381	3	0	4	4.3	CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2	10.1016/j.bmc.2012.08.032
	2267	559	None	45	Human	Functional	pKd	=	9.7	9.7	32	14	Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay	ChEMBL	381	3	0	4	4.3	CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2	10.1016/j.bmcl.2016.11.022
	2267.0	559	None	45	Human	Functional	pKd	=	9.7	9.7	32	14	Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay	ChEMBL	381	3	0	4	4.3	CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2	10.1016/j.bmcl.2016.11.022
	271	559	None	45	Human	Functional	pKd	=	9.7	9.7	32	14	Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay	ChEMBL	381	3	0	4	4.3	CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2	10.1016/j.bmcl.2016.11.022
	7121	559	None	45	Human	Functional	pKd	=	9.7	9.7	32	14	Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay	ChEMBL	381	3	0	4	4.3	CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2	10.1016/j.bmcl.2016.11.022
	CHEMBL639	559	None	45	Human	Functional	pKd	=	9.7	9.7	32	14	Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay	ChEMBL	381	3	0	4	4.3	CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2	10.1016/j.bmcl.2016.11.022
	DB00972	559	None	45	Human	Functional	pKd	=	9.7	9.7	32	14	Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay	ChEMBL	381	3	0	4	4.3	CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2	10.1016/j.bmcl.2016.11.022
	2267	559	None	45	Human	Functional	pKd	=	9.7	9.7	32	14	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	381	3	0	4	4.3	CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2	10.1016/j.bmcl.2017.09.020
	2267.0	559	None	45	Human	Functional	pKd	=	9.7	9.7	32	14	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	381	3	0	4	4.3	CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2	10.1016/j.bmcl.2017.09.020
	271	559	None	45	Human	Functional	pKd	=	9.7	9.7	32	14	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	381	3	0	4	4.3	CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2	10.1016/j.bmcl.2017.09.020
	7121	559	None	45	Human	Functional	pKd	=	9.7	9.7	32	14	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	381	3	0	4	4.3	CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2	10.1016/j.bmcl.2017.09.020
	CHEMBL639	559	None	45	Human	Functional	pKd	=	9.7	9.7	32	14	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	381	3	0	4	4.3	CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2	10.1016/j.bmcl.2017.09.020
	DB00972	559	None	45	Human	Functional	pKd	=	9.7	9.7	32	14	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	381	3	0	4	4.3	CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2	10.1016/j.bmcl.2017.09.020
	24824726	161203	None	1	Human	Functional	pKd	=	9.7	9.7	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	496	11	1	6	3.6	COCCCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O	10.1016/j.bmcl.2017.09.020
	CHEMBL4060529	161203	None	1	Human	Functional	pKd	=	9.7	9.7	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	496	11	1	6	3.6	COCCCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O	10.1016/j.bmcl.2017.09.020
	CHEMBL4117079	161203	None	1	Human	Functional	pKd	=	9.7	9.7	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	496	11	1	6	3.6	COCCCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O	10.1016/j.bmcl.2017.09.020
	CHEMBL5282336	161203	None	1	Human	Functional	pKd	=	9.7	9.7	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	496	11	1	6	3.6	COCCCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O	10.1016/j.bmcl.2017.09.020
	CHEMBL5286389	161203	None	1	Human	Functional	pKd	=	9.7	9.7	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	496	11	1	6	3.6	COCCCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O	10.1016/j.bmcl.2017.09.020
	25189511	161212	None	0	Human	Functional	pKd	=	9.7	9.7	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	461	13	1	5	4.5	CCCCc1cc(OC2CCN(CCCCNS(=O)(=O)CCC)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	CHEMBL4059750	161212	None	0	Human	Functional	pKd	=	9.7	9.7	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	461	13	1	5	4.5	CCCCc1cc(OC2CCN(CCCCNS(=O)(=O)CCC)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	CHEMBL4117137	161212	None	0	Human	Functional	pKd	=	9.7	9.7	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	461	13	1	5	4.5	CCCCc1cc(OC2CCN(CCCCNS(=O)(=O)CCC)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	2267	559	None	45	Human	Functional	pKd	=	9.7	9.7	32	14	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assay	ChEMBL	381	3	0	4	4.3	CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2	10.1021/jm1013874
	2267.0	559	None	45	Human	Functional	pKd	=	9.7	9.7	32	14	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assay	ChEMBL	381	3	0	4	4.3	CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2	10.1021/jm1013874
	271	559	None	45	Human	Functional	pKd	=	9.7	9.7	32	14	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assay	ChEMBL	381	3	0	4	4.3	CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2	10.1021/jm1013874
	7121	559	None	45	Human	Functional	pKd	=	9.7	9.7	32	14	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assay	ChEMBL	381	3	0	4	4.3	CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2	10.1021/jm1013874
	CHEMBL639	559	None	45	Human	Functional	pKd	=	9.7	9.7	32	14	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assay	ChEMBL	381	3	0	4	4.3	CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2	10.1021/jm1013874
	DB00972	559	None	45	Human	Functional	pKd	=	9.7	9.7	32	14	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assay	ChEMBL	381	3	0	4	4.3	CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2	10.1021/jm1013874
	71452871	80499	None	0	Human	Functional	pKd	=	9.6	9.6	-	0	Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay	ChEMBL	412	7	0	6	3.1	COCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cnccc2c1=O	10.1016/j.bmc.2012.08.032
	CHEMBL2146801	80499	None	0	Human	Functional	pKd	=	9.6	9.6	-	0	Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay	ChEMBL	412	7	0	6	3.1	COCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cnccc2c1=O	10.1016/j.bmc.2012.08.032
	25190195	158004	None	0	Human	Functional	pKd	=	9.6	9.6	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	446	9	0	5	5.0	CCCCc1cc(OC2CCN(CCCS(=O)(=O)C(C)(C)C)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	CHEMBL4084325	158004	None	0	Human	Functional	pKd	=	9.6	9.6	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	446	9	0	5	5.0	CCCCc1cc(OC2CCN(CCCS(=O)(=O)C(C)(C)C)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	71458203	80503	None	0	Human	Functional	pKd	=	9.5	9.5	-	0	Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay	ChEMBL	368	4	0	5	3.1	CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cnccc2c1=O	10.1016/j.bmc.2012.08.032
	CHEMBL2146805	80503	None	0	Human	Functional	pKd	=	9.5	9.5	-	0	Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay	ChEMBL	368	4	0	5	3.1	CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cnccc2c1=O	10.1016/j.bmc.2012.08.032
	71451044	80505	None	0	Human	Functional	pKd	=	9.5	9.5	-	0	Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay	ChEMBL	410	7	0	5	4.3	CCCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cccnc2c1=O	10.1016/j.bmc.2012.08.032
	CHEMBL2146807	80505	None	0	Human	Functional	pKd	=	9.5	9.5	-	0	Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay	ChEMBL	410	7	0	5	4.3	CCCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cccnc2c1=O	10.1016/j.bmc.2012.08.032
	71458204	80507	None	0	Human	Functional	pKd	=	9.5	9.5	-	0	Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay	ChEMBL	368	4	0	5	3.1	CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ncccc2c1=O	10.1016/j.bmc.2012.08.032
	CHEMBL2146809	80507	None	0	Human	Functional	pKd	=	9.5	9.5	-	0	Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay	ChEMBL	368	4	0	5	3.1	CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ncccc2c1=O	10.1016/j.bmc.2012.08.032
	1530	2182	None	36	Guinea pig	Functional	pKd	=	9.5	9.5	-	25	H1-antihistamine activity in guinea pig ileumH1-antihistamine activity in guinea pig ileum	ChEMBL	309	0	0	3	4.0	CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1	10.1021/jm00161a022
	3827	2182	None	36	Guinea pig	Functional	pKd	=	9.5	9.5	-	25	H1-antihistamine activity in guinea pig ileumH1-antihistamine activity in guinea pig ileum	ChEMBL	309	0	0	3	4.0	CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1	10.1021/jm00161a022
	3827.0	2182	None	36	Guinea pig	Functional	pKd	=	9.5	9.5	-	25	H1-antihistamine activity in guinea pig ileumH1-antihistamine activity in guinea pig ileum	ChEMBL	309	0	0	3	4.0	CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1	10.1021/jm00161a022
	7206	2182	None	36	Guinea pig	Functional	pKd	=	9.5	9.5	-	25	H1-antihistamine activity in guinea pig ileumH1-antihistamine activity in guinea pig ileum	ChEMBL	309	0	0	3	4.0	CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1	10.1021/jm00161a022
	CHEMBL534	2182	None	36	Guinea pig	Functional	pKd	=	9.5	9.5	-	25	H1-antihistamine activity in guinea pig ileumH1-antihistamine activity in guinea pig ileum	ChEMBL	309	0	0	3	4.0	CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1	10.1021/jm00161a022
	DB00920	2182	None	36	Guinea pig	Functional	pKd	=	9.5	9.5	-	25	H1-antihistamine activity in guinea pig ileumH1-antihistamine activity in guinea pig ileum	ChEMBL	309	0	0	3	4.0	CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1	10.1021/jm00161a022
	1530	2182	None	36	Guinea pig	Functional	pKd	=	9.5	9.5	-	25	H1-antihistamine activity on guinea pig ileumH1-antihistamine activity on guinea pig ileum	ChEMBL	309	0	0	3	4.0	CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1	10.1021/jm00377a013
	3827	2182	None	36	Guinea pig	Functional	pKd	=	9.5	9.5	-	25	H1-antihistamine activity on guinea pig ileumH1-antihistamine activity on guinea pig ileum	ChEMBL	309	0	0	3	4.0	CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1	10.1021/jm00377a013
	3827.0	2182	None	36	Guinea pig	Functional	pKd	=	9.5	9.5	-	25	H1-antihistamine activity on guinea pig ileumH1-antihistamine activity on guinea pig ileum	ChEMBL	309	0	0	3	4.0	CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1	10.1021/jm00377a013
	7206	2182	None	36	Guinea pig	Functional	pKd	=	9.5	9.5	-	25	H1-antihistamine activity on guinea pig ileumH1-antihistamine activity on guinea pig ileum	ChEMBL	309	0	0	3	4.0	CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1	10.1021/jm00377a013
	CHEMBL534	2182	None	36	Guinea pig	Functional	pKd	=	9.5	9.5	-	25	H1-antihistamine activity on guinea pig ileumH1-antihistamine activity on guinea pig ileum	ChEMBL	309	0	0	3	4.0	CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1	10.1021/jm00377a013
	DB00920	2182	None	36	Guinea pig	Functional	pKd	=	9.5	9.5	-	25	H1-antihistamine activity on guinea pig ileumH1-antihistamine activity on guinea pig ileum	ChEMBL	309	0	0	3	4.0	CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1	10.1021/jm00377a013
	25190192	161089	None	0	Human	Functional	pKd	=	9.5	9.5	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	418	10	0	5	4.2	CCCCc1cc(OC2CCN(CCCS(=O)(=O)CC)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	CHEMBL4098917	161089	None	0	Human	Functional	pKd	=	9.5	9.5	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	418	10	0	5	4.2	CCCCc1cc(OC2CCN(CCCS(=O)(=O)CC)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	CHEMBL4116155	161089	None	0	Human	Functional	pKd	=	9.5	9.5	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	418	10	0	5	4.2	CCCCc1cc(OC2CCN(CCCS(=O)(=O)CC)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	1227	2489	None	32	Guinea pig	Functional	pKd	=	9.4	9.4	-2	14	Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1016/s0960-894x(03)00113-6
	2331	2489	None	32	Guinea pig	Functional	pKd	=	9.4	9.4	-2	14	Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1016/s0960-894x(03)00113-6
	3957	2489	None	32	Guinea pig	Functional	pKd	=	9.4	9.4	-2	14	Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1016/s0960-894x(03)00113-6
	4992	2489	None	32	Guinea pig	Functional	pKd	=	9.4	9.4	-2	14	Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1016/s0960-894x(03)00113-6
	4992.0	2489	None	32	Guinea pig	Functional	pKd	=	9.4	9.4	-2	14	Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1016/s0960-894x(03)00113-6
	CHEMBL511	2489	None	32	Guinea pig	Functional	pKd	=	9.4	9.4	-2	14	Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1016/s0960-894x(03)00113-6
	DB06691	2489	None	32	Guinea pig	Functional	pKd	=	9.4	9.4	-2	14	Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1016/s0960-894x(03)00113-6
	25190372	161069	None	0	Human	Functional	pKd	=	9.4	9.4	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	433	11	1	5	3.8	CCCCc1cc(OC2CCN(CCCCNS(C)(=O)=O)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	CHEMBL4098192	161069	None	0	Human	Functional	pKd	=	9.4	9.4	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	433	11	1	5	3.8	CCCCc1cc(OC2CCN(CCCCNS(C)(=O)=O)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	CHEMBL4115992	161069	None	0	Human	Functional	pKd	=	9.4	9.4	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	433	11	1	5	3.8	CCCCc1cc(OC2CCN(CCCCNS(C)(=O)=O)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	25190194	161256	None	0	Human	Functional	pKd	=	9.4	9.4	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	432	10	0	5	4.6	CCCCc1cc(OC2CCN(CCCS(=O)(=O)C(C)C)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	CHEMBL4102287	161256	None	0	Human	Functional	pKd	=	9.4	9.4	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	432	10	0	5	4.6	CCCCc1cc(OC2CCN(CCCS(=O)(=O)C(C)C)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	CHEMBL4117432	161256	None	0	Human	Functional	pKd	=	9.4	9.4	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	432	10	0	5	4.6	CCCCc1cc(OC2CCN(CCCS(=O)(=O)C(C)C)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	71452872	80465	None	0	Human	Functional	pKd	=	9.3	9.3	-	0	Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay	ChEMBL	368	4	0	5	3.1	CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cccnc2c1=O	10.1016/j.bmc.2012.08.032
	CHEMBL2146484	80465	None	0	Human	Functional	pKd	=	9.3	9.3	-	0	Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay	ChEMBL	368	4	0	5	3.1	CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cccnc2c1=O	10.1016/j.bmc.2012.08.032
	25164129	161254	None	0	Human	Functional	pKd	=	9.3	9.3	-	1	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	447	12	1	5	4.1	CCCCc1cc(OC2CCN(CCCCNS(=O)(=O)CC)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	CHEMBL4088036	161254	None	0	Human	Functional	pKd	=	9.3	9.3	-	1	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	447	12	1	5	4.1	CCCCc1cc(OC2CCN(CCCCNS(=O)(=O)CC)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	CHEMBL4117406	161254	None	0	Human	Functional	pKd	=	9.3	9.3	-	1	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	447	12	1	5	4.1	CCCCc1cc(OC2CCN(CCCCNS(=O)(=O)CC)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	25189509	161166	None	0	Human	Functional	pKd	=	9.2	9.2	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	461	10	1	5	4.5	CCCCc1cc(OC2CCN(CCCS(=O)(=O)NC(C)(C)C)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	CHEMBL4069073	161166	None	0	Human	Functional	pKd	=	9.2	9.2	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	461	10	1	5	4.5	CCCCc1cc(OC2CCN(CCCS(=O)(=O)NC(C)(C)C)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	CHEMBL4116734	161166	None	0	Human	Functional	pKd	=	9.2	9.2	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	461	10	1	5	4.5	CCCCc1cc(OC2CCN(CCCS(=O)(=O)NC(C)(C)C)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	44320707	106086	None	0	Guinea pig	Functional	pKd	=	9.2	9.2	-	0	Contractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileumContractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileum	ChEMBL	293	4	1	2	2.9	CN(C)CCc1c[nH]c(-c2cccc(Br)c2)n1	10.1016/s0960-894x(98)00461-2
	CHEMBL313301	106086	None	0	Guinea pig	Functional	pKd	=	9.2	9.2	-	0	Contractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileumContractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileum	ChEMBL	293	4	1	2	2.9	CN(C)CCc1c[nH]c(-c2cccc(Br)c2)n1	10.1016/s0960-894x(98)00461-2
	10403687	2511	None	2	Guinea pig	Functional	pKd	=	9.1	9.1	1	2	Antagonism of guinea pig ileum contraction at 100 nM mepyramineAntagonism of guinea pig ileum contraction at 100 nM mepyramine	ChEMBL	319	8	2	2	3.9	CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm991056a
	1205	2511	None	2	Guinea pig	Functional	pKd	=	9.1	9.1	1	2	Antagonism of guinea pig ileum contraction at 100 nM mepyramineAntagonism of guinea pig ileum contraction at 100 nM mepyramine	ChEMBL	319	8	2	2	3.9	CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm991056a
	CHEMBL275035	2511	None	2	Guinea pig	Functional	pKd	=	9.1	9.1	1	2	Antagonism of guinea pig ileum contraction at 100 nM mepyramineAntagonism of guinea pig ileum contraction at 100 nM mepyramine	ChEMBL	319	8	2	2	3.9	CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm991056a
	25190193	161293	None	0	Human	Functional	pKd	=	9.1	9.1	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	432	11	0	5	4.6	CCCCc1cc(OC2CCN(CCCS(=O)(=O)CCC)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	CHEMBL4080880	161293	None	0	Human	Functional	pKd	=	9.1	9.1	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	432	11	0	5	4.6	CCCCc1cc(OC2CCN(CCCS(=O)(=O)CCC)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	CHEMBL4117740	161293	None	0	Human	Functional	pKd	=	9.1	9.1	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	432	11	0	5	4.6	CCCCc1cc(OC2CCN(CCCS(=O)(=O)CCC)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	1194	45	None	1	Guinea pig	Functional	pKd	=	9.1	9.1	-	2	Contractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileumContractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileum	ChEMBL	265	3	2	2	2.3	NCCc1cnc([nH]1)c1cccc(c1)Br	10.1016/s0960-894x(98)00461-2
	23786499	45	None	1	Guinea pig	Functional	pKd	=	9.1	9.1	-	2	Contractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileumContractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileum	ChEMBL	265	3	2	2	2.3	NCCc1cnc([nH]1)c1cccc(c1)Br	10.1016/s0960-894x(98)00461-2
	CHEMBL26116	45	None	1	Guinea pig	Functional	pKd	=	9.1	9.1	-	2	Contractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileumContractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileum	ChEMBL	265	3	2	2	2.3	NCCc1cnc([nH]1)c1cccc(c1)Br	10.1016/s0960-894x(98)00461-2
	44320708	208835	None	0	Guinea pig	Functional	pKd	=	9.1	9.1	-	0	Contractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileumContractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileum	ChEMBL	295	5	2	2	3.4	FC(F)(F)c1cccc(-c2nc(CCNC3CC3)c[nH]2)c1	10.1016/s0960-894x(98)00461-2
	CHEMBL87583	208835	None	0	Guinea pig	Functional	pKd	=	9.1	9.1	-	0	Contractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileumContractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileum	ChEMBL	295	5	2	2	3.4	FC(F)(F)c1cccc(-c2nc(CCNC3CC3)c[nH]2)c1	10.1016/s0960-894x(98)00461-2
	44320686	208911	None	0	Guinea pig	Functional	pKd	=	9.1	9.1	-	0	Contractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileumContractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileum	ChEMBL	279	4	2	2	2.6	CNCCc1c[nH]c(-c2cccc(Br)c2)n1	10.1016/s0960-894x(98)00461-2
	CHEMBL88075	208911	None	0	Guinea pig	Functional	pKd	=	9.1	9.1	-	0	Contractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileumContractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileum	ChEMBL	279	4	2	2	2.6	CNCCc1c[nH]c(-c2cccc(Br)c2)n1	10.1016/s0960-894x(98)00461-2
	10042467	1426	None	1	Guinea pig	Functional	pKd	=	9.1	9.1	-1	2	Antagonism of guinea pig ileum contraction at 100 nM mepyramineAntagonism of guinea pig ileum contraction at 100 nM mepyramine	ChEMBL	333	8	1	2	4.3	CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C	10.1021/jm991056a
	1203	1426	None	1	Guinea pig	Functional	pKd	=	9.1	9.1	-1	2	Antagonism of guinea pig ileum contraction at 100 nM mepyramineAntagonism of guinea pig ileum contraction at 100 nM mepyramine	ChEMBL	333	8	1	2	4.3	CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C	10.1021/jm991056a
	CHEMBL11553	1426	None	1	Guinea pig	Functional	pKd	=	9.1	9.1	-1	2	Antagonism of guinea pig ileum contraction at 100 nM mepyramineAntagonism of guinea pig ileum contraction at 100 nM mepyramine	ChEMBL	333	8	1	2	4.3	CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C	10.1021/jm991056a
	10447834	1933	None	1	Guinea pig	Functional	pKd	=	9.1	9.1	2	3	Antagonism of guinea pig ileum contraction at 100 nM mepyramineAntagonism of guinea pig ileum contraction at 100 nM mepyramine	ChEMBL	305	7	2	2	3.7	NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm991056a
	4026	1933	None	1	Guinea pig	Functional	pKd	=	9.1	9.1	2	3	Antagonism of guinea pig ileum contraction at 100 nM mepyramineAntagonism of guinea pig ileum contraction at 100 nM mepyramine	ChEMBL	305	7	2	2	3.7	NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm991056a
	CHEMBL275507	1933	None	1	Guinea pig	Functional	pKd	=	9.1	9.1	2	3	Antagonism of guinea pig ileum contraction at 100 nM mepyramineAntagonism of guinea pig ileum contraction at 100 nM mepyramine	ChEMBL	305	7	2	2	3.7	NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm991056a
	1204	1932	None	74	Guinea pig	Functional	pKd	=	9.1	9.1	-10	11	Compound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nM	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm991056a
	1247	1932	None	74	Guinea pig	Functional	pKd	=	9.1	9.1	-10	11	Compound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nM	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm991056a
	1375	1932	None	74	Guinea pig	Functional	pKd	=	9.1	9.1	-10	11	Compound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nM	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm991056a
	774	1932	None	74	Guinea pig	Functional	pKd	=	9.1	9.1	-10	11	Compound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nM	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm991056a
	774.0	1932	None	74	Guinea pig	Functional	pKd	=	9.1	9.1	-10	11	Compound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nM	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm991056a
	CHEMBL90	1932	None	74	Guinea pig	Functional	pKd	=	9.1	9.1	-10	11	Compound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nM	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm991056a
	DB05381	1932	None	74	Guinea pig	Functional	pKd	=	9.1	9.1	-10	11	Compound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nM	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm991056a
	1204	1932	None	74	Guinea pig	Functional	pKd	=	9.1	9.1	-10	11	Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/s0960-894x(98)00461-2
	1247	1932	None	74	Guinea pig	Functional	pKd	=	9.1	9.1	-10	11	Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/s0960-894x(98)00461-2
	1375	1932	None	74	Guinea pig	Functional	pKd	=	9.1	9.1	-10	11	Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/s0960-894x(98)00461-2
	774	1932	None	74	Guinea pig	Functional	pKd	=	9.1	9.1	-10	11	Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/s0960-894x(98)00461-2
	774.0	1932	None	74	Guinea pig	Functional	pKd	=	9.1	9.1	-10	11	Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/s0960-894x(98)00461-2
	CHEMBL90	1932	None	74	Guinea pig	Functional	pKd	=	9.1	9.1	-10	11	Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/s0960-894x(98)00461-2
	DB05381	1932	None	74	Guinea pig	Functional	pKd	=	9.1	9.1	-10	11	Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/s0960-894x(98)00461-2
	17747460	61349	None	13	Human	Functional	pKd	=	9.1	9.1	-	2	Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay	ChEMBL	640	14	0	6	7.8	O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1	10.1016/j.bmc.2012.08.032
	CHEMBL1767164	61349	None	13	Human	Functional	pKd	=	9.1	9.1	-	2	Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay	ChEMBL	640	14	0	6	7.8	O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1	10.1016/j.bmc.2012.08.032
	71456360	80506	None	0	Human	Functional	pKd	=	9.1	9.1	-	0	Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay	ChEMBL	412	7	0	6	3.1	COCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cccnc2c1=O	10.1016/j.bmc.2012.08.032
	CHEMBL2146808	80506	None	0	Human	Functional	pKd	=	9.1	9.1	-	0	Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay	ChEMBL	412	7	0	6	3.1	COCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cccnc2c1=O	10.1016/j.bmc.2012.08.032
	17747460	61349	None	13	Human	Functional	pKd	=	9.1	9.1	-	2	Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay	ChEMBL	640	14	0	6	7.8	O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1	10.1016/j.bmcl.2016.11.022
	CHEMBL1767164	61349	None	13	Human	Functional	pKd	=	9.1	9.1	-	2	Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay	ChEMBL	640	14	0	6	7.8	O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1	10.1016/j.bmcl.2016.11.022
	17747460	61349	None	13	Human	Functional	pKd	=	9.1	9.1	-	2	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assay	ChEMBL	640	14	0	6	7.8	O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1	10.1021/jm1013874
	CHEMBL1767164	61349	None	13	Human	Functional	pKd	=	9.1	9.1	-	2	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assay	ChEMBL	640	14	0	6	7.8	O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1	10.1021/jm1013874
	1227	2489	None	32	Guinea pig	Functional	pKd	=	9.1	9.1	-2	14	H1-antihistamine activity in guinea pig ileumH1-antihistamine activity in guinea pig ileum	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1021/jm00161a022
	2331	2489	None	32	Guinea pig	Functional	pKd	=	9.1	9.1	-2	14	H1-antihistamine activity in guinea pig ileumH1-antihistamine activity in guinea pig ileum	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1021/jm00161a022
	3957	2489	None	32	Guinea pig	Functional	pKd	=	9.1	9.1	-2	14	H1-antihistamine activity in guinea pig ileumH1-antihistamine activity in guinea pig ileum	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1021/jm00161a022
	4992	2489	None	32	Guinea pig	Functional	pKd	=	9.1	9.1	-2	14	H1-antihistamine activity in guinea pig ileumH1-antihistamine activity in guinea pig ileum	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1021/jm00161a022
	4992.0	2489	None	32	Guinea pig	Functional	pKd	=	9.1	9.1	-2	14	H1-antihistamine activity in guinea pig ileumH1-antihistamine activity in guinea pig ileum	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1021/jm00161a022
	CHEMBL511	2489	None	32	Guinea pig	Functional	pKd	=	9.1	9.1	-2	14	H1-antihistamine activity in guinea pig ileumH1-antihistamine activity in guinea pig ileum	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1021/jm00161a022
	DB06691	2489	None	32	Guinea pig	Functional	pKd	=	9.1	9.1	-2	14	H1-antihistamine activity in guinea pig ileumH1-antihistamine activity in guinea pig ileum	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1021/jm00161a022
	13676700	207242	None	0	Guinea pig	Functional	pKd	=	9.1	9.1	-	0	H1-antihistamine activity in guinea pig ileumH1-antihistamine activity in guinea pig ileum	ChEMBL	453	7	1	8	3.7	Oc1c2nnnc-2oc2cc(OCCCN3CCN(Cc4ccc(Cl)cc4)CC3)ccc12	10.1021/jm00161a022
	CHEMBL74870	207242	None	0	Guinea pig	Functional	pKd	=	9.1	9.1	-	0	H1-antihistamine activity in guinea pig ileumH1-antihistamine activity in guinea pig ileum	ChEMBL	453	7	1	8	3.7	Oc1c2nnnc-2oc2cc(OCCCN3CCN(Cc4ccc(Cl)cc4)CC3)ccc12	10.1021/jm00161a022
	1227	2489	None	32	Guinea pig	Functional	pKd	=	9.1	9.1	-2	14	H1-antihistamine activity on guinea pig ileumH1-antihistamine activity on guinea pig ileum	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1021/jm00377a013
	2331	2489	None	32	Guinea pig	Functional	pKd	=	9.1	9.1	-2	14	H1-antihistamine activity on guinea pig ileumH1-antihistamine activity on guinea pig ileum	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1021/jm00377a013
	3957	2489	None	32	Guinea pig	Functional	pKd	=	9.1	9.1	-2	14	H1-antihistamine activity on guinea pig ileumH1-antihistamine activity on guinea pig ileum	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1021/jm00377a013
	4992	2489	None	32	Guinea pig	Functional	pKd	=	9.1	9.1	-2	14	H1-antihistamine activity on guinea pig ileumH1-antihistamine activity on guinea pig ileum	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1021/jm00377a013
	4992.0	2489	None	32	Guinea pig	Functional	pKd	=	9.1	9.1	-2	14	H1-antihistamine activity on guinea pig ileumH1-antihistamine activity on guinea pig ileum	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1021/jm00377a013
	CHEMBL511	2489	None	32	Guinea pig	Functional	pKd	=	9.1	9.1	-2	14	H1-antihistamine activity on guinea pig ileumH1-antihistamine activity on guinea pig ileum	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1021/jm00377a013
	DB06691	2489	None	32	Guinea pig	Functional	pKd	=	9.1	9.1	-2	14	H1-antihistamine activity on guinea pig ileumH1-antihistamine activity on guinea pig ileum	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1021/jm00377a013
	25190374	161272	None	0	Human	Functional	pKd	=	9.1	9.1	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	475	13	1	5	4.8	CCCCc1cc(OC2CCN(CCCCNS(=O)(=O)CC(C)C)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	CHEMBL4082646	161272	None	0	Human	Functional	pKd	=	9.1	9.1	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	475	13	1	5	4.8	CCCCc1cc(OC2CCN(CCCCNS(=O)(=O)CC(C)C)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	CHEMBL4117608	161272	None	0	Human	Functional	pKd	=	9.1	9.1	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	475	13	1	5	4.8	CCCCc1cc(OC2CCN(CCCCNS(=O)(=O)CC(C)C)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	9993212	208665	None	0	Guinea pig	Functional	pKd	=	9.1	9.1	-	0	Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.	ChEMBL	269	4	2	2	2.9	CNCCc1c[nH]c(-c2cccc(C(F)(F)F)c2)n1	10.1016/s0960-894x(98)00461-2
	CHEMBL86522	208665	None	0	Guinea pig	Functional	pKd	=	9.1	9.1	-	0	Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.	ChEMBL	269	4	2	2	2.9	CNCCc1c[nH]c(-c2cccc(C(F)(F)F)c2)n1	10.1016/s0960-894x(98)00461-2
	1227	2489	None	32	Guinea pig	Functional	pKd	=	9.1	9.1	-2	14	Antagonism against H1 histamine receptor of guinea pig ileumAntagonism against H1 histamine receptor of guinea pig ileum	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1016/0960-894X(95)00092-8
	2331	2489	None	32	Guinea pig	Functional	pKd	=	9.1	9.1	-2	14	Antagonism against H1 histamine receptor of guinea pig ileumAntagonism against H1 histamine receptor of guinea pig ileum	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1016/0960-894X(95)00092-8
	3957	2489	None	32	Guinea pig	Functional	pKd	=	9.1	9.1	-2	14	Antagonism against H1 histamine receptor of guinea pig ileumAntagonism against H1 histamine receptor of guinea pig ileum	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1016/0960-894X(95)00092-8
	4992	2489	None	32	Guinea pig	Functional	pKd	=	9.1	9.1	-2	14	Antagonism against H1 histamine receptor of guinea pig ileumAntagonism against H1 histamine receptor of guinea pig ileum	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1016/0960-894X(95)00092-8
	4992.0	2489	None	32	Guinea pig	Functional	pKd	=	9.1	9.1	-2	14	Antagonism against H1 histamine receptor of guinea pig ileumAntagonism against H1 histamine receptor of guinea pig ileum	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1016/0960-894X(95)00092-8
	CHEMBL511	2489	None	32	Guinea pig	Functional	pKd	=	9.1	9.1	-2	14	Antagonism against H1 histamine receptor of guinea pig ileumAntagonism against H1 histamine receptor of guinea pig ileum	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1016/0960-894X(95)00092-8
	DB06691	2489	None	32	Guinea pig	Functional	pKd	=	9.1	9.1	-2	14	Antagonism against H1 histamine receptor of guinea pig ileumAntagonism against H1 histamine receptor of guinea pig ileum	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1016/0960-894X(95)00092-8
	1227	2489	None	32	Guinea pig	Functional	pKd	=	9.1	9.1	-2	14	Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1016/j.bmcl.2011.09.001
	2331	2489	None	32	Guinea pig	Functional	pKd	=	9.1	9.1	-2	14	Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1016/j.bmcl.2011.09.001
	3957	2489	None	32	Guinea pig	Functional	pKd	=	9.1	9.1	-2	14	Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1016/j.bmcl.2011.09.001
	4992	2489	None	32	Guinea pig	Functional	pKd	=	9.1	9.1	-2	14	Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1016/j.bmcl.2011.09.001
	4992.0	2489	None	32	Guinea pig	Functional	pKd	=	9.1	9.1	-2	14	Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1016/j.bmcl.2011.09.001
	CHEMBL511	2489	None	32	Guinea pig	Functional	pKd	=	9.1	9.1	-2	14	Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1016/j.bmcl.2011.09.001
	DB06691	2489	None	32	Guinea pig	Functional	pKd	=	9.1	9.1	-2	14	Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1016/j.bmcl.2011.09.001
	1204	1932	None	74	Guinea pig	Functional	pKd	=	9.1	9.1	-10	11	Compound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nM	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm991056a
	1247	1932	None	74	Guinea pig	Functional	pKd	=	9.1	9.1	-10	11	Compound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nM	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm991056a
	1375	1932	None	74	Guinea pig	Functional	pKd	=	9.1	9.1	-10	11	Compound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nM	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm991056a
	774	1932	None	74	Guinea pig	Functional	pKd	=	9.1	9.1	-10	11	Compound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nM	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm991056a
	774.0	1932	None	74	Guinea pig	Functional	pKd	=	9.1	9.1	-10	11	Compound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nM	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm991056a
	CHEMBL90	1932	None	74	Guinea pig	Functional	pKd	=	9.1	9.1	-10	11	Compound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nM	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm991056a
	DB05381	1932	None	74	Guinea pig	Functional	pKd	=	9.1	9.1	-10	11	Compound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nM	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm991056a
	1204	1932	None	74	Guinea pig	Functional	pKd	=	9.1	9.1	-10	11	Contractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileumContractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileum	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/s0960-894x(98)00461-2
	1247	1932	None	74	Guinea pig	Functional	pKd	=	9.1	9.1	-10	11	Contractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileumContractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileum	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/s0960-894x(98)00461-2
	1375	1932	None	74	Guinea pig	Functional	pKd	=	9.1	9.1	-10	11	Contractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileumContractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileum	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/s0960-894x(98)00461-2
	774	1932	None	74	Guinea pig	Functional	pKd	=	9.1	9.1	-10	11	Contractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileumContractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileum	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/s0960-894x(98)00461-2
	774.0	1932	None	74	Guinea pig	Functional	pKd	=	9.1	9.1	-10	11	Contractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileumContractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileum	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/s0960-894x(98)00461-2
	CHEMBL90	1932	None	74	Guinea pig	Functional	pKd	=	9.1	9.1	-10	11	Contractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileumContractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileum	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/s0960-894x(98)00461-2
	DB05381	1932	None	74	Guinea pig	Functional	pKd	=	9.1	9.1	-10	11	Contractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileumContractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileum	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/s0960-894x(98)00461-2
	5310982	93665	None	1	Guinea pig	Functional	pKd	=	9.1	9.1	-	2	Contractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileumContractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileum	ChEMBL	255	3	2	2	2.6	NCCc1c[nH]c(-c2cccc(C(F)(F)F)c2)n1	10.1016/s0960-894x(98)00461-2
	CHEMBL24665	93665	None	1	Guinea pig	Functional	pKd	=	9.1	9.1	-	2	Contractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileumContractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileum	ChEMBL	255	3	2	2	2.6	NCCc1c[nH]c(-c2cccc(C(F)(F)F)c2)n1	10.1016/s0960-894x(98)00461-2
	9993212	208665	None	0	Guinea pig	Functional	pKd	=	9.0	9.0	-	0	Contractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileumContractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileum	ChEMBL	269	4	2	2	2.9	CNCCc1c[nH]c(-c2cccc(C(F)(F)F)c2)n1	10.1016/s0960-894x(98)00461-2
	CHEMBL86522	208665	None	0	Guinea pig	Functional	pKd	=	9.0	9.0	-	0	Contractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileumContractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileum	ChEMBL	269	4	2	2	2.9	CNCCc1c[nH]c(-c2cccc(C(F)(F)F)c2)n1	10.1016/s0960-894x(98)00461-2
	10689833	12770	None	0	Guinea pig	Functional	pKd	=	9.0	9.0	4	2	Compound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nM; value ranges from 9.02 to 9.42Compound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nM; value ranges from 9.02 to 9.42	ChEMBL	359	8	1	2	4.8	c1ccc(C(CCc2nc(CCN3CCCC3)c[nH]2)c2ccccc2)cc1	10.1021/jm991056a
	CHEMBL11879	12770	None	0	Guinea pig	Functional	pKd	=	9.0	9.0	4	2	Compound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nM; value ranges from 9.02 to 9.42Compound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nM; value ranges from 9.02 to 9.42	ChEMBL	359	8	1	2	4.8	c1ccc(C(CCc2nc(CCN3CCCC3)c[nH]2)c2ccccc2)cc1	10.1021/jm991056a
	10447834	1933	None	1	Guinea pig	Functional	pKd	=	9.0	9.0	2	3	Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nM	ChEMBL	305	7	2	2	3.7	NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm991056a
	4026	1933	None	1	Guinea pig	Functional	pKd	=	9.0	9.0	2	3	Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nM	ChEMBL	305	7	2	2	3.7	NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm991056a
	CHEMBL275507	1933	None	1	Guinea pig	Functional	pKd	=	9.0	9.0	2	3	Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nM	ChEMBL	305	7	2	2	3.7	NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm991056a
	5310982	93665	None	1	Guinea pig	Functional	pKd	=	9.0	9.0	-	2	Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.	ChEMBL	255	3	2	2	2.6	NCCc1c[nH]c(-c2cccc(C(F)(F)F)c2)n1	10.1016/s0960-894x(98)00461-2
	CHEMBL24665	93665	None	1	Guinea pig	Functional	pKd	=	9.0	9.0	-	2	Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.	ChEMBL	255	3	2	2	2.6	NCCc1c[nH]c(-c2cccc(C(F)(F)F)c2)n1	10.1016/s0960-894x(98)00461-2
	44320686	208911	None	0	Guinea pig	Functional	pKd	=	9.0	9.0	-	0	Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.	ChEMBL	279	4	2	2	2.6	CNCCc1c[nH]c(-c2cccc(Br)c2)n1	10.1016/s0960-894x(98)00461-2
	CHEMBL88075	208911	None	0	Guinea pig	Functional	pKd	=	9.0	9.0	-	0	Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.	ChEMBL	279	4	2	2	2.6	CNCCc1c[nH]c(-c2cccc(Br)c2)n1	10.1016/s0960-894x(98)00461-2
	24804150	80511	None	0	Human	Functional	pKd	=	9	9.0	-	0	Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay	ChEMBL	641	14	0	7	7.2	O=c1c2ccncc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1	10.1016/j.bmc.2012.08.032
	CHEMBL2146813	80511	None	0	Human	Functional	pKd	=	9	9.0	-	0	Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay	ChEMBL	641	14	0	7	7.2	O=c1c2ccncc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1	10.1016/j.bmc.2012.08.032
	25189510	156200	None	0	Human	Functional	pKd	=	9	9.0	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	461	13	1	5	4.5	CCCCc1cc(OC2CCN(CCCCS(=O)(=O)NCCC)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	CHEMBL4063163	156200	None	0	Human	Functional	pKd	=	9	9.0	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	461	13	1	5	4.5	CCCCc1cc(OC2CCN(CCCCS(=O)(=O)NCCC)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	25190375	161178	None	0	Human	Functional	pKd	=	9	9.0	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	501	12	1	5	5.5	CCCCc1cc(OC2CCN(CCCCNS(=O)(=O)C3CCCCC3)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	CHEMBL4088039	161178	None	0	Human	Functional	pKd	=	9	9.0	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	501	12	1	5	5.5	CCCCc1cc(OC2CCN(CCCCNS(=O)(=O)C3CCCCC3)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	CHEMBL4116791	161178	None	0	Human	Functional	pKd	=	9	9.0	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	501	12	1	5	5.5	CCCCc1cc(OC2CCN(CCCCNS(=O)(=O)C3CCCCC3)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	25190431	161307	None	0	Human	Functional	pKd	=	9	9.0	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	461	12	0	5	4.5	CCCCc1cc(OC2CCN(CCCCN(C)S(=O)(=O)CC)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	CHEMBL4065123	161307	None	0	Human	Functional	pKd	=	9	9.0	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	461	12	0	5	4.5	CCCCc1cc(OC2CCN(CCCCN(C)S(=O)(=O)CC)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	CHEMBL4117871	161307	None	0	Human	Functional	pKd	=	9	9.0	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	461	12	0	5	4.5	CCCCc1cc(OC2CCN(CCCCN(C)S(=O)(=O)CC)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	1204	1932	None	74	Guinea pig	Functional	pKd	=	9	9.0	-10	11	Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nM	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm991056a
	1247	1932	None	74	Guinea pig	Functional	pKd	=	9	9.0	-10	11	Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nM	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm991056a
	1375	1932	None	74	Guinea pig	Functional	pKd	=	9	9.0	-10	11	Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nM	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm991056a
	774	1932	None	74	Guinea pig	Functional	pKd	=	9	9.0	-10	11	Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nM	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm991056a
	774.0	1932	None	74	Guinea pig	Functional	pKd	=	9	9.0	-10	11	Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nM	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm991056a
	CHEMBL90	1932	None	74	Guinea pig	Functional	pKd	=	9	9.0	-10	11	Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nM	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm991056a
	DB05381	1932	None	74	Guinea pig	Functional	pKd	=	9	9.0	-10	11	Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nM	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm991056a
	54710796	120487	None	0	Guinea pig	Functional	pKd	=	9	9.0	-	0	H1-antihistamine activity on guinea pig ileumH1-antihistamine activity on guinea pig ileum	ChEMBL	473	8	1	8	3.6	O=c1oc2cc(OCCCN3CCN(Cc4ccc(Cl)cc4)CC3)ccc2c(O)c1[N+](=O)[O-]	10.1021/jm00377a013
	CHEMBL35376	120487	None	0	Guinea pig	Functional	pKd	=	9	9.0	-	0	H1-antihistamine activity on guinea pig ileumH1-antihistamine activity on guinea pig ileum	ChEMBL	473	8	1	8	3.6	O=c1oc2cc(OCCCN3CCN(Cc4ccc(Cl)cc4)CC3)ccc2c(O)c1[N+](=O)[O-]	10.1021/jm00377a013
	1227	2489	None	32	Guinea pig	Functional	pKd	=	9	9.0	-2	14	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1021/jm00093a025
	2331	2489	None	32	Guinea pig	Functional	pKd	=	9	9.0	-2	14	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1021/jm00093a025
	3957	2489	None	32	Guinea pig	Functional	pKd	=	9	9.0	-2	14	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1021/jm00093a025
	4992	2489	None	32	Guinea pig	Functional	pKd	=	9	9.0	-2	14	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1021/jm00093a025
	4992.0	2489	None	32	Guinea pig	Functional	pKd	=	9	9.0	-2	14	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1021/jm00093a025
	CHEMBL511	2489	None	32	Guinea pig	Functional	pKd	=	9	9.0	-2	14	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1021/jm00093a025
	DB06691	2489	None	32	Guinea pig	Functional	pKd	=	9	9.0	-2	14	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1021/jm00093a025
	1204	1932	None	74	Guinea pig	Functional	pKd	=	9	9.0	-10	11	Relative potency against Histamine H1 receptor in endothelium-Denuded rings of guinea pig AortaRelative potency against Histamine H1 receptor in endothelium-Denuded rings of guinea pig Aorta	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm0309147
	1247	1932	None	74	Guinea pig	Functional	pKd	=	9	9.0	-10	11	Relative potency against Histamine H1 receptor in endothelium-Denuded rings of guinea pig AortaRelative potency against Histamine H1 receptor in endothelium-Denuded rings of guinea pig Aorta	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm0309147
	1375	1932	None	74	Guinea pig	Functional	pKd	=	9	9.0	-10	11	Relative potency against Histamine H1 receptor in endothelium-Denuded rings of guinea pig AortaRelative potency against Histamine H1 receptor in endothelium-Denuded rings of guinea pig Aorta	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm0309147
	774	1932	None	74	Guinea pig	Functional	pKd	=	9	9.0	-10	11	Relative potency against Histamine H1 receptor in endothelium-Denuded rings of guinea pig AortaRelative potency against Histamine H1 receptor in endothelium-Denuded rings of guinea pig Aorta	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm0309147
	774.0	1932	None	74	Guinea pig	Functional	pKd	=	9	9.0	-10	11	Relative potency against Histamine H1 receptor in endothelium-Denuded rings of guinea pig AortaRelative potency against Histamine H1 receptor in endothelium-Denuded rings of guinea pig Aorta	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm0309147
	CHEMBL90	1932	None	74	Guinea pig	Functional	pKd	=	9	9.0	-10	11	Relative potency against Histamine H1 receptor in endothelium-Denuded rings of guinea pig AortaRelative potency against Histamine H1 receptor in endothelium-Denuded rings of guinea pig Aorta	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm0309147
	DB05381	1932	None	74	Guinea pig	Functional	pKd	=	9	9.0	-10	11	Relative potency against Histamine H1 receptor in endothelium-Denuded rings of guinea pig AortaRelative potency against Histamine H1 receptor in endothelium-Denuded rings of guinea pig Aorta	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm0309147
	44320685	208910	None	0	Guinea pig	Functional	pKd	=	9.0	9.0	-	0	Contractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileumContractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileum	ChEMBL	283	5	2	2	3.2	CCNCCc1c[nH]c(-c2cccc(C(F)(F)F)c2)n1	10.1016/s0960-894x(98)00461-2
	CHEMBL88074	208910	None	0	Guinea pig	Functional	pKd	=	9.0	9.0	-	0	Contractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileumContractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileum	ChEMBL	283	5	2	2	3.2	CCNCCc1c[nH]c(-c2cccc(C(F)(F)F)c2)n1	10.1016/s0960-894x(98)00461-2
	1227	2489	None	32	Guinea pig	Functional	pKd	=	9.0	9.0	-2	14	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as histamine-induced contractions	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1016/j.ejmech.2008.09.019
	2331	2489	None	32	Guinea pig	Functional	pKd	=	9.0	9.0	-2	14	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as histamine-induced contractions	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1016/j.ejmech.2008.09.019
	3957	2489	None	32	Guinea pig	Functional	pKd	=	9.0	9.0	-2	14	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as histamine-induced contractions	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1016/j.ejmech.2008.09.019
	4992	2489	None	32	Guinea pig	Functional	pKd	=	9.0	9.0	-2	14	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as histamine-induced contractions	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1016/j.ejmech.2008.09.019
	4992.0	2489	None	32	Guinea pig	Functional	pKd	=	9.0	9.0	-2	14	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as histamine-induced contractions	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1016/j.ejmech.2008.09.019
	CHEMBL511	2489	None	32	Guinea pig	Functional	pKd	=	9.0	9.0	-2	14	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as histamine-induced contractions	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1016/j.ejmech.2008.09.019
	DB06691	2489	None	32	Guinea pig	Functional	pKd	=	9.0	9.0	-2	14	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as histamine-induced contractions	ChEMBL	285	7	0	4	2.7	COc1ccc(cc1)CN(c1ccccn1)CCN(C)C	10.1016/j.ejmech.2008.09.019
	44320707	106086	None	0	Guinea pig	Functional	pKd	=	8.9	8.9	-	0	Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.	ChEMBL	293	4	1	2	2.9	CN(C)CCc1c[nH]c(-c2cccc(Br)c2)n1	10.1016/s0960-894x(98)00461-2
	CHEMBL313301	106086	None	0	Guinea pig	Functional	pKd	=	8.9	8.9	-	0	Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.	ChEMBL	293	4	1	2	2.9	CN(C)CCc1c[nH]c(-c2cccc(Br)c2)n1	10.1016/s0960-894x(98)00461-2
	10407870	106817	None	0	Guinea pig	Functional	pKd	=	8.9	8.9	-	0	Contractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileumContractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileum	ChEMBL	283	4	1	2	3.2	CN(C)CCc1c[nH]c(-c2cccc(C(F)(F)F)c2)n1	10.1016/s0960-894x(98)00461-2
	CHEMBL314438	106817	None	0	Guinea pig	Functional	pKd	=	8.9	8.9	-	0	Contractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileumContractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileum	ChEMBL	283	4	1	2	3.2	CN(C)CCc1c[nH]c(-c2cccc(C(F)(F)F)c2)n1	10.1016/s0960-894x(98)00461-2
	25190317	161152	None	0	Human	Functional	pKd	=	8.9	8.9	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	433	11	1	5	3.8	CCCCc1cc(OC2CCN(CCCNS(=O)(=O)CC)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	CHEMBL4080166	161152	None	0	Human	Functional	pKd	=	8.9	8.9	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	433	11	1	5	3.8	CCCCc1cc(OC2CCN(CCCNS(=O)(=O)CC)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	CHEMBL4116610	161152	None	0	Human	Functional	pKd	=	8.9	8.9	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	433	11	1	5	3.8	CCCCc1cc(OC2CCN(CCCNS(=O)(=O)CC)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	24803638	61350	None	0	Human	Functional	pKd	=	8.9	8.9	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assay	ChEMBL	636	15	0	7	7.1	COc1ccc(Cc2nn(C[C@H]3CCCN3CCCCc3ccc(OCCCN4CCCCCC4)cc3)c(=O)c3ccccc23)cc1	10.1021/jm1013874
	CHEMBL1767165	61350	None	0	Human	Functional	pKd	=	8.9	8.9	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assay	ChEMBL	636	15	0	7	7.1	COc1ccc(Cc2nn(C[C@H]3CCCN3CCCCc3ccc(OCCCN4CCCCCC4)cc3)c(=O)c3ccccc23)cc1	10.1021/jm1013874
	24803483	61352	None	0	Human	Functional	pKd	=	8.9	8.9	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assay	ChEMBL	654	15	0	6	8.2	O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCCc1ccc(OCCCN2CCCCCC2)cc1	10.1021/jm1013874
	CHEMBL1767167	61352	None	0	Human	Functional	pKd	=	8.9	8.9	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assay	ChEMBL	654	15	0	6	8.2	O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCCc1ccc(OCCCN2CCCCCC2)cc1	10.1021/jm1013874
	1194	45	None	1	Guinea pig	Functional	pKd	=	8.9	8.9	-	2	Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.	ChEMBL	265	3	2	2	2.3	NCCc1cnc([nH]1)c1cccc(c1)Br	10.1016/s0960-894x(98)00461-2
	23786499	45	None	1	Guinea pig	Functional	pKd	=	8.9	8.9	-	2	Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.	ChEMBL	265	3	2	2	2.3	NCCc1cnc([nH]1)c1cccc(c1)Br	10.1016/s0960-894x(98)00461-2
	CHEMBL26116	45	None	1	Guinea pig	Functional	pKd	=	8.9	8.9	-	2	Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.	ChEMBL	265	3	2	2	2.3	NCCc1cnc([nH]1)c1cccc(c1)Br	10.1016/s0960-894x(98)00461-2
	10403687	2511	None	2	Guinea pig	Functional	pKd	=	8.9	8.9	1	2	Antagonism of guinea pig ileum contraction at 100 nM mepyramineAntagonism of guinea pig ileum contraction at 100 nM mepyramine	ChEMBL	319	8	2	2	3.9	CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm991056a
	1205	2511	None	2	Guinea pig	Functional	pKd	=	8.9	8.9	1	2	Antagonism of guinea pig ileum contraction at 100 nM mepyramineAntagonism of guinea pig ileum contraction at 100 nM mepyramine	ChEMBL	319	8	2	2	3.9	CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm991056a
	CHEMBL275035	2511	None	2	Guinea pig	Functional	pKd	=	8.9	8.9	1	2	Antagonism of guinea pig ileum contraction at 100 nM mepyramineAntagonism of guinea pig ileum contraction at 100 nM mepyramine	ChEMBL	319	8	2	2	3.9	CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm991056a
	10042467	1426	None	1	Guinea pig	Functional	pKd	=	8.9	8.9	-1	2	Antagonism of guinea pig ileum contraction at 100 nM mepyramineAntagonism of guinea pig ileum contraction at 100 nM mepyramine	ChEMBL	333	8	1	2	4.3	CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C	10.1021/jm991056a
	1203	1426	None	1	Guinea pig	Functional	pKd	=	8.9	8.9	-1	2	Antagonism of guinea pig ileum contraction at 100 nM mepyramineAntagonism of guinea pig ileum contraction at 100 nM mepyramine	ChEMBL	333	8	1	2	4.3	CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C	10.1021/jm991056a
	CHEMBL11553	1426	None	1	Guinea pig	Functional	pKd	=	8.9	8.9	-1	2	Antagonism of guinea pig ileum contraction at 100 nM mepyramineAntagonism of guinea pig ileum contraction at 100 nM mepyramine	ChEMBL	333	8	1	2	4.3	CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C	10.1021/jm991056a
	1524	2181	None	61	Guinea pig	Functional	pKd	=	8.9	8.9	-	18	Antagonism against H1 histamine receptor of guinea pig ileumAntagonism against H1 histamine receptor of guinea pig ileum	ChEMBL	395	5	1	5	2.4	Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2	10.1016/0960-894X(95)00092-8
	197	2181	None	61	Guinea pig	Functional	pKd	=	8.9	8.9	-	18	Antagonism against H1 histamine receptor of guinea pig ileumAntagonism against H1 histamine receptor of guinea pig ileum	ChEMBL	395	5	1	5	2.4	Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2	10.1016/0960-894X(95)00092-8
	3822	2181	None	61	Guinea pig	Functional	pKd	=	8.9	8.9	-	18	Antagonism against H1 histamine receptor of guinea pig ileumAntagonism against H1 histamine receptor of guinea pig ileum	ChEMBL	395	5	1	5	2.4	Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2	10.1016/0960-894X(95)00092-8
	3822.0	2181	None	61	Guinea pig	Functional	pKd	=	8.9	8.9	-	18	Antagonism against H1 histamine receptor of guinea pig ileumAntagonism against H1 histamine receptor of guinea pig ileum	ChEMBL	395	5	1	5	2.4	Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2	10.1016/0960-894X(95)00092-8
	88	2181	None	61	Guinea pig	Functional	pKd	=	8.9	8.9	-	18	Antagonism against H1 histamine receptor of guinea pig ileumAntagonism against H1 histamine receptor of guinea pig ileum	ChEMBL	395	5	1	5	2.4	Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2	10.1016/0960-894X(95)00092-8
	CHEMBL51	2181	None	61	Guinea pig	Functional	pKd	=	8.9	8.9	-	18	Antagonism against H1 histamine receptor of guinea pig ileumAntagonism against H1 histamine receptor of guinea pig ileum	ChEMBL	395	5	1	5	2.4	Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2	10.1016/0960-894X(95)00092-8
	DB12465	2181	None	61	Guinea pig	Functional	pKd	=	8.9	8.9	-	18	Antagonism against H1 histamine receptor of guinea pig ileumAntagonism against H1 histamine receptor of guinea pig ileum	ChEMBL	395	5	1	5	2.4	Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2	10.1016/0960-894X(95)00092-8
	11791817	98356	None	0	Guinea pig	Functional	pKd	=	8.9	8.9	-1	2	Antagonism of guinea pig ileum contraction at 100 nM mepyramineAntagonism of guinea pig ileum contraction at 100 nM mepyramine	ChEMBL	345	9	2	2	4.5	c1ccc(C(CCc2nc(CCNC3CC3)c[nH]2)c2ccccc2)cc1	10.1021/jm991056a
	CHEMBL274831	98356	None	0	Guinea pig	Functional	pKd	=	8.9	8.9	-1	2	Antagonism of guinea pig ileum contraction at 100 nM mepyramineAntagonism of guinea pig ileum contraction at 100 nM mepyramine	ChEMBL	345	9	2	2	4.5	c1ccc(C(CCc2nc(CCNC3CC3)c[nH]2)c2ccccc2)cc1	10.1021/jm991056a
	25190253	161211	None	0	Human	Functional	pKd	=	8.9	8.9	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	460	10	0	5	5.4	CCCCc1cc(OC2CCN(CCCCS(=O)(=O)C(C)(C)C)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	CHEMBL4095759	161211	None	0	Human	Functional	pKd	=	8.9	8.9	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	460	10	0	5	5.4	CCCCc1cc(OC2CCN(CCCCS(=O)(=O)C(C)(C)C)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	CHEMBL4117136	161211	None	0	Human	Functional	pKd	=	8.9	8.9	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	460	10	0	5	5.4	CCCCc1cc(OC2CCN(CCCCS(=O)(=O)C(C)(C)C)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	10407870	106817	None	0	Guinea pig	Functional	pKd	=	8.9	8.9	-	0	Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.	ChEMBL	283	4	1	2	3.2	CN(C)CCc1c[nH]c(-c2cccc(C(F)(F)F)c2)n1	10.1016/s0960-894x(98)00461-2
	CHEMBL314438	106817	None	0	Guinea pig	Functional	pKd	=	8.9	8.9	-	0	Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.	ChEMBL	283	4	1	2	3.2	CN(C)CCc1c[nH]c(-c2cccc(C(F)(F)F)c2)n1	10.1016/s0960-894x(98)00461-2
	10688111	10042	None	1	Guinea pig	Functional	pKd	=	8.8	8.8	2	2	Antagonism of guinea pig ileum contraction at 100 nM mepyramineAntagonism of guinea pig ileum contraction at 100 nM mepyramine	ChEMBL	333	9	2	2	4.3	CCNCCc1c[nH]c(CCC(c2ccccc2)c2ccccc2)n1	10.1021/jm991056a
	CHEMBL11515	10042	None	1	Guinea pig	Functional	pKd	=	8.8	8.8	2	2	Antagonism of guinea pig ileum contraction at 100 nM mepyramineAntagonism of guinea pig ileum contraction at 100 nM mepyramine	ChEMBL	333	9	2	2	4.3	CCNCCc1c[nH]c(CCC(c2ccccc2)c2ccccc2)n1	10.1021/jm991056a
	57780020	143537	None	0	Human	Functional	pKd	=	8.8	8.8	-	0	Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay	ChEMBL	600	15	1	6	6.6	CCCCc1cc(N2CCN(CCc3ccc(OCCCN4CCCCCC4)cc3)CC2)c2nc(CCC(=O)O)ccc2c1	10.1016/j.bmcl.2016.11.022
	CHEMBL3898341	143537	None	0	Human	Functional	pKd	=	8.8	8.8	-	0	Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay	ChEMBL	600	15	1	6	6.6	CCCCc1cc(N2CCN(CCc3ccc(OCCCN4CCCCCC4)cc3)CC2)c2nc(CCC(=O)O)ccc2c1	10.1016/j.bmcl.2016.11.022
	10447834	1933	None	1	Guinea pig	Functional	pKd	=	8.8	8.8	2	3	Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nM	ChEMBL	305	7	2	2	3.7	NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm991056a
	4026	1933	None	1	Guinea pig	Functional	pKd	=	8.8	8.8	2	3	Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nM	ChEMBL	305	7	2	2	3.7	NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm991056a
	CHEMBL275507	1933	None	1	Guinea pig	Functional	pKd	=	8.8	8.8	2	3	Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nM	ChEMBL	305	7	2	2	3.7	NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm991056a
	13676694	103767	None	0	Guinea pig	Functional	pKd	=	8.8	8.8	-	0	H1-antihistamine activity in guinea pig ileumH1-antihistamine activity in guinea pig ileum	ChEMBL	467	7	1	8	4.0	Cc1c(OCCCN2CCN(Cc3ccc(Cl)cc3)CC2)ccc2c(O)c3nnnc-3oc12	10.1021/jm00161a022
	CHEMBL308791	103767	None	0	Guinea pig	Functional	pKd	=	8.8	8.8	-	0	H1-antihistamine activity in guinea pig ileumH1-antihistamine activity in guinea pig ileum	ChEMBL	467	7	1	8	4.0	Cc1c(OCCCN2CCN(Cc3ccc(Cl)cc3)CC2)ccc2c(O)c3nnnc-3oc12	10.1021/jm00161a022
	10410901	119811	None	0	Guinea pig	Functional	pKd	=	8.8	8.8	23	2	Apparent pA2 value of compound at 10 nM concentration of mepyramine in guinea pig ileumApparent pA2 value of compound at 10 nM concentration of mepyramine in guinea pig ileum	ChEMBL	438	13	2	3	5.7	c1ccc(C(CCc2nc(CCNCCCCc3ccccn3)c[nH]2)c2ccccc2)cc1	10.1021/jm0309147
	CHEMBL347796	119811	None	0	Guinea pig	Functional	pKd	=	8.8	8.8	23	2	Apparent pA2 value of compound at 10 nM concentration of mepyramine in guinea pig ileumApparent pA2 value of compound at 10 nM concentration of mepyramine in guinea pig ileum	ChEMBL	438	13	2	3	5.7	c1ccc(C(CCc2nc(CCNCCCCc3ccccn3)c[nH]2)c2ccccc2)cc1	10.1021/jm0309147
	10403687	2511	None	2	Guinea pig	Functional	pKd	=	8.8	8.8	1	2	Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nM	ChEMBL	319	8	2	2	3.9	CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm991056a
	1205	2511	None	2	Guinea pig	Functional	pKd	=	8.8	8.8	1	2	Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nM	ChEMBL	319	8	2	2	3.9	CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm991056a
	CHEMBL275035	2511	None	2	Guinea pig	Functional	pKd	=	8.8	8.8	1	2	Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nM	ChEMBL	319	8	2	2	3.9	CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm991056a
	10484346	98780	None	0	Guinea pig	Functional	pKd	=	8.7	8.7	-	0	Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand	ChEMBL	646	22	2	11	5.8	COc1ccc(CN(CCN(C)CCCCCCNC(=O)CCCCCNc2ccc([N+](=O)[O-])c3nonc23)c2ccccn2)cc1	10.1016/s0960-894x(03)00113-6
	CHEMBL277848	98780	None	0	Guinea pig	Functional	pKd	=	8.7	8.7	-	0	Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand	ChEMBL	646	22	2	11	5.8	COc1ccc(CN(CCN(C)CCCCCCNC(=O)CCCCCNc2ccc([N+](=O)[O-])c3nonc23)c2ccccn2)cc1	10.1016/s0960-894x(03)00113-6
	25190435	158496	None	0	Human	Functional	pKd	=	8.7	8.7	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	447	9	1	5	4.1	CCCCc1cc(OC2CCN(CCS(=O)(=O)NC(C)(C)C)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	CHEMBL4090136	158496	None	0	Human	Functional	pKd	=	8.7	8.7	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	447	9	1	5	4.1	CCCCc1cc(OC2CCN(CCS(=O)(=O)NC(C)(C)C)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	25190373	161182	None	0	Human	Functional	pKd	=	8.7	8.7	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	461	12	1	5	4.5	CCCCc1cc(OC2CCN(CCCCNS(=O)(=O)C(C)C)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	CHEMBL4060765	161182	None	0	Human	Functional	pKd	=	8.7	8.7	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	461	12	1	5	4.5	CCCCc1cc(OC2CCN(CCCCNS(=O)(=O)C(C)C)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	CHEMBL4116847	161182	None	0	Human	Functional	pKd	=	8.7	8.7	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	461	12	1	5	4.5	CCCCc1cc(OC2CCN(CCCCNS(=O)(=O)C(C)C)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	25190254	161197	None	0	Human	Functional	pKd	=	8.7	8.7	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	432	10	0	5	4.6	CCCCc1cc(OC2CCN(CCC(C)S(=O)(=O)CC)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	CHEMBL4068414	161197	None	0	Human	Functional	pKd	=	8.7	8.7	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	432	10	0	5	4.6	CCCCc1cc(OC2CCN(CCC(C)S(=O)(=O)CC)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	CHEMBL4117012	161197	None	0	Human	Functional	pKd	=	8.7	8.7	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	432	10	0	5	4.6	CCCCc1cc(OC2CCN(CCC(C)S(=O)(=O)CC)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	3529324	210813	None	1	Guinea pig	Functional	pKd	=	8.7	8.7	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	306	6	0	3	3.3	CC(C)c1ccc(C2SCC(=O)N2CCCN(C)C)cc1	10.1021/jm00093a025
	CHEMBL1202934	210813	None	1	Guinea pig	Functional	pKd	=	8.7	8.7	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	306	6	0	3	3.3	CC(C)c1ccc(C2SCC(=O)N2CCCN(C)C)cc1	10.1021/jm00093a025
	CHEMBL99417	210813	None	1	Guinea pig	Functional	pKd	=	8.7	8.7	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	306	6	0	3	3.3	CC(C)c1ccc(C2SCC(=O)N2CCCN(C)C)cc1	10.1021/jm00093a025
	57780008	149814	None	0	Human	Functional	pKd	=	8	8.0	-	0	Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay	ChEMBL	472	9	0	5	5.2	c1cnc2c(N3CCN(CCc4ccc(OCCCN5CCCCCC5)cc4)CC3)cccc2c1	10.1016/j.bmcl.2016.11.022
	CHEMBL3947980	149814	None	0	Human	Functional	pKd	=	8	8.0	-	0	Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay	ChEMBL	472	9	0	5	5.2	c1cnc2c(N3CCN(CCc4ccc(OCCCN5CCCCCC5)cc4)CC3)cccc2c1	10.1016/j.bmcl.2016.11.022
	1204	1932	None	74	Guinea pig	Functional	pKd	=	8	8.0	-10	11	Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nM	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm991056a
	1247	1932	None	74	Guinea pig	Functional	pKd	=	8	8.0	-10	11	Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nM	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm991056a
	1375	1932	None	74	Guinea pig	Functional	pKd	=	8	8.0	-10	11	Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nM	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm991056a
	774	1932	None	74	Guinea pig	Functional	pKd	=	8	8.0	-10	11	Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nM	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm991056a
	774.0	1932	None	74	Guinea pig	Functional	pKd	=	8	8.0	-10	11	Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nM	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm991056a
	CHEMBL90	1932	None	74	Guinea pig	Functional	pKd	=	8	8.0	-10	11	Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nM	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm991056a
	DB05381	1932	None	74	Guinea pig	Functional	pKd	=	8	8.0	-10	11	Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nM	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm991056a
	1204	1932	None	74	Rat	Functional	pKd	=	8	8.0	-25	11	Relative potency against Histamine H1 receptor in rat aortaRelative potency against Histamine H1 receptor in rat aorta	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm0309147
	1247	1932	None	74	Rat	Functional	pKd	=	8	8.0	-25	11	Relative potency against Histamine H1 receptor in rat aortaRelative potency against Histamine H1 receptor in rat aorta	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm0309147
	1375	1932	None	74	Rat	Functional	pKd	=	8	8.0	-25	11	Relative potency against Histamine H1 receptor in rat aortaRelative potency against Histamine H1 receptor in rat aorta	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm0309147
	774	1932	None	74	Rat	Functional	pKd	=	8	8.0	-25	11	Relative potency against Histamine H1 receptor in rat aortaRelative potency against Histamine H1 receptor in rat aorta	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm0309147
	774.0	1932	None	74	Rat	Functional	pKd	=	8	8.0	-25	11	Relative potency against Histamine H1 receptor in rat aortaRelative potency against Histamine H1 receptor in rat aorta	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm0309147
	CHEMBL90	1932	None	74	Rat	Functional	pKd	=	8	8.0	-25	11	Relative potency against Histamine H1 receptor in rat aortaRelative potency against Histamine H1 receptor in rat aorta	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm0309147
	DB05381	1932	None	74	Rat	Functional	pKd	=	8	8.0	-25	11	Relative potency against Histamine H1 receptor in rat aortaRelative potency against Histamine H1 receptor in rat aorta	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm0309147
	10364258	45783	None	0	Rat	Functional	pKd	=	8.0	8.0	-12	2	Apparent pA2 value of compound at 50 nM concentration of mepyramine in rat aortaApparent pA2 value of compound at 50 nM concentration of mepyramine in rat aorta	ChEMBL	410	11	2	3	4.9	c1ccc(C(CCc2nc(CCNCCc3ccccn3)c[nH]2)c2ccccc2)cc1	10.1021/jm0309147
	CHEMBL153067	45783	None	0	Rat	Functional	pKd	=	8.0	8.0	-12	2	Apparent pA2 value of compound at 50 nM concentration of mepyramine in rat aortaApparent pA2 value of compound at 50 nM concentration of mepyramine in rat aorta	ChEMBL	410	11	2	3	4.9	c1ccc(C(CCc2nc(CCNCCc3ccccn3)c[nH]2)c2ccccc2)cc1	10.1021/jm0309147
	10042467	1426	None	1	Guinea pig	Functional	pKd	=	8.0	8.0	-1	2	Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nM	ChEMBL	333	8	1	2	4.3	CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C	10.1021/jm991056a
	1203	1426	None	1	Guinea pig	Functional	pKd	=	8.0	8.0	-1	2	Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nM	ChEMBL	333	8	1	2	4.3	CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C	10.1021/jm991056a
	CHEMBL11553	1426	None	1	Guinea pig	Functional	pKd	=	8.0	8.0	-1	2	Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nM	ChEMBL	333	8	1	2	4.3	CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C	10.1021/jm991056a
	57402471	67898	None	0	Guinea pig	Functional	pKd	=	8.0	8.0	-	0	Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins	ChEMBL	469	8	1	5	4.0	COc1ccc(CN(CCN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)c2ccccn2)cc1	10.1016/j.bmcl.2011.09.001
	CHEMBL1910378	67898	None	0	Guinea pig	Functional	pKd	=	8.0	8.0	-	0	Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins	ChEMBL	469	8	1	5	4.0	COc1ccc(CN(CCN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)c2ccccn2)cc1	10.1016/j.bmcl.2011.09.001
	14113352	170311	None	0	Guinea pig	Functional	pKd	=	7	7.0	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	394	10	4	4	3.4	N=C(NCCCc1c[nH]cn1)NCCSC(c1ccccc1)c1ccccn1	10.1021/jm00128a045
	CHEMBL444531	170311	None	0	Guinea pig	Functional	pKd	=	7	7.0	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	394	10	4	4	3.4	N=C(NCCCc1c[nH]cn1)NCCSC(c1ccccc1)c1ccccn1	10.1021/jm00128a045
	14984030	107386	None	0	Guinea pig	Functional	pKd	=	6	6.0	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	279	5	1	4	1.8	CN(C)CCCN1C(=O)CSC1c1ccc(N)cc1	10.1021/jm00093a025
	CHEMBL1202935	107386	None	0	Guinea pig	Functional	pKd	=	6	6.0	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	279	5	1	4	1.8	CN(C)CCCN1C(=O)CSC1c1ccc(N)cc1	10.1021/jm00093a025
	CHEMBL317518	107386	None	0	Guinea pig	Functional	pKd	=	6	6.0	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	279	5	1	4	1.8	CN(C)CCCN1C(=O)CSC1c1ccc(N)cc1	10.1021/jm00093a025
	10246247	98346	None	0	Guinea pig	Functional	pKd	=	6	6.0	-	0	Relative potency was recorded in endothelium-denuded guinea pig; value ranges from 5.75 to 6.25Relative potency was recorded in endothelium-denuded guinea pig; value ranges from 5.75 to 6.25	ChEMBL	333	9	2	2	4.5	NCCc1c[nH]c(CCCCC(c2ccccc2)c2ccccc2)n1	10.1021/jm991056a
	CHEMBL274767	98346	None	0	Guinea pig	Functional	pKd	=	6	6.0	-	0	Relative potency was recorded in endothelium-denuded guinea pig; value ranges from 5.75 to 6.25Relative potency was recorded in endothelium-denuded guinea pig; value ranges from 5.75 to 6.25	ChEMBL	333	9	2	2	4.5	NCCc1c[nH]c(CCCCC(c2ccccc2)c2ccccc2)n1	10.1021/jm991056a
	10684712	11396	None	0	Guinea pig	Functional	pKd	=	5	5.0	-	0	Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum	ChEMBL	287	8	2	4	3.4	CCC/C(=N\O)c1ccc(OCCCc2c[nH]cn2)cc1	10.1021/jm000971p
	CHEMBL112301	11396	None	0	Guinea pig	Functional	pKd	=	5	5.0	-	0	Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum	ChEMBL	287	8	2	4	3.4	CCC/C(=N\O)c1ccc(OCCCc2c[nH]cn2)cc1	10.1021/jm000971p
	CHEMBL1180048	11396	None	0	Guinea pig	Functional	pKd	=	5	5.0	-	0	Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum	ChEMBL	287	8	2	4	3.4	CCC/C(=N\O)c1ccc(OCCCc2c[nH]cn2)cc1	10.1021/jm000971p
	6422121	207907	None	0	Guinea pig	Functional	pKd	=	5	5.0	-	0	Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum	ChEMBL	285	7	2	4	3.0	O/N=C(/c1ccc(OCCCc2c[nH]cn2)cc1)C1CC1	10.1021/jm000971p
	CHEMBL116270	207907	None	0	Guinea pig	Functional	pKd	=	5	5.0	-	0	Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum	ChEMBL	285	7	2	4	3.0	O/N=C(/c1ccc(OCCCc2c[nH]cn2)cc1)C1CC1	10.1021/jm000971p
	CHEMBL80348	207907	None	0	Guinea pig	Functional	pKd	=	5	5.0	-	0	Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum	ChEMBL	285	7	2	4	3.0	O/N=C(/c1ccc(OCCCc2c[nH]cn2)cc1)C1CC1	10.1021/jm000971p
	2860933	210631	None	2	Guinea pig	Functional	pKd	=	5	5.0	-	0	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	294	6	0	4	2.2	COc1ccc(C2SCC(=O)N2CCCN(C)C)cc1	10.1021/jm00093a025
	CHEMBL1202929	210631	None	2	Guinea pig	Functional	pKd	=	5	5.0	-	0	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	294	6	0	4	2.2	COc1ccc(C2SCC(=O)N2CCCN(C)C)cc1	10.1021/jm00093a025
	CHEMBL98319	210631	None	2	Guinea pig	Functional	pKd	=	5	5.0	-	0	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	294	6	0	4	2.2	COc1ccc(C2SCC(=O)N2CCCN(C)C)cc1	10.1021/jm00093a025
	54726349	112433	None	0	Guinea pig	Functional	pKd	=	4	4.0	-	0	H1-antihistamine activity on guinea pig ileumH1-antihistamine activity on guinea pig ileum	ChEMBL	363	6	1	8	1.4	CN1CCN(CCCOc2ccc3c(O)c([N+](=O)[O-])c(=O)oc3c2)CC1	10.1021/jm00377a013
	CHEMBL32953	112433	None	0	Guinea pig	Functional	pKd	=	4	4.0	-	0	H1-antihistamine activity on guinea pig ileumH1-antihistamine activity on guinea pig ileum	ChEMBL	363	6	1	8	1.4	CN1CCN(CCCOc2ccc3c(O)c([N+](=O)[O-])c(=O)oc3c2)CC1	10.1021/jm00377a013
	10246247	98346	None	0	Rat	Functional	pKd	=	6.0	6.0	-	0	Relative potency was recorded in in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619 valueRelative potency was recorded in in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619 value	ChEMBL	333	9	2	2	4.5	NCCc1c[nH]c(CCCCC(c2ccccc2)c2ccccc2)n1	10.1021/jm991056a
	CHEMBL274767	98346	None	0	Rat	Functional	pKd	=	6.0	6.0	-	0	Relative potency was recorded in in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619 valueRelative potency was recorded in in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619 value	ChEMBL	333	9	2	2	4.5	NCCc1c[nH]c(CCCCC(c2ccccc2)c2ccccc2)n1	10.1021/jm991056a
	11779175	63186	None	0	Guinea pig	Functional	pKd	=	5.0	5.0	-	1	Antagonist activity at histamine H1 receptor in guinea-pig ileumAntagonist activity at histamine H1 receptor in guinea-pig ileum	ChEMBL	293	8	2	3	3.4	O=C(NCCCC1CCCCC1)OCCCc1c[nH]cn1	10.1016/j.bmc.2011.03.046
	CHEMBL1774600	63186	None	0	Guinea pig	Functional	pKd	=	5.0	5.0	-	1	Antagonist activity at histamine H1 receptor in guinea-pig ileumAntagonist activity at histamine H1 receptor in guinea-pig ileum	ChEMBL	293	8	2	3	3.4	O=C(NCCCC1CCCCC1)OCCCc1c[nH]cn1	10.1016/j.bmc.2011.03.046
	CHEMBL1789801	63186	None	0	Guinea pig	Functional	pKd	=	5.0	5.0	-	1	Antagonist activity at histamine H1 receptor in guinea-pig ileumAntagonist activity at histamine H1 receptor in guinea-pig ileum	ChEMBL	293	8	2	3	3.4	O=C(NCCCC1CCCCC1)OCCCc1c[nH]cn1	10.1016/j.bmc.2011.03.046
	14660374	100744	None	0	Guinea pig	Functional	pKd	=	6.0	6.0	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	394	9	3	3	3.6	CN(CCC(c1ccc(F)cc1)c1ccccn1)C(=N)NCCCc1c[nH]cn1	10.1021/jm00128a045
	CHEMBL292395	100744	None	0	Guinea pig	Functional	pKd	=	6.0	6.0	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	394	9	3	3	3.6	CN(CCC(c1ccc(F)cc1)c1ccccn1)C(=N)NCCCc1c[nH]cn1	10.1021/jm00128a045
	1224	1432	None	51	Guinea pig	Functional	pKd	=	7.9	7.9	85	22	Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins	ChEMBL	255	6	0	2	3.4	CN(CCOC(c1ccccc1)c1ccccc1)C	10.1016/j.bmcl.2011.09.001
	3100	1432	None	51	Guinea pig	Functional	pKd	=	7.9	7.9	85	22	Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins	ChEMBL	255	6	0	2	3.4	CN(CCOC(c1ccccc1)c1ccccc1)C	10.1016/j.bmcl.2011.09.001
	3100.0	1432	None	51	Guinea pig	Functional	pKd	=	7.9	7.9	85	22	Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins	ChEMBL	255	6	0	2	3.4	CN(CCOC(c1ccccc1)c1ccccc1)C	10.1016/j.bmcl.2011.09.001
	8980	1432	None	51	Guinea pig	Functional	pKd	=	7.9	7.9	85	22	Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins	ChEMBL	255	6	0	2	3.4	CN(CCOC(c1ccccc1)c1ccccc1)C	10.1016/j.bmcl.2011.09.001
	916	1432	None	51	Guinea pig	Functional	pKd	=	7.9	7.9	85	22	Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins	ChEMBL	255	6	0	2	3.4	CN(CCOC(c1ccccc1)c1ccccc1)C	10.1016/j.bmcl.2011.09.001
	CHEMBL657	1432	None	51	Guinea pig	Functional	pKd	=	7.9	7.9	85	22	Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins	ChEMBL	255	6	0	2	3.4	CN(CCOC(c1ccccc1)c1ccccc1)C	10.1016/j.bmcl.2011.09.001
	DB01075	1432	None	51	Guinea pig	Functional	pKd	=	7.9	7.9	85	22	Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins	ChEMBL	255	6	0	2	3.4	CN(CCOC(c1ccccc1)c1ccccc1)C	10.1016/j.bmcl.2011.09.001
	25149611	179281	None	0	Guinea pig	Functional	pKd	=	5.0	5.0	-	0	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity	ChEMBL	376	8	4	4	2.6	N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1ccccn1	10.1021/jm800841w
	CHEMBL472272	179281	None	0	Guinea pig	Functional	pKd	=	5.0	5.0	-	0	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity	ChEMBL	376	8	4	4	2.6	N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1ccccn1	10.1021/jm800841w
	14660410	201510	None	0	Guinea pig	Functional	pKd	=	6.9	6.9	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	396	9	4	4	2.1	N/C(=N\CCC(O)(c1ccc(F)cc1)c1ccccn1)NCCCc1c[nH]cn1	10.1021/jm00128a045
	CHEMBL58621	201510	None	0	Guinea pig	Functional	pKd	=	6.9	6.9	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	396	9	4	4	2.1	N/C(=N\CCC(O)(c1ccc(F)cc1)c1ccccn1)NCCCc1c[nH]cn1	10.1021/jm00128a045
	57398985	67905	None	0	Guinea pig	Functional	pKd	=	7.9	7.9	-	0	Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins	ChEMBL	569	12	2	7	4.4	COc1ccc(CN(CCN(C)CC(C)Nc2ccc3[nH]c(C(=O)N4CCN(C)CC4)cc3c2)c2ccccn2)cc1	10.1016/j.bmcl.2011.09.001
	CHEMBL1910385	67905	None	0	Guinea pig	Functional	pKd	=	7.9	7.9	-	0	Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins	ChEMBL	569	12	2	7	4.4	COc1ccc(CN(CCN(C)CC(C)Nc2ccc3[nH]c(C(=O)N4CCN(C)CC4)cc3c2)c2ccccn2)cc1	10.1016/j.bmcl.2011.09.001
	54710799	96834	None	0	Guinea pig	Functional	pKd	=	7.9	7.9	-	0	H1-antihistamine activity on guinea pig ileumH1-antihistamine activity on guinea pig ileum	ChEMBL	439	8	1	8	3.0	O=c1oc2cc(OCCCN3CCN(Cc4ccccc4)CC3)ccc2c(O)c1[N+](=O)[O-]	10.1021/jm00377a013
	CHEMBL264756	96834	None	0	Guinea pig	Functional	pKd	=	7.9	7.9	-	0	H1-antihistamine activity on guinea pig ileumH1-antihistamine activity on guinea pig ileum	ChEMBL	439	8	1	8	3.0	O=c1oc2cc(OCCCN3CCN(Cc4ccccc4)CC3)ccc2c(O)c1[N+](=O)[O-]	10.1021/jm00377a013
	19762600	80030	None	0	Guinea pig	Functional	pKd	=	7.9	7.9	-	0	Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand	ChEMBL	370	13	1	5	3.5	COc1ccc(CN(CCN(C)CCCCCCN)c2ccccn2)cc1	10.1016/s0960-894x(03)00113-6
	CHEMBL21278	80030	None	0	Guinea pig	Functional	pKd	=	7.9	7.9	-	0	Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand	ChEMBL	370	13	1	5	3.5	COc1ccc(CN(CCN(C)CCCCCCN)c2ccccn2)cc1	10.1016/s0960-894x(03)00113-6
	10003410	203098	None	0	Guinea pig	Functional	pKd	=	6.9	6.9	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	440	9	4	3	3.8	N=C(NCCCc1c[nH]cn1)NCCC(c1ccc(Br)cc1)c1ccccn1	10.1021/jm00128a045
	CHEMBL59951	203098	None	0	Guinea pig	Functional	pKd	=	6.9	6.9	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	440	9	4	3	3.8	N=C(NCCCc1c[nH]cn1)NCCC(c1ccc(Br)cc1)c1ccccn1	10.1021/jm00128a045
	10852834	11397	None	0	Guinea pig	Functional	pKd	=	4.9	4.9	-	0	Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum	ChEMBL	315	10	2	4	4.2	CCCCC/C(=N\O)c1ccc(OCCCc2c[nH]cn2)cc1	10.1021/jm000971p
	CHEMBL112629	11397	None	0	Guinea pig	Functional	pKd	=	4.9	4.9	-	0	Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum	ChEMBL	315	10	2	4	4.2	CCCCC/C(=N\O)c1ccc(OCCCc2c[nH]cn2)cc1	10.1021/jm000971p
	CHEMBL1180064	11397	None	0	Guinea pig	Functional	pKd	=	4.9	4.9	-	0	Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum	ChEMBL	315	10	2	4	4.2	CCCCC/C(=N\O)c1ccc(OCCCc2c[nH]cn2)cc1	10.1021/jm000971p
	10659856	11401	None	0	Guinea pig	Functional	pKd	=	4.9	4.9	-	0	Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum	ChEMBL	273	7	1	4	2.8	CO/N=C(\C)c1ccc(OCCCc2c[nH]cn2)cc1	10.1021/jm000971p
	CHEMBL112753	11401	None	0	Guinea pig	Functional	pKd	=	4.9	4.9	-	0	Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum	ChEMBL	273	7	1	4	2.8	CO/N=C(\C)c1ccc(OCCCc2c[nH]cn2)cc1	10.1021/jm000971p
	CHEMBL1180075	11401	None	0	Guinea pig	Functional	pKd	=	4.9	4.9	-	0	Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum	ChEMBL	273	7	1	4	2.8	CO/N=C(\C)c1ccc(OCCCc2c[nH]cn2)cc1	10.1021/jm000971p
	10828008	11414	None	0	Guinea pig	Functional	pKd	=	4.9	4.9	-	0	Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum	ChEMBL	299	6	1	3	2.7	O=C(c1ccc(OCCCc2c[nH]cn2)cc1)N1CCCC1	10.1021/jm000971p
	CHEMBL115169	11414	None	0	Guinea pig	Functional	pKd	=	4.9	4.9	-	0	Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum	ChEMBL	299	6	1	3	2.7	O=C(c1ccc(OCCCc2c[nH]cn2)cc1)N1CCCC1	10.1021/jm000971p
	CHEMBL1180148	11414	None	0	Guinea pig	Functional	pKd	=	4.9	4.9	-	0	Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum	ChEMBL	299	6	1	3	2.7	O=C(c1ccc(OCCCc2c[nH]cn2)cc1)N1CCCC1	10.1021/jm000971p
	19762590	162357	None	1	Guinea pig	Functional	pKd	=	7.9	7.9	-	0	Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand	ChEMBL	314	9	1	5	2.0	COc1ccc(CN(CCN(C)CCN)c2ccccn2)cc1	10.1016/s0960-894x(03)00113-6
	CHEMBL416378	162357	None	1	Guinea pig	Functional	pKd	=	7.9	7.9	-	0	Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand	ChEMBL	314	9	1	5	2.0	COc1ccc(CN(CCN(C)CCN)c2ccccn2)cc1	10.1016/s0960-894x(03)00113-6
	25149335	184331	None	0	Guinea pig	Functional	pKd	=	5.9	5.9	-	3	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractions	ChEMBL	313	7	3	2	2.0	CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1	10.1021/jm9000693
	CHEMBL483406	184331	None	0	Guinea pig	Functional	pKd	=	5.9	5.9	-	3	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractions	ChEMBL	313	7	3	2	2.0	CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1	10.1021/jm9000693
	25149335	184331	None	0	Guinea pig	Functional	pKd	=	5.9	5.9	-	3	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity	ChEMBL	313	7	3	2	2.0	CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1	10.1021/jm800841w
	CHEMBL483406	184331	None	0	Guinea pig	Functional	pKd	=	5.9	5.9	-	3	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity	ChEMBL	313	7	3	2	2.0	CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1	10.1021/jm800841w
	52949049	10558	None	0	Guinea pig	Functional	pKd	=	7.8	7.8	-	0	Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand	ChEMBL	673	17	1	7	7.2	COc1ccc(CN(CCN(C)CCCCCCNC(=O)CCC2=C3C(C)=CC(C)N3[B-](F)(F)n3c(C)cc(C)c32)c2ccccn2)cc1	10.1016/s0960-894x(03)00113-6
	CHEMBL1169587	10558	None	0	Guinea pig	Functional	pKd	=	7.8	7.8	-	0	Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand	ChEMBL	673	17	1	7	7.2	COc1ccc(CN(CCN(C)CCCCCCNC(=O)CCC2=C3C(C)=CC(C)N3[B-](F)(F)n3c(C)cc(C)c32)c2ccccn2)cc1	10.1016/s0960-894x(03)00113-6
	14660389	204750	None	0	Guinea pig	Functional	pKd	=	6.9	6.9	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	393	10	4	2	4.0	N=C(NCCCc1c[nH]cn1)NCCC(Cc1ccccc1)c1ccc(F)cc1	10.1021/jm00128a045
	CHEMBL61022	204750	None	0	Guinea pig	Functional	pKd	=	6.9	6.9	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	393	10	4	2	4.0	N=C(NCCCc1c[nH]cn1)NCCC(Cc1ccccc1)c1ccc(F)cc1	10.1021/jm00128a045
	44457703	99600	None	0	Guinea pig	Functional	pKd	=	6.8	6.8	-	0	Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand	ChEMBL	672	13	3	9	5.7	COc1ccc(CN(CCN(C)CCNC(=O)c2ccc(C(=O)O)c(-c3c4ccc(=O)cc-4oc4cc(O)ccc34)c2)c2ccccn2)cc1	10.1016/s0960-894x(03)00113-6
	CHEMBL283527	99600	None	0	Guinea pig	Functional	pKd	=	6.8	6.8	-	0	Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand	ChEMBL	672	13	3	9	5.7	COc1ccc(CN(CCN(C)CCNC(=O)c2ccc(C(=O)O)c(-c3c4ccc(=O)cc-4oc4cc(O)ccc34)c2)c2ccccn2)cc1	10.1016/s0960-894x(03)00113-6
	14660348	202110	None	0	Guinea pig	Functional	pKd	=	6.8	6.8	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	376	9	3	3	3.2	Cc1ccc(C(CC/N=C(\N)NCCCc2c[nH]cn2)c2ccccn2)cc1	10.1021/jm00128a045
	CHEMBL59294	202110	None	0	Guinea pig	Functional	pKd	=	6.8	6.8	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	376	9	3	3	3.2	Cc1ccc(C(CC/N=C(\N)NCCCc2c[nH]cn2)c2ccccn2)cc1	10.1021/jm00128a045
	13676692	105540	None	0	Guinea pig	Functional	pKd	=	7.8	7.8	-	0	Compound was tested for H1-antihistamine activity in guinea pig ileum.Compound was tested for H1-antihistamine activity in guinea pig ileum.	ChEMBL	447	7	1	8	3.6	Cc1ccc(CN2CCN(CCCOc3ccc4c(O)c5nnnc-5oc4c3C)CC2)cc1	10.1021/jm00161a022
	CHEMBL312083	105540	None	0	Guinea pig	Functional	pKd	=	7.8	7.8	-	0	Compound was tested for H1-antihistamine activity in guinea pig ileum.Compound was tested for H1-antihistamine activity in guinea pig ileum.	ChEMBL	447	7	1	8	3.6	Cc1ccc(CN2CCN(CCCOc3ccc4c(O)c5nnnc-5oc4c3C)CC2)cc1	10.1021/jm00161a022
	13676699	163863	None	0	Guinea pig	Functional	pKd	=	7.8	7.8	-	0	H1-antihistamine activity in guinea pig ileumH1-antihistamine activity in guinea pig ileum	ChEMBL	434	7	1	9	2.7	Cc1c(OCCCN2CCN(Cc3ccccn3)CC2)ccc2c(O)c3nnnc-3oc12	10.1021/jm00161a022
	CHEMBL420567	163863	None	0	Guinea pig	Functional	pKd	=	7.8	7.8	-	0	H1-antihistamine activity in guinea pig ileumH1-antihistamine activity in guinea pig ileum	ChEMBL	434	7	1	9	2.7	Cc1c(OCCCN2CCN(Cc3ccccn3)CC2)ccc2c(O)c3nnnc-3oc12	10.1021/jm00161a022
	14660357	205159	None	0	Guinea pig	Functional	pKd	=	6.8	6.8	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	380	9	4	3	3.2	N=C(NCCCc1c[nH]cn1)NCCC(c1cccc(F)c1)c1ccccn1	10.1021/jm00128a045
	CHEMBL61675	205159	None	0	Guinea pig	Functional	pKd	=	6.8	6.8	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	380	9	4	3	3.2	N=C(NCCCc1c[nH]cn1)NCCC(c1cccc(F)c1)c1ccccn1	10.1021/jm00128a045
	54710801	99961	None	0	Guinea pig	Functional	pKd	=	6.8	6.8	-	0	H1-antihistamine activity on guinea pig ileumH1-antihistamine activity on guinea pig ileum	ChEMBL	459	7	1	8	3.3	O=c1oc2cc(OCCN3CCN(Cc4ccc(Cl)cc4)CC3)ccc2c(O)c1[N+](=O)[O-]	10.1021/jm00377a013
	CHEMBL286094	99961	None	0	Guinea pig	Functional	pKd	=	6.8	6.8	-	0	H1-antihistamine activity on guinea pig ileumH1-antihistamine activity on guinea pig ileum	ChEMBL	459	7	1	8	3.3	O=c1oc2cc(OCCN3CCN(Cc4ccc(Cl)cc4)CC3)ccc2c(O)c1[N+](=O)[O-]	10.1021/jm00377a013
	10825231	9632	None	0	Guinea pig	Functional	pKd	=	6.8	6.8	-	0	Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum	ChEMBL	260	6	1	4	2.2	COC(=O)c1ccc(OCCCc2c[nH]cn2)cc1	10.1021/jm000971p
	CHEMBL112670	9632	None	0	Guinea pig	Functional	pKd	=	6.8	6.8	-	0	Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum	ChEMBL	260	6	1	4	2.2	COC(=O)c1ccc(OCCCc2c[nH]cn2)cc1	10.1021/jm000971p
	1278	2150	None	56	Guinea pig	Functional	pKd	=	5.8	5.8	-	4	Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins	ChEMBL	277	1	1	2	2.2	CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl	10.1016/j.bmcl.2011.09.001
	1279	2150	None	56	Guinea pig	Functional	pKd	=	5.8	5.8	-	4	Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins	ChEMBL	277	1	1	2	2.2	CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl	10.1016/j.bmcl.2011.09.001
	4908365	2150	None	56	Guinea pig	Functional	pKd	=	5.8	5.8	-	4	Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins	ChEMBL	277	1	1	2	2.2	CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl	10.1016/j.bmcl.2011.09.001
	CHEMBL129198	2150	None	56	Guinea pig	Functional	pKd	=	5.8	5.8	-	4	Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins	ChEMBL	277	1	1	2	2.2	CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl	10.1016/j.bmcl.2011.09.001
	15179507	206637	None	0	Guinea pig	Functional	pKd	=	5.8	5.8	-	0	Histamine H1 receptor antagonistic activity on the isolated guinea pig ileum determined by Schild plot.Histamine H1 receptor antagonistic activity on the isolated guinea pig ileum determined by Schild plot.	ChEMBL	729	11	4	6	3.7	N#CN/C(=N\CCNC(=O)c1cc(I)c(N)c(I)c1)NCCCOc1cccc(CN2CCCCC2)c1	10.1021/jm00090a013
	CHEMBL70746	206637	None	0	Guinea pig	Functional	pKd	=	5.8	5.8	-	0	Histamine H1 receptor antagonistic activity on the isolated guinea pig ileum determined by Schild plot.Histamine H1 receptor antagonistic activity on the isolated guinea pig ileum determined by Schild plot.	ChEMBL	729	11	4	6	3.7	N#CN/C(=N\CCNC(=O)c1cc(I)c(N)c(I)c1)NCCCOc1cccc(CN2CCCCC2)c1	10.1021/jm00090a013
	11459067	11352	None	0	Guinea pig	Functional	pKd	=	4.8	4.8	-	0	Functional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileum	ChEMBL	238	11	1	2	3.7	CCCCCCCCOCCCc1c[nH]cn1	10.1021/jm031065q
	CHEMBL1179647	11352	None	0	Guinea pig	Functional	pKd	=	4.8	4.8	-	0	Functional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileum	ChEMBL	238	11	1	2	3.7	CCCCCCCCOCCCc1c[nH]cn1	10.1021/jm031065q
	CHEMBL91523	11352	None	0	Guinea pig	Functional	pKd	=	4.8	4.8	-	0	Functional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileum	ChEMBL	238	11	1	2	3.7	CCCCCCCCOCCCc1c[nH]cn1	10.1021/jm031065q
	10730975	12109	None	0	Guinea pig	Functional	pKd	=	4.8	4.8	-	0	Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum	ChEMBL	273	6	2	4	2.9	C/C(=N\O)c1ccc(OCCCc2c[nH]cn2)c(C)c1	10.1021/jm000971p
	CHEMBL1183977	12109	None	0	Guinea pig	Functional	pKd	=	4.8	4.8	-	0	Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum	ChEMBL	273	6	2	4	2.9	C/C(=N\O)c1ccc(OCCCc2c[nH]cn2)c(C)c1	10.1021/jm000971p
	CHEMBL326624	12109	None	0	Guinea pig	Functional	pKd	=	4.8	4.8	-	0	Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum	ChEMBL	273	6	2	4	2.9	C/C(=N\O)c1ccc(OCCCc2c[nH]cn2)c(C)c1	10.1021/jm000971p
	14660414	201528	None	0	Guinea pig	Functional	pKd	=	5.8	5.8	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	407	10	3	5	2.8	N/C(=N\CCC(c1cccc([N+](=O)[O-])c1)c1ccccn1)NCCCc1c[nH]cn1	10.1021/jm00128a045
	CHEMBL58750	201528	None	0	Guinea pig	Functional	pKd	=	5.8	5.8	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	407	10	3	5	2.8	N/C(=N\CCC(c1cccc([N+](=O)[O-])c1)c1ccccn1)NCCCc1c[nH]cn1	10.1021/jm00128a045
	44457690	85560	None	0	Guinea pig	Functional	pKd	=	7.8	7.8	-	0	Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand	ChEMBL	603	17	1	7	5.8	COc1ccc(CN(CCN(C)CCCCCCNS(=O)(=O)c2cccc3c(N(C)C)cccc23)c2ccccn2)cc1	10.1016/s0960-894x(03)00113-6
	CHEMBL22749	85560	None	0	Guinea pig	Functional	pKd	=	7.8	7.8	-	0	Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand	ChEMBL	603	17	1	7	5.8	COc1ccc(CN(CCN(C)CCCCCCNS(=O)(=O)c2cccc3c(N(C)C)cccc23)c2ccccn2)cc1	10.1016/s0960-894x(03)00113-6
	25149427	186067	None	0	Guinea pig	Functional	pKd	=	5.7	5.7	-	0	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity	ChEMBL	313	8	4	3	2.0	N=C(NCCCc1c[nH]cn1)NC(=O)CCCc1ccccc1	10.1021/jm800841w
	CHEMBL486962	186067	None	0	Guinea pig	Functional	pKd	=	5.7	5.7	-	0	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity	ChEMBL	313	8	4	3	2.0	N=C(NCCCc1c[nH]cn1)NC(=O)CCCc1ccccc1	10.1021/jm800841w
	10423703	107351	None	0	Guinea pig	Functional	pKd	=	7.7	7.7	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	278	5	0	3	2.5	Cc1cccc(C2SCC(=O)N2CCCN(C)C)c1	10.1021/jm00093a025
	CHEMBL1202942	107351	None	0	Guinea pig	Functional	pKd	=	7.7	7.7	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	278	5	0	3	2.5	Cc1cccc(C2SCC(=O)N2CCCN(C)C)c1	10.1021/jm00093a025
	CHEMBL317171	107351	None	0	Guinea pig	Functional	pKd	=	7.7	7.7	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	278	5	0	3	2.5	Cc1cccc(C2SCC(=O)N2CCCN(C)C)c1	10.1021/jm00093a025
	14660380	201163	None	0	Guinea pig	Functional	pKd	=	6.7	6.7	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	380	9	4	3	3.2	N=C(NCCCc1c[nH]cn1)NCCC(c1ccc(F)cc1)c1cccnc1	10.1021/jm00128a045
	CHEMBL58170	201163	None	0	Guinea pig	Functional	pKd	=	6.7	6.7	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	380	9	4	3	3.2	N=C(NCCCc1c[nH]cn1)NCCC(c1ccc(F)cc1)c1cccnc1	10.1021/jm00128a045
	10342634	202475	None	0	Guinea pig	Functional	pKd	=	6.7	6.7	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	429	9	4	2	5.0	N=C(NCCCc1c[nH]cn1)NCCC(c1ccccc1)c1ccc(Cl)c(Cl)c1	10.1021/jm00128a045
	CHEMBL59544	202475	None	0	Guinea pig	Functional	pKd	=	6.7	6.7	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	429	9	4	2	5.0	N=C(NCCCc1c[nH]cn1)NCCC(c1ccccc1)c1ccc(Cl)c(Cl)c1	10.1021/jm00128a045
	11436304	11341	None	0	Guinea pig	Functional	pKd	=	4.7	4.7	-	0	Functional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileum	ChEMBL	236	8	1	2	3.3	c1nc(CCCOCCCC2CCCC2)c[nH]1	10.1021/jm031065q
	CHEMBL1179594	11341	None	0	Guinea pig	Functional	pKd	=	4.7	4.7	-	0	Functional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileum	ChEMBL	236	8	1	2	3.3	c1nc(CCCOCCCC2CCCC2)c[nH]1	10.1021/jm031065q
	CHEMBL88306	11341	None	0	Guinea pig	Functional	pKd	=	4.7	4.7	-	0	Functional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileum	ChEMBL	236	8	1	2	3.3	c1nc(CCCOCCCC2CCCC2)c[nH]1	10.1021/jm031065q
	10375442	11344	None	0	Guinea pig	Functional	pKd	=	4.7	4.7	-	1	Functional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileum	ChEMBL	196	8	1	2	2.5	CCCCCOCCCc1c[nH]cn1	10.1021/jm031065q
	CHEMBL1179604	11344	None	0	Guinea pig	Functional	pKd	=	4.7	4.7	-	1	Functional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileum	ChEMBL	196	8	1	2	2.5	CCCCCOCCCc1c[nH]cn1	10.1021/jm031065q
	CHEMBL88746	11344	None	0	Guinea pig	Functional	pKd	=	4.7	4.7	-	1	Functional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileum	ChEMBL	196	8	1	2	2.5	CCCCCOCCCc1c[nH]cn1	10.1021/jm031065q
	25190258	161246	None	0	Human	Functional	pKd	=	8.7	8.7	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	419	10	1	5	3.4	CCCCc1cc(OC2CCN(CCNS(=O)(=O)CC)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	CHEMBL4079248	161246	None	0	Human	Functional	pKd	=	8.7	8.7	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	419	10	1	5	3.4	CCCCc1cc(OC2CCN(CCNS(=O)(=O)CC)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	CHEMBL4117327	161246	None	0	Human	Functional	pKd	=	8.7	8.7	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	419	10	1	5	3.4	CCCCc1cc(OC2CCN(CCNS(=O)(=O)CC)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	11791817	98356	None	0	Guinea pig	Functional	pKd	=	8.7	8.7	-1	2	Antagonism of guinea pig ileum contraction at 100 nM mepyramineAntagonism of guinea pig ileum contraction at 100 nM mepyramine	ChEMBL	345	9	2	2	4.5	c1ccc(C(CCc2nc(CCNC3CC3)c[nH]2)c2ccccc2)cc1	10.1021/jm991056a
	CHEMBL274831	98356	None	0	Guinea pig	Functional	pKd	=	8.7	8.7	-1	2	Antagonism of guinea pig ileum contraction at 100 nM mepyramineAntagonism of guinea pig ileum contraction at 100 nM mepyramine	ChEMBL	345	9	2	2	4.5	c1ccc(C(CCc2nc(CCNC3CC3)c[nH]2)c2ccccc2)cc1	10.1021/jm991056a
	71449250	80502	None	0	Human	Functional	pKd	=	8.6	8.6	-	0	Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay	ChEMBL	368	4	0	5	3.1	CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccncc2c1=O	10.1016/j.bmc.2012.08.032
	CHEMBL2146804	80502	None	0	Human	Functional	pKd	=	8.6	8.6	-	0	Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay	ChEMBL	368	4	0	5	3.1	CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccncc2c1=O	10.1016/j.bmc.2012.08.032
	57780007	147079	None	0	Human	Functional	pKd	=	8.6	8.6	-	0	Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay	ChEMBL	572	13	1	6	5.8	CCc1cc(N2CCN(CCc3ccc(OCCCN4CCCCCC4)cc3)CC2)c2nc(CCC(=O)O)ccc2c1	10.1016/j.bmcl.2016.11.022
	CHEMBL3926412	147079	None	0	Human	Functional	pKd	=	8.6	8.6	-	0	Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay	ChEMBL	572	13	1	6	5.8	CCc1cc(N2CCN(CCc3ccc(OCCCN4CCCCCC4)cc3)CC2)c2nc(CCC(=O)O)ccc2c1	10.1016/j.bmcl.2016.11.022
	25190254	161197	None	0	Human	Functional	pKd	=	8.6	8.6	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	432	10	0	5	4.6	CCCCc1cc(OC2CCN(CCC(C)S(=O)(=O)CC)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	CHEMBL4068414	161197	None	0	Human	Functional	pKd	=	8.6	8.6	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	432	10	0	5	4.6	CCCCc1cc(OC2CCN(CCC(C)S(=O)(=O)CC)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	CHEMBL4117012	161197	None	0	Human	Functional	pKd	=	8.6	8.6	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	432	10	0	5	4.6	CCCCc1cc(OC2CCN(CCC(C)S(=O)(=O)CC)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	10042467	1426	None	1	Guinea pig	Functional	pKd	=	8.6	8.6	-1	2	Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nM	ChEMBL	333	8	1	2	4.3	CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C	10.1021/jm991056a
	1203	1426	None	1	Guinea pig	Functional	pKd	=	8.6	8.6	-1	2	Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nM	ChEMBL	333	8	1	2	4.3	CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C	10.1021/jm991056a
	CHEMBL11553	1426	None	1	Guinea pig	Functional	pKd	=	8.6	8.6	-1	2	Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nM	ChEMBL	333	8	1	2	4.3	CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C	10.1021/jm991056a
	57390224	67899	None	0	Guinea pig	Functional	pKd	=	7.7	7.7	-	0	Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins	ChEMBL	503	8	1	5	4.7	COc1ccc(CN(CCN2CCN(C(=O)c3cc4cc(Cl)ccc4[nH]3)CC2)c2ccccn2)cc1	10.1016/j.bmcl.2011.09.001
	CHEMBL1910379	67899	None	0	Guinea pig	Functional	pKd	=	7.7	7.7	-	0	Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins	ChEMBL	503	8	1	5	4.7	COc1ccc(CN(CCN2CCN(C(=O)c3cc4cc(Cl)ccc4[nH]3)CC2)c2ccccn2)cc1	10.1016/j.bmcl.2011.09.001
	44457702	83201	None	0	Guinea pig	Functional	pKd	=	7.7	7.7	-	0	Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand	ChEMBL	728	17	3	9	7.3	COc1ccc(CN(CCN(C)CCCCCCNC(=O)c2ccc(-c3c4ccc(=O)cc-4oc4cc(O)ccc34)c(C(=O)O)c2)c2ccccn2)cc1	10.1016/s0960-894x(03)00113-6
	CHEMBL21833	83201	None	0	Guinea pig	Functional	pKd	=	7.7	7.7	-	0	Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand	ChEMBL	728	17	3	9	7.3	COc1ccc(CN(CCN(C)CCCCCCNC(=O)c2ccc(-c3c4ccc(=O)cc-4oc4cc(O)ccc34)c(C(=O)O)c2)c2ccccn2)cc1	10.1016/s0960-894x(03)00113-6
	25149712	179092	None	0	Guinea pig	Functional	pKd	=	5.7	5.7	-	3	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity	ChEMBL	299	7	4	3	1.6	N=C(NCCCc1c[nH]cn1)NC(=O)CCc1ccccc1	10.1021/jm800841w
	CHEMBL470790	179092	None	0	Guinea pig	Functional	pKd	=	5.7	5.7	-	3	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity	ChEMBL	299	7	4	3	1.6	N=C(NCCCc1c[nH]cn1)NC(=O)CCc1ccccc1	10.1021/jm800841w
	11956130	186071	None	0	Guinea pig	Functional	pKd	=	5.7	5.7	-	0	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity	ChEMBL	319	7	4	3	2.6	CC(CC(=O)NC(=N)NCCCc1c[nH]cn1)C1CCCCC1	10.1021/jm800841w
	CHEMBL486965	186071	None	0	Guinea pig	Functional	pKd	=	5.7	5.7	-	0	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity	ChEMBL	319	7	4	3	2.6	CC(CC(=O)NC(=N)NCCCc1c[nH]cn1)C1CCCCC1	10.1021/jm800841w
	1221	475	None	6	Guinea pig	Functional	pKd	=	7.7	7.7	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	380	9	3	3	3.0	NC(=NCCCc1[nH]cnc1)NCCC(c1ccccn1)c1ccc(cc1)F	10.1021/jm00128a045
	65895	475	None	6	Guinea pig	Functional	pKd	=	7.7	7.7	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	380	9	3	3	3.0	NC(=NCCCc1[nH]cnc1)NCCC(c1ccccn1)c1ccc(cc1)F	10.1021/jm00128a045
	CHEMBL293802	475	None	6	Guinea pig	Functional	pKd	=	7.7	7.7	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	380	9	3	3	3.0	NC(=NCCCc1[nH]cnc1)NCCC(c1ccccn1)c1ccc(cc1)F	10.1021/jm00128a045
	1221	475	None	6	Guinea pig	Functional	pKd	=	7.7	7.7	-	0	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity	ChEMBL	380	9	3	3	3.0	NC(=NCCCc1[nH]cnc1)NCCC(c1ccccn1)c1ccc(cc1)F	10.1021/jm800841w
	65895	475	None	6	Guinea pig	Functional	pKd	=	7.7	7.7	-	0	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity	ChEMBL	380	9	3	3	3.0	NC(=NCCCc1[nH]cnc1)NCCC(c1ccccn1)c1ccc(cc1)F	10.1021/jm800841w
	CHEMBL293802	475	None	6	Guinea pig	Functional	pKd	=	7.7	7.7	-	0	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity	ChEMBL	380	9	3	3	3.0	NC(=NCCCc1[nH]cnc1)NCCC(c1ccccn1)c1ccc(cc1)F	10.1021/jm800841w
	19762580	80824	None	0	Guinea pig	Functional	pKd	=	7.7	7.7	-	0	Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand	ChEMBL	342	11	1	5	2.8	COc1ccc(CN(CCN(C)CCCCN)c2ccccn2)cc1	10.1016/s0960-894x(03)00113-6
	CHEMBL21520	80824	None	0	Guinea pig	Functional	pKd	=	7.7	7.7	-	0	Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand	ChEMBL	342	11	1	5	2.8	COc1ccc(CN(CCN(C)CCCCN)c2ccccn2)cc1	10.1016/s0960-894x(03)00113-6
	15179508	207153	None	0	Guinea pig	Functional	pKd	=	5.7	5.7	-	0	Histamine H1 receptor antagonistic activity on the isolated guinea pig ileum determined by Schild plot.Histamine H1 receptor antagonistic activity on the isolated guinea pig ileum determined by Schild plot.	ChEMBL	588	11	3	5	3.5	N#CN/C(=N\CCNC(=O)c1cccc(I)c1)NCCCOc1cccc(CN2CCCCC2)c1	10.1021/jm00090a013
	CHEMBL73994	207153	None	0	Guinea pig	Functional	pKd	=	5.7	5.7	-	0	Histamine H1 receptor antagonistic activity on the isolated guinea pig ileum determined by Schild plot.Histamine H1 receptor antagonistic activity on the isolated guinea pig ileum determined by Schild plot.	ChEMBL	588	11	3	5	3.5	N#CN/C(=N\CCNC(=O)c1cccc(I)c1)NCCCOc1cccc(CN2CCCCC2)c1	10.1021/jm00090a013
	14660391	201509	None	0	Guinea pig	Functional	pKd	=	6.6	6.6	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	272	5	3	2	2.2	N=C(N)NCCC(c1ccc(F)cc1)c1ccccn1	10.1021/jm00128a045
	CHEMBL58620	201509	None	0	Guinea pig	Functional	pKd	=	6.6	6.6	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	272	5	3	2	2.2	N=C(N)NCCC(c1ccc(F)cc1)c1ccccn1	10.1021/jm00128a045
	25149429	186070	None	0	Guinea pig	Functional	pKd	=	5.6	5.6	-	0	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity	ChEMBL	305	6	4	3	2.2	CC(C(=O)NC(=N)NCCCc1c[nH]cn1)C1CCCCC1	10.1021/jm800841w
	CHEMBL486964	186070	None	0	Guinea pig	Functional	pKd	=	5.6	5.6	-	0	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity	ChEMBL	305	6	4	3	2.2	CC(C(=O)NC(=N)NCCCc1c[nH]cn1)C1CCCCC1	10.1021/jm800841w
	25149814	185430	None	0	Guinea pig	Functional	pKd	=	5.6	5.6	-	0	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity	ChEMBL	291	6	4	3	2.0	N=C(NCCCc1c[nH]cn1)NC(=O)CC1CCCCC1	10.1021/jm800841w
	CHEMBL485958	185430	None	0	Guinea pig	Functional	pKd	=	5.6	5.6	-	0	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity	ChEMBL	291	6	4	3	2.0	N=C(NCCCc1c[nH]cn1)NC(=O)CC1CCCCC1	10.1021/jm800841w
	10022429	162884	None	0	Guinea pig	Functional	pKd	=	6.6	6.6	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	376	10	4	3	3.5	N=C(NCCCc1c[nH]cn1)NCCCC(c1ccccc1)c1ccccn1	10.1021/jm00128a045
	CHEMBL417221	162884	None	0	Guinea pig	Functional	pKd	=	6.6	6.6	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	376	10	4	3	3.5	N=C(NCCCc1c[nH]cn1)NCCCC(c1ccccc1)c1ccccn1	10.1021/jm00128a045
	11276413	12075	None	0	Guinea pig	Functional	pKd	=	5.6	5.6	-	0	Functional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileum	ChEMBL	236	7	1	2	3.3	c1nc(CCCOCCC2CCCCC2)c[nH]1	10.1021/jm031065q
	CHEMBL1183700	12075	None	0	Guinea pig	Functional	pKd	=	5.6	5.6	-	0	Functional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileum	ChEMBL	236	7	1	2	3.3	c1nc(CCCOCCC2CCCCC2)c[nH]1	10.1021/jm031065q
	CHEMBL313803	12075	None	0	Guinea pig	Functional	pKd	=	5.6	5.6	-	0	Functional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileum	ChEMBL	236	7	1	2	3.3	c1nc(CCCOCCC2CCCCC2)c[nH]1	10.1021/jm031065q
	54710792	126485	None	0	Guinea pig	Functional	pKd	=	5.6	5.6	-	0	H1-antihistamine activity on guinea pig ileumH1-antihistamine activity on guinea pig ileum	ChEMBL	429	5	1	7	3.4	O=c1oc2cc(CN3CCN(Cc4ccc(Cl)cc4)CC3)ccc2c(O)c1[N+](=O)[O-]	10.1021/jm00377a013
	CHEMBL36517	126485	None	0	Guinea pig	Functional	pKd	=	5.6	5.6	-	0	H1-antihistamine activity on guinea pig ileumH1-antihistamine activity on guinea pig ileum	ChEMBL	429	5	1	7	3.4	O=c1oc2cc(CN3CCN(Cc4ccc(Cl)cc4)CC3)ccc2c(O)c1[N+](=O)[O-]	10.1021/jm00377a013
	2861271	4255	None	7	Guinea pig	Functional	pKd	=	5.6	5.6	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	298	5	0	3	2.9	CN(C)CCCN1C(=O)CSC1c1ccc(Cl)cc1	10.1021/jm00093a025
	CHEMBL100486	4255	None	7	Guinea pig	Functional	pKd	=	5.6	5.6	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	298	5	0	3	2.9	CN(C)CCCN1C(=O)CSC1c1ccc(Cl)cc1	10.1021/jm00093a025
	10729993	11412	None	1	Guinea pig	Functional	pKd	=	4.6	4.6	-	0	Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum	ChEMBL	259	6	2	4	2.6	C/C(=N\O)c1ccc(OCCCc2c[nH]cn2)cc1	10.1021/jm000971p
	CHEMBL114085	11412	None	1	Guinea pig	Functional	pKd	=	4.6	4.6	-	0	Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum	ChEMBL	259	6	2	4	2.6	C/C(=N\O)c1ccc(OCCCc2c[nH]cn2)cc1	10.1021/jm000971p
	CHEMBL1180120	11412	None	1	Guinea pig	Functional	pKd	=	4.6	4.6	-	0	Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum	ChEMBL	259	6	2	4	2.6	C/C(=N\O)c1ccc(OCCCc2c[nH]cn2)cc1	10.1021/jm000971p
	10492497	12378	None	0	Guinea pig	Functional	pKd	=	4.6	4.6	-	0	Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum	ChEMBL	273	7	2	4	3.0	CC/C(=N\O)c1ccc(OCCCc2c[nH]cn2)cc1	10.1021/jm000971p
	CHEMBL1185539	12378	None	0	Guinea pig	Functional	pKd	=	4.6	4.6	-	0	Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum	ChEMBL	273	7	2	4	3.0	CC/C(=N\O)c1ccc(OCCCc2c[nH]cn2)cc1	10.1021/jm000971p
	CHEMBL420124	12378	None	0	Guinea pig	Functional	pKd	=	4.6	4.6	-	0	Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum	ChEMBL	273	7	2	4	3.0	CC/C(=N\O)c1ccc(OCCCc2c[nH]cn2)cc1	10.1021/jm000971p
	44274554	83325	None	0	Guinea pig	Functional	pKd	=	7.6	7.6	-	0	Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand	ChEMBL	726	17	4	9	7.3	COc1ccc(CN(CCN(C)CCCCCCNC(=O)c2ccc(-c3c4ccc(=N)cc-4oc4cc(N)ccc34)c(C(=O)O)c2)c2ccccn2)cc1	10.1016/s0960-894x(03)00113-6
	CHEMBL21898	83325	None	0	Guinea pig	Functional	pKd	=	7.6	7.6	-	0	Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand	ChEMBL	726	17	4	9	7.3	COc1ccc(CN(CCN(C)CCCCCCNC(=O)c2ccc(-c3c4ccc(=N)cc-4oc4cc(N)ccc34)c(C(=O)O)c2)c2ccccn2)cc1	10.1016/s0960-894x(03)00113-6
	44457689	94202	None	0	Guinea pig	Functional	pKd	=	7.6	7.6	-	0	Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand	ChEMBL	728	17	3	9	7.3	COc1ccc(CN(CCN(C)CCCCCCNC(=O)c2ccc(C(=O)O)c(-c3c4ccc(=O)cc-4oc4cc(O)ccc34)c2)c2ccccn2)cc1	10.1016/s0960-894x(03)00113-6
	CHEMBL24940	94202	None	0	Guinea pig	Functional	pKd	=	7.6	7.6	-	0	Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand	ChEMBL	728	17	3	9	7.3	COc1ccc(CN(CCN(C)CCCCCCNC(=O)c2ccc(C(=O)O)c(-c3c4ccc(=O)cc-4oc4cc(O)ccc34)c2)c2ccccn2)cc1	10.1016/s0960-894x(03)00113-6
	14660350	201899	None	0	Guinea pig	Functional	pKd	=	6.6	6.6	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	392	10	3	4	2.9	COc1ccc(C(CC/N=C(\N)NCCCc2c[nH]cn2)c2ccccn2)cc1	10.1021/jm00128a045
	CHEMBL59138	201899	None	0	Guinea pig	Functional	pKd	=	6.6	6.6	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	392	10	3	4	2.9	COc1ccc(C(CC/N=C(\N)NCCCc2c[nH]cn2)c2ccccn2)cc1	10.1021/jm00128a045
	164435	207000	None	22	Guinea pig	Functional	pKd	=	4.6	4.6	-	0	Histamine H1 receptor antagonistic activity on the isolated guinea pig ileum determined by Schild plot.Histamine H1 receptor antagonistic activity on the isolated guinea pig ileum determined by Schild plot.	ChEMBL	477	11	4	6	2.5	N#CN/C(=N\CCNC(=O)c1ccc(N)cc1)NCCCOc1cccc(CN2CCCCC2)c1	10.1021/jm00090a013
	CHEMBL72844	207000	None	22	Guinea pig	Functional	pKd	=	4.6	4.6	-	0	Histamine H1 receptor antagonistic activity on the isolated guinea pig ileum determined by Schild plot.Histamine H1 receptor antagonistic activity on the isolated guinea pig ileum determined by Schild plot.	ChEMBL	477	11	4	6	2.5	N#CN/C(=N\CCNC(=O)c1ccc(N)cc1)NCCCOc1cccc(CN2CCCCC2)c1	10.1021/jm00090a013
	3081064	202891	None	8	Guinea pig	Functional	pKd	=	6.6	6.6	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	398	9	4	3	3.4	N=C(NCCCc1c[nH]cn1)NCCC(c1cc(F)cc(F)c1)c1ccccn1	10.1021/jm00128a045
	CHEMBL59832	202891	None	8	Guinea pig	Functional	pKd	=	6.6	6.6	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	398	9	4	3	3.4	N=C(NCCCc1c[nH]cn1)NCCC(c1cc(F)cc(F)c1)c1ccccn1	10.1021/jm00128a045
	14660355	100599	None	0	Guinea pig	Functional	pKd	=	6.6	6.6	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	430	9	4	3	4.1	N=C(NCCCc1c[nH]cn1)NCCC(c1ccc(C(F)(F)F)cc1)c1ccccn1	10.1021/jm00128a045
	CHEMBL291396	100599	None	0	Guinea pig	Functional	pKd	=	6.6	6.6	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	430	9	4	3	4.1	N=C(NCCCc1c[nH]cn1)NCCC(c1ccc(C(F)(F)F)cc1)c1ccccn1	10.1021/jm00128a045
	14660372	201687	None	0	Guinea pig	Functional	pKd	=	6.5	6.5	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	430	9	4	3	4.4	N=C(NCCCc1c[nH]cn1)NCCC(c1ccccn1)c1ccc(Cl)cc1Cl	10.1021/jm00128a045
	CHEMBL58999	201687	None	0	Guinea pig	Functional	pKd	=	6.5	6.5	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	430	9	4	3	4.4	N=C(NCCCc1c[nH]cn1)NCCC(c1ccccn1)c1ccc(Cl)cc1Cl	10.1021/jm00128a045
	11741669	96806	None	0	Guinea pig	Functional	pKd	=	8.5	8.5	39	2	Apparent pA2 value of compound at 10 nM concentration of mepyramine in guinea pig ileumApparent pA2 value of compound at 10 nM concentration of mepyramine in guinea pig ileum	ChEMBL	399	11	3	3	4.3	c1ccc(C(CCc2nc(CCNCCc3cnc[nH]3)c[nH]2)c2ccccc2)cc1	10.1021/jm0309147
	CHEMBL264491	96806	None	0	Guinea pig	Functional	pKd	=	8.5	8.5	39	2	Apparent pA2 value of compound at 10 nM concentration of mepyramine in guinea pig ileumApparent pA2 value of compound at 10 nM concentration of mepyramine in guinea pig ileum	ChEMBL	399	11	3	3	4.3	c1ccc(C(CCc2nc(CCNCCc3cnc[nH]3)c[nH]2)c2ccccc2)cc1	10.1021/jm0309147
	11269875	121068	None	0	Guinea pig	Functional	pKd	=	8.5	8.5	-	1	Apparent pA2 value of compound at 10 nM concentration of mepyramine in guinea pig ileumApparent pA2 value of compound at 10 nM concentration of mepyramine in guinea pig ileum	ChEMBL	410	11	2	3	4.9	c1ccc(C(CCc2nc(CCNCCc3cccnc3)c[nH]2)c2ccccc2)cc1	10.1021/jm0309147
	CHEMBL356449	121068	None	0	Guinea pig	Functional	pKd	=	8.5	8.5	-	1	Apparent pA2 value of compound at 10 nM concentration of mepyramine in guinea pig ileumApparent pA2 value of compound at 10 nM concentration of mepyramine in guinea pig ileum	ChEMBL	410	11	2	3	4.9	c1ccc(C(CCc2nc(CCNCCc3cccnc3)c[nH]2)c2ccccc2)cc1	10.1021/jm0309147
	44274585	82334	None	0	Guinea pig	Functional	pKd	=	8.5	8.5	-	0	Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand	ChEMBL	756	19	3	9	8.1	COc1ccc(CN(CCN(C)CCCCCCCCNC(=O)c2ccc(-c3c4ccc(=O)cc-4oc4cc(O)ccc34)c(C(=O)O)c2)c2ccccn2)cc1	10.1016/s0960-894x(03)00113-6
	CHEMBL21721	82334	None	0	Guinea pig	Functional	pKd	=	8.5	8.5	-	0	Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand	ChEMBL	756	19	3	9	8.1	COc1ccc(CN(CCN(C)CCCCCCCCNC(=O)c2ccc(-c3c4ccc(=O)cc-4oc4cc(O)ccc34)c(C(=O)O)c2)c2ccccn2)cc1	10.1016/s0960-894x(03)00113-6
	25190134	161238	None	0	Human	Functional	pKd	=	8.4	8.4	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	404	9	0	5	3.9	CCCCc1cc(OC2CCN(CCS(=O)(=O)CC)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	CHEMBL4085417	161238	None	0	Human	Functional	pKd	=	8.4	8.4	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	404	9	0	5	3.9	CCCCc1cc(OC2CCN(CCS(=O)(=O)CC)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	CHEMBL4117296	161238	None	0	Human	Functional	pKd	=	8.4	8.4	-	0	Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR methodAntagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method	ChEMBL	404	9	0	5	3.9	CCCCc1cc(OC2CCN(CCS(=O)(=O)CC)CC2)c2ncccc2c1	10.1016/j.bmcl.2017.09.020
	2247	505	None	55	Guinea pig	Functional	pKd	=	8.4	8.4	-	42	Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	10.1016/j.bmcl.2011.09.001
	249	505	None	55	Guinea pig	Functional	pKd	=	8.4	8.4	-	42	Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	10.1016/j.bmcl.2011.09.001
	2603	505	None	55	Guinea pig	Functional	pKd	=	8.4	8.4	-	42	Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	10.1016/j.bmcl.2011.09.001
	CHEMBL296419	505	None	55	Guinea pig	Functional	pKd	=	8.4	8.4	-	42	Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	10.1016/j.bmcl.2011.09.001
	DB00637	505	None	55	Guinea pig	Functional	pKd	=	8.4	8.4	-	42	Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	10.1016/j.bmcl.2011.09.001
	57393730	67906	None	0	Guinea pig	Functional	pKd	=	8.4	8.4	-	0	Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins	ChEMBL	579	8	2	6	5.0	O=C(c1cc2ccccc2[nH]1)N1CCN(CCN2CCC(Nc3nc4ccccc4n3Cc3ccc(F)cc3)CC2)CC1	10.1016/j.bmcl.2011.09.001
	CHEMBL1910386	67906	None	0	Guinea pig	Functional	pKd	=	8.4	8.4	-	0	Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins	ChEMBL	579	8	2	6	5.0	O=C(c1cc2ccccc2[nH]1)N1CCN(CCN2CCC(Nc3nc4ccccc4n3Cc3ccc(F)cc3)CC2)CC1	10.1016/j.bmcl.2011.09.001
	71456361	80510	None	0	Human	Functional	pKd	=	8.4	8.4	-	0	Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay	ChEMBL	369	4	0	6	2.5	CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2nccnc2c1=O	10.1016/j.bmc.2012.08.032
	CHEMBL2146812	80510	None	0	Human	Functional	pKd	=	8.4	8.4	-	0	Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assayAntagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay	ChEMBL	369	4	0	6	2.5	CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2nccnc2c1=O	10.1016/j.bmc.2012.08.032
	24803639	61351	None	0	Human	Functional	pKd	=	8.4	8.4	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assay	ChEMBL	622	14	1	7	6.8	O=c1c2ccccc2c(Cc2ccc(O)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1	10.1021/jm1013874
	CHEMBL1767166	61351	None	0	Human	Functional	pKd	=	8.4	8.4	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assay	ChEMBL	622	14	1	7	6.8	O=c1c2ccccc2c(Cc2ccc(O)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1	10.1021/jm1013874
	13676696	164168	None	0	Guinea pig	Functional	pKd	=	8.4	8.4	-	0	H1-antihistamine activity in guinea pig ileumH1-antihistamine activity in guinea pig ileum	ChEMBL	467	7	1	8	4.0	Cc1c(OCCCN2CCN(Cc3cccc(Cl)c3)CC2)ccc2c(O)c3nnnc-3oc12	10.1021/jm00161a022
	CHEMBL420934	164168	None	0	Guinea pig	Functional	pKd	=	8.4	8.4	-	0	H1-antihistamine activity in guinea pig ileumH1-antihistamine activity in guinea pig ileum	ChEMBL	467	7	1	8	4.0	Cc1c(OCCCN2CCN(Cc3cccc(Cl)c3)CC2)ccc2c(O)c3nnnc-3oc12	10.1021/jm00161a022
	13676697	207252	None	0	Guinea pig	Functional	pKd	=	8.4	8.4	-	0	H1-antihistamine activity in guinea pig ileumH1-antihistamine activity in guinea pig ileum	ChEMBL	467	7	1	8	4.0	Cc1c(OCCCN2CCN(Cc3ccccc3Cl)CC2)ccc2c(O)c3nnnc-3oc12	10.1021/jm00161a022
	CHEMBL74989	207252	None	0	Guinea pig	Functional	pKd	=	8.4	8.4	-	0	H1-antihistamine activity in guinea pig ileumH1-antihistamine activity in guinea pig ileum	ChEMBL	467	7	1	8	4.0	Cc1c(OCCCN2CCN(Cc3ccccc3Cl)CC2)ccc2c(O)c3nnnc-3oc12	10.1021/jm00161a022
	54710795	99951	None	0	Guinea pig	Functional	pKd	=	8.4	8.4	-	0	H1-antihistamine activity on guinea pig ileumH1-antihistamine activity on guinea pig ileum	ChEMBL	531	10	2	9	3.6	CCCc1c(OCC(O)CN2CCN(Cc3ccc(Cl)cc3)CC2)ccc2c(O)c([N+](=O)[O-])c(=O)oc12	10.1021/jm00377a013
	CHEMBL286017	99951	None	0	Guinea pig	Functional	pKd	=	8.4	8.4	-	0	H1-antihistamine activity on guinea pig ileumH1-antihistamine activity on guinea pig ileum	ChEMBL	531	10	2	9	3.6	CCCc1c(OCC(O)CN2CCN(Cc3ccc(Cl)cc3)CC2)ccc2c(O)c([N+](=O)[O-])c(=O)oc12	10.1021/jm00377a013
	42625223	180031	None	0	Guinea pig	Functional	pKd	=	5.5	5.5	-	3	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractions	ChEMBL	395	8	4	3	1.4	CN(CCC(=O)/N=C(\N)NCCCc1c[nH]cn1)C(=O)c1cc2ccccc2[nH]1	10.1021/jm9000693
	CHEMBL474617	180031	None	0	Guinea pig	Functional	pKd	=	5.5	5.5	-	3	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractions	ChEMBL	395	8	4	3	1.4	CN(CCC(=O)/N=C(\N)NCCCc1c[nH]cn1)C(=O)c1cc2ccccc2[nH]1	10.1021/jm9000693
	44274584	80715	None	0	Guinea pig	Functional	pKd	=	7.5	7.5	-	0	Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand	ChEMBL	700	15	3	9	6.5	COc1ccc(CN(CCN(C)CCCCNC(=O)c2ccc(C(=O)O)c(-c3c4ccc(=O)cc-4oc4cc(O)ccc34)c2)c2ccccn2)cc1	10.1016/s0960-894x(03)00113-6
	CHEMBL21514	80715	None	0	Guinea pig	Functional	pKd	=	7.5	7.5	-	0	Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand	ChEMBL	700	15	3	9	6.5	COc1ccc(CN(CCN(C)CCCCNC(=O)c2ccc(C(=O)O)c(-c3c4ccc(=O)cc-4oc4cc(O)ccc34)c2)c2ccccn2)cc1	10.1016/s0960-894x(03)00113-6
	44274555	77036	None	0	Guinea pig	Functional	pKd	=	7.5	7.5	-	0	Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand	ChEMBL	782	18	1	9	6.0	COc1ccc(CN(CCN(C)CCCCCCNC(=O)c2ccc(-c3c4ccc(=[N+](C)C)cc-4oc4cc(N(C)C)ccc34)c(C(=O)[O-])c2)c2ccccn2)cc1	10.1016/s0960-894x(03)00113-6
	CHEMBL20713	77036	None	0	Guinea pig	Functional	pKd	=	7.5	7.5	-	0	Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand	ChEMBL	782	18	1	9	6.0	COc1ccc(CN(CCN(C)CCCCCCNC(=O)c2ccc(-c3c4ccc(=[N+](C)C)cc-4oc4cc(N(C)C)ccc34)c(C(=O)[O-])c2)c2ccccn2)cc1	10.1016/s0960-894x(03)00113-6
	14660378	100701	None	0	Guinea pig	Functional	pKd	=	5.5	5.5	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	348	8	4	3	2.7	N=C(NCCCc1c[nH]cn1)NCC(c1ccccc1)c1ccccn1	10.1021/jm00128a045
	CHEMBL292170	100701	None	0	Guinea pig	Functional	pKd	=	5.5	5.5	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	348	8	4	3	2.7	N=C(NCCCc1c[nH]cn1)NCC(c1ccccc1)c1ccccn1	10.1021/jm00128a045
	1226	2019	None	19	Guinea pig	Functional	pKd	=	5.5	5.5	-	1	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity	ChEMBL	321	9	4	4	1.2	NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C	10.1021/jm800841w
	41376	2019	None	19	Guinea pig	Functional	pKd	=	5.5	5.5	-	1	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity	ChEMBL	321	9	4	4	1.2	NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C	10.1021/jm800841w
	CHEMBL12608	2019	None	19	Guinea pig	Functional	pKd	=	5.5	5.5	-	1	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity	ChEMBL	321	9	4	4	1.2	NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C	10.1021/jm800841w
	14660384	205190	None	0	Guinea pig	Functional	pKd	=	7.5	7.5	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	379	9	4	2	3.8	N=C(NCCCc1c[nH]cn1)NCCC(c1ccccc1)c1ccc(F)cc1	10.1021/jm00128a045
	CHEMBL61852	205190	None	0	Guinea pig	Functional	pKd	=	7.5	7.5	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	379	9	4	2	3.8	N=C(NCCCc1c[nH]cn1)NCCC(c1ccccc1)c1ccc(F)cc1	10.1021/jm00128a045
	14660395	205238	None	0	Guinea pig	Functional	pKd	=	6.5	6.5	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	378	8	4	3	3.1	N=C(NC/C=C(\c1ccc(F)cc1)c1ccccn1)NCCCc1c[nH]cn1	10.1021/jm00128a045
	CHEMBL62147	205238	None	0	Guinea pig	Functional	pKd	=	6.5	6.5	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	378	8	4	3	3.1	N=C(NC/C=C(\c1ccc(F)cc1)c1ccccn1)NCCCc1c[nH]cn1	10.1021/jm00128a045
	42625386	178458	None	0	Guinea pig	Functional	pKd	=	5.5	5.5	-	4	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractions	ChEMBL	237	6	3	2	0.6	CCCC(=O)/N=C(\N)NCCCc1c[nH]cn1	10.1021/jm9000693
	CHEMBL465170	178458	None	0	Guinea pig	Functional	pKd	=	5.5	5.5	-	4	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractions	ChEMBL	237	6	3	2	0.6	CCCC(=O)/N=C(\N)NCCCc1c[nH]cn1	10.1021/jm9000693
	44274553	82431	None	0	Guinea pig	Functional	pKd	=	7.4	7.4	-	0	Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand	ChEMBL	828	17	3	9	9.7	COc1ccc(CN(CCN(C)CCCCCCNC(=O)c2ccc(-c3c4ccc5cc(O)ccc5c4oc4c3ccc3cc(=O)ccc34)c(C(=O)O)c2)c2ccccn2)cc1	10.1016/s0960-894x(03)00113-6
	CHEMBL21727	82431	None	0	Guinea pig	Functional	pKd	=	7.4	7.4	-	0	Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand	ChEMBL	828	17	3	9	9.7	COc1ccc(CN(CCN(C)CCCCCCNC(=O)c2ccc(-c3c4ccc5cc(O)ccc5c4oc4c3ccc3cc(=O)ccc34)c(C(=O)O)c2)c2ccccn2)cc1	10.1016/s0960-894x(03)00113-6
	14660382	201116	None	0	Guinea pig	Functional	pKd	=	7.4	7.4	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	380	9	4	3	3.2	N=C(NCCCc1c[nH]cn1)NCCC(c1ccncc1)c1ccc(F)cc1	10.1021/jm00128a045
	CHEMBL57933	201116	None	0	Guinea pig	Functional	pKd	=	7.4	7.4	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	380	9	4	3	3.2	N=C(NCCCc1c[nH]cn1)NCCC(c1ccncc1)c1ccc(F)cc1	10.1021/jm00128a045
	1199	2976	None	0	Guinea pig	Functional	pKd	=	5.4	5.4	-	0	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity	ChEMBL	394	8	3	4	2.5	NC(=NCCCc1[nH]cnc1)NC(=O)CC(c1ccccn1)c1ccc(cc1)F	10.1021/jm800841w
	25149244	2976	None	0	Guinea pig	Functional	pKd	=	5.4	5.4	-	0	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity	ChEMBL	394	8	3	4	2.5	NC(=NCCCc1[nH]cnc1)NC(=O)CC(c1ccccn1)c1ccc(cc1)F	10.1021/jm800841w
	CHEMBL472273	2976	None	0	Guinea pig	Functional	pKd	=	5.4	5.4	-	0	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity	ChEMBL	394	8	3	4	2.5	NC(=NCCCc1[nH]cnc1)NC(=O)CC(c1ccccn1)c1ccc(cc1)F	10.1021/jm800841w
	42626109	179874	None	0	Guinea pig	Functional	pKd	=	7.4	7.4	-	2	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractions	ChEMBL	324	6	4	2	1.5	N/C(=N\C(=O)Cc1c[nH]c2ccccc12)NCCCc1c[nH]cn1	10.1021/jm9000693
	CHEMBL474447	179874	None	0	Guinea pig	Functional	pKd	=	7.4	7.4	-	2	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractions	ChEMBL	324	6	4	2	1.5	N/C(=N\C(=O)Cc1c[nH]c2ccccc12)NCCCc1c[nH]cn1	10.1021/jm9000693
	14660376	205025	None	0	Guinea pig	Functional	pKd	=	6.4	6.4	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	363	9	4	4	2.5	N=C(NCCCc1c[nH]cn1)NCCC(c1ccccn1)c1ccccn1	10.1021/jm00128a045
	CHEMBL61185	205025	None	0	Guinea pig	Functional	pKd	=	6.4	6.4	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	363	9	4	4	2.5	N=C(NCCCc1c[nH]cn1)NCCC(c1ccccn1)c1ccccn1	10.1021/jm00128a045
	2861590	107316	None	5	Guinea pig	Functional	pKd	=	7.4	7.4	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	342	5	0	3	3.0	CN(C)CCCN1C(=O)CSC1c1ccc(Br)cc1	10.1021/jm00093a025
	CHEMBL1202937	107316	None	5	Guinea pig	Functional	pKd	=	7.4	7.4	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	342	5	0	3	3.0	CN(C)CCCN1C(=O)CSC1c1ccc(Br)cc1	10.1021/jm00093a025
	CHEMBL316951	107316	None	5	Guinea pig	Functional	pKd	=	7.4	7.4	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	342	5	0	3	3.0	CN(C)CCCN1C(=O)CSC1c1ccc(Br)cc1	10.1021/jm00093a025
	126624	210749	None	5	Guinea pig	Functional	pKd	=	7.4	7.4	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	264	5	0	3	2.2	CN(C)CCCN1C(=O)CSC1c1ccccc1	10.1021/jm00093a025
	CHEMBL1202936	210749	None	5	Guinea pig	Functional	pKd	=	7.4	7.4	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	264	5	0	3	2.2	CN(C)CCCN1C(=O)CSC1c1ccccc1	10.1021/jm00093a025
	CHEMBL98989	210749	None	5	Guinea pig	Functional	pKd	=	7.4	7.4	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	264	5	0	3	2.2	CN(C)CCCN1C(=O)CSC1c1ccccc1	10.1021/jm00093a025
	42625221	189697	None	0	Guinea pig	Functional	pKd	=	6.4	6.4	-	2	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractions	ChEMBL	338	7	4	2	1.9	N/C(=N\C(=O)CCc1c[nH]c2ccccc12)NCCCc1c[nH]cn1	10.1021/jm9000693
	CHEMBL514641	189697	None	0	Guinea pig	Functional	pKd	=	6.4	6.4	-	2	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractions	ChEMBL	338	7	4	2	1.9	N/C(=N\C(=O)CCc1c[nH]c2ccccc12)NCCCc1c[nH]cn1	10.1021/jm9000693
	14984033	210637	None	0	Guinea pig	Functional	pKd	=	6.4	6.4	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	294	6	0	4	2.2	COc1cccc(C2SCC(=O)N2CCCN(C)C)c1	10.1021/jm00093a025
	CHEMBL1202941	210637	None	0	Guinea pig	Functional	pKd	=	6.4	6.4	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	294	6	0	4	2.2	COc1cccc(C2SCC(=O)N2CCCN(C)C)c1	10.1021/jm00093a025
	CHEMBL98334	210637	None	0	Guinea pig	Functional	pKd	=	6.4	6.4	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	294	6	0	4	2.2	COc1cccc(C2SCC(=O)N2CCCN(C)C)c1	10.1021/jm00093a025
	14984032	210800	None	0	Guinea pig	Functional	pKd	=	6.4	6.4	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	342	5	0	3	3.0	CN(C)CCCN1C(=O)CSC1c1cccc(Br)c1	10.1021/jm00093a025
	CHEMBL1202932	210800	None	0	Guinea pig	Functional	pKd	=	6.4	6.4	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	342	5	0	3	3.0	CN(C)CCCN1C(=O)CSC1c1cccc(Br)c1	10.1021/jm00093a025
	CHEMBL99350	210800	None	0	Guinea pig	Functional	pKd	=	6.4	6.4	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	342	5	0	3	3.0	CN(C)CCCN1C(=O)CSC1c1cccc(Br)c1	10.1021/jm00093a025
	14984031	210832	None	0	Guinea pig	Functional	pKd	=	6.4	6.4	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	282	5	0	3	2.4	CN(C)CCCN1C(=O)CSC1c1cccc(F)c1	10.1021/jm00093a025
	CHEMBL1202933	210832	None	0	Guinea pig	Functional	pKd	=	6.4	6.4	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	282	5	0	3	2.4	CN(C)CCCN1C(=O)CSC1c1cccc(F)c1	10.1021/jm00093a025
	CHEMBL99529	210832	None	0	Guinea pig	Functional	pKd	=	6.4	6.4	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	282	5	0	3	2.4	CN(C)CCCN1C(=O)CSC1c1cccc(F)c1	10.1021/jm00093a025
	2861786	210636	None	5	Guinea pig	Functional	pKd	=	5.4	5.4	-	0	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	309	6	0	5	2.1	CN(C)CCCN1C(=O)CSC1c1cccc([N+](=O)[O-])c1	10.1021/jm00093a025
	CHEMBL1202940	210636	None	5	Guinea pig	Functional	pKd	=	5.4	5.4	-	0	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	309	6	0	5	2.1	CN(C)CCCN1C(=O)CSC1c1cccc([N+](=O)[O-])c1	10.1021/jm00093a025
	CHEMBL98333	210636	None	5	Guinea pig	Functional	pKd	=	5.4	5.4	-	0	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	309	6	0	5	2.1	CN(C)CCCN1C(=O)CSC1c1cccc([N+](=O)[O-])c1	10.1021/jm00093a025
	10364258	45783	None	0	Guinea pig	Functional	pKd	=	8.4	8.4	12	2	Apparent pA2 value of compound at 10 nM concentration of mepyramine in guinea pig ileumApparent pA2 value of compound at 10 nM concentration of mepyramine in guinea pig ileum	ChEMBL	410	11	2	3	4.9	c1ccc(C(CCc2nc(CCNCCc3ccccn3)c[nH]2)c2ccccc2)cc1	10.1021/jm0309147
	CHEMBL153067	45783	None	0	Guinea pig	Functional	pKd	=	8.4	8.4	12	2	Apparent pA2 value of compound at 10 nM concentration of mepyramine in guinea pig ileumApparent pA2 value of compound at 10 nM concentration of mepyramine in guinea pig ileum	ChEMBL	410	11	2	3	4.9	c1ccc(C(CCc2nc(CCNCCc3ccccn3)c[nH]2)c2ccccc2)cc1	10.1021/jm0309147
	44274569	80872	None	0	Guinea pig	Functional	pKd	=	8.4	8.4	-	0	Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand	ChEMBL	700	15	3	9	6.5	COc1ccc(CN(CCN(C)CCCCNC(=O)c2ccc(-c3c4ccc(=O)cc-4oc4cc(O)ccc34)c(C(=O)O)c2)c2ccccn2)cc1	10.1016/s0960-894x(03)00113-6
	CHEMBL21525	80872	None	0	Guinea pig	Functional	pKd	=	8.4	8.4	-	0	Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand	ChEMBL	700	15	3	9	6.5	COc1ccc(CN(CCN(C)CCCCNC(=O)c2ccc(-c3c4ccc(=O)cc-4oc4cc(O)ccc34)c(C(=O)O)c2)c2ccccn2)cc1	10.1016/s0960-894x(03)00113-6
	44274548	99240	None	0	Guinea pig	Functional	pKd	=	8.3	8.3	-	0	Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand	ChEMBL	477	12	1	10	3.6	COc1ccc(CN(CCN(C)CCNc2ccc([N+](=O)[O-])c3nonc23)c2ccccn2)cc1	10.1016/s0960-894x(03)00113-6
	CHEMBL281365	99240	None	0	Guinea pig	Functional	pKd	=	8.3	8.3	-	0	Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand	ChEMBL	477	12	1	10	3.6	COc1ccc(CN(CCN(C)CCNc2ccc([N+](=O)[O-])c3nonc23)c2ccccn2)cc1	10.1016/s0960-894x(03)00113-6
	57402472	67901	None	0	Guinea pig	Functional	pKd	=	8.3	8.3	-	0	Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins	ChEMBL	526	11	1	6	4.0	COc1ccc(CN(CCN(C)CCN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)c2ccccn2)cc1	10.1016/j.bmcl.2011.09.001
	CHEMBL1910381	67901	None	0	Guinea pig	Functional	pKd	=	8.3	8.3	-	0	Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins	ChEMBL	526	11	1	6	4.0	COc1ccc(CN(CCN(C)CCN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)c2ccccn2)cc1	10.1016/j.bmcl.2011.09.001
	1200	3963	None	2	Guinea pig	Functional	pKd	=	5.4	5.4	-	0	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity	ChEMBL	335	8	4	5	0.7	O=C(NC(=NCCCc1cnc[nH]1)N)CSCc1nc[nH]c1C	10.1021/jm800841w
	25149519	3963	None	2	Guinea pig	Functional	pKd	=	5.4	5.4	-	0	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity	ChEMBL	335	8	4	5	0.7	O=C(NC(=NCCCc1cnc[nH]1)N)CSCc1nc[nH]c1C	10.1021/jm800841w
	CHEMBL513056	3963	None	2	Guinea pig	Functional	pKd	=	5.4	5.4	-	0	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity	ChEMBL	335	8	4	5	0.7	O=C(NC(=NCCCc1cnc[nH]1)N)CSCc1nc[nH]c1C	10.1021/jm800841w
	14660370	163340	None	0	Guinea pig	Functional	pKd	=	7.4	7.4	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	430	9	4	3	4.4	N=C(NCCCc1c[nH]cn1)NCCC(c1cc(Cl)cc(Cl)c1)c1ccccn1	10.1021/jm00128a045
	CHEMBL418508	163340	None	0	Guinea pig	Functional	pKd	=	7.4	7.4	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	430	9	4	3	4.4	N=C(NCCCc1c[nH]cn1)NCCC(c1cc(Cl)cc(Cl)c1)c1ccccn1	10.1021/jm00128a045
	14660363	205135	None	0	Guinea pig	Functional	pKd	=	6.4	6.4	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	380	9	4	3	3.2	N=C(NCCCc1c[nH]cn1)NCCC(c1ccccn1)c1ccccc1F	10.1021/jm00128a045
	CHEMBL61523	205135	None	0	Guinea pig	Functional	pKd	=	6.4	6.4	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	380	9	4	3	3.2	N=C(NCCCc1c[nH]cn1)NCCC(c1ccccn1)c1ccccc1F	10.1021/jm00128a045
	14660411	202170	None	0	Guinea pig	Functional	pKd	=	7.3	7.3	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	368	9	4	4	3.1	N=C(NCCCc1c[nH]cn1)NCCC(c1ccccn1)c1cccs1	10.1021/jm00128a045
	CHEMBL59339	202170	None	0	Guinea pig	Functional	pKd	=	7.3	7.3	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	368	9	4	4	3.1	N=C(NCCCc1c[nH]cn1)NCCC(c1ccccn1)c1cccs1	10.1021/jm00128a045
	14660345	201549	None	0	Guinea pig	Functional	pKd	=	7.3	7.3	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	394	10	4	3	3.6	N=C(NCCCc1c[nH]cn1)NCCCC(c1ccc(F)cc1)c1ccccn1	10.1021/jm00128a045
	CHEMBL58869	201549	None	0	Guinea pig	Functional	pKd	=	7.3	7.3	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	394	10	4	3	3.6	N=C(NCCCc1c[nH]cn1)NCCCC(c1ccc(F)cc1)c1ccccn1	10.1021/jm00128a045
	25149613	179306	None	0	Guinea pig	Functional	pKd	=	5.3	5.3	-	2	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity	ChEMBL	382	8	4	5	2.7	N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1nccs1	10.1021/jm800841w
	CHEMBL472441	179306	None	0	Guinea pig	Functional	pKd	=	5.3	5.3	-	2	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity	ChEMBL	382	8	4	5	2.7	N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1nccs1	10.1021/jm800841w
	25149246	189585	None	0	Guinea pig	Functional	pKd	=	5.3	5.3	-	0	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity	ChEMBL	418	8	4	5	2.9	N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccc(F)c(F)c1)c1nccs1	10.1021/jm800841w
	CHEMBL513755	189585	None	0	Guinea pig	Functional	pKd	=	5.3	5.3	-	0	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity	ChEMBL	418	8	4	5	2.9	N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccc(F)c(F)c1)c1nccs1	10.1021/jm800841w
	54587323	63136	None	0	Guinea pig	Functional	pKd	=	4.3	4.3	-	1	Antagonist activity at histamine H1 receptor in guinea-pig ileumAntagonist activity at histamine H1 receptor in guinea-pig ileum	ChEMBL	277	7	2	3	3.0	O=C(NCCC1=CCCCC1)OCCCc1c[nH]cn1	10.1016/j.bmc.2011.03.046
	CHEMBL1774596	63136	None	0	Guinea pig	Functional	pKd	=	4.3	4.3	-	1	Antagonist activity at histamine H1 receptor in guinea-pig ileumAntagonist activity at histamine H1 receptor in guinea-pig ileum	ChEMBL	277	7	2	3	3.0	O=C(NCCC1=CCCCC1)OCCCc1c[nH]cn1	10.1016/j.bmc.2011.03.046
	CHEMBL1789341	63136	None	0	Guinea pig	Functional	pKd	=	4.3	4.3	-	1	Antagonist activity at histamine H1 receptor in guinea-pig ileumAntagonist activity at histamine H1 receptor in guinea-pig ileum	ChEMBL	277	7	2	3	3.0	O=C(NCCC1=CCCCC1)OCCCc1c[nH]cn1	10.1016/j.bmc.2011.03.046
	134136763	142935	None	0	Human	Functional	pKd	=	8.3	8.3	-	0	Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay	ChEMBL	500	11	0	5	6.0	c1cnc2c(N3CCN(CCCCc4ccc(OCCCN5CCCCCC5)cc4)CC3)cccc2c1	10.1016/j.bmcl.2016.11.022
	CHEMBL3893197	142935	None	0	Human	Functional	pKd	=	8.3	8.3	-	0	Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay	ChEMBL	500	11	0	5	6.0	c1cnc2c(N3CCN(CCCCc4ccc(OCCCN5CCCCCC5)cc4)CC3)cccc2c1	10.1016/j.bmcl.2016.11.022
	54710793	108877	None	0	Guinea pig	Functional	pKd	=	8.3	8.3	-	0	H1-antihistamine activity on guinea pig ileumH1-antihistamine activity on guinea pig ileum	ChEMBL	489	8	2	9	2.6	O=c1oc2cc(OCC(O)CN3CCN(Cc4ccc(Cl)cc4)CC3)ccc2c(O)c1[N+](=O)[O-]	10.1021/jm00377a013
	CHEMBL32097	108877	None	0	Guinea pig	Functional	pKd	=	8.3	8.3	-	0	H1-antihistamine activity on guinea pig ileumH1-antihistamine activity on guinea pig ileum	ChEMBL	489	8	2	9	2.6	O=c1oc2cc(OCC(O)CN3CCN(Cc4ccc(Cl)cc4)CC3)ccc2c(O)c1[N+](=O)[O-]	10.1021/jm00377a013
	44274583	98781	None	0	Guinea pig	Functional	pKd	=	8.3	8.3	-	0	Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand	ChEMBL	756	19	3	9	8.1	COc1ccc(CN(CCN(C)CCCCCCCCNC(=O)c2ccc(C(=O)O)c(-c3c4ccc(=O)cc-4oc4cc(O)ccc34)c2)c2ccccn2)cc1	10.1016/s0960-894x(03)00113-6
	CHEMBL277850	98781	None	0	Guinea pig	Functional	pKd	=	8.3	8.3	-	0	Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand	ChEMBL	756	19	3	9	8.1	COc1ccc(CN(CCN(C)CCCCCCCCNC(=O)c2ccc(C(=O)O)c(-c3c4ccc(=O)cc-4oc4cc(O)ccc34)c2)c2ccccn2)cc1	10.1016/s0960-894x(03)00113-6
	4440380	4256	None	1	Guinea pig	Functional	pKd	=	8.3	8.3	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	278	5	0	3	2.5	Cc1ccc(C2SCC(=O)N2CCCN(C)C)cc1	10.1021/jm00093a025
	CHEMBL100487	4256	None	1	Guinea pig	Functional	pKd	=	8.3	8.3	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	278	5	0	3	2.5	Cc1ccc(C2SCC(=O)N2CCCN(C)C)cc1	10.1021/jm00093a025
	CHEMBL1202938	4256	None	1	Guinea pig	Functional	pKd	=	8.3	8.3	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	278	5	0	3	2.5	Cc1ccc(C2SCC(=O)N2CCCN(C)C)cc1	10.1021/jm00093a025
	11791817	98356	None	0	Guinea pig	Functional	pKd	=	8.2	8.2	-1	2	Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nM	ChEMBL	345	9	2	2	4.5	c1ccc(C(CCc2nc(CCNC3CC3)c[nH]2)c2ccccc2)cc1	10.1021/jm991056a
	CHEMBL274831	98356	None	0	Guinea pig	Functional	pKd	=	8.2	8.2	-1	2	Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nM	ChEMBL	345	9	2	2	4.5	c1ccc(C(CCc2nc(CCNC3CC3)c[nH]2)c2ccccc2)cc1	10.1021/jm991056a
	10083274	11398	None	0	Guinea pig	Functional	pKd	=	4.3	4.3	-	0	Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum	ChEMBL	246	6	2	3	2.5	CC(O)c1ccc(OCCCc2c[nH]cn2)cc1	10.1021/jm000971p
	CHEMBL112676	11398	None	0	Guinea pig	Functional	pKd	=	4.3	4.3	-	0	Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum	ChEMBL	246	6	2	3	2.5	CC(O)c1ccc(OCCCc2c[nH]cn2)cc1	10.1021/jm000971p
	CHEMBL1180069	11398	None	0	Guinea pig	Functional	pKd	=	4.3	4.3	-	0	Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum	ChEMBL	246	6	2	3	2.5	CC(O)c1ccc(OCCCc2c[nH]cn2)cc1	10.1021/jm000971p
	14660365	202443	None	0	Guinea pig	Functional	pKd	=	6.3	6.3	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	396	9	4	3	3.7	N=C(NCCCc1c[nH]cn1)NCCC(c1ccccn1)c1ccccc1Cl	10.1021/jm00128a045
	CHEMBL59521	202443	None	0	Guinea pig	Functional	pKd	=	6.3	6.3	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	396	9	4	3	3.7	N=C(NCCCc1c[nH]cn1)NCCC(c1ccccn1)c1ccccc1Cl	10.1021/jm00128a045
	42625303	180872	None	0	Guinea pig	Functional	pKd	=	5.3	5.3	-	6	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractions	ChEMBL	223	5	3	2	0.2	CCC(=O)/N=C(\N)NCCCc1c[nH]cn1	10.1021/jm9000693
	CHEMBL475621	180872	None	0	Guinea pig	Functional	pKd	=	5.3	5.3	-	6	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractions	ChEMBL	223	5	3	2	0.2	CCC(=O)/N=C(\N)NCCCc1c[nH]cn1	10.1021/jm9000693
	25149431	185543	None	0	Guinea pig	Functional	pKd	=	5.3	5.3	-	0	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity	ChEMBL	277	5	4	3	1.6	N=C(NCCCc1c[nH]cn1)NC(=O)C1CCCCC1	10.1021/jm800841w
	CHEMBL486153	185543	None	0	Guinea pig	Functional	pKd	=	5.3	5.3	-	0	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity	ChEMBL	277	5	4	3	1.6	N=C(NCCCc1c[nH]cn1)NC(=O)C1CCCCC1	10.1021/jm800841w
	14660361	203959	None	0	Guinea pig	Functional	pKd	=	6.3	6.3	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	430	9	4	3	4.1	N=C(NCCCc1c[nH]cn1)NCCC(c1cccc(C(F)(F)F)c1)c1ccccn1	10.1021/jm00128a045
	CHEMBL60515	203959	None	0	Guinea pig	Functional	pKd	=	6.3	6.3	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	430	9	4	3	4.1	N=C(NCCCc1c[nH]cn1)NCCC(c1cccc(C(F)(F)F)c1)c1ccccn1	10.1021/jm00128a045
	25149811	186068	None	0	Guinea pig	Functional	pKd	=	6.3	6.3	-	0	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity	ChEMBL	327	9	4	3	2.4	N=C(NCCCc1c[nH]cn1)NC(=O)CCCCc1ccccc1	10.1021/jm800841w
	CHEMBL486963	186068	None	0	Guinea pig	Functional	pKd	=	6.3	6.3	-	0	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity	ChEMBL	327	9	4	3	2.4	N=C(NCCCc1c[nH]cn1)NC(=O)CCCCc1ccccc1	10.1021/jm800841w
	25149425	188312	None	0	Guinea pig	Functional	pKd	=	6.2	6.2	-	0	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity	ChEMBL	285	6	4	3	1.2	N=C(NCCCc1c[nH]cn1)NC(=O)Cc1ccccc1	10.1021/jm800841w
	CHEMBL499092	188312	None	0	Guinea pig	Functional	pKd	=	6.2	6.2	-	0	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity	ChEMBL	285	6	4	3	1.2	N=C(NCCCc1c[nH]cn1)NC(=O)Cc1ccccc1	10.1021/jm800841w
	10410901	119811	None	0	Rat	Functional	pKd	=	8.2	8.2	-23	2	Apparent pA2 value of compound at 50 nM concentration of mepyramine in rat aortaApparent pA2 value of compound at 50 nM concentration of mepyramine in rat aorta	ChEMBL	438	13	2	3	5.7	c1ccc(C(CCc2nc(CCNCCCCc3ccccn3)c[nH]2)c2ccccc2)cc1	10.1021/jm0309147
	CHEMBL347796	119811	None	0	Rat	Functional	pKd	=	8.2	8.2	-23	2	Apparent pA2 value of compound at 50 nM concentration of mepyramine in rat aortaApparent pA2 value of compound at 50 nM concentration of mepyramine in rat aorta	ChEMBL	438	13	2	3	5.7	c1ccc(C(CCc2nc(CCNCCCCc3ccccn3)c[nH]2)c2ccccc2)cc1	10.1021/jm0309147
	23582308	145952	None	0	Human	Functional	pKd	=	8.2	8.2	-	0	Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay	ChEMBL	634	14	1	6	6.9	O=C(O)CCc1ccc2cc(Cc3ccccc3)cc(N3CCN(CCc4ccc(OCCCN5CCCCCC5)cc4)CC3)c2n1	10.1016/j.bmcl.2016.11.022
	CHEMBL3917428	145952	None	0	Human	Functional	pKd	=	8.2	8.2	-	0	Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay	ChEMBL	634	14	1	6	6.9	O=C(O)CCc1ccc2cc(Cc3ccccc3)cc(N3CCN(CCc4ccc(OCCCN5CCCCCC5)cc4)CC3)c2n1	10.1016/j.bmcl.2016.11.022
	153224	205285	None	19	Guinea pig	Functional	pKd	=	8.2	8.2	-	0	Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand	ChEMBL	271	7	1	4	2.3	CNCCN(Cc1ccc(OC)cc1)c1ccccn1	10.1016/s0960-894x(03)00113-6
	CHEMBL624	205285	None	19	Guinea pig	Functional	pKd	=	8.2	8.2	-	0	Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand	ChEMBL	271	7	1	4	2.3	CNCCN(Cc1ccc(OC)cc1)c1ccccn1	10.1016/s0960-894x(03)00113-6
	25149433	186082	None	2	Guinea pig	Functional	pKd	=	5.2	5.2	-	0	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity	ChEMBL	305	7	4	3	2.3	N=C(NCCCc1c[nH]cn1)NC(=O)CCC1CCCCC1	10.1021/jm800841w
	CHEMBL486974	186082	None	2	Guinea pig	Functional	pKd	=	5.2	5.2	-	0	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity	ChEMBL	305	7	4	3	2.3	N=C(NCCCc1c[nH]cn1)NC(=O)CCC1CCCCC1	10.1021/jm800841w
	13676693	103056	None	0	Guinea pig	Functional	pKd	=	7.2	7.2	-	0	Compound was tested for H1-antihistamine activity in guinea pig ileum.Compound was tested for H1-antihistamine activity in guinea pig ileum.	ChEMBL	463	8	1	9	3.3	COc1ccc(CN2CCN(CCCOc3ccc4c(O)c5nnnc-5oc4c3C)CC2)cc1	10.1021/jm00161a022
	CHEMBL306807	103056	None	0	Guinea pig	Functional	pKd	=	7.2	7.2	-	0	Compound was tested for H1-antihistamine activity in guinea pig ileum.Compound was tested for H1-antihistamine activity in guinea pig ileum.	ChEMBL	463	8	1	9	3.3	COc1ccc(CN2CCN(CCCOc3ccc4c(O)c5nnnc-5oc4c3C)CC2)cc1	10.1021/jm00161a022
	2860026	108432	None	5	Guinea pig	Functional	pKd	=	6.2	6.2	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	298	5	0	3	2.9	CN(C)CCCN1C(=O)CSC1c1cccc(Cl)c1	10.1021/jm00093a025
	CHEMBL319829	108432	None	5	Guinea pig	Functional	pKd	=	6.2	6.2	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	298	5	0	3	2.9	CN(C)CCCN1C(=O)CSC1c1cccc(Cl)c1	10.1021/jm00093a025
	2861042	111646	None	6	Guinea pig	Functional	pKd	=	5.2	5.2	-	0	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	309	6	0	5	2.1	CN(C)CCCN1C(=O)CSC1c1ccc([N+](=O)[O-])cc1	10.1021/jm00093a025
	CHEMBL1202943	111646	None	6	Guinea pig	Functional	pKd	=	5.2	5.2	-	0	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	309	6	0	5	2.1	CN(C)CCCN1C(=O)CSC1c1ccc([N+](=O)[O-])cc1	10.1021/jm00093a025
	CHEMBL328201	111646	None	6	Guinea pig	Functional	pKd	=	5.2	5.2	-	0	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	309	6	0	5	2.1	CN(C)CCCN1C(=O)CSC1c1ccc([N+](=O)[O-])cc1	10.1021/jm00093a025
	11356502	11342	None	0	Guinea pig	Functional	pKd	=	4.2	4.2	-	0	Functional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileum	ChEMBL	222	6	1	2	3.3	c1nc(COCCCC2CCCCC2)c[nH]1	10.1021/jm031065q
	CHEMBL1179596	11342	None	0	Guinea pig	Functional	pKd	=	4.2	4.2	-	0	Functional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileum	ChEMBL	222	6	1	2	3.3	c1nc(COCCCC2CCCCC2)c[nH]1	10.1021/jm031065q
	CHEMBL88362	11342	None	0	Guinea pig	Functional	pKd	=	4.2	4.2	-	0	Functional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileum	ChEMBL	222	6	1	2	3.3	c1nc(COCCCC2CCCCC2)c[nH]1	10.1021/jm031065q
	14660412	204663	None	0	Guinea pig	Functional	pKd	=	6.2	6.2	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pigAntagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig	ChEMBL	378	9	4	4	2.6	N/C(=N\CCC(c1ccc(O)cc1)c1ccccn1)NCCCc1c[nH]cn1	10.1021/jm00128a045
	CHEMBL60972	204663	None	0	Guinea pig	Functional	pKd	=	6.2	6.2	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pigAntagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig	ChEMBL	378	9	4	4	2.6	N/C(=N\CCC(c1ccc(O)cc1)c1ccccn1)NCCCc1c[nH]cn1	10.1021/jm00128a045
	44457674	84345	None	0	Guinea pig	Functional	pKd	=	7.2	7.2	-	0	Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand	ChEMBL	672	13	3	9	5.7	COc1ccc(CN(CCN(C)CCNC(=O)c2ccc(-c3c4ccc(=O)cc-4oc4cc(O)ccc34)c(C(=O)O)c2)c2ccccn2)cc1	10.1016/s0960-894x(03)00113-6
	CHEMBL22152	84345	None	0	Guinea pig	Functional	pKd	=	7.2	7.2	-	0	Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand	ChEMBL	672	13	3	9	5.7	COc1ccc(CN(CCN(C)CCNC(=O)c2ccc(-c3c4ccc(=O)cc-4oc4cc(O)ccc34)c(C(=O)O)c2)c2ccccn2)cc1	10.1016/s0960-894x(03)00113-6
	57391869	63140	None	0	Guinea pig	Functional	pKd	=	4.2	4.2	-	1	Antagonist activity at histamine H1 receptor in guinea-pig ileumAntagonist activity at histamine H1 receptor in guinea-pig ileum	ChEMBL	223	6	2	3	1.6	CC=CCNC(=O)OCCCc1c[nH]cn1	10.1016/j.bmc.2011.03.046
	CHEMBL1774589	63140	None	0	Guinea pig	Functional	pKd	=	4.2	4.2	-	1	Antagonist activity at histamine H1 receptor in guinea-pig ileumAntagonist activity at histamine H1 receptor in guinea-pig ileum	ChEMBL	223	6	2	3	1.6	CC=CCNC(=O)OCCCc1c[nH]cn1	10.1016/j.bmc.2011.03.046
	CHEMBL1789349	63140	None	0	Guinea pig	Functional	pKd	=	4.2	4.2	-	1	Antagonist activity at histamine H1 receptor in guinea-pig ileumAntagonist activity at histamine H1 receptor in guinea-pig ileum	ChEMBL	223	6	2	3	1.6	CC=CCNC(=O)OCCCc1c[nH]cn1	10.1016/j.bmc.2011.03.046
	57400700	67900	None	0	Guinea pig	Functional	pKd	=	8.1	8.1	-	0	Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins	ChEMBL	470	8	1	6	3.4	COc1ccc(CN(CCN2CCN(C(=O)c3nc4ccccc4[nH]3)CC2)c2ccccn2)cc1	10.1016/j.bmcl.2011.09.001
	CHEMBL1910380	67900	None	0	Guinea pig	Functional	pKd	=	8.1	8.1	-	0	Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins	ChEMBL	470	8	1	6	3.4	COc1ccc(CN(CCN2CCN(C(=O)c3nc4ccccc4[nH]3)CC2)c2ccccn2)cc1	10.1016/j.bmcl.2011.09.001
	57397301	67902	None	0	Guinea pig	Functional	pKd	=	8.1	8.1	-	0	Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins	ChEMBL	560	11	1	6	4.6	COc1ccc(CN(CCN(C)CCN2CCN(C(=O)c3cc4cc(Cl)ccc4[nH]3)CC2)c2ccccn2)cc1	10.1016/j.bmcl.2011.09.001
	CHEMBL1910382	67902	None	0	Guinea pig	Functional	pKd	=	8.1	8.1	-	0	Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins	ChEMBL	560	11	1	6	4.6	COc1ccc(CN(CCN(C)CCN2CCN(C(=O)c3cc4cc(Cl)ccc4[nH]3)CC2)c2ccccn2)cc1	10.1016/j.bmcl.2011.09.001
	145961372	161701	None	0	Guinea pig	Functional	pKd	=	6.2	6.2	-	1	Antagonist potency at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions at 0.3 to 3 uM after 15 minsAntagonist potency at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions at 0.3 to 3 uM after 15 mins	ChEMBL	311	7	0	2	5.3	c1ccc2c(OCCCCCN3CCCCCC3)cccc2c1	10.1016/j.bmc.2018.04.023
	CHEMBL4129589	161701	None	0	Guinea pig	Functional	pKd	=	6.2	6.2	-	1	Antagonist potency at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions at 0.3 to 3 uM after 15 minsAntagonist potency at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions at 0.3 to 3 uM after 15 mins	ChEMBL	311	7	0	2	5.3	c1ccc2c(OCCCCCN3CCCCCC3)cccc2c1	10.1016/j.bmc.2018.04.023
	2200	20210	None	38	Guinea pig	Functional	pKd	=	7.1	7.1	-	12	Antagonist potency at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions after 15 minsAntagonist potency at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions after 15 mins	ChEMBL	265	5	1	3	2.7	c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1	10.1016/j.bmc.2018.04.023
	2200.0	20210	None	38	Guinea pig	Functional	pKd	=	7.1	7.1	-	12	Antagonist potency at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions after 15 minsAntagonist potency at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions after 15 mins	ChEMBL	265	5	1	3	2.7	c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1	10.1016/j.bmc.2018.04.023
	CHEMBL1256819	20210	None	38	Guinea pig	Functional	pKd	=	7.1	7.1	-	12	Antagonist potency at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions after 15 minsAntagonist potency at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions after 15 mins	ChEMBL	265	5	1	3	2.7	c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1	10.1016/j.bmc.2018.04.023
	CHEMBL1305	20210	None	38	Guinea pig	Functional	pKd	=	7.1	7.1	-	12	Antagonist potency at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions after 15 minsAntagonist potency at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions after 15 mins	ChEMBL	265	5	1	3	2.7	c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1	10.1016/j.bmc.2018.04.023
	DB08799	20210	None	38	Guinea pig	Functional	pKd	=	7.1	7.1	-	12	Antagonist potency at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions after 15 minsAntagonist potency at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions after 15 mins	ChEMBL	265	5	1	3	2.7	c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1	10.1016/j.bmc.2018.04.023
	42625224	180870	None	0	Guinea pig	Functional	pKd	=	6.1	6.1	-	1	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractions	ChEMBL	395	9	5	3	1.5	N/C(=N\C(=O)CCCNC(=O)c1cc2ccccc2[nH]1)NCCCc1c[nH]cn1	10.1021/jm9000693
	CHEMBL475620	180870	None	0	Guinea pig	Functional	pKd	=	6.1	6.1	-	1	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractions	ChEMBL	395	9	5	3	1.5	N/C(=N\C(=O)CCCNC(=O)c1cc2ccccc2[nH]1)NCCCc1c[nH]cn1	10.1021/jm9000693
	25149521	179158	None	0	Guinea pig	Functional	pKd	=	6.1	6.1	-	2	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity	ChEMBL	375	8	4	3	3.2	N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1ccccc1	10.1021/jm800841w
	CHEMBL471413	179158	None	0	Guinea pig	Functional	pKd	=	6.1	6.1	-	2	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity	ChEMBL	375	8	4	3	3.2	N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1ccccc1	10.1021/jm800841w
	25149515	185936	None	0	Guinea pig	Functional	pKd	=	6.1	6.1	-	0	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity	ChEMBL	319	8	4	3	2.7	N=C(NCCCc1c[nH]cn1)NC(=O)CCCC1CCCCC1	10.1021/jm800841w
	CHEMBL486746	185936	None	0	Guinea pig	Functional	pKd	=	6.1	6.1	-	0	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity	ChEMBL	319	8	4	3	2.7	N=C(NCCCc1c[nH]cn1)NC(=O)CCCC1CCCCC1	10.1021/jm800841w
	1219	737	None	0	Guinea pig	Functional	pKd	=	7.1	7.1	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	396	9	3	3	3.5	NC(=NCCCc1[nH]cnc1)NCCC(c1ccccn1)c1ccc(cc1)Cl	10.1021/jm00128a045
	14660352	737	None	0	Guinea pig	Functional	pKd	=	7.1	7.1	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	396	9	3	3	3.5	NC(=NCCCc1[nH]cnc1)NCCC(c1ccccn1)c1ccc(cc1)Cl	10.1021/jm00128a045
	CHEMBL304239	737	None	0	Guinea pig	Functional	pKd	=	7.1	7.1	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	396	9	3	3	3.5	NC(=NCCCc1[nH]cnc1)NCCC(c1ccccn1)c1ccc(cc1)Cl	10.1021/jm00128a045
	42625304	179206	None	0	Guinea pig	Functional	pKd	=	5.1	5.1	-	4	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractions	ChEMBL	237	5	3	2	0.4	CC(C)C(=O)/N=C(\N)NCCCc1c[nH]cn1	10.1021/jm9000693
	CHEMBL471724	179206	None	0	Guinea pig	Functional	pKd	=	5.1	5.1	-	4	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractions	ChEMBL	237	5	3	2	0.4	CC(C)C(=O)/N=C(\N)NCCCc1c[nH]cn1	10.1021/jm9000693
	10094258	201526	None	0	Guinea pig	Functional	pKd	=	7.1	7.1	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	430	9	4	3	4.4	N=C(NCCCc1c[nH]cn1)NCCC(c1ccc(Cl)c(Cl)c1)c1ccccn1	10.1021/jm00128a045
	CHEMBL58740	201526	None	0	Guinea pig	Functional	pKd	=	7.1	7.1	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	430	9	4	3	4.4	N=C(NCCCc1c[nH]cn1)NCCC(c1ccc(Cl)c(Cl)c1)c1ccccn1	10.1021/jm00128a045
	13676703	207063	None	0	Guinea pig	Functional	pKd	=	7.1	7.1	-	0	Compound was tested for H1-antihistamine activity in guinea pig ileum.Compound was tested for H1-antihistamine activity in guinea pig ileum.	ChEMBL	469	10	1	8	4.2	Cc1c(OCCCN(C)CCN(C)Cc2ccc(Cl)cc2)ccc2c(O)c3nnnc-3oc12	10.1021/jm00161a022
	CHEMBL73265	207063	None	0	Guinea pig	Functional	pKd	=	7.1	7.1	-	0	Compound was tested for H1-antihistamine activity in guinea pig ileum.Compound was tested for H1-antihistamine activity in guinea pig ileum.	ChEMBL	469	10	1	8	4.2	Cc1c(OCCCN(C)CCN(C)Cc2ccc(Cl)cc2)ccc2c(O)c3nnnc-3oc12	10.1021/jm00161a022
	2872050	210685	None	2	Guinea pig	Functional	pKd	=	7.1	7.1	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	282	5	0	3	2.4	CN(C)CCCN1C(=O)CSC1c1ccc(F)cc1	10.1021/jm00093a025
	CHEMBL1202939	210685	None	2	Guinea pig	Functional	pKd	=	7.1	7.1	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	282	5	0	3	2.4	CN(C)CCCN1C(=O)CSC1c1ccc(F)cc1	10.1021/jm00093a025
	CHEMBL98605	210685	None	2	Guinea pig	Functional	pKd	=	7.1	7.1	-	1	In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileumIn vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum	ChEMBL	282	5	0	3	2.4	CN(C)CCCN1C(=O)CSC1c1ccc(F)cc1	10.1021/jm00093a025
	11345716	11348	None	0	Guinea pig	Functional	pKd	=	5.1	5.1	-	0	Functional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileum	ChEMBL	250	8	1	2	3.7	c1nc(CCCOCCCC2CCCCC2)c[nH]1	10.1021/jm031065q
	CHEMBL1179627	11348	None	0	Guinea pig	Functional	pKd	=	5.1	5.1	-	0	Functional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileum	ChEMBL	250	8	1	2	3.7	c1nc(CCCOCCCC2CCCCC2)c[nH]1	10.1021/jm031065q
	CHEMBL89999	11348	None	0	Guinea pig	Functional	pKd	=	5.1	5.1	-	0	Functional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileum	ChEMBL	250	8	1	2	3.7	c1nc(CCCOCCCC2CCCCC2)c[nH]1	10.1021/jm031065q
	11413171	12114	None	0	Guinea pig	Functional	pKd	=	5.1	5.1	-	1	Functional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileum	ChEMBL	210	9	1	2	2.9	CCCCCCOCCCc1c[nH]cn1	10.1021/jm031065q
	CHEMBL1184057	12114	None	0	Guinea pig	Functional	pKd	=	5.1	5.1	-	1	Functional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileum	ChEMBL	210	9	1	2	2.9	CCCCCCOCCCc1c[nH]cn1	10.1021/jm031065q
	CHEMBL330688	12114	None	0	Guinea pig	Functional	pKd	=	5.1	5.1	-	1	Functional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileum	ChEMBL	210	9	1	2	2.9	CCCCCCOCCCc1c[nH]cn1	10.1021/jm031065q
	54584376	63188	None	0	Guinea pig	Functional	pKd	=	4.1	4.1	-	1	Antagonist activity at histamine H1 receptor in guinea-pig ileumAntagonist activity at histamine H1 receptor in guinea-pig ileum	ChEMBL	237	7	2	3	2.0	CC/C=C\CNC(=O)OCCCc1c[nH]cn1	10.1016/j.bmc.2011.03.046
	CHEMBL1774592	63188	None	0	Guinea pig	Functional	pKd	=	4.1	4.1	-	1	Antagonist activity at histamine H1 receptor in guinea-pig ileumAntagonist activity at histamine H1 receptor in guinea-pig ileum	ChEMBL	237	7	2	3	2.0	CC/C=C\CNC(=O)OCCCc1c[nH]cn1	10.1016/j.bmc.2011.03.046
	CHEMBL1789809	63188	None	0	Guinea pig	Functional	pKd	=	4.1	4.1	-	1	Antagonist activity at histamine H1 receptor in guinea-pig ileumAntagonist activity at histamine H1 receptor in guinea-pig ileum	ChEMBL	237	7	2	3	2.0	CC/C=C\CNC(=O)OCCCc1c[nH]cn1	10.1016/j.bmc.2011.03.046
	10635074	11408	None	0	Guinea pig	Functional	pKd	=	4.1	4.1	-	0	Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum	ChEMBL	260	6	3	4	1.0	NNC(=O)c1ccc(OCCCc2c[nH]cn2)cc1	10.1021/jm000971p
	CHEMBL113404	11408	None	0	Guinea pig	Functional	pKd	=	4.1	4.1	-	0	Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum	ChEMBL	260	6	3	4	1.0	NNC(=O)c1ccc(OCCCc2c[nH]cn2)cc1	10.1021/jm000971p
	CHEMBL1180094	11408	None	0	Guinea pig	Functional	pKd	=	4.1	4.1	-	0	Histamine H1-receptor activity on isolated guinea pig ileumHistamine H1-receptor activity on isolated guinea pig ileum	ChEMBL	260	6	3	4	1.0	NNC(=O)c1ccc(OCCCc2c[nH]cn2)cc1	10.1021/jm000971p
	57390225	67904	None	0	Guinea pig	Functional	pKd	=	8.1	8.1	-	0	Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins	ChEMBL	469	9	2	5	4.1	COc1ccc(CN(CCN[C@H]2CCN(C(=O)c3cc4ccccc4[nH]3)C2)c2ccccn2)cc1	10.1016/j.bmcl.2011.09.001
	CHEMBL1910384	67904	None	0	Guinea pig	Functional	pKd	=	8.1	8.1	-	0	Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsAntagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins	ChEMBL	469	9	2	5	4.1	COc1ccc(CN(CCN[C@H]2CCN(C(=O)c3cc4ccccc4[nH]3)C2)c2ccccn2)cc1	10.1016/j.bmcl.2011.09.001
	10246247	98346	None	0	Guinea pig	Functional	pKd	=	6.1	6.1	-	0	Relative potency was recorded in endothelium-denuded guinea pig(pre contracted with PGF-2 alpha); value ranges from 5.76 to 6.40Relative potency was recorded in endothelium-denuded guinea pig(pre contracted with PGF-2 alpha); value ranges from 5.76 to 6.40	ChEMBL	333	9	2	2	4.5	NCCc1c[nH]c(CCCCC(c2ccccc2)c2ccccc2)n1	10.1021/jm991056a
	CHEMBL274767	98346	None	0	Guinea pig	Functional	pKd	=	6.1	6.1	-	0	Relative potency was recorded in endothelium-denuded guinea pig(pre contracted with PGF-2 alpha); value ranges from 5.76 to 6.40Relative potency was recorded in endothelium-denuded guinea pig(pre contracted with PGF-2 alpha); value ranges from 5.76 to 6.40	ChEMBL	333	9	2	2	4.5	NCCc1c[nH]c(CCCCC(c2ccccc2)c2ccccc2)n1	10.1021/jm991056a
	3081063	203966	None	18	Guinea pig	Functional	pKd	=	7.1	7.1	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	398	9	4	3	3.4	N=C(NCCCc1c[nH]cn1)NCCC(c1ccc(F)c(F)c1)c1ccccn1	10.1021/jm00128a045
	CHEMBL60519	203966	None	18	Guinea pig	Functional	pKd	=	7.1	7.1	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	398	9	4	3	3.4	N=C(NCCCc1c[nH]cn1)NCCC(c1ccc(F)c(F)c1)c1ccccn1	10.1021/jm00128a045
	14660416	203185	None	1	Guinea pig	Functional	pKd	=	6.1	6.1	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	377	9	4	4	2.4	N/C(=N\CCC(c1cccc(N)c1)c1ccccn1)NCCCc1c[nH]cn1	10.1021/jm00128a045
	CHEMBL60006	203185	None	1	Guinea pig	Functional	pKd	=	6.1	6.1	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	377	9	4	4	2.4	N/C(=N\CCC(c1cccc(N)c1)c1ccccn1)NCCCc1c[nH]cn1	10.1021/jm00128a045
	42625384	169876	None	0	Guinea pig	Functional	pKd	=	5.1	5.1	-	4	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractions	ChEMBL	209	4	3	2	-0.2	CC(=O)/N=C(\N)NCCCc1c[nH]cn1	10.1021/jm9000693
	CHEMBL443896	169876	None	0	Guinea pig	Functional	pKd	=	5.1	5.1	-	4	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractionsAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractions	ChEMBL	209	4	3	2	-0.2	CC(=O)/N=C(\N)NCCCc1c[nH]cn1	10.1021/jm9000693
	14660359	201585	None	0	Guinea pig	Functional	pKd	=	7.1	7.1	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	396	9	4	3	3.7	N=C(NCCCc1c[nH]cn1)NCCC(c1cccc(Cl)c1)c1ccccn1	10.1021/jm00128a045
	CHEMBL58922	201585	None	0	Guinea pig	Functional	pKd	=	7.1	7.1	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	396	9	4	3	3.7	N=C(NCCCc1c[nH]cn1)NCCC(c1cccc(Cl)c1)c1ccccn1	10.1021/jm00128a045
	10447834	1933	None	1	Rat	Functional	pKd	=	8.0	8.0	-2	3	Compound was evaluated for mepyramine antagonism effects in rat aorta (relaxation) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in rat aorta (relaxation) at a mepyramine concentration of 100 nM	ChEMBL	305	7	2	2	3.7	NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm991056a
	4026	1933	None	1	Rat	Functional	pKd	=	8.0	8.0	-2	3	Compound was evaluated for mepyramine antagonism effects in rat aorta (relaxation) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in rat aorta (relaxation) at a mepyramine concentration of 100 nM	ChEMBL	305	7	2	2	3.7	NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm991056a
	CHEMBL275507	1933	None	1	Rat	Functional	pKd	=	8.0	8.0	-2	3	Compound was evaluated for mepyramine antagonism effects in rat aorta (relaxation) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in rat aorta (relaxation) at a mepyramine concentration of 100 nM	ChEMBL	305	7	2	2	3.7	NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm991056a
	10447834	1933	None	1	Rat	Functional	pKd	=	8.0	8.0	-2	3	Maximum response (E max) against Histamine H1 receptor in rat aortaMaximum response (E max) against Histamine H1 receptor in rat aorta	ChEMBL	305	7	2	2	3.7	NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm0309147
	4026	1933	None	1	Rat	Functional	pKd	=	8.0	8.0	-2	3	Maximum response (E max) against Histamine H1 receptor in rat aortaMaximum response (E max) against Histamine H1 receptor in rat aorta	ChEMBL	305	7	2	2	3.7	NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm0309147
	CHEMBL275507	1933	None	1	Rat	Functional	pKd	=	8.0	8.0	-2	3	Maximum response (E max) against Histamine H1 receptor in rat aortaMaximum response (E max) against Histamine H1 receptor in rat aorta	ChEMBL	305	7	2	2	3.7	NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm0309147
	11741669	96806	None	0	Rat	Functional	pKd	=	8.0	8.0	-39	2	Apparent pA2 value of compound at 50 nM concentration of mepyramine in rat aortaApparent pA2 value of compound at 50 nM concentration of mepyramine in rat aorta	ChEMBL	399	11	3	3	4.3	c1ccc(C(CCc2nc(CCNCCc3cnc[nH]3)c[nH]2)c2ccccc2)cc1	10.1021/jm0309147
	CHEMBL264491	96806	None	0	Rat	Functional	pKd	=	8.0	8.0	-39	2	Apparent pA2 value of compound at 50 nM concentration of mepyramine in rat aortaApparent pA2 value of compound at 50 nM concentration of mepyramine in rat aorta	ChEMBL	399	11	3	3	4.3	c1ccc(C(CCc2nc(CCNCCc3cnc[nH]3)c[nH]2)c2ccccc2)cc1	10.1021/jm0309147
	10403687	2511	None	2	Rat	Functional	pKd	=	8.0	8.0	-1	2	Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nM	ChEMBL	319	8	2	2	3.9	CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm991056a
	1205	2511	None	2	Rat	Functional	pKd	=	8.0	8.0	-1	2	Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nM	ChEMBL	319	8	2	2	3.9	CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm991056a
	CHEMBL275035	2511	None	2	Rat	Functional	pKd	=	8.0	8.0	-1	2	Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nMCompound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nM	ChEMBL	319	8	2	2	3.9	CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm991056a
	10403687	2511	None	2	Rat	Functional	pKd	=	8.0	8.0	-1	2	Maximum response (E max) against Histamine H1 receptor in guinea pig ileumMaximum response (E max) against Histamine H1 receptor in guinea pig ileum	ChEMBL	319	8	2	2	3.9	CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm0309147
	1205	2511	None	2	Rat	Functional	pKd	=	8.0	8.0	-1	2	Maximum response (E max) against Histamine H1 receptor in guinea pig ileumMaximum response (E max) against Histamine H1 receptor in guinea pig ileum	ChEMBL	319	8	2	2	3.9	CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm0309147
	CHEMBL275035	2511	None	2	Rat	Functional	pKd	=	8.0	8.0	-1	2	Maximum response (E max) against Histamine H1 receptor in guinea pig ileumMaximum response (E max) against Histamine H1 receptor in guinea pig ileum	ChEMBL	319	8	2	2	3.9	CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1	10.1021/jm0309147
	44274460	82443	None	0	Guinea pig	Functional	pKd	=	8.0	8.0	-	0	Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand	ChEMBL	398	15	1	5	4.3	COc1ccc(CN(CCN(C)CCCCCCCCN)c2ccccn2)cc1	10.1016/s0960-894x(03)00113-6
	CHEMBL21735	82443	None	0	Guinea pig	Functional	pKd	=	8.0	8.0	-	0	Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligandHistamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand	ChEMBL	398	15	1	5	4.3	COc1ccc(CN(CCN(C)CCCCCCCCN)c2ccccn2)cc1	10.1016/s0960-894x(03)00113-6
	11726167	202113	None	0	Guinea pig	Functional	pKd	=	7.0	7.0	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	362	9	4	3	3.1	N=C(NCCCc1c[nH]cn1)NCCC(c1ccccc1)c1ccccn1	10.1021/jm00128a045
	CHEMBL59295	202113	None	0	Guinea pig	Functional	pKd	=	7.0	7.0	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	362	9	4	3	3.1	N=C(NCCCc1c[nH]cn1)NCCC(c1ccccc1)c1ccccn1	10.1021/jm00128a045
	14660386	205237	None	0	Guinea pig	Functional	pKd	=	7.0	7.0	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	395	9	4	2	4.3	N=C(NCCCc1c[nH]cn1)NCCC(c1ccccc1)c1ccc(Cl)cc1	10.1021/jm00128a045
	CHEMBL62142	205237	None	0	Guinea pig	Functional	pKd	=	7.0	7.0	-	0	Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig.	ChEMBL	395	9	4	2	4.3	N=C(NCCCc1c[nH]cn1)NCCC(c1ccccc1)c1ccc(Cl)cc1	10.1021/jm00128a045
	1201	3964	None	1	Guinea pig	Functional	pKd	=	5.0	5.0	-	0	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity	ChEMBL	361	7	3	3	2.6	O=C(CC(c1ccccc1)c1ccccc1)NC(=NCCc1cnc[nH]1)N	10.1021/jm800841w
	25150700	3964	None	1	Guinea pig	Functional	pKd	=	5.0	5.0	-	0	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity	ChEMBL	361	7	3	3	2.6	O=C(CC(c1ccccc1)c1ccccc1)NC(=NCCc1cnc[nH]1)N	10.1021/jm800841w
	CHEMBL499301	3964	None	1	Guinea pig	Functional	pKd	=	5.0	5.0	-	0	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity	ChEMBL	361	7	3	3	2.6	O=C(CC(c1ccccc1)c1ccccc1)NC(=NCCc1cnc[nH]1)N	10.1021/jm800841w
	52937526	61322	None	0	Human	Functional	pKi	=	10	10.0	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	363	5	0	5	3.1	COc1ccc(Cc2nn(C[C@H]3CCCN3C)c(=O)c3ccccc23)cc1	10.1021/jm1013874
	CHEMBL1767137	61322	None	0	Human	Functional	pKi	=	10	10.0	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	363	5	0	5	3.1	COc1ccc(Cc2nn(C[C@H]3CCCN3C)c(=O)c3ccccc23)cc1	10.1021/jm1013874
	1530	2182	None	36	Human	Functional	pKi	=	9.8	9.8	3	25	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	309	0	0	3	4.0	CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1	10.1021/jm100856p
	3827	2182	None	36	Human	Functional	pKi	=	9.8	9.8	3	25	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	309	0	0	3	4.0	CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1	10.1021/jm100856p
	3827.0	2182	None	36	Human	Functional	pKi	=	9.8	9.8	3	25	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	309	0	0	3	4.0	CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1	10.1021/jm100856p
	7206	2182	None	36	Human	Functional	pKi	=	9.8	9.8	3	25	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	309	0	0	3	4.0	CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1	10.1021/jm100856p
	CHEMBL534	2182	None	36	Human	Functional	pKi	=	9.8	9.8	3	25	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	309	0	0	3	4.0	CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1	10.1021/jm100856p
	DB00920	2182	None	36	Human	Functional	pKi	=	9.8	9.8	3	25	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	309	0	0	3	4.0	CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1	10.1021/jm100856p
	15254720	61321	None	0	Human	Functional	pKi	=	9.8	9.8	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	367	4	0	4	3.7	CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O	10.1021/jm1013874
	CHEMBL1767136	61321	None	0	Human	Functional	pKi	=	9.8	9.8	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	367	4	0	4	3.7	CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O	10.1021/jm1013874
	52937527	61323	None	0	Human	Functional	pKi	=	9.8	9.8	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	349	4	1	5	2.8	CN1CCC[C@@H]1Cn1nc(Cc2ccc(O)cc2)c2ccccc2c1=O	10.1021/jm1013874
	CHEMBL1767138	61323	None	0	Human	Functional	pKi	=	9.8	9.8	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	349	4	1	5	2.8	CN1CCC[C@@H]1Cn1nc(Cc2ccc(O)cc2)c2ccccc2c1=O	10.1021/jm1013874
	15254720	61321	None	0	Human	Functional	pKi	=	9.8	9.8	-	0	Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay	ChEMBL	367	4	0	4	3.7	CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O	10.1016/j.bmc.2012.08.032
	CHEMBL1767136	61321	None	0	Human	Functional	pKi	=	9.8	9.8	-	0	Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay	ChEMBL	367	4	0	4	3.7	CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O	10.1016/j.bmc.2012.08.032
	52937631	61327	None	0	Human	Functional	pKi	=	9.7	9.7	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	347	4	0	4	3.4	Cc1ccc(Cc2nn(C[C@H]3CCCN3C)c(=O)c3ccccc23)cc1	10.1021/jm1013874
	CHEMBL1767141	61327	None	0	Human	Functional	pKi	=	9.7	9.7	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	347	4	0	4	3.4	Cc1ccc(Cc2nn(C[C@H]3CCCN3C)c(=O)c3ccccc23)cc1	10.1021/jm1013874
	71452871	80499	None	0	Human	Functional	pKi	=	9.6	9.6	-	0	Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay	ChEMBL	412	7	0	6	3.1	COCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cnccc2c1=O	10.1016/j.bmc.2012.08.032
	CHEMBL2146801	80499	None	0	Human	Functional	pKi	=	9.6	9.6	-	0	Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay	ChEMBL	412	7	0	6	3.1	COCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cnccc2c1=O	10.1016/j.bmc.2012.08.032
	203096	61319	None	1	Human	Functional	pKi	=	9.6	9.6	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	341	5	0	4	3.2	CN(C)CCn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O	10.1021/jm1013874
	CHEMBL1767134	61319	None	1	Human	Functional	pKi	=	9.6	9.6	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	341	5	0	4	3.2	CN(C)CCn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O	10.1021/jm1013874
	52937732	61334	None	0	Human	Functional	pKi	=	9.6	9.6	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	369	4	0	4	3.4	CN1CCC[C@@H]1Cn1nc(Cc2ccc(F)c(F)c2)c2ccccc2c1=O	10.1021/jm1013874
	CHEMBL1767149	61334	None	0	Human	Functional	pKi	=	9.6	9.6	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	369	4	0	4	3.4	CN1CCC[C@@H]1Cn1nc(Cc2ccc(F)c(F)c2)c2ccccc2c1=O	10.1021/jm1013874
	71458204	80507	None	0	Human	Functional	pKi	=	9.5	9.5	-	0	Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay	ChEMBL	368	4	0	5	3.1	CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ncccc2c1=O	10.1016/j.bmc.2012.08.032
	CHEMBL2146809	80507	None	0	Human	Functional	pKi	=	9.5	9.5	-	0	Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay	ChEMBL	368	4	0	5	3.1	CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ncccc2c1=O	10.1016/j.bmc.2012.08.032
	52937630	61326	None	0	Human	Functional	pKi	=	9.5	9.5	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	351	4	0	4	3.2	CN1CCC[C@@H]1Cn1nc(Cc2ccc(F)cc2)c2ccccc2c1=O	10.1021/jm1013874
	CHEMBL1767140	61326	None	0	Human	Functional	pKi	=	9.5	9.5	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	351	4	0	4	3.2	CN1CCC[C@@H]1Cn1nc(Cc2ccc(F)cc2)c2ccccc2c1=O	10.1021/jm1013874
	52937830	61339	None	0	Human	Functional	pKi	=	9.5	9.5	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	367	4	0	4	3.7	CN1CCC[C@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O	10.1021/jm1013874
	CHEMBL1767154	61339	None	0	Human	Functional	pKi	=	9.5	9.5	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	367	4	0	4	3.7	CN1CCC[C@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O	10.1021/jm1013874
	71458203	80503	None	0	Human	Functional	pKi	=	9.5	9.5	-	0	Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay	ChEMBL	368	4	0	5	3.1	CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cnccc2c1=O	10.1016/j.bmc.2012.08.032
	CHEMBL2146805	80503	None	0	Human	Functional	pKi	=	9.5	9.5	-	0	Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay	ChEMBL	368	4	0	5	3.1	CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cnccc2c1=O	10.1016/j.bmc.2012.08.032
	71452872	80465	None	0	Human	Functional	pKi	=	9.5	9.5	-	0	Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay	ChEMBL	368	4	0	5	3.1	CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cccnc2c1=O	10.1016/j.bmc.2012.08.032
	CHEMBL2146484	80465	None	0	Human	Functional	pKi	=	9.5	9.5	-	0	Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay	ChEMBL	368	4	0	5	3.1	CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cccnc2c1=O	10.1016/j.bmc.2012.08.032
	71461782	80504	None	0	Human	Functional	pKi	=	9.4	9.4	-	0	Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay	ChEMBL	410	7	0	5	4.3	CCCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cnccc2c1=O	10.1016/j.bmc.2012.08.032
	CHEMBL2146806	80504	None	0	Human	Functional	pKi	=	9.4	9.4	-	0	Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay	ChEMBL	410	7	0	5	4.3	CCCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cnccc2c1=O	10.1016/j.bmc.2012.08.032
	46861860	7493	None	1	Human	Functional	pKi	=	9.3	9.3	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	323	3	0	3	4.0	CN1CCCC(c2nc3ccccc3n2Cc2ccc(F)cc2)C1	10.1016/j.bmcl.2011.10.115
	CHEMBL1087089	7493	None	1	Human	Functional	pKi	=	9.3	9.3	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	323	3	0	3	4.0	CN1CCCC(c2nc3ccccc3n2Cc2ccc(F)cc2)C1	10.1016/j.bmcl.2011.10.115
	52937728	61330	None	0	Human	Functional	pKi	=	9.3	9.3	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	351	4	0	4	3.2	CN1CCC[C@@H]1Cn1nc(Cc2cccc(F)c2)c2ccccc2c1=O	10.1021/jm1013874
	CHEMBL1767145	61330	None	0	Human	Functional	pKi	=	9.3	9.3	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	351	4	0	4	3.2	CN1CCC[C@@H]1Cn1nc(Cc2cccc(F)c2)c2ccccc2c1=O	10.1021/jm1013874
	71456359	80501	None	0	Human	Functional	pKi	=	9.3	9.3	-	0	Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay	ChEMBL	411	7	0	5	3.8	COCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O	10.1016/j.bmc.2012.08.032
	CHEMBL2146803	80501	None	0	Human	Functional	pKi	=	9.3	9.3	-	0	Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay	ChEMBL	411	7	0	5	3.8	COCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O	10.1016/j.bmc.2012.08.032
	71458205	80509	None	0	Human	Functional	pKi	=	9.3	9.3	-	0	Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay	ChEMBL	412	7	0	6	3.1	COCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ncccc2c1=O	10.1016/j.bmc.2012.08.032
	CHEMBL2146811	80509	None	0	Human	Functional	pKi	=	9.3	9.3	-	0	Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay	ChEMBL	412	7	0	6	3.1	COCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ncccc2c1=O	10.1016/j.bmc.2012.08.032
	71451044	80505	None	0	Human	Functional	pKi	=	9.2	9.2	-	0	Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay	ChEMBL	410	7	0	5	4.3	CCCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cccnc2c1=O	10.1016/j.bmc.2012.08.032
	CHEMBL2146807	80505	None	0	Human	Functional	pKi	=	9.2	9.2	-	0	Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay	ChEMBL	410	7	0	5	4.3	CCCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cccnc2c1=O	10.1016/j.bmc.2012.08.032
	71454639	80508	None	0	Human	Functional	pKi	=	9.2	9.2	-	0	Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay	ChEMBL	410	7	0	5	4.3	CCCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ncccc2c1=O	10.1016/j.bmc.2012.08.032
	CHEMBL2146810	80508	None	0	Human	Functional	pKi	=	9.2	9.2	-	0	Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay	ChEMBL	410	7	0	5	4.3	CCCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ncccc2c1=O	10.1016/j.bmc.2012.08.032
	49864841	15738	None	0	Human	Functional	pKi	=	9.2	9.2	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay	ChEMBL	266	1	1	4	1.6	C1=C(N2CCNCC2)c2nccn2Cc2ccccc21	10.1016/j.bmcl.2010.07.029
	CHEMBL1222552	15738	None	0	Human	Functional	pKi	=	9.2	9.2	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay	ChEMBL	266	1	1	4	1.6	C1=C(N2CCNCC2)c2nccn2Cc2ccccc21	10.1016/j.bmcl.2010.07.029
	71449250	80502	None	0	Human	Functional	pKi	=	9.2	9.2	-	0	Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay	ChEMBL	368	4	0	5	3.1	CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccncc2c1=O	10.1016/j.bmc.2012.08.032
	CHEMBL2146804	80502	None	0	Human	Functional	pKi	=	9.2	9.2	-	0	Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay	ChEMBL	368	4	0	5	3.1	CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccncc2c1=O	10.1016/j.bmc.2012.08.032
	52937731	61333	None	0	Human	Functional	pKi	=	9.1	9.1	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	347	4	0	4	3.4	Cc1cccc(Cc2nn(C[C@H]3CCCN3C)c(=O)c3ccccc23)c1	10.1021/jm1013874
	CHEMBL1767148	61333	None	0	Human	Functional	pKi	=	9.1	9.1	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	347	4	0	4	3.4	Cc1cccc(Cc2nn(C[C@H]3CCCN3C)c(=O)c3ccccc23)c1	10.1021/jm1013874
	46861858	8564	None	0	Human	Functional	pKi	=	9.1	9.1	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	335	5	0	4	3.9	CN1CCCC(c2nc3ccccc3n2CCOc2ccccc2)C1	10.1016/j.bmcl.2011.10.115
	CHEMBL1094510	8564	None	0	Human	Functional	pKi	=	9.1	9.1	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	335	5	0	4	3.9	CN1CCCC(c2nc3ccccc3n2CCOc2ccccc2)C1	10.1016/j.bmcl.2011.10.115
	57402315	69734	None	0	Human	Functional	pKi	=	9.1	9.1	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	311	3	1	4	2.9	Fc1ccc(Cn2c([C@H]3CNCCO3)nc3ccccc32)cc1	10.1016/j.bmcl.2011.10.115
	CHEMBL1935442	69734	None	0	Human	Functional	pKi	=	9.1	9.1	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	311	3	1	4	2.9	Fc1ccc(Cn2c([C@H]3CNCCO3)nc3ccccc32)cc1	10.1016/j.bmcl.2011.10.115
	46888857	8714	None	0	Human	Functional	pKi	=	9.1	9.1	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	323	3	0	3	4.0	CN1CCC[C@@H](c2nc3ccccc3n2Cc2ccc(F)cc2)C1	10.1016/j.bmcl.2011.10.115
	CHEMBL1095819	8714	None	0	Human	Functional	pKi	=	9.1	9.1	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	323	3	0	3	4.0	CN1CCC[C@@H](c2nc3ccccc3n2Cc2ccc(F)cc2)C1	10.1016/j.bmcl.2011.10.115
	71461781	80500	None	0	Human	Functional	pKi	=	9.0	9.0	-	0	Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay	ChEMBL	409	7	0	4	4.9	CCCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O	10.1016/j.bmc.2012.08.032
	CHEMBL2146802	80500	None	0	Human	Functional	pKi	=	9.0	9.0	-	0	Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay	ChEMBL	409	7	0	4	4.9	CCCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O	10.1016/j.bmc.2012.08.032
	57398830	69728	None	0	Human	Functional	pKi	=	9	9.0	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	353	5	1	4	3.4	OCCN1CCCC(c2nc3ccccc3n2Cc2ccc(F)cc2)C1	10.1016/j.bmcl.2011.10.115
	CHEMBL1935436	69728	None	0	Human	Functional	pKi	=	9	9.0	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	353	5	1	4	3.4	OCCN1CCCC(c2nc3ccccc3n2Cc2ccc(F)cc2)C1	10.1016/j.bmcl.2011.10.115
	57400501	69730	None	0	Human	Functional	pKi	=	9	9.0	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	321	5	1	4	3.6	c1ccc(OCCn2c(C3CCCNC3)nc3ccccc32)cc1	10.1016/j.bmcl.2011.10.115
	CHEMBL1935438	69730	None	0	Human	Functional	pKi	=	9	9.0	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	321	5	1	4	3.6	c1ccc(OCCn2c(C3CCCNC3)nc3ccccc32)cc1	10.1016/j.bmcl.2011.10.115
	57395287	69733	None	0	Human	Functional	pKi	=	9	9.0	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	307	3	1	4	3.1	Cc1ccc(Cn2c([C@H]3CNCCO3)nc3ccccc32)cc1	10.1016/j.bmcl.2011.10.115
	CHEMBL1935441	69733	None	0	Human	Functional	pKi	=	9	9.0	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	307	3	1	4	3.1	Cc1ccc(Cn2c([C@H]3CNCCO3)nc3ccccc32)cc1	10.1016/j.bmcl.2011.10.115
	71456360	80506	None	0	Human	Functional	pKi	=	9	9.0	-	0	Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay	ChEMBL	412	7	0	6	3.1	COCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cccnc2c1=O	10.1016/j.bmc.2012.08.032
	CHEMBL2146808	80506	None	0	Human	Functional	pKi	=	9	9.0	-	0	Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay	ChEMBL	412	7	0	6	3.1	COCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2cccnc2c1=O	10.1016/j.bmc.2012.08.032
	52937222	61341	None	0	Human	Functional	pKi	=	9	9.0	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	367	3	0	4	3.9	CN1CCC(n2nc(Cc3ccc(Cl)cc3)c3ccccc3c2=O)CC1	10.1021/jm1013874
	CHEMBL1767156	61341	None	0	Human	Functional	pKi	=	9	9.0	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	367	3	0	4	3.9	CN1CCC(n2nc(Cc3ccc(Cl)cc3)c3ccccc3c2=O)CC1	10.1021/jm1013874
	57404030	69729	None	0	Human	Functional	pKi	=	8.9	8.9	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	309	3	1	3	3.7	Fc1ccc(Cn2c([C@@H]3CCCNC3)nc3ccccc32)cc1	10.1016/j.bmcl.2011.10.115
	CHEMBL1935437	69729	None	0	Human	Functional	pKi	=	8.9	8.9	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	309	3	1	3	3.7	Fc1ccc(Cn2c([C@@H]3CCCNC3)nc3ccccc32)cc1	10.1016/j.bmcl.2011.10.115
	2267	559	None	45	Human	Functional	pKi	=	8.9	8.9	32	14	Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay	ChEMBL	381	3	0	4	4.3	CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2	10.1016/j.bmc.2012.08.032
	2267.0	559	None	45	Human	Functional	pKi	=	8.9	8.9	32	14	Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay	ChEMBL	381	3	0	4	4.3	CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2	10.1016/j.bmc.2012.08.032
	271	559	None	45	Human	Functional	pKi	=	8.9	8.9	32	14	Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay	ChEMBL	381	3	0	4	4.3	CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2	10.1016/j.bmc.2012.08.032
	7121	559	None	45	Human	Functional	pKi	=	8.9	8.9	32	14	Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay	ChEMBL	381	3	0	4	4.3	CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2	10.1016/j.bmc.2012.08.032
	CHEMBL639	559	None	45	Human	Functional	pKi	=	8.9	8.9	32	14	Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay	ChEMBL	381	3	0	4	4.3	CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2	10.1016/j.bmc.2012.08.032
	DB00972	559	None	45	Human	Functional	pKi	=	8.9	8.9	32	14	Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay	ChEMBL	381	3	0	4	4.3	CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2	10.1016/j.bmc.2012.08.032
	2267	559	None	45	Human	Functional	pKi	=	8.9	8.9	32	14	Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay	ChEMBL	381	3	0	4	4.3	CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2	10.1016/j.bmcl.2016.11.022
	2267.0	559	None	45	Human	Functional	pKi	=	8.9	8.9	32	14	Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay	ChEMBL	381	3	0	4	4.3	CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2	10.1016/j.bmcl.2016.11.022
	271	559	None	45	Human	Functional	pKi	=	8.9	8.9	32	14	Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay	ChEMBL	381	3	0	4	4.3	CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2	10.1016/j.bmcl.2016.11.022
	7121	559	None	45	Human	Functional	pKi	=	8.9	8.9	32	14	Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay	ChEMBL	381	3	0	4	4.3	CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2	10.1016/j.bmcl.2016.11.022
	CHEMBL639	559	None	45	Human	Functional	pKi	=	8.9	8.9	32	14	Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay	ChEMBL	381	3	0	4	4.3	CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2	10.1016/j.bmcl.2016.11.022
	DB00972	559	None	45	Human	Functional	pKi	=	8.9	8.9	32	14	Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay	ChEMBL	381	3	0	4	4.3	CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2	10.1016/j.bmcl.2016.11.022
	2267	559	None	45	Human	Functional	pKi	=	8.9	8.9	32	14	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	381	3	0	4	4.3	CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2	10.1021/jm1013874
	2267.0	559	None	45	Human	Functional	pKi	=	8.9	8.9	32	14	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	381	3	0	4	4.3	CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2	10.1021/jm1013874
	271	559	None	45	Human	Functional	pKi	=	8.9	8.9	32	14	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	381	3	0	4	4.3	CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2	10.1021/jm1013874
	7121	559	None	45	Human	Functional	pKi	=	8.9	8.9	32	14	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	381	3	0	4	4.3	CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2	10.1021/jm1013874
	CHEMBL639	559	None	45	Human	Functional	pKi	=	8.9	8.9	32	14	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	381	3	0	4	4.3	CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2	10.1021/jm1013874
	DB00972	559	None	45	Human	Functional	pKi	=	8.9	8.9	32	14	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	381	3	0	4	4.3	CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2	10.1021/jm1013874
	71456361	80510	None	0	Human	Functional	pKi	=	8.9	8.9	-	0	Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay	ChEMBL	369	4	0	6	2.5	CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2nccnc2c1=O	10.1016/j.bmc.2012.08.032
	CHEMBL2146812	80510	None	0	Human	Functional	pKi	=	8.9	8.9	-	0	Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay	ChEMBL	369	4	0	6	2.5	CN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2nccnc2c1=O	10.1016/j.bmc.2012.08.032
	57400503	69736	None	0	Human	Functional	pKi	=	8.9	8.9	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	323	3	1	4	3.8	Cc1ccc(Cn2c(C3CNCCS3)nc3ccccc32)cc1	10.1016/j.bmcl.2011.10.115
	CHEMBL1935444	69736	None	0	Human	Functional	pKi	=	8.9	8.9	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	323	3	1	4	3.8	Cc1ccc(Cn2c(C3CNCCS3)nc3ccccc32)cc1	10.1016/j.bmcl.2011.10.115
	57397056	69738	None	0	Human	Functional	pKi	=	8.9	8.9	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	327	3	1	4	3.6	Fc1ccc(Cn2c([C@H]3CNCCS3)nc3ccccc32)cc1	10.1016/j.bmcl.2011.10.115
	CHEMBL1935446	69738	None	0	Human	Functional	pKi	=	8.9	8.9	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	327	3	1	4	3.6	Fc1ccc(Cn2c([C@H]3CNCCS3)nc3ccccc32)cc1	10.1016/j.bmcl.2011.10.115
	57400505	69739	None	0	Human	Functional	pKi	=	8.9	8.9	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	339	4	1	5	3.5	COc1ccc(Cn2c([C@H]3CNCCS3)nc3ccccc32)cc1	10.1016/j.bmcl.2011.10.115
	CHEMBL1935447	69739	None	0	Human	Functional	pKi	=	8.9	8.9	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	339	4	1	5	3.5	COc1ccc(Cn2c([C@H]3CNCCS3)nc3ccccc32)cc1	10.1016/j.bmcl.2011.10.115
	57400503	69736	None	0	Human	Functional	pKi	=	8.8	8.8	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	323	3	1	4	3.8	Cc1ccc(Cn2c(C3CNCCS3)nc3ccccc32)cc1	10.1016/j.bmcl.2011.10.115
	CHEMBL1935444	69736	None	0	Human	Functional	pKi	=	8.8	8.8	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	323	3	1	4	3.8	Cc1ccc(Cn2c(C3CNCCS3)nc3ccccc32)cc1	10.1016/j.bmcl.2011.10.115
	52937729	61331	None	0	Human	Functional	pKi	=	8.8	8.8	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	367	4	0	4	3.7	CN1CCC[C@@H]1Cn1nc(Cc2cccc(Cl)c2)c2ccccc2c1=O	10.1021/jm1013874
	CHEMBL1767146	61331	None	0	Human	Functional	pKi	=	8.8	8.8	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	367	4	0	4	3.7	CN1CCC[C@@H]1Cn1nc(Cc2cccc(Cl)c2)c2ccccc2c1=O	10.1021/jm1013874
	52937829	61338	None	0	Human	Functional	pKi	=	8.8	8.8	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	313	6	0	4	3.2	CCCCCc1nn(C[C@H]2CCCN2C)c(=O)c2ccccc12	10.1021/jm1013874
	CHEMBL1767153	61338	None	0	Human	Functional	pKi	=	8.8	8.8	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	313	6	0	4	3.2	CCCCCc1nn(C[C@H]2CCCN2C)c(=O)c2ccccc12	10.1021/jm1013874
	57400502	69735	None	0	Human	Functional	pKi	=	8.7	8.7	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	321	3	1	4	3.4	Cc1ccc(Cn2c(C3CNCCO3)nc3ccccc32)cc1C	10.1016/j.bmcl.2011.10.115
	CHEMBL1935443	69735	None	0	Human	Functional	pKi	=	8.7	8.7	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	321	3	1	4	3.4	Cc1ccc(Cn2c(C3CNCCO3)nc3ccccc32)cc1C	10.1016/j.bmcl.2011.10.115
	52937730	61332	None	0	Human	Functional	pKi	=	8.7	8.7	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	363	5	0	5	3.1	COc1cccc(Cc2nn(C[C@H]3CCCN3C)c(=O)c3ccccc23)c1	10.1021/jm1013874
	CHEMBL1767147	61332	None	0	Human	Functional	pKi	=	8.7	8.7	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	363	5	0	5	3.1	COc1cccc(Cc2nn(C[C@H]3CCCN3C)c(=O)c3ccccc23)c1	10.1021/jm1013874
	52945978	18803	None	0	Human	Functional	pKi	=	8	8.0	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	335	4	2	2	3.7	O=C(O)CCNC1CC[C@]2(Cc3ccccc3Cc3ccccc32)C1	10.1021/jm100856p
	CHEMBL1278114	18803	None	0	Human	Functional	pKi	=	8	8.0	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	335	4	2	2	3.7	O=C(O)CCNC1CC[C@]2(Cc3ccccc3Cc3ccccc32)C1	10.1021/jm100856p
	17747460	61349	None	13	Human	Functional	pKi	=	8	8.0	-	2	Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay	ChEMBL	640	14	0	6	7.8	O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1	10.1016/j.bmc.2012.08.032
	CHEMBL1767164	61349	None	13	Human	Functional	pKi	=	8	8.0	-	2	Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay	ChEMBL	640	14	0	6	7.8	O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1	10.1016/j.bmc.2012.08.032
	17747460	61349	None	13	Human	Functional	pKi	=	8	8.0	-	2	Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay	ChEMBL	640	14	0	6	7.8	O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1	10.1016/j.bmcl.2016.11.022
	CHEMBL1767164	61349	None	13	Human	Functional	pKi	=	8	8.0	-	2	Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay	ChEMBL	640	14	0	6	7.8	O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1	10.1016/j.bmcl.2016.11.022
	52937018	61320	None	0	Human	Functional	pKi	=	8	8.0	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	355	6	0	4	3.6	CN(C)CCCn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O	10.1021/jm1013874
	CHEMBL1767135	61320	None	0	Human	Functional	pKi	=	8	8.0	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	355	6	0	4	3.6	CN(C)CCCn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O	10.1021/jm1013874
	17747460	61349	None	13	Human	Functional	pKi	=	8	8.0	-	2	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	640	14	0	6	7.8	O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1	10.1021/jm1013874
	CHEMBL1767164	61349	None	13	Human	Functional	pKi	=	8	8.0	-	2	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	640	14	0	6	7.8	O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1	10.1021/jm1013874
	49836636	18684	None	0	Human	Functional	pKi	=	7	7.0	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	375	2	1	3	4.5	O=C(O)C1=CCCN(C2CCC3(Cc4ccccc4Oc4ccccc43)C2)C1	10.1021/jm100856p
	CHEMBL1277125	18684	None	0	Human	Functional	pKi	=	7	7.0	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	375	2	1	3	4.5	O=C(O)C1=CCCN(C2CCC3(Cc4ccccc4Oc4ccccc43)C2)C1	10.1021/jm100856p
	49836522	18802	None	0	Human	Functional	pKi	=	7	7.0	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	376	2	2	3	3.0	O=C(O)C1CN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)CCN1	10.1021/jm100856p
	CHEMBL1278113	18802	None	0	Human	Functional	pKi	=	7	7.0	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	376	2	2	3	3.0	O=C(O)C1CN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)CCN1	10.1021/jm100856p
	11648990	95699	None	0	Human	Functional	pKi	=	7	7.0	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	498	6	0	8	5.4	Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6onc(C)c6cc5CC4)n3C)cccc2n1	10.1016/j.bmcl.2007.12.066
	CHEMBL257946	95699	None	0	Human	Functional	pKi	=	7	7.0	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	498	6	0	8	5.4	Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6onc(C)c6cc5CC4)n3C)cccc2n1	10.1016/j.bmcl.2007.12.066
	185	4006	None	43	Human	Functional	pKi	=	6	6.0	-	1	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	373	7	1	4	3.8	COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O	10.1021/jm100856p
	5311271	4006	None	43	Human	Functional	pKi	=	6	6.0	-	1	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	373	7	1	4	3.8	COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O	10.1021/jm100856p
	CHEMBL74355	4006	None	43	Human	Functional	pKi	=	6	6.0	-	1	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	373	7	1	4	3.8	COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O	10.1021/jm100856p
	DB16351	4006	None	43	Human	Functional	pKi	=	6	6.0	-	1	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	373	7	1	4	3.8	COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O	10.1021/jm100856p
	49836740	18711	None	0	Human	Functional	pKi	=	6	6.0	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	425	2	1	4	4.9	O=C(O)C1CCN(C2CCC3(C2)C(=O)c2cc(Cl)ccc2Oc2ccccc23)CC1	10.1021/jm100856p
	CHEMBL1277401	18711	None	0	Human	Functional	pKi	=	6	6.0	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	425	2	1	4	4.9	O=C(O)C1CCN(C2CCC3(C2)C(=O)c2cc(Cl)ccc2Oc2ccccc23)CC1	10.1021/jm100856p
	44454458	95178	None	0	Human	Functional	pKi	=	6	6.0	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	618	6	0	8	7.1	Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6nc(C(C)(C)C)oc6c(Br)c5CC4)n3C)cccc2n1	10.1016/j.bmcl.2007.12.066
	CHEMBL255566	95178	None	0	Human	Functional	pKi	=	6	6.0	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	618	6	0	8	7.1	Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6nc(C(C)(C)C)oc6c(Br)c5CC4)n3C)cccc2n1	10.1016/j.bmcl.2007.12.066
	44454382	95635	None	0	Human	Functional	pKi	=	6	6.0	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	517	6	0	8	5.2	Cc1ccc2c(-c3nnc(SCCCN4CCc5nc6ccc(Cl)cn6c5CC4)n3C)cccc2n1	10.1016/j.bmcl.2007.12.042
	CHEMBL257716	95635	None	0	Human	Functional	pKi	=	6	6.0	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	517	6	0	8	5.2	Cc1ccc2c(-c3nnc(SCCCN4CCc5nc6ccc(Cl)cn6c5CC4)n3C)cccc2n1	10.1016/j.bmcl.2007.12.042
	11642163	97558	None	0	Human	Functional	pKi	=	6	6.0	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	522	6	0	9	5.3	Cc1nc(C)c(-c2nnc(SCCCN3CCc4ccc5oc(C(F)(F)F)nc5c4CC3)n2C)s1	10.1016/j.bmcl.2007.12.042
	CHEMBL270376	97558	None	0	Human	Functional	pKi	=	6	6.0	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	522	6	0	9	5.3	Cc1nc(C)c(-c2nnc(SCCCN3CCc4ccc5oc(C(F)(F)F)nc5c4CC3)n2C)s1	10.1016/j.bmcl.2007.12.042
	11663526	97805	None	0	Human	Functional	pKi	=	6	6.0	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	514	6	0	8	5.8	Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6nc(C)sc6cc5CC4)n3C)cccc2n1	10.1016/j.bmcl.2007.12.066
	CHEMBL271632	97805	None	0	Human	Functional	pKi	=	6	6.0	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	514	6	0	8	5.8	Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6nc(C)sc6cc5CC4)n3C)cccc2n1	10.1016/j.bmcl.2007.12.066
	44454223	98027	None	0	Human	Functional	pKi	=	6	6.0	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	542	6	0	8	4.7	CC(=O)N1CCOc2cc3c(cc21)CCN(CCCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3	10.1016/j.bmcl.2007.12.066
	CHEMBL272702	98027	None	0	Human	Functional	pKi	=	6	6.0	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	542	6	0	8	4.7	CC(=O)N1CCOc2cc3c(cc21)CCN(CCCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3	10.1016/j.bmcl.2007.12.066
	11527195	98111	None	0	Human	Functional	pKi	=	6	6.0	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	590	6	0	8	6.5	Cc1ccc2c(-c3nnc(SCCC(C)N4CCc5cc6nc(C)oc6c(Br)c5CC4)n3C)cccc2n1	10.1016/j.bmcl.2007.12.066
	CHEMBL273165	98111	None	0	Human	Functional	pKi	=	6	6.0	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	590	6	0	8	6.5	Cc1ccc2c(-c3nnc(SCCC(C)N4CCc5cc6nc(C)oc6c(Br)c5CC4)n3C)cccc2n1	10.1016/j.bmcl.2007.12.066
	11721190	155364	None	0	Human	Functional	pKi	=	6	6.0	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	578	7	0	10	5.8	Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc6oc(-c7cc(C)nn7C)nc6c5CC4)n3C)cccc2n1	10.1016/j.bmcl.2007.12.042
	CHEMBL402853	155364	None	0	Human	Functional	pKi	=	6	6.0	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	578	7	0	10	5.8	Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc6oc(-c7cc(C)nn7C)nc6c5CC4)n3C)cccc2n1	10.1016/j.bmcl.2007.12.042
	134143913	150418	None	0	Human	Functional	pKi	=	6	6.0	-	0	Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay	ChEMBL	497	9	0	6	5.1	N#Cc1ccc(N2CCN(CCc3ccc(OCCCN4CCCCCC4)cc3)CC2)c2ncccc12	10.1016/j.bmcl.2016.11.022
	CHEMBL3953018	150418	None	0	Human	Functional	pKi	=	6	6.0	-	0	Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay	ChEMBL	497	9	0	6	5.1	N#Cc1ccc(N2CCN(CCc3ccc(OCCCN4CCCCCC4)cc3)CC2)c2ncccc12	10.1016/j.bmcl.2016.11.022
	57393573	69731	None	0	Human	Functional	pKi	=	7.9	7.9	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	406	7	0	5	3.4	CN(C)C(=O)CN1CCCC(c2nc3ccccc3n2CCOc2ccccc2)C1	10.1016/j.bmcl.2011.10.115
	CHEMBL1935439	69731	None	0	Human	Functional	pKi	=	7.9	7.9	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	406	7	0	5	3.4	CN(C)C(=O)CN1CCCC(c2nc3ccccc3n2CCOc2ccccc2)C1	10.1016/j.bmcl.2011.10.115
	49836525	18814	None	0	Human	Functional	pKi	=	7.9	7.9	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	375	2	1	2	4.4	CC1(C(=O)O)CCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1	10.1021/jm100856p
	CHEMBL1278202	18814	None	0	Human	Functional	pKi	=	7.9	7.9	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	375	2	1	2	4.4	CC1(C(=O)O)CCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1	10.1021/jm100856p
	57780020	143537	None	0	Human	Functional	pKi	=	7.9	7.9	-	0	Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay	ChEMBL	600	15	1	6	6.6	CCCCc1cc(N2CCN(CCc3ccc(OCCCN4CCCCCC4)cc3)CC2)c2nc(CCC(=O)O)ccc2c1	10.1016/j.bmcl.2016.11.022
	CHEMBL3898341	143537	None	0	Human	Functional	pKi	=	7.9	7.9	-	0	Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay	ChEMBL	600	15	1	6	6.6	CCCCc1cc(N2CCN(CCc3ccc(OCCCN4CCCCCC4)cc3)CC2)c2nc(CCC(=O)O)ccc2c1	10.1016/j.bmcl.2016.11.022
	57780017	148206	None	0	Human	Functional	pKi	=	7.9	7.9	-	0	Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay	ChEMBL	544	12	1	6	5.3	O=C(O)CCc1ccc2cccc(N3CCN(CCc4ccc(OCCCN5CCCCCC5)cc4)CC3)c2n1	10.1016/j.bmcl.2016.11.022
	CHEMBL3935303	148206	None	0	Human	Functional	pKi	=	7.9	7.9	-	0	Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay	ChEMBL	544	12	1	6	5.3	O=C(O)CCc1ccc2cccc(N3CCN(CCc4ccc(OCCCN5CCCCCC5)cc4)CC3)c2n1	10.1016/j.bmcl.2016.11.022
	49834051	15754	None	0	Human	Functional	pKi	=	7.9	7.9	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay	ChEMBL	364	3	1	5	2.2	O=C(O)C1CC(N2CCN(C3=Cc4ccccc4Cn4ccnc43)CC2)C1	10.1016/j.bmcl.2010.07.029
	CHEMBL1222626	15754	None	0	Human	Functional	pKi	=	7.9	7.9	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay	ChEMBL	364	3	1	5	2.2	O=C(O)C1CC(N2CCN(C3=Cc4ccccc4Cn4ccnc43)CC2)C1	10.1016/j.bmcl.2010.07.029
	24803639	61351	None	0	Human	Functional	pKi	=	7.9	7.9	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	622	14	1	7	6.8	O=c1c2ccccc2c(Cc2ccc(O)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1	10.1021/jm1013874
	CHEMBL1767166	61351	None	0	Human	Functional	pKi	=	7.9	7.9	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	622	14	1	7	6.8	O=c1c2ccccc2c(Cc2ccc(O)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1	10.1021/jm1013874
	24803483	61352	None	0	Human	Functional	pKi	=	7.9	7.9	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	654	15	0	6	8.2	O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCCc1ccc(OCCCN2CCCCCC2)cc1	10.1021/jm1013874
	CHEMBL1767167	61352	None	0	Human	Functional	pKi	=	7.9	7.9	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	654	15	0	6	8.2	O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCCc1ccc(OCCCN2CCCCCC2)cc1	10.1021/jm1013874
	49836738	18701	None	0	Human	Functional	pKi	=	6.9	6.9	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	377	2	1	3	4.6	O=C(O)[C@@H]1CCCN(C2CCC3(Cc4ccccc4Oc4ccccc43)C2)C1	10.1021/jm100856p
	CHEMBL1277311	18701	None	0	Human	Functional	pKi	=	6.9	6.9	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	377	2	1	3	4.6	O=C(O)[C@@H]1CCCN(C2CCC3(Cc4ccccc4Oc4ccccc43)C2)C1	10.1021/jm100856p
	11591601	155423	None	0	Human	Functional	pKi	=	6.9	6.9	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	512	7	0	8	5.6	CCc1noc2cc3c(cc12)CCN(CCCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3	10.1016/j.bmcl.2007.12.066
	CHEMBL403181	155423	None	0	Human	Functional	pKi	=	6.9	6.9	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	512	7	0	8	5.6	CCc1noc2cc3c(cc12)CCN(CCCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3	10.1016/j.bmcl.2007.12.066
	49833882	15767	None	0	Human	Functional	pKi	=	6.9	6.9	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay	ChEMBL	392	3	1	5	3.0	O=C(O)C1CCC(N2CCN(C3=Cc4ccccc4Cn4ccnc43)CC2)CC1	10.1016/j.bmcl.2010.07.029
	CHEMBL1222692	15767	None	0	Human	Functional	pKi	=	6.9	6.9	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay	ChEMBL	392	3	1	5	3.0	O=C(O)C1CCC(N2CCN(C3=Cc4ccccc4Cn4ccnc43)CC2)CC1	10.1016/j.bmcl.2010.07.029
	49833886	15785	None	0	Human	Functional	pKi	=	6.9	6.9	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay	ChEMBL	396	5	1	6	2.5	COc1cnc2n1Cc1ccccc1C=C2N1CCN(CC(C)(C)C(=O)O)CC1	10.1016/j.bmcl.2010.07.029
	CHEMBL1222764	15785	None	0	Human	Functional	pKi	=	6.9	6.9	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay	ChEMBL	396	5	1	6	2.5	COc1cnc2n1Cc1ccccc1C=C2N1CCN(CC(C)(C)C(=O)O)CC1	10.1016/j.bmcl.2010.07.029
	11657494	95562	None	0	Human	Functional	pKi	=	5.9	5.9	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	644	7	0	8	7.2	Cc1ccc2c(-c3nnc(SCCCCN4CCc5cc6nc(C(F)(F)F)oc6c(Br)c5CC4)n3C)cccc2n1	10.1016/j.bmcl.2007.12.066
	CHEMBL257369	95562	None	0	Human	Functional	pKi	=	5.9	5.9	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	644	7	0	8	7.2	Cc1ccc2c(-c3nnc(SCCCCN4CCc5cc6nc(C(F)(F)F)oc6c(Br)c5CC4)n3C)cccc2n1	10.1016/j.bmcl.2007.12.066
	11641641	97560	None	0	Human	Functional	pKi	=	5.9	5.9	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	487	6	0	7	5.2	Cn1c(SCCCN2CCc3ccc4oc(C(F)(F)F)nc4c3CC2)nnc1-c1ccccc1	10.1016/j.bmcl.2007.12.042
	CHEMBL270387	97560	None	0	Human	Functional	pKi	=	5.9	5.9	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	487	6	0	7	5.2	Cn1c(SCCCN2CCc3ccc4oc(C(F)(F)F)nc4c3CC2)nnc1-c1ccccc1	10.1016/j.bmcl.2007.12.042
	24749507	14013	None	3	Human	Functional	pKi	=	5.9	5.9	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilizationAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization	ChEMBL	421	7	0	4	3.4	O=C(c1ccccc1)N1CCN(c2ccc(OCCCN3CCCCC3)cc2)C(=O)C1	10.1021/jm0708228
	CHEMBL1197067	14013	None	3	Human	Functional	pKi	=	5.9	5.9	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilizationAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization	ChEMBL	421	7	0	4	3.4	O=C(c1ccccc1)N1CCN(c2ccc(OCCCN3CCCCC3)cc2)C(=O)C1	10.1021/jm0708228
	CHEMBL559206	14013	None	3	Human	Functional	pKi	=	5.9	5.9	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilizationAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization	ChEMBL	421	7	0	4	3.4	O=C(c1ccccc1)N1CCN(c2ccc(OCCCN3CCCCC3)cc2)C(=O)C1	10.1021/jm0708228
	57397055	69727	None	0	Human	Functional	pKi	=	7.9	7.9	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	390	5	0	5	4.6	Fc1ccc(Cn2c(C3CCCN(Cc4ncco4)C3)nc3ccccc32)cc1	10.1016/j.bmcl.2011.10.115
	CHEMBL1935435	69727	None	0	Human	Functional	pKi	=	7.9	7.9	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	390	5	0	5	4.6	Fc1ccc(Cn2c(C3CCCN(Cc4ncco4)C3)nc3ccccc32)cc1	10.1016/j.bmcl.2011.10.115
	49836294	18786	None	0	Human	Functional	pKi	=	7.8	7.8	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	387	2	0	3	4.4	COC(=O)C1=CCCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1	10.1021/jm100856p
	CHEMBL1278020	18786	None	0	Human	Functional	pKi	=	7.8	7.8	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	387	2	0	3	4.4	COC(=O)C1=CCCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1	10.1021/jm100856p
	49836524	18813	None	0	Human	Functional	pKi	=	7.8	7.8	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	361	2	1	2	4.0	O=C(O)C1CCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1	10.1021/jm100856p
	CHEMBL1278201	18813	None	0	Human	Functional	pKi	=	7.8	7.8	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	361	2	1	2	4.0	O=C(O)C1CCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1	10.1021/jm100856p
	134136763	142935	None	0	Human	Functional	pKi	=	7.8	7.8	-	0	Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay	ChEMBL	500	11	0	5	6.0	c1cnc2c(N3CCN(CCCCc4ccc(OCCCN5CCCCCC5)cc4)CC3)cccc2c1	10.1016/j.bmcl.2016.11.022
	CHEMBL3893197	142935	None	0	Human	Functional	pKi	=	7.8	7.8	-	0	Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay	ChEMBL	500	11	0	5	6.0	c1cnc2c(N3CCN(CCCCc4ccc(OCCCN5CCCCCC5)cc4)CC3)cccc2c1	10.1016/j.bmcl.2016.11.022
	57780007	147079	None	0	Human	Functional	pKi	=	7.8	7.8	-	0	Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay	ChEMBL	572	13	1	6	5.8	CCc1cc(N2CCN(CCc3ccc(OCCCN4CCCCCC4)cc3)CC2)c2nc(CCC(=O)O)ccc2c1	10.1016/j.bmcl.2016.11.022
	CHEMBL3926412	147079	None	0	Human	Functional	pKi	=	7.8	7.8	-	0	Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay	ChEMBL	572	13	1	6	5.8	CCc1cc(N2CCN(CCc3ccc(OCCCN4CCCCCC4)cc3)CC2)c2nc(CCC(=O)O)ccc2c1	10.1016/j.bmcl.2016.11.022
	24803797	61100	None	0	Human	Functional	pKi	=	7.8	7.8	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	626	11	0	6	7.6	O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C1CCCN(CCc2ccc(OCCCN3CCCCCC3)cc2)CC1	10.1021/jm1013874
	CHEMBL1765111	61100	None	0	Human	Functional	pKi	=	7.8	7.8	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	626	11	0	6	7.6	O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C1CCCN(CCc2ccc(OCCCN3CCCCCC3)cc2)CC1	10.1021/jm1013874
	24803798	61345	None	0	Human	Functional	pKi	=	7.8	7.8	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	640	12	0	6	7.9	O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C1CCCN(CCCc2ccc(OCCCN3CCCCCC3)cc2)CC1	10.1021/jm1013874
	CHEMBL1767160	61345	None	0	Human	Functional	pKi	=	7.8	7.8	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	640	12	0	6	7.9	O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C1CCCN(CCCc2ccc(OCCCN3CCCCCC3)cc2)CC1	10.1021/jm1013874
	49836737	18692	None	0	Human	Functional	pKi	=	6.8	6.8	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	395	2	1	3	4.7	O=C(O)C1(F)CCN(C2CCC3(Cc4ccccc4Oc4ccccc43)C2)CC1	10.1021/jm100856p
	CHEMBL1277217	18692	None	0	Human	Functional	pKi	=	6.8	6.8	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	395	2	1	3	4.7	O=C(O)C1(F)CCN(C2CCC3(Cc4ccccc4Oc4ccccc43)C2)CC1	10.1021/jm100856p
	49836189	18787	None	0	Human	Functional	pKi	=	6.8	6.8	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	373	2	1	2	4.3	O=C(O)C1=CCCN(C2CC[C@@]3(Cc4ccccc4Cc4ccccc43)C2)C1	10.1021/jm100856p
	CHEMBL1278021	18787	None	0	Human	Functional	pKi	=	6.8	6.8	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	373	2	1	2	4.3	O=C(O)C1=CCCN(C2CC[C@@]3(Cc4ccccc4Cc4ccccc43)C2)C1	10.1021/jm100856p
	44454309	97692	None	0	Human	Functional	pKi	=	6.8	6.8	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	514	6	1	8	4.3	Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6c(cc5CC4)OCC(=O)N6)n3C)cccc2n1	10.1016/j.bmcl.2007.12.066
	CHEMBL271066	97692	None	0	Human	Functional	pKi	=	6.8	6.8	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	514	6	1	8	4.3	Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6c(cc5CC4)OCC(=O)N6)n3C)cccc2n1	10.1016/j.bmcl.2007.12.066
	11568714	95360	None	0	Human	Functional	pKi	=	5.8	5.8	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	454	6	0	9	4.3	Cc1nc2cc3c(cc2s1)CCN(CCCSc1nnc(-c2ocnc2C)n1C)CC3	10.1016/j.bmcl.2007.12.066
	CHEMBL256471	95360	None	0	Human	Functional	pKi	=	5.8	5.8	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	454	6	0	9	4.3	Cc1nc2cc3c(cc2s1)CCN(CCCSc1nnc(-c2ocnc2C)n1C)CC3	10.1016/j.bmcl.2007.12.066
	11606378	95368	None	0	Human	Functional	pKi	=	5.8	5.8	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	548	7	0	8	6.2	Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc6nc(C(C)(F)F)oc6c5CC4)n3C)cccc2n1	10.1016/j.bmcl.2007.12.042
	CHEMBL256488	95368	None	0	Human	Functional	pKi	=	5.8	5.8	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	548	7	0	8	6.2	Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc6nc(C(C)(F)F)oc6c5CC4)n3C)cccc2n1	10.1016/j.bmcl.2007.12.042
	11533473	97604	None	0	Human	Functional	pKi	=	5.8	5.8	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	503	6	0	9	4.3	Cc1cnc(-c2nnc(SCCCN3CCc4ccc5oc(C(F)(F)F)nc5c4CC3)n2C)cn1	10.1016/j.bmcl.2007.12.042
	CHEMBL270602	97604	None	0	Human	Functional	pKi	=	5.8	5.8	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	503	6	0	9	4.3	Cc1cnc(-c2nnc(SCCCN3CCc4ccc5oc(C(F)(F)F)nc5c4CC3)n2C)cn1	10.1016/j.bmcl.2007.12.042
	44454401	155230	None	0	Human	Functional	pKi	=	5.8	5.8	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	554	6	0	8	6.7	Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6nc(C(C)(C)C)oc6c(C)c5CC4)n3C)cccc2n1	10.1016/j.bmcl.2007.12.066
	CHEMBL402087	155230	None	0	Human	Functional	pKi	=	5.8	5.8	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	554	6	0	8	6.7	Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6nc(C(C)(C)C)oc6c(C)c5CC4)n3C)cccc2n1	10.1016/j.bmcl.2007.12.066
	11504077	168932	None	0	Human	Functional	pKi	=	5.8	5.8	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	488	7	0	9	4.6	Cc1ncoc1-c1nnc(SCCCN2CCc3ccc4oc(C(C)(F)F)nc4c3CC2)n1C	10.1016/j.bmcl.2007.12.042
	CHEMBL437792	168932	None	0	Human	Functional	pKi	=	5.8	5.8	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	488	7	0	9	4.6	Cc1ncoc1-c1nnc(SCCCN2CCc3ccc4oc(C(C)(F)F)nc4c3CC2)n1C	10.1016/j.bmcl.2007.12.042
	52937733	61335	None	0	Human	Functional	pKi	=	5.8	5.8	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	393	6	0	6	3.1	COc1ccc(Cc2nn(C[C@H]3CCCN3C)c(=O)c3ccccc23)cc1OC	10.1021/jm1013874
	CHEMBL1767150	61335	None	0	Human	Functional	pKi	=	5.8	5.8	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	393	6	0	6	3.1	COc1ccc(Cc2nn(C[C@H]3CCCN3C)c(=O)c3ccccc23)cc1OC	10.1021/jm1013874
	57391843	69726	None	0	Human	Functional	pKi	=	7.8	7.8	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	436	5	0	5	3.3	O=C(CN1CCCC(c2nc3ccccc3n2Cc2ccc(F)cc2)C1)N1CCOCC1	10.1016/j.bmcl.2011.10.115
	CHEMBL1935434	69726	None	0	Human	Functional	pKi	=	7.8	7.8	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	436	5	0	5	3.3	O=C(CN1CCCC(c2nc3ccccc3n2Cc2ccc(F)cc2)C1)N1CCOCC1	10.1016/j.bmcl.2011.10.115
	24804150	80511	None	0	Human	Functional	pKi	=	7.8	7.8	-	0	Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay	ChEMBL	641	14	0	7	7.2	O=c1c2ccncc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1	10.1016/j.bmc.2012.08.032
	CHEMBL2146813	80511	None	0	Human	Functional	pKi	=	7.8	7.8	-	0	Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay	ChEMBL	641	14	0	7	7.2	O=c1c2ccncc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1	10.1016/j.bmc.2012.08.032
	49836412	18731	None	0	Human	Functional	pKi	=	7.7	7.7	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	375	2	1	2	4.4	O=C(O)[C@@H]1CCCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1	10.1021/jm100856p
	CHEMBL1277584	18731	None	0	Human	Functional	pKi	=	7.7	7.7	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	375	2	1	2	4.4	O=C(O)[C@@H]1CCCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1	10.1021/jm100856p
	49836295	18773	None	0	Human	Functional	pKi	=	7.7	7.7	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	373	2	1	2	4.3	O=C(O)C1=CCCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1	10.1021/jm100856p
	CHEMBL1277935	18773	None	0	Human	Functional	pKi	=	7.7	7.7	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	373	2	1	2	4.3	O=C(O)C1=CCCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1	10.1021/jm100856p
	57780008	149814	None	0	Human	Functional	pKi	=	7.7	7.7	-	0	Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay	ChEMBL	472	9	0	5	5.2	c1cnc2c(N3CCN(CCc4ccc(OCCCN5CCCCCC5)cc4)CC3)cccc2c1	10.1016/j.bmcl.2016.11.022
	CHEMBL3947980	149814	None	0	Human	Functional	pKi	=	7.7	7.7	-	0	Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay	ChEMBL	472	9	0	5	5.2	c1cnc2c(N3CCN(CCc4ccc(OCCCN5CCCCCC5)cc4)CC3)cccc2c1	10.1016/j.bmcl.2016.11.022
	49864886	15752	None	0	Human	Functional	pKi	=	7.7	7.7	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay	ChEMBL	366	4	1	5	2.6	CC1CN(C2=Cc3ccccc3Cn3ccnc32)CC(C)N1CCC(=O)O	10.1016/j.bmcl.2010.07.029
	CHEMBL1222624	15752	None	0	Human	Functional	pKi	=	7.7	7.7	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay	ChEMBL	366	4	1	5	2.6	CC1CN(C2=Cc3ccccc3Cn3ccnc32)CC(C)N1CCC(=O)O	10.1016/j.bmcl.2010.07.029
	24803799	61346	None	0	Human	Functional	pKi	=	7.7	7.7	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	654	13	0	6	8.3	O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C1CCCN(CCCCc2ccc(OCCCN3CCCCCC3)cc2)CC1	10.1021/jm1013874
	CHEMBL1767161	61346	None	0	Human	Functional	pKi	=	7.7	7.7	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	654	13	0	6	8.3	O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C1CCCN(CCCCc2ccc(OCCCN3CCCCCC3)cc2)CC1	10.1021/jm1013874
	49836635	18674	None	0	Human	Functional	pKi	=	6.7	6.7	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	359	2	1	2	4.0	O=C(O)C=C1CN(C2CCC3(Cc4ccccc4Cc4ccccc43)C2)C1	10.1021/jm100856p
	CHEMBL1277035	18674	None	0	Human	Functional	pKi	=	6.7	6.7	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	359	2	1	2	4.0	O=C(O)C=C1CN(C2CCC3(Cc4ccccc4Cc4ccccc43)C2)C1	10.1021/jm100856p
	49836741	18720	None	0	Human	Functional	pKi	=	6.7	6.7	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	425	2	1	4	4.8	O=C(O)C1CCN(C2CCC3(C2)C(=O)c2cc(F)ccc2Sc2ccccc23)CC1	10.1021/jm100856p
	CHEMBL1277491	18720	None	0	Human	Functional	pKi	=	6.7	6.7	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	425	2	1	4	4.8	O=C(O)C1CCN(C2CCC3(C2)C(=O)c2cc(F)ccc2Sc2ccccc23)CC1	10.1021/jm100856p
	49836842	18721	None	0	Human	Functional	pKi	=	6.7	6.7	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	425	2	1	4	4.9	O=C(O)[C@@H]1CCCN(C2CCC3(C2)C(=O)c2cc(Cl)ccc2Oc2ccccc23)C1	10.1021/jm100856p
	CHEMBL1277492	18721	None	0	Human	Functional	pKi	=	6.7	6.7	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	425	2	1	4	4.9	O=C(O)[C@@H]1CCCN(C2CCC3(C2)C(=O)c2cc(Cl)ccc2Oc2ccccc23)C1	10.1021/jm100856p
	57780016	150385	None	0	Human	Functional	pKi	=	6.7	6.7	-	0	Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay	ChEMBL	542	11	1	6	5.3	O=C(O)/C=C/c1ccc2cccc(N3CCN(CCc4ccc(OCCCN5CCCCCC5)cc4)CC3)c2n1	10.1016/j.bmcl.2016.11.022
	CHEMBL3952802	150385	None	0	Human	Functional	pKi	=	6.7	6.7	-	0	Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay	ChEMBL	542	11	1	6	5.3	O=C(O)/C=C/c1ccc2cccc(N3CCN(CCc4ccc(OCCCN5CCCCCC5)cc4)CC3)c2n1	10.1016/j.bmcl.2016.11.022
	11585248	95367	None	0	Human	Functional	pKi	=	5.7	5.7	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	604	8	0	8	6.8	CCc1nc2cc3c(c(Br)c2o1)CCN(CCCCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3	10.1016/j.bmcl.2007.12.066
	CHEMBL256482	95367	None	0	Human	Functional	pKi	=	5.7	5.7	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	604	8	0	8	6.8	CCc1nc2cc3c(c(Br)c2o1)CCN(CCCCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3	10.1016/j.bmcl.2007.12.066
	11669953	95593	None	0	Human	Functional	pKi	=	5.7	5.7	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	468	6	0	9	2.7	Cc1ncoc1-c1nnc(SCCCN2CCc3cc4c(cc3CC2)N(C)C(=O)CO4)n1C	10.1016/j.bmcl.2007.12.066
	CHEMBL257534	95593	None	0	Human	Functional	pKi	=	5.7	5.7	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	468	6	0	9	2.7	Cc1ncoc1-c1nnc(SCCCN2CCc3cc4c(cc3CC2)N(C)C(=O)CO4)n1C	10.1016/j.bmcl.2007.12.066
	44454278	95594	None	0	Human	Functional	pKi	=	5.7	5.7	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	454	6	1	9	2.7	Cc1ncoc1-c1nnc(SCCCN2CCc3cc4c(cc3CC2)OCC(=O)N4)n1C	10.1016/j.bmcl.2007.12.066
	CHEMBL257536	95594	None	0	Human	Functional	pKi	=	5.7	5.7	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	454	6	1	9	2.7	Cc1ncoc1-c1nnc(SCCCN2CCc3cc4c(cc3CC2)OCC(=O)N4)n1C	10.1016/j.bmcl.2007.12.066
	11621352	97686	None	0	Human	Functional	pKi	=	5.7	5.7	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	602	7	0	8	6.7	Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc6oc(C(F)(F)C(F)(F)F)nc6c5CC4)n3C)cccc2n1	10.1016/j.bmcl.2007.12.042
	CHEMBL271034	97686	None	0	Human	Functional	pKi	=	5.7	5.7	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	602	7	0	8	6.7	Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc6oc(C(F)(F)C(F)(F)F)nc6c5CC4)n3C)cccc2n1	10.1016/j.bmcl.2007.12.042
	11677768	155664	None	0	Human	Functional	pKi	=	5.7	5.7	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	502	6	0	8	4.9	Cc1ccc(-c2nnc(SCCCN3CCc4ccc5oc(C(F)(F)F)nc5c4CC3)n2C)cn1	10.1016/j.bmcl.2007.12.042
	CHEMBL404404	155664	None	0	Human	Functional	pKi	=	5.7	5.7	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	502	6	0	8	4.9	Cc1ccc(-c2nnc(SCCCN3CCc4ccc5oc(C(F)(F)F)nc5c4CC3)n2C)cn1	10.1016/j.bmcl.2007.12.042
	44454353	156512	None	0	Human	Functional	pKi	=	5.7	5.7	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	483	6	0	8	4.6	Cc1ccc2c(-c3nnc(SCCCN4CCc5nc6ccccn6c5CC4)n3C)cccc2n1	10.1016/j.bmcl.2007.12.042
	CHEMBL406678	156512	None	0	Human	Functional	pKi	=	5.7	5.7	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	483	6	0	8	4.6	Cc1ccc2c(-c3nnc(SCCCN4CCc5nc6ccccn6c5CC4)n3C)cccc2n1	10.1016/j.bmcl.2007.12.042
	15986135	12333	None	0	Human	Functional	pKi	=	5.7	5.7	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilizationAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization	ChEMBL	457	7	0	4	3.7	O=C(c1ccc(F)cc1F)N1CCN(c2ccc(OCCCN3CCCCC3)cc2)C(=O)C1	10.1021/jm0708228
	CHEMBL1185220	12333	None	0	Human	Functional	pKi	=	5.7	5.7	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilizationAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization	ChEMBL	457	7	0	4	3.7	O=C(c1ccc(F)cc1F)N1CCN(c2ccc(OCCCN3CCCCC3)cc2)C(=O)C1	10.1021/jm0708228
	CHEMBL398812	12333	None	0	Human	Functional	pKi	=	5.7	5.7	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilizationAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization	ChEMBL	457	7	0	4	3.7	O=C(c1ccc(F)cc1F)N1CCN(c2ccc(OCCCN3CCCCC3)cc2)C(=O)C1	10.1021/jm0708228
	15986915	12778	None	0	Human	Functional	pKi	=	5.7	5.7	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilizationAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization	ChEMBL	455	7	0	4	4.1	O=C(c1ccc(Cl)cc1)N1CCN(c2ccc(OCCCN3CCCCC3)cc2)C(=O)C1	10.1021/jm0708228
	CHEMBL1187963	12778	None	0	Human	Functional	pKi	=	5.7	5.7	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilizationAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization	ChEMBL	455	7	0	4	4.1	O=C(c1ccc(Cl)cc1)N1CCN(c2ccc(OCCCN3CCCCC3)cc2)C(=O)C1	10.1021/jm0708228
	CHEMBL534512	12778	None	0	Human	Functional	pKi	=	5.7	5.7	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilizationAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization	ChEMBL	455	7	0	4	4.1	O=C(c1ccc(Cl)cc1)N1CCN(c2ccc(OCCCN3CCCCC3)cc2)C(=O)C1	10.1021/jm0708228
	24749508	12793	None	0	Human	Functional	pKi	=	5.7	5.7	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilizationAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization	ChEMBL	446	7	0	5	3.3	N#Cc1ccc(C(=O)N2CCN(c3ccc(OCCCN4CCCCC4)cc3)C(=O)C2)cc1	10.1021/jm0708228
	CHEMBL1188060	12793	None	0	Human	Functional	pKi	=	5.7	5.7	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilizationAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization	ChEMBL	446	7	0	5	3.3	N#Cc1ccc(C(=O)N2CCN(c3ccc(OCCCN4CCCCC4)cc3)C(=O)C2)cc1	10.1021/jm0708228
	CHEMBL534958	12793	None	0	Human	Functional	pKi	=	5.7	5.7	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilizationAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization	ChEMBL	446	7	0	5	3.3	N#Cc1ccc(C(=O)N2CCN(c3ccc(OCCCN4CCCCC4)cc3)C(=O)C2)cc1	10.1021/jm0708228
	15986914	12863	None	0	Human	Functional	pKi	=	5.7	5.7	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilizationAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization	ChEMBL	435	7	0	4	3.7	Cc1ccc(C(=O)N2CCN(c3ccc(OCCCN4CCCCC4)cc3)C(=O)C2)cc1	10.1021/jm0708228
	CHEMBL1188657	12863	None	0	Human	Functional	pKi	=	5.7	5.7	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilizationAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization	ChEMBL	435	7	0	4	3.7	Cc1ccc(C(=O)N2CCN(c3ccc(OCCCN4CCCCC4)cc3)C(=O)C2)cc1	10.1021/jm0708228
	CHEMBL536991	12863	None	0	Human	Functional	pKi	=	5.7	5.7	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilizationAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization	ChEMBL	435	7	0	4	3.7	Cc1ccc(C(=O)N2CCN(c3ccc(OCCCN4CCCCC4)cc3)C(=O)C2)cc1	10.1021/jm0708228
	15987452	91467	None	0	Human	Functional	pKi	=	5.7	5.7	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilizationAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization	ChEMBL	443	7	0	4	3.3	O=C(c1ccc(F)cc1F)N1CCN(c2ccc(OCCCN3CCCC3)cc2)C(=O)C1	10.1021/jm0708228
	CHEMBL240352	91467	None	0	Human	Functional	pKi	=	5.7	5.7	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilizationAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization	ChEMBL	443	7	0	4	3.3	O=C(c1ccc(F)cc1F)N1CCN(c2ccc(OCCCN3CCCC3)cc2)C(=O)C1	10.1021/jm0708228
	1524	2181	None	61	Human	Functional	pKi	=	8.7	8.7	-47	18	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	395	5	1	5	2.4	Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2	10.1021/jm300338m
	197	2181	None	61	Human	Functional	pKi	=	8.7	8.7	-47	18	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	395	5	1	5	2.4	Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2	10.1021/jm300338m
	3822	2181	None	61	Human	Functional	pKi	=	8.7	8.7	-47	18	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	395	5	1	5	2.4	Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2	10.1021/jm300338m
	3822.0	2181	None	61	Human	Functional	pKi	=	8.7	8.7	-47	18	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	395	5	1	5	2.4	Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2	10.1021/jm300338m
	88	2181	None	61	Human	Functional	pKi	=	8.7	8.7	-47	18	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	395	5	1	5	2.4	Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2	10.1021/jm300338m
	CHEMBL51	2181	None	61	Human	Functional	pKi	=	8.7	8.7	-47	18	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	395	5	1	5	2.4	Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2	10.1021/jm300338m
	DB12465	2181	None	61	Human	Functional	pKi	=	8.7	8.7	-47	18	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	395	5	1	5	2.4	Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2	10.1021/jm300338m
	45358442	61343	None	0	Human	Functional	pKi	=	8.6	8.6	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	381	3	0	4	4.3	CN1CCCCC(n2nc(Cc3ccc(Cl)cc3)c3ccccc3c2=O)C1	10.1021/jm1013874
	CHEMBL1767158	61343	None	0	Human	Functional	pKi	=	8.6	8.6	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	381	3	0	4	4.3	CN1CCCCC(n2nc(Cc3ccc(Cl)cc3)c3ccccc3c2=O)C1	10.1021/jm1013874
	53359025	62373	None	0	Human	Functional	pKi	=	5.6	5.6	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	339	5	1	3	2.5	O=C(CCCN1C2C3C4CC5C6C4C2C6C1(O)C53)c1ccc(F)cc1	10.1016/j.bmcl.2011.04.098
	CHEMBL1779058	62373	None	0	Human	Functional	pKi	=	5.6	5.6	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	339	5	1	3	2.5	O=C(CCCN1C2C3C4CC5C6C4C2C6C1(O)C53)c1ccc(F)cc1	10.1016/j.bmcl.2011.04.098
	57404031	69732	None	0	Human	Functional	pKi	=	7.6	7.6	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	402	7	0	6	4.5	c1ccc(OCCn2c(C3CCCN(Cc4ncco4)C3)nc3ccccc32)cc1	10.1016/j.bmcl.2011.10.115
	CHEMBL1935440	69732	None	0	Human	Functional	pKi	=	7.6	7.6	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	402	7	0	6	4.5	c1ccc(OCCn2c(C3CCCN(Cc4ncco4)C3)nc3ccccc32)cc1	10.1016/j.bmcl.2011.10.115
	49836411	18732	None	0	Human	Functional	pKi	=	7.6	7.6	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	389	3	1	2	4.8	O=C(O)CC1CCN(C2CCC3(Cc4ccccc4Cc4ccccc43)C2)CC1	10.1021/jm100856p
	CHEMBL1277585	18732	None	0	Human	Functional	pKi	=	7.6	7.6	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	389	3	1	2	4.8	O=C(O)CC1CCN(C2CCC3(Cc4ccccc4Cc4ccccc43)C2)CC1	10.1021/jm100856p
	49836295	18773	None	0	Human	Functional	pKi	=	7.6	7.6	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	373	2	1	2	4.3	O=C(O)C1=CCCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1	10.1021/jm100856p
	CHEMBL1277935	18773	None	0	Human	Functional	pKi	=	7.6	7.6	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	373	2	1	2	4.3	O=C(O)C1=CCCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1	10.1021/jm100856p
	49836187	18804	None	0	Human	Functional	pKi	=	7.6	7.6	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	335	4	2	2	3.7	O=C(O)CCNC1CC[C@@]2(Cc3ccccc3Cc3ccccc32)C1	10.1021/jm100856p
	CHEMBL1278115	18804	None	0	Human	Functional	pKi	=	7.6	7.6	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	335	4	2	2	3.7	O=C(O)CCNC1CC[C@@]2(Cc3ccccc3Cc3ccccc32)C1	10.1021/jm100856p
	23582308	145952	None	0	Human	Functional	pKi	=	7.6	7.6	-	0	Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay	ChEMBL	634	14	1	6	6.9	O=C(O)CCc1ccc2cc(Cc3ccccc3)cc(N3CCN(CCc4ccc(OCCCN5CCCCCC5)cc4)CC3)c2n1	10.1016/j.bmcl.2016.11.022
	CHEMBL3917428	145952	None	0	Human	Functional	pKi	=	7.6	7.6	-	0	Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay	ChEMBL	634	14	1	6	6.9	O=C(O)CCc1ccc2cc(Cc3ccccc3)cc(N3CCN(CCc4ccc(OCCCN5CCCCCC5)cc4)CC3)c2n1	10.1016/j.bmcl.2016.11.022
	46933089	15740	None	0	Human	Functional	pKi	=	7.6	7.6	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay	ChEMBL	366	4	1	5	2.5	CC(C)(CN1CCN(C2=Cc3ccccc3Cn3ccnc32)CC1)C(=O)O	10.1016/j.bmcl.2010.07.029
	CHEMBL1222554	15740	None	0	Human	Functional	pKi	=	7.6	7.6	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay	ChEMBL	366	4	1	5	2.5	CC(C)(CN1CCN(C2=Cc3ccccc3Cn3ccnc32)CC1)C(=O)O	10.1016/j.bmcl.2010.07.029
	49834051	15754	None	0	Human	Functional	pKi	=	7.6	7.6	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay	ChEMBL	364	3	1	5	2.2	O=C(O)C1CC(N2CCN(C3=Cc4ccccc4Cn4ccnc43)CC2)C1	10.1016/j.bmcl.2010.07.029
	CHEMBL1222626	15754	None	0	Human	Functional	pKi	=	7.6	7.6	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay	ChEMBL	364	3	1	5	2.2	O=C(O)C1CC(N2CCN(C3=Cc4ccccc4Cn4ccnc43)CC2)C1	10.1016/j.bmcl.2010.07.029
	24803482	61353	None	0	Human	Functional	pKi	=	7.6	7.6	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	640	14	0	6	7.8	O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1	10.1021/jm1013874
	CHEMBL1767168	61353	None	0	Human	Functional	pKi	=	7.6	7.6	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	640	14	0	6	7.8	O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1	10.1021/jm1013874
	11627879	95400	None	0	Human	Functional	pKi	=	6.6	6.6	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	528	6	0	8	4.3	Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6c(cc5CC4)N(C)C(=O)CO6)n3C)cccc2n1	10.1016/j.bmcl.2007.12.066
	CHEMBL256652	95400	None	0	Human	Functional	pKi	=	6.6	6.6	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	528	6	0	8	4.3	Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6c(cc5CC4)N(C)C(=O)CO6)n3C)cccc2n1	10.1016/j.bmcl.2007.12.066
	11577158	97860	None	0	Human	Functional	pKi	=	6.6	6.6	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	514	6	0	8	5.8	Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc6nc(C)sc6c5CC4)n3C)cccc2n1	10.1016/j.bmcl.2007.12.042
	CHEMBL271909	97860	None	0	Human	Functional	pKi	=	6.6	6.6	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	514	6	0	8	5.8	Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc6nc(C)sc6c5CC4)n3C)cccc2n1	10.1016/j.bmcl.2007.12.042
	134143679	145990	None	0	Human	Functional	pKi	=	6.6	6.6	-	0	Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay	ChEMBL	516	10	1	6	4.9	O=C(O)c1ccc2cccc(N3CCN(CCc4ccc(OCCCN5CCCCCC5)cc4)CC3)c2n1	10.1016/j.bmcl.2016.11.022
	CHEMBL3917794	145990	None	0	Human	Functional	pKi	=	6.6	6.6	-	0	Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay	ChEMBL	516	10	1	6	4.9	O=C(O)c1ccc2cccc(N3CCN(CCc4ccc(OCCCN5CCCCCC5)cc4)CC3)c2n1	10.1016/j.bmcl.2016.11.022
	44454120	95225	None	0	Human	Functional	pKi	=	5.6	5.6	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	438	6	0	9	3.8	Cc1nc2cc3c(cc2o1)CCN(CCCSc1nnc(-c2ocnc2C)n1C)CC3	10.1016/j.bmcl.2007.12.066
	CHEMBL255827	95225	None	0	Human	Functional	pKi	=	5.6	5.6	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	438	6	0	9	3.8	Cc1nc2cc3c(cc2o1)CCN(CCCSc1nnc(-c2ocnc2C)n1C)CC3	10.1016/j.bmcl.2007.12.066
	11548755	97708	None	0	Human	Functional	pKi	=	5.6	5.6	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	580	7	0	8	6.8	Cc1ccc2c(-c3nnc(SCCCCN4CCc5cc6nc(C(F)(F)F)oc6c(C)c5CC4)n3C)cccc2n1	10.1016/j.bmcl.2007.12.066
	CHEMBL271097	97708	None	0	Human	Functional	pKi	=	5.6	5.6	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	580	7	0	8	6.8	Cc1ccc2c(-c3nnc(SCCCCN4CCc5cc6nc(C(F)(F)F)oc6c(C)c5CC4)n3C)cccc2n1	10.1016/j.bmcl.2007.12.066
	44454443	97816	None	0	Human	Functional	pKi	=	5.6	5.6	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	449	6	0	9	3.6	Cc1cnc(-c2nnc(SCCCN3CCc4ccc5c(C)noc5c4CC3)n2C)cn1	10.1016/j.bmcl.2007.12.042
	CHEMBL271702	97816	None	0	Human	Functional	pKi	=	5.6	5.6	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	449	6	0	9	3.6	Cc1cnc(-c2nnc(SCCCN3CCc4ccc5c(C)noc5c4CC3)n2C)cn1	10.1016/j.bmcl.2007.12.042
	11641596	97851	None	0	Human	Functional	pKi	=	5.6	5.6	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	484	6	0	8	5.1	Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6ncoc6cc5CC4)n3C)cccc2n1	10.1016/j.bmcl.2007.12.066
	CHEMBL271844	97851	None	0	Human	Functional	pKi	=	5.6	5.6	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	484	6	0	8	5.1	Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6ncoc6cc5CC4)n3C)cccc2n1	10.1016/j.bmcl.2007.12.066
	15986645	12875	None	0	Human	Functional	pKi	=	5.6	5.6	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilizationAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization	ChEMBL	451	5	0	4	3.7	O=C(c1ccc(F)cc1)N1CCN(c2ccc(OC3CCN(C4CCC4)CC3)cc2)C(=O)C1	10.1021/jm0708228
	CHEMBL1188742	12875	None	0	Human	Functional	pKi	=	5.6	5.6	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilizationAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization	ChEMBL	451	5	0	4	3.7	O=C(c1ccc(F)cc1)N1CCN(c2ccc(OC3CCN(C4CCC4)CC3)cc2)C(=O)C1	10.1021/jm0708228
	CHEMBL537219	12875	None	0	Human	Functional	pKi	=	5.6	5.6	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilizationAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization	ChEMBL	451	5	0	4	3.7	O=C(c1ccc(F)cc1)N1CCN(c2ccc(OC3CCN(C4CCC4)CC3)cc2)C(=O)C1	10.1021/jm0708228
	44250284	197678	None	0	Human	Functional	pKi	=	8.4	8.4	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	436	6	0	5	4.6	CN(CC1CCOCC1)C1CCN(c2nc3ccccc3n2Cc2ccc(F)cc2)CC1	10.1016/j.bmcl.2011.10.115
	CHEMBL550818	197678	None	0	Human	Functional	pKi	=	8.4	8.4	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	436	6	0	5	4.6	CN(CC1CCOCC1)C1CCN(c2nc3ccccc3n2Cc2ccc(F)cc2)CC1	10.1016/j.bmcl.2011.10.115
	52944115	18805	None	0	Human	Functional	pKi	=	8.4	8.4	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	291	1	0	1	4.2	CN(C)C1CC[C@]2(Cc3ccccc3Cc3ccccc32)C1	10.1021/jm100856p
	CHEMBL1278116	18805	None	0	Human	Functional	pKi	=	8.4	8.4	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	291	1	0	1	4.2	CN(C)C1CC[C@]2(Cc3ccccc3Cc3ccccc32)C1	10.1021/jm100856p
	49836526	18655	None	0	Human	Functional	pKi	=	7.5	7.5	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	375	3	1	2	4.4	O=C(O)CC1CCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1	10.1021/jm100856p
	CHEMBL1276859	18655	None	0	Human	Functional	pKi	=	7.5	7.5	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	375	3	1	2	4.4	O=C(O)CC1CCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1	10.1021/jm100856p
	49836528	18665	None	0	Human	Functional	pKi	=	7.5	7.5	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	373	2	1	2	4.0	O=C(O)[C@]12C[C@H]1CN(C1CC[C@]3(Cc4ccccc4Cc4ccccc43)C1)C2	10.1021/jm100856p
	CHEMBL1276947	18665	None	0	Human	Functional	pKi	=	7.5	7.5	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	373	2	1	2	4.0	O=C(O)[C@]12C[C@H]1CN(C1CC[C@]3(Cc4ccccc4Cc4ccccc43)C1)C2	10.1021/jm100856p
	49834052	15753	None	0	Human	Functional	pKi	=	7.5	7.5	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay	ChEMBL	350	4	1	5	2.0	C=C(CN1CCN(C2=Cc3ccccc3Cn3ccnc32)CC1)C(=O)O	10.1016/j.bmcl.2010.07.029
	CHEMBL1222625	15753	None	0	Human	Functional	pKi	=	7.5	7.5	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay	ChEMBL	350	4	1	5	2.0	C=C(CN1CCN(C2=Cc3ccccc3Cn3ccnc32)CC1)C(=O)O	10.1016/j.bmcl.2010.07.029
	52937828	61337	None	0	Human	Functional	pKi	=	7.5	7.5	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	347	5	0	4	3.3	CN1CCC[C@@H]1Cn1nc(CCc2ccccc2)c2ccccc2c1=O	10.1021/jm1013874
	CHEMBL1767152	61337	None	0	Human	Functional	pKi	=	7.5	7.5	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	347	5	0	4	3.3	CN1CCC[C@@H]1Cn1nc(CCc2ccccc2)c2ccccc2c1=O	10.1021/jm1013874
	49836634	18673	None	0	Human	Functional	pKi	=	6.5	6.5	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	361	3	1	2	4.0	O=C(O)CC1CN(C2CCC3(Cc4ccccc4Cc4ccccc43)C2)C1	10.1021/jm100856p
	CHEMBL1277034	18673	None	0	Human	Functional	pKi	=	6.5	6.5	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	361	3	1	2	4.0	O=C(O)CC1CN(C2CCC3(Cc4ccccc4Cc4ccccc43)C2)C1	10.1021/jm100856p
	44454434	97960	None	0	Human	Functional	pKi	=	5.5	5.5	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	512	6	0	7	4.5	Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6c(cc5CC4)C(=O)N(C)C6)n3C)cccc2n1	10.1016/j.bmcl.2007.12.066
	CHEMBL272480	97960	None	0	Human	Functional	pKi	=	5.5	5.5	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	512	6	0	7	4.5	Cc1ccc2c(-c3nnc(SCCCN4CCc5cc6c(cc5CC4)C(=O)N(C)C6)n3C)cccc2n1	10.1016/j.bmcl.2007.12.066
	57400502	69735	None	0	Human	Functional	pKi	=	6.4	6.4	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	321	3	1	4	3.4	Cc1ccc(Cn2c(C3CNCCO3)nc3ccccc32)cc1C	10.1016/j.bmcl.2011.10.115
	CHEMBL1935443	69735	None	0	Human	Functional	pKi	=	6.4	6.4	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	321	3	1	4	3.4	Cc1ccc(Cn2c(C3CNCCO3)nc3ccccc32)cc1C	10.1016/j.bmcl.2011.10.115
	49836527	18656	None	0	Human	Functional	pKi	=	7.4	7.4	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	373	2	1	2	3.9	O=C(O)[C@@H]1[C@H]2CN(C3CCC4(Cc5ccccc5Cc5ccccc54)C3)C[C@H]21	10.1021/jm100856p
	CHEMBL1276860	18656	None	0	Human	Functional	pKi	=	7.4	7.4	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	373	2	1	2	3.9	O=C(O)[C@@H]1[C@H]2CN(C3CCC4(Cc5ccccc5Cc5ccccc54)C3)C[C@H]21	10.1021/jm100856p
	49836410	18742	None	0	Human	Functional	pKi	=	7.4	7.4	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	393	2	1	2	4.5	O=C(O)C1(F)CCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)CC1	10.1021/jm100856p
	CHEMBL1277678	18742	None	0	Human	Functional	pKi	=	7.4	7.4	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	393	2	1	2	4.5	O=C(O)C1(F)CCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)CC1	10.1021/jm100856p
	49836298	18760	None	0	Human	Functional	pKi	=	7.4	7.4	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	373	2	1	2	4.3	O=C(O)C1=CCN(C2CCC3(Cc4ccccc4Cc4ccccc43)C2)CC1	10.1021/jm100856p
	CHEMBL1277854	18760	None	0	Human	Functional	pKi	=	7.4	7.4	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	373	2	1	2	4.3	O=C(O)C1=CCN(C2CCC3(Cc4ccccc4Cc4ccccc43)C2)CC1	10.1021/jm100856p
	49836296	18761	None	0	Human	Functional	pKi	=	7.4	7.4	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	391	2	1	2	4.5	O=C(O)C1=CCCN(C2CCC3(Cc4cc(F)ccc4Cc4ccccc43)C2)C1	10.1021/jm100856p
	CHEMBL1277855	18761	None	0	Human	Functional	pKi	=	7.4	7.4	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	391	2	1	2	4.5	O=C(O)C1=CCCN(C2CCC3(Cc4cc(F)ccc4Cc4ccccc43)C2)C1	10.1021/jm100856p
	57780018	144641	None	0	Human	Functional	pKi	=	7.4	7.4	-	0	Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay	ChEMBL	544	12	1	6	5.3	O=C(O)CCc1cnc2c(N3CCN(CCc4ccc(OCCCN5CCCCCC5)cc4)CC3)cccc2c1	10.1016/j.bmcl.2016.11.022
	CHEMBL3907368	144641	None	0	Human	Functional	pKi	=	7.4	7.4	-	0	Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay	ChEMBL	544	12	1	6	5.3	O=C(O)CCc1cnc2c(N3CCN(CCc4ccc(OCCCN5CCCCCC5)cc4)CC3)cccc2c1	10.1016/j.bmcl.2016.11.022
	49833883	15768	None	0	Human	Functional	pKi	=	7.4	7.4	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay	ChEMBL	394	4	1	5	3.1	Cc1nc2n(c1C)Cc1ccccc1C=C2N1CCN(CC(C)(C)C(=O)O)CC1	10.1016/j.bmcl.2010.07.029
	CHEMBL1222693	15768	None	0	Human	Functional	pKi	=	7.4	7.4	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay	ChEMBL	394	4	1	5	3.1	Cc1nc2n(c1C)Cc1ccccc1C=C2N1CCN(CC(C)(C)C(=O)O)CC1	10.1016/j.bmcl.2010.07.029
	46933090	15783	None	0	Human	Functional	pKi	=	7.4	7.4	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay	ChEMBL	400	4	1	5	3.1	CC(C)(CN1CCN(C2=Cc3ccccc3Cn3c(Cl)cnc32)CC1)C(=O)O	10.1016/j.bmcl.2010.07.029
	CHEMBL1222762	15783	None	0	Human	Functional	pKi	=	7.4	7.4	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay	ChEMBL	400	4	1	5	3.1	CC(C)(CN1CCN(C2=Cc3ccccc3Cn3c(Cl)cnc32)CC1)C(=O)O	10.1016/j.bmcl.2010.07.029
	49834053	15784	None	0	Human	Functional	pKi	=	7.4	7.4	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay	ChEMBL	384	4	1	5	2.6	CC(C)(CN1CCN(C2=Cc3ccccc3Cn3cc(F)nc32)CC1)C(=O)O	10.1016/j.bmcl.2010.07.029
	CHEMBL1222763	15784	None	0	Human	Functional	pKi	=	7.4	7.4	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay	ChEMBL	384	4	1	5	2.6	CC(C)(CN1CCN(C2=Cc3ccccc3Cn3cc(F)nc32)CC1)C(=O)O	10.1016/j.bmcl.2010.07.029
	24803316	61347	None	0	Human	Functional	pKi	=	7.4	7.4	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	600	15	1	6	6.9	O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1CCNCCCCc1ccc(OCCCN2CCCCCC2)cc1	10.1021/jm1013874
	CHEMBL1767162	61347	None	0	Human	Functional	pKi	=	7.4	7.4	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	600	15	1	6	6.9	O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1CCNCCCCc1ccc(OCCCN2CCCCCC2)cc1	10.1021/jm1013874
	24803480	61348	None	0	Human	Functional	pKi	=	7.4	7.4	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	614	15	0	6	7.2	CN(CCCCc1ccc(OCCCN2CCCCCC2)cc1)CCn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O	10.1021/jm1013874
	CHEMBL1767163	61348	None	0	Human	Functional	pKi	=	7.4	7.4	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	614	15	0	6	7.2	CN(CCCCc1ccc(OCCCN2CCCCCC2)cc1)CCn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O	10.1021/jm1013874
	11548239	95352	None	0	Human	Functional	pKi	=	6.4	6.4	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	528	7	0	8	6.1	CCc1nc2ccc3c(c2s1)CCN(CCCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3	10.1016/j.bmcl.2007.12.042
	CHEMBL256442	95352	None	0	Human	Functional	pKi	=	6.4	6.4	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	528	7	0	8	6.1	CCc1nc2ccc3c(c2s1)CCN(CCCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3	10.1016/j.bmcl.2007.12.042
	134150412	152191	None	0	Human	Functional	pKi	=	6.4	6.4	-	0	Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay	ChEMBL	516	10	1	6	4.9	O=C(O)c1cnc2c(N3CCN(CCc4ccc(OCCCN5CCCCCC5)cc4)CC3)cccc2c1	10.1016/j.bmcl.2016.11.022
	CHEMBL3967709	152191	None	0	Human	Functional	pKi	=	6.4	6.4	-	0	Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay	ChEMBL	516	10	1	6	4.9	O=C(O)c1cnc2c(N3CCN(CCc4ccc(OCCCN5CCCCCC5)cc4)CC3)cccc2c1	10.1016/j.bmcl.2016.11.022
	52937632	61328	None	0	Human	Functional	pKi	=	6.4	6.4	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	389	4	0	4	4.4	CN1CCC[C@@H]1Cn1nc(Cc2ccc(C(C)(C)C)cc2)c2ccccc2c1=O	10.1021/jm1013874
	CHEMBL1767142	61328	None	0	Human	Functional	pKi	=	6.4	6.4	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	389	4	0	4	4.4	CN1CCC[C@@H]1Cn1nc(Cc2ccc(C(C)(C)C)cc2)c2ccccc2c1=O	10.1021/jm1013874
	11497679	155654	None	0	Human	Functional	pKi	=	5.4	5.4	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	552	6	0	8	6.1	Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc6nc(C(F)(F)F)oc6c5CC4)n3C)cccc2n1	10.1016/j.bmcl.2007.12.042
	CHEMBL404363	155654	None	0	Human	Functional	pKi	=	5.4	5.4	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	552	6	0	8	6.1	Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc6nc(C(F)(F)F)oc6c5CC4)n3C)cccc2n1	10.1016/j.bmcl.2007.12.042
	57400504	69737	None	0	Human	Functional	pKi	=	8.4	8.4	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	327	3	1	4	3.6	Fc1ccc(Cn2c(C3CNCCS3)nc3ccccc32)cc1	10.1016/j.bmcl.2011.10.115
	CHEMBL1935445	69737	None	0	Human	Functional	pKi	=	8.4	8.4	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	327	3	1	4	3.6	Fc1ccc(Cn2c(C3CNCCS3)nc3ccccc32)cc1	10.1016/j.bmcl.2011.10.115
	57402314	69725	None	0	Human	Functional	pKi	=	8.3	8.3	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	434	5	0	4	4.4	O=C(CN1CCCC(c2nc3ccccc3n2Cc2ccc(F)cc2)C1)N1CCCCC1	10.1016/j.bmcl.2011.10.115
	CHEMBL1935433	69725	None	0	Human	Functional	pKi	=	8.3	8.3	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	434	5	0	4	4.4	O=C(CN1CCCC(c2nc3ccccc3n2Cc2ccc(F)cc2)C1)N1CCCCC1	10.1016/j.bmcl.2011.10.115
	57393573	69731	None	0	Human	Functional	pKi	=	8.3	8.3	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	406	7	0	5	3.4	CN(C)C(=O)CN1CCCC(c2nc3ccccc3n2CCOc2ccccc2)C1	10.1016/j.bmcl.2011.10.115
	CHEMBL1935439	69731	None	0	Human	Functional	pKi	=	8.3	8.3	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	406	7	0	5	3.4	CN(C)C(=O)CN1CCCC(c2nc3ccccc3n2CCOc2ccccc2)C1	10.1016/j.bmcl.2011.10.115
	16681693	82604	None	1	Human	Functional	pKi	=	7.3	7.3	-	0	Antagonist activity at histamine H1 receptor expressed in human PC3 cells inhibition of histamine-induced calcium influx by cell based assayAntagonist activity at histamine H1 receptor expressed in human PC3 cells inhibition of histamine-induced calcium influx by cell based assay	ChEMBL	487	5	1	5	3.6	Cc1ccc(C(=O)N2CCC(=CC(=O)N[C@@H]3CCN(Cc4ccc5cc(F)ccc5c4)C3)CC2)nn1	10.1021/jm300682j
	CHEMBL2178580	82604	None	1	Human	Functional	pKi	=	7.3	7.3	-	0	Antagonist activity at histamine H1 receptor expressed in human PC3 cells inhibition of histamine-induced calcium influx by cell based assayAntagonist activity at histamine H1 receptor expressed in human PC3 cells inhibition of histamine-induced calcium influx by cell based assay	ChEMBL	487	5	1	5	3.6	Cc1ccc(C(=O)N2CCC(=CC(=O)N[C@@H]3CCN(Cc4ccc5cc(F)ccc5c4)C3)CC2)nn1	10.1021/jm300682j
	52937629	61324	None	0	Human	Functional	pKi	=	8.3	8.3	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	377	6	0	5	3.5	CCOc1ccc(Cc2nn(C[C@H]3CCCN3C)c(=O)c3ccccc23)cc1	10.1021/jm1013874
	CHEMBL1767139	61324	None	0	Human	Functional	pKi	=	8.3	8.3	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	377	6	0	5	3.5	CCOc1ccc(Cc2nn(C[C@H]3CCCN3C)c(=O)c3ccccc23)cc1	10.1021/jm1013874
	57395286	69723	None	0	Human	Functional	pKi	=	8.2	8.2	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	394	5	0	4	3.5	CN(C)C(=O)CN1CCCC(c2nc3ccccc3n2Cc2ccc(F)cc2)C1	10.1016/j.bmcl.2011.10.115
	CHEMBL1935431	69723	None	0	Human	Functional	pKi	=	8.2	8.2	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	394	5	0	4	3.5	CN(C)C(=O)CN1CCCC(c2nc3ccccc3n2Cc2ccc(F)cc2)C1	10.1016/j.bmcl.2011.10.115
	49836637	18685	None	0	Human	Functional	pKi	=	7.3	7.3	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	375	2	1	3	4.5	O=C(O)C1=CCN(C2CCC3(Cc4ccccc4Oc4ccccc43)C2)CC1	10.1021/jm100856p
	CHEMBL1277126	18685	None	0	Human	Functional	pKi	=	7.3	7.3	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	375	2	1	3	4.5	O=C(O)C1=CCN(C2CCC3(Cc4ccccc4Oc4ccccc43)C2)CC1	10.1021/jm100856p
	25184832	18702	None	0	Human	Functional	pKi	=	7.3	7.3	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	349	2	1	3	3.8	O=C(O)C1CN(C2CCC3(Cc4ccccc4Oc4ccccc43)C2)C1	10.1021/jm100856p
	CHEMBL1277312	18702	None	0	Human	Functional	pKi	=	7.3	7.3	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	349	2	1	3	3.8	O=C(O)C1CN(C2CCC3(Cc4ccccc4Oc4ccccc43)C2)C1	10.1021/jm100856p
	49836409	18743	None	0	Human	Functional	pKi	=	7.3	7.3	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	391	2	2	3	3.5	O=C(O)C1(O)CCN(C2CCC3(Cc4ccccc4Cc4ccccc43)C2)CC1	10.1021/jm100856p
	CHEMBL1277679	18743	None	0	Human	Functional	pKi	=	7.3	7.3	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	391	2	2	3	3.5	O=C(O)C1(O)CCN(C2CCC3(Cc4ccccc4Cc4ccccc43)C2)CC1	10.1021/jm100856p
	49836300	18750	None	0	Human	Functional	pKi	=	7.3	7.3	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	389	2	1	2	4.8	CC1(C(=O)O)CCN(C2CCC3(Cc4ccccc4Cc4ccccc43)C2)CC1	10.1021/jm100856p
	CHEMBL1277769	18750	None	0	Human	Functional	pKi	=	7.3	7.3	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	389	2	1	2	4.8	CC1(C(=O)O)CCN(C2CCC3(Cc4ccccc4Cc4ccccc43)C2)CC1	10.1021/jm100856p
	49836299	18751	None	0	Human	Functional	pKi	=	7.3	7.3	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	375	2	1	2	4.4	O=C(O)C1CCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)CC1	10.1021/jm100856p
	CHEMBL1277770	18751	None	0	Human	Functional	pKi	=	7.3	7.3	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	375	2	1	2	4.4	O=C(O)C1CCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)CC1	10.1021/jm100856p
	49834050	15739	None	0	Human	Functional	pKi	=	7.3	7.3	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay	ChEMBL	338	4	1	5	1.8	O=C(O)CCN1CCN(C2=Cc3ccccc3Cn3ccnc32)CC1	10.1016/j.bmcl.2010.07.029
	CHEMBL1222553	15739	None	0	Human	Functional	pKi	=	7.3	7.3	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay	ChEMBL	338	4	1	5	1.8	O=C(O)CCN1CCN(C2=Cc3ccccc3Cn3ccnc32)CC1	10.1016/j.bmcl.2010.07.029
	49864885	15751	None	0	Human	Functional	pKi	=	7.3	7.3	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay	ChEMBL	380	4	1	5	2.9	CC(C)(CN1CCCN(C2=Cc3ccccc3Cn3ccnc32)CC1)C(=O)O	10.1016/j.bmcl.2010.07.029
	CHEMBL1222623	15751	None	0	Human	Functional	pKi	=	7.3	7.3	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay	ChEMBL	380	4	1	5	2.9	CC(C)(CN1CCCN(C2=Cc3ccccc3Cn3ccnc32)CC1)C(=O)O	10.1016/j.bmcl.2010.07.029
	49833884	15769	None	0	Human	Functional	pKi	=	7.3	7.3	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay	ChEMBL	380	4	1	5	2.8	Cc1cn2c(n1)C(N1CCN(CC(C)(C)C(=O)O)CC1)=Cc1ccccc1C2	10.1016/j.bmcl.2010.07.029
	CHEMBL1222694	15769	None	0	Human	Functional	pKi	=	7.3	7.3	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay	ChEMBL	380	4	1	5	2.8	Cc1cn2c(n1)C(N1CCN(CC(C)(C)C(=O)O)CC1)=Cc1ccccc1C2	10.1016/j.bmcl.2010.07.029
	24803641	61344	None	0	Human	Functional	pKi	=	7.3	7.3	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	612	10	0	6	7.5	O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C1CCCN(Cc2ccc(OCCCN3CCCCCC3)cc2)CC1	10.1021/jm1013874
	CHEMBL1767159	61344	None	0	Human	Functional	pKi	=	7.3	7.3	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	612	10	0	6	7.5	O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C1CCCN(Cc2ccc(OCCCN3CCCCCC3)cc2)CC1	10.1021/jm1013874
	11497680	97905	None	7	Human	Functional	pKi	=	6.3	6.3	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	552	6	0	8	6.1	Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc6oc(C(F)(F)F)nc6c5CC4)n3C)cccc2n1	10.1016/j.bmcl.2007.12.042
	CHEMBL272150	97905	None	7	Human	Functional	pKi	=	6.3	6.3	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	552	6	0	8	6.1	Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc6oc(C(F)(F)F)nc6c5CC4)n3C)cccc2n1	10.1016/j.bmcl.2007.12.042
	11519133	169526	None	0	Human	Functional	pKi	=	6.3	6.3	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	512	7	0	8	5.6	CCc1nc2c3c(ccc2o1)CCN(CCCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3	10.1016/j.bmcl.2007.12.042
	CHEMBL442456	169526	None	0	Human	Functional	pKi	=	6.3	6.3	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	512	7	0	8	5.6	CCc1nc2c3c(ccc2o1)CCN(CCCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3	10.1016/j.bmcl.2007.12.042
	57398829	69724	None	0	Human	Functional	pKi	=	8.2	8.2	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	422	7	0	4	4.3	CCN(CC)C(=O)CN1CCCC(c2nc3ccccc3n2Cc2ccc(F)cc2)C1	10.1016/j.bmcl.2011.10.115
	CHEMBL1935432	69724	None	0	Human	Functional	pKi	=	8.2	8.2	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	422	7	0	4	4.3	CCN(CC)C(=O)CN1CCCC(c2nc3ccccc3n2Cc2ccc(F)cc2)C1	10.1016/j.bmcl.2011.10.115
	49836633	18666	None	0	Human	Functional	pKi	=	8.2	8.2	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	347	2	1	2	3.6	O=C(O)C1CN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1	10.1021/jm100856p
	CHEMBL1276948	18666	None	0	Human	Functional	pKi	=	8.2	8.2	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	347	2	1	2	3.6	O=C(O)C1CN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1	10.1021/jm100856p
	52937119	61340	None	0	Human	Functional	pKi	=	8.2	8.2	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	367	4	0	4	3.6	CN1CCC(Cn2nc(Cc3ccc(Cl)cc3)c3ccccc3c2=O)C1	10.1021/jm1013874
	CHEMBL1767155	61340	None	0	Human	Functional	pKi	=	8.2	8.2	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	367	4	0	4	3.6	CN1CCC(Cn2nc(Cc3ccc(Cl)cc3)c3ccccc3c2=O)C1	10.1021/jm1013874
	45272895	198113	None	18	Human	Functional	pKi	=	8.2	8.2	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	389	4	0	5	4.6	Cc1cnn(C2CCN(c3nc4ccccc4n3Cc3ccc(F)cc3)CC2)c1	10.1016/j.bmcl.2011.10.115
	CHEMBL556450	198113	None	18	Human	Functional	pKi	=	8.2	8.2	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	389	4	0	5	4.6	Cc1cnn(C2CCN(c3nc4ccccc4n3Cc3ccc(F)cc3)CC2)c1	10.1016/j.bmcl.2011.10.115
	57400503	69736	None	0	Human	Functional	pKi	=	7.2	7.2	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	323	3	1	4	3.8	Cc1ccc(Cn2c(C3CNCCS3)nc3ccccc32)cc1	10.1016/j.bmcl.2011.10.115
	CHEMBL1935444	69736	None	0	Human	Functional	pKi	=	7.2	7.2	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	323	3	1	4	3.8	Cc1ccc(Cn2c(C3CNCCS3)nc3ccccc32)cc1	10.1016/j.bmcl.2011.10.115
	49836414	18801	None	0	Human	Functional	pKi	=	7.2	7.2	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	377	2	1	3	3.4	O=C(O)C1CN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)CCO1	10.1021/jm100856p
	CHEMBL1278112	18801	None	0	Human	Functional	pKi	=	7.2	7.2	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	377	2	1	3	3.4	O=C(O)C1CN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)CCO1	10.1021/jm100856p
	49833882	15767	None	0	Human	Functional	pKi	=	7.2	7.2	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay	ChEMBL	392	3	1	5	3.0	O=C(O)C1CCC(N2CCN(C3=Cc4ccccc4Cn4ccnc43)CC2)CC1	10.1016/j.bmcl.2010.07.029
	CHEMBL1222692	15767	None	0	Human	Functional	pKi	=	7.2	7.2	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay	ChEMBL	392	3	1	5	3.0	O=C(O)C1CCC(N2CCN(C3=Cc4ccccc4Cn4ccnc43)CC2)CC1	10.1016/j.bmcl.2010.07.029
	52937223	61342	None	20	Human	Functional	pKi	=	7.2	7.2	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	381	5	0	4	4.1	CN1CCCC1CCn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O	10.1021/jm1013874
	CHEMBL1767157	61342	None	20	Human	Functional	pKi	=	7.2	7.2	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	381	5	0	4	4.1	CN1CCCC1CCn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O	10.1021/jm1013874
	143	3515	None	36	Human	Functional	pKi	=	6.2	6.2	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	438	5	1	4	4.8	N#Cc1ccc2c(c1)CCN(C2)CC[C@@H]1CC[C@H](CC1)NC(=O)c1ccnc2c1cccc2	10.1016/j.bmcl.2007.12.042
	143	3515	None	36	Human	Functional	pKi	=	6.2	6.2	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	438	5	1	4	4.8	N#Cc1ccc2c(c1)CCN(C2)CC[C@@H]1CC[C@H](CC1)NC(=O)c1ccnc2c1cccc2	10.1016/j.bmcl.2007.12.066
	5311096	3515	None	36	Human	Functional	pKi	=	6.2	6.2	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	438	5	1	4	4.8	N#Cc1ccc2c(c1)CCN(C2)CC[C@@H]1CC[C@H](CC1)NC(=O)c1ccnc2c1cccc2	10.1016/j.bmcl.2007.12.042
	5311096	3515	None	36	Human	Functional	pKi	=	6.2	6.2	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	438	5	1	4	4.8	N#Cc1ccc2c(c1)CCN(C2)CC[C@@H]1CC[C@H](CC1)NC(=O)c1ccnc2c1cccc2	10.1016/j.bmcl.2007.12.066
	CHEMBL85606	3515	None	36	Human	Functional	pKi	=	6.2	6.2	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	438	5	1	4	4.8	N#Cc1ccc2c(c1)CCN(C2)CC[C@@H]1CC[C@H](CC1)NC(=O)c1ccnc2c1cccc2	10.1016/j.bmcl.2007.12.042
	CHEMBL85606	3515	None	36	Human	Functional	pKi	=	6.2	6.2	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	438	5	1	4	4.8	N#Cc1ccc2c(c1)CCN(C2)CC[C@@H]1CC[C@H](CC1)NC(=O)c1ccnc2c1cccc2	10.1016/j.bmcl.2007.12.066
	11569996	95365	None	0	Human	Functional	pKi	=	6.2	6.2	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	525	7	0	8	5.4	CCc1nn(C)c2cc3c(cc12)CCN(CCCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3	10.1016/j.bmcl.2007.12.066
	CHEMBL256477	95365	None	0	Human	Functional	pKi	=	6.2	6.2	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	525	7	0	8	5.4	CCc1nn(C)c2cc3c(cc12)CCN(CCCSc1nnc(-c2cccc4nc(C)ccc24)n1C)CC3	10.1016/j.bmcl.2007.12.066
	11518972	155122	None	0	Human	Functional	pKi	=	6.2	6.2	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	501	6	0	7	5.5	Cc1noc2cc3c(cc12)CCN(CCCSc1nnc(-c2ccc(C(F)(F)F)cc2)n1C)CC3	10.1016/j.bmcl.2007.12.066
	CHEMBL401576	155122	None	0	Human	Functional	pKi	=	6.2	6.2	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	501	6	0	7	5.5	Cc1noc2cc3c(cc12)CCN(CCCSc1nnc(-c2ccc(C(F)(F)F)cc2)n1C)CC3	10.1016/j.bmcl.2007.12.066
	52937633	61329	None	0	Human	Functional	pKi	=	6.2	6.2	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	391	5	0	6	2.9	COC(=O)c1ccc(Cc2nn(C[C@H]3CCCN3C)c(=O)c3ccccc23)cc1	10.1021/jm1013874
	CHEMBL1767143	61329	None	0	Human	Functional	pKi	=	6.2	6.2	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	391	5	0	6	2.9	COC(=O)c1ccc(Cc2nn(C[C@H]3CCCN3C)c(=O)c3ccccc23)cc1	10.1021/jm1013874
	24803638	61350	None	0	Human	Functional	pKi	=	8.1	8.1	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	636	15	0	7	7.1	COc1ccc(Cc2nn(C[C@H]3CCCN3CCCCc3ccc(OCCCN4CCCCCC4)cc3)c(=O)c3ccccc23)cc1	10.1021/jm1013874
	CHEMBL1767165	61350	None	0	Human	Functional	pKi	=	8.1	8.1	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	636	15	0	7	7.1	COc1ccc(Cc2nn(C[C@H]3CCCN3CCCCc3ccc(OCCCN4CCCCCC4)cc3)c(=O)c3ccccc23)cc1	10.1021/jm1013874
	49836639	18691	None	0	Human	Functional	pKi	=	7.1	7.1	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	377	2	1	3	4.6	O=C(O)C1CCN(C2CCC3(Cc4ccccc4Oc4ccccc43)C2)CC1	10.1021/jm100856p
	CHEMBL1277216	18691	None	0	Human	Functional	pKi	=	7.1	7.1	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	377	2	1	3	4.6	O=C(O)C1CCN(C2CCC3(Cc4ccccc4Oc4ccccc43)C2)CC1	10.1021/jm100856p
	49836739	18710	None	0	Human	Functional	pKi	=	7.1	7.1	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	387	2	1	3	4.0	O=C(O)C1=CCCN(C2CCC3(C2)C(=O)c2ccccc2Cc2ccccc23)C1	10.1021/jm100856p
	CHEMBL1277400	18710	None	0	Human	Functional	pKi	=	7.1	7.1	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	387	2	1	3	4.0	O=C(O)C1=CCCN(C2CCC3(C2)C(=O)c2ccccc2Cc2ccccc23)C1	10.1021/jm100856p
	134139893	146501	None	0	Human	Functional	pKi	=	7.1	7.1	-	0	Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay	ChEMBL	486	10	0	5	5.6	c1cnc2c(N3CCN(CCCc4ccc(OCCCN5CCCCCC5)cc4)CC3)cccc2c1	10.1016/j.bmcl.2016.11.022
	CHEMBL3921827	146501	None	0	Human	Functional	pKi	=	7.1	7.1	-	0	Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assayAntagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay	ChEMBL	486	10	0	5	5.6	c1cnc2c(N3CCN(CCCc4ccc(OCCCN5CCCCCC5)cc4)CC3)cccc2c1	10.1016/j.bmcl.2016.11.022
	46933091	15770	None	0	Human	Functional	pKi	=	7.1	7.1	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay	ChEMBL	400	4	1	5	3.1	CC(C)(CN1CCN(C2=Cc3ccccc3Cn3cc(Cl)nc32)CC1)C(=O)O	10.1016/j.bmcl.2010.07.029
	CHEMBL1222695	15770	None	0	Human	Functional	pKi	=	7.1	7.1	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in CHO cells by FLPR assay	ChEMBL	400	4	1	5	3.1	CC(C)(CN1CCN(C2=Cc3ccccc3Cn3cc(Cl)nc32)CC1)C(=O)O	10.1016/j.bmcl.2010.07.029
	52937734	61336	None	0	Human	Functional	pKi	=	7.1	7.1	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	339	4	0	4	3.6	CN1CCC[C@@H]1Cn1nc(CC2CCCCC2)c2ccccc2c1=O	10.1021/jm1013874
	CHEMBL1767151	61336	None	0	Human	Functional	pKi	=	7.1	7.1	-	0	Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay	ChEMBL	339	4	0	4	3.6	CN1CCC[C@@H]1Cn1nc(CC2CCCCC2)c2ccccc2c1=O	10.1021/jm1013874
	49836413	18784	None	0	Human	Functional	pKi	=	6.1	6.1	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	393	2	1	2	4.5	O=C(O)C1(F)CCCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1	10.1021/jm100856p
	CHEMBL1278019	18784	None	0	Human	Functional	pKi	=	6.1	6.1	-	0	Antagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assayAntagonist activity against human histamine H1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	393	2	1	2	4.5	O=C(O)C1(F)CCCN(C2CC[C@]3(Cc4ccccc4Cc4ccccc43)C2)C1	10.1021/jm100856p
	11584660	93321	None	8	Human	Functional	pKi	=	6.1	6.1	-	5	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	537	7	0	8	5.6	Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc(-c6cc(C)nn6C)cc5CC4)n3C)cccc2n1	10.1016/j.bmcl.2007.12.042
	CHEMBL244946	93321	None	8	Human	Functional	pKi	=	6.1	6.1	-	5	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	537	7	0	8	5.6	Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc(-c6cc(C)nn6C)cc5CC4)n3C)cccc2n1	10.1016/j.bmcl.2007.12.042
	44454190	98118	None	0	Human	Functional	pKi	=	6.1	6.1	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	537	7	0	8	5.6	Cc1cc2c(-c3nnc(SCCCN4CCc5ccc(-c6cc(C)nn6C)cc5CC4)n3C)cccc2cn1	10.1016/j.bmcl.2007.12.066
	CHEMBL273199	98118	None	0	Human	Functional	pKi	=	6.1	6.1	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	537	7	0	8	5.6	Cc1cc2c(-c3nnc(SCCCN4CCc5ccc(-c6cc(C)nn6C)cc5CC4)n3C)cccc2cn1	10.1016/j.bmcl.2007.12.066
	44454351	160701	None	0	Human	Functional	pKi	=	6.1	6.1	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	551	6	0	8	5.6	Cc1ccc2c(-c3nnc(SCCCN4CCc5nc6cc(C(F)(F)F)ccn6c5CC4)n3C)cccc2n1	10.1016/j.bmcl.2007.12.042
	CHEMBL411293	160701	None	0	Human	Functional	pKi	=	6.1	6.1	-	0	Antagonist activity at histamine H1 receptor by FLIPR assayAntagonist activity at histamine H1 receptor by FLIPR assay	ChEMBL	551	6	0	8	5.6	Cc1ccc2c(-c3nnc(SCCCN4CCc5nc6cc(C(F)(F)F)ccn6c5CC4)n3C)cccc2n1	10.1016/j.bmcl.2007.12.042
	57397055	69727	None	0	Human	Functional	pKi	=	8.1	8.1	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	390	5	0	5	4.6	Fc1ccc(Cn2c(C3CCCN(Cc4ncco4)C3)nc3ccccc32)cc1	10.1016/j.bmcl.2011.10.115
	CHEMBL1935435	69727	None	0	Human	Functional	pKi	=	8.1	8.1	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	390	5	0	5	4.6	Fc1ccc(Cn2c(C3CCCN(Cc4ncco4)C3)nc3ccccc32)cc1	10.1016/j.bmcl.2011.10.115
	57395286	69723	None	0	Human	Functional	pKi	=	8.1	8.1	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	394	5	0	4	3.5	CN(C)C(=O)CN1CCCC(c2nc3ccccc3n2Cc2ccc(F)cc2)C1	10.1016/j.bmcl.2011.10.115
	CHEMBL1935431	69723	None	0	Human	Functional	pKi	=	8.1	8.1	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	394	5	0	4	3.5	CN(C)C(=O)CN1CCCC(c2nc3ccccc3n2Cc2ccc(F)cc2)C1	10.1016/j.bmcl.2011.10.115
	57402230	69740	None	0	Human	Functional	pKi	=	7.0	7.0	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	339	4	1	5	3.5	COc1ccc(Cn2c(C3CNCCS3)nc3ccccc32)cc1	10.1016/j.bmcl.2011.10.115
	CHEMBL1935448	69740	None	0	Human	Functional	pKi	=	7.0	7.0	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	339	4	1	5	3.5	COc1ccc(Cn2c(C3CNCCS3)nc3ccccc32)cc1	10.1016/j.bmcl.2011.10.115
	57400504	69737	None	0	Human	Functional	pKi	=	7.0	7.0	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	327	3	1	4	3.6	Fc1ccc(Cn2c(C3CNCCS3)nc3ccccc32)cc1	10.1016/j.bmcl.2011.10.115
	CHEMBL1935445	69737	None	0	Human	Functional	pKi	=	7.0	7.0	-	0	Antagonist activity at histamine H1 receptorAntagonist activity at histamine H1 receptor	ChEMBL	327	3	1	4	3.6	Fc1ccc(Cn2c(C3CNCCS3)nc3ccccc32)cc1	10.1016/j.bmcl.2011.10.115
	2247	505	None	55	Human	Functional	pA2	=	8.1	8.1	-4	42	NoneNone	Drug Central	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	None
	249	505	None	55	Human	Functional	pA2	=	8.1	8.1	-4	42	NoneNone	Drug Central	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	None
	2603	505	None	55	Human	Functional	pA2	=	8.1	8.1	-4	42	NoneNone	Drug Central	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	None
	CHEMBL296419	505	None	55	Human	Functional	pA2	=	8.1	8.1	-4	42	NoneNone	Drug Central	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	None
	DB00637	505	None	55	Human	Functional	pA2	=	8.1	8.1	-4	42	NoneNone	Drug Central	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	None
	1204	1932	None	74	Rat	Functional	pEC50	=	8.3	8.3	-25	11	NoneNone	Drug Central	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
	1247	1932	None	74	Rat	Functional	pEC50	=	8.3	8.3	-25	11	NoneNone	Drug Central	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
	1375	1932	None	74	Rat	Functional	pEC50	=	8.3	8.3	-25	11	NoneNone	Drug Central	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
	774	1932	None	74	Rat	Functional	pEC50	=	8.3	8.3	-25	11	NoneNone	Drug Central	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
	774.0	1932	None	74	Rat	Functional	pEC50	=	8.3	8.3	-25	11	NoneNone	Drug Central	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
	CHEMBL90	1932	None	74	Rat	Functional	pEC50	=	8.3	8.3	-25	11	NoneNone	Drug Central	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
	DB05381	1932	None	74	Rat	Functional	pEC50	=	8.3	8.3	-25	11	NoneNone	Drug Central	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
	1204	1932	None	74	Guinea pig	Functional	pEC50	=	8.2	8.2	-10	11	NoneNone	Drug Central	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
	1247	1932	None	74	Guinea pig	Functional	pEC50	=	8.2	8.2	-10	11	NoneNone	Drug Central	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
	1375	1932	None	74	Guinea pig	Functional	pEC50	=	8.2	8.2	-10	11	NoneNone	Drug Central	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
	774	1932	None	74	Guinea pig	Functional	pEC50	=	8.2	8.2	-10	11	NoneNone	Drug Central	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
	774.0	1932	None	74	Guinea pig	Functional	pEC50	=	8.2	8.2	-10	11	NoneNone	Drug Central	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
	CHEMBL90	1932	None	74	Guinea pig	Functional	pEC50	=	8.2	8.2	-10	11	NoneNone	Drug Central	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
	DB05381	1932	None	74	Guinea pig	Functional	pEC50	=	8.2	8.2	-10	11	NoneNone	Drug Central	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
	1427	2013	None	42	Rat	Functional	pIC50	=	8.0	8.0	5	30	Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor	Drug Central	280	4	0	2	3.9	CN(CCCN1c2ccccc2CCc2c1cccc2)C	None
	357	2013	None	42	Rat	Functional	pIC50	=	8.0	8.0	5	30	Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor	Drug Central	280	4	0	2	3.9	CN(CCCN1c2ccccc2CCc2c1cccc2)C	None
	3696	2013	None	42	Rat	Functional	pIC50	=	8.0	8.0	5	30	Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor	Drug Central	280	4	0	2	3.9	CN(CCCN1c2ccccc2CCc2c1cccc2)C	None
	CHEMBL11	2013	None	42	Rat	Functional	pIC50	=	8.0	8.0	5	30	Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor	Drug Central	280	4	0	2	3.9	CN(CCCN1c2ccccc2CCc2c1cccc2)C	None
	DB00458	2013	None	42	Rat	Functional	pIC50	=	8.0	8.0	5	30	Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor	Drug Central	280	4	0	2	3.9	CN(CCCN1c2ccccc2CCc2c1cccc2)C	None
	1971	2866	None	32	Rat	Functional	pIC50	=	8.0	8.0	6	32	Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor	Drug Central	263	3	1	1	3.8	CNCCC=C1c2ccccc2CCc2c1cccc2	None
	2404	2866	None	32	Rat	Functional	pIC50	=	8.0	8.0	6	32	Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor	Drug Central	263	3	1	1	3.8	CNCCC=C1c2ccccc2CCc2c1cccc2	None
	4543	2866	None	32	Rat	Functional	pIC50	=	8.0	8.0	6	32	Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor	Drug Central	263	3	1	1	3.8	CNCCC=C1c2ccccc2CCc2c1cccc2	None
	4543.0	2866	None	32	Rat	Functional	pIC50	=	8.0	8.0	6	32	Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor	Drug Central	263	3	1	1	3.8	CNCCC=C1c2ccccc2CCc2c1cccc2	None
	CHEMBL445	2866	None	32	Rat	Functional	pIC50	=	8.0	8.0	6	32	Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor	Drug Central	263	3	1	1	3.8	CNCCC=C1c2ccccc2CCc2c1cccc2	None
	DB00540	2866	None	32	Rat	Functional	pIC50	=	8.0	8.0	6	32	Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor	Drug Central	263	3	1	1	3.8	CNCCC=C1c2ccccc2CCc2c1cccc2	None
	180	401	None	38	Rat	Functional	pIC50	=	8.0	8.0	3	38	Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor	Drug Central	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	None
	200	401	None	38	Rat	Functional	pIC50	=	8.0	8.0	3	38	Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor	Drug Central	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	None
	2160	401	None	38	Rat	Functional	pIC50	=	8.0	8.0	3	38	Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor	Drug Central	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	None
	2160.0	401	None	38	Rat	Functional	pIC50	=	8.0	8.0	3	38	Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor	Drug Central	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	None
	CHEMBL629	401	None	38	Rat	Functional	pIC50	=	8.0	8.0	3	38	Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor	Drug Central	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	None
	DB00321	401	None	38	Rat	Functional	pIC50	=	8.0	8.0	3	38	Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor	Drug Central	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	None
	40466858	16162	None	49	Guinea pig	Functional	pIC50	=	8.3	8.3	-5	4	Inhibition of H1 receptor in Cavia porcellus Hartley (guinea pig) ileum assessed as inhibition of histamine-induced spasms incubated 2 min prior histamine-challengeInhibition of H1 receptor in Cavia porcellus Hartley (guinea pig) ileum assessed as inhibition of histamine-induced spasms incubated 2 min prior histamine-challenge	Drug Central	348	6	1	3	4.0	Cc1ccc(/C(=C\CN2CCCC2)c2cccc(/C=C/C(=O)O)n2)cc1	None
	5284514	16162	None	49	Guinea pig	Functional	pIC50	=	8.3	8.3	-5	4	Inhibition of H1 receptor in Cavia porcellus Hartley (guinea pig) ileum assessed as inhibition of histamine-induced spasms incubated 2 min prior histamine-challengeInhibition of H1 receptor in Cavia porcellus Hartley (guinea pig) ileum assessed as inhibition of histamine-induced spasms incubated 2 min prior histamine-challenge	Drug Central	348	6	1	3	4.0	Cc1ccc(/C(=C\CN2CCCC2)c2cccc(/C=C/C(=O)O)n2)cc1	None
	5284514.0	16162	None	49	Guinea pig	Functional	pIC50	=	8.3	8.3	-5	4	Inhibition of H1 receptor in Cavia porcellus Hartley (guinea pig) ileum assessed as inhibition of histamine-induced spasms incubated 2 min prior histamine-challengeInhibition of H1 receptor in Cavia porcellus Hartley (guinea pig) ileum assessed as inhibition of histamine-induced spasms incubated 2 min prior histamine-challenge	Drug Central	348	6	1	3	4.0	Cc1ccc(/C(=C\CN2CCCC2)c2cccc(/C=C/C(=O)O)n2)cc1	None
	CHEMBL1224	16162	None	49	Guinea pig	Functional	pIC50	=	8.3	8.3	-5	4	Inhibition of H1 receptor in Cavia porcellus Hartley (guinea pig) ileum assessed as inhibition of histamine-induced spasms incubated 2 min prior histamine-challengeInhibition of H1 receptor in Cavia porcellus Hartley (guinea pig) ileum assessed as inhibition of histamine-induced spasms incubated 2 min prior histamine-challenge	Drug Central	348	6	1	3	4.0	Cc1ccc(/C(=C\CN2CCCC2)c2cccc(/C=C/C(=O)O)n2)cc1	None
	DB09488	16162	None	49	Guinea pig	Functional	pIC50	=	8.3	8.3	-5	4	Inhibition of H1 receptor in Cavia porcellus Hartley (guinea pig) ileum assessed as inhibition of histamine-induced spasms incubated 2 min prior histamine-challengeInhibition of H1 receptor in Cavia porcellus Hartley (guinea pig) ileum assessed as inhibition of histamine-induced spasms incubated 2 min prior histamine-challenge	Drug Central	348	6	1	3	4.0	Cc1ccc(/C(=C\CN2CCCC2)c2cccc(/C=C/C(=O)O)n2)cc1	None
	1599	2341	None	28	Human	Functional	pIC50	=	8.2	8.2	-3	32	NoneNone	Drug Central	476	7	1	3	5.1	Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1	None
	3955	2341	None	28	Human	Functional	pIC50	=	8.2	8.2	-3	32	NoneNone	Drug Central	476	7	1	3	5.1	Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1	None
	3955.0	2341	None	28	Human	Functional	pIC50	=	8.2	8.2	-3	32	NoneNone	Drug Central	476	7	1	3	5.1	Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1	None
	7215	2341	None	28	Human	Functional	pIC50	=	8.2	8.2	-3	32	NoneNone	Drug Central	476	7	1	3	5.1	Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1	None
	CHEMBL841	2341	None	28	Human	Functional	pIC50	=	8.2	8.2	-3	32	NoneNone	Drug Central	476	7	1	3	5.1	Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1	None
	DB00836	2341	None	28	Human	Functional	pIC50	=	8.2	8.2	-3	32	NoneNone	Drug Central	476	7	1	3	5.1	Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1	None
	4223	3992	None	57	Human	Functional	pIC50	=	8.2	8.2	-199	17	NoneNone	Drug Central	441	7	2	5	4.0	N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2	None
	6918314	3992	None	57	Human	Functional	pIC50	=	8.2	8.2	-199	17	NoneNone	Drug Central	441	7	2	5	4.0	N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2	None
	6918314.0	3992	None	57	Human	Functional	pIC50	=	8.2	8.2	-199	17	NoneNone	Drug Central	441	7	2	5	4.0	N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2	None
	7427	3992	None	57	Human	Functional	pIC50	=	8.2	8.2	-199	17	NoneNone	Drug Central	441	7	2	5	4.0	N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2	None
	CHEMBL439849	3992	None	57	Human	Functional	pIC50	=	8.2	8.2	-199	17	NoneNone	Drug Central	441	7	2	5	4.0	N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2	None
	DB06684	3992	None	57	Human	Functional	pIC50	=	8.2	8.2	-199	17	NoneNone	Drug Central	441	7	2	5	4.0	N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2	None
	40466858	16162	None	49	Human	Functional	pIC50	=	8.2	8.2	5	4	NoneNone	Drug Central	348	6	1	3	4.0	Cc1ccc(/C(=C\CN2CCCC2)c2cccc(/C=C/C(=O)O)n2)cc1	None
	5284514	16162	None	49	Human	Functional	pIC50	=	8.2	8.2	5	4	NoneNone	Drug Central	348	6	1	3	4.0	Cc1ccc(/C(=C\CN2CCCC2)c2cccc(/C=C/C(=O)O)n2)cc1	None
	5284514.0	16162	None	49	Human	Functional	pIC50	=	8.2	8.2	5	4	NoneNone	Drug Central	348	6	1	3	4.0	Cc1ccc(/C(=C\CN2CCCC2)c2cccc(/C=C/C(=O)O)n2)cc1	None
	CHEMBL1224	16162	None	49	Human	Functional	pIC50	=	8.2	8.2	5	4	NoneNone	Drug Central	348	6	1	3	4.0	Cc1ccc(/C(=C\CN2CCCC2)c2cccc(/C=C/C(=O)O)n2)cc1	None
	DB09488	16162	None	49	Human	Functional	pIC50	=	8.2	8.2	5	4	NoneNone	Drug Central	348	6	1	3	4.0	Cc1ccc(/C(=C\CN2CCCC2)c2cccc(/C=C/C(=O)O)n2)cc1	None
	2762	3863	None	23	Human	Functional	pIC50	=	8.1	8.1	100	9	Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor	Drug Central	255	6	0	3	2.7	CN(CCN(c1ccccn1)Cc1ccccc1)C	None
	5587	3863	None	23	Human	Functional	pIC50	=	8.1	8.1	100	9	Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor	Drug Central	255	6	0	3	2.7	CN(CCN(c1ccccn1)Cc1ccccc1)C	None
	5587.0	3863	None	23	Human	Functional	pIC50	=	8.1	8.1	100	9	Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor	Drug Central	255	6	0	3	2.7	CN(CCN(c1ccccn1)Cc1ccccc1)C	None
	7318	3863	None	23	Human	Functional	pIC50	=	8.1	8.1	100	9	Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor	Drug Central	255	6	0	3	2.7	CN(CCN(c1ccccn1)Cc1ccccc1)C	None
	CHEMBL1241	3863	None	23	Human	Functional	pIC50	=	8.1	8.1	100	9	Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor	Drug Central	255	6	0	3	2.7	CN(CCN(c1ccccn1)Cc1ccccc1)C	None
	DB00792	3863	None	23	Human	Functional	pIC50	=	8.1	8.1	100	9	Inhibitory activity against human Histamine H1 receptorInhibitory activity against human Histamine H1 receptor	Drug Central	255	6	0	3	2.7	CN(CCN(c1ccccn1)Cc1ccccc1)C	None
	1427	2013	None	42	Human	Functional	pIC50	=	8.1	8.1	-19	30	NoneNone	Drug Central	280	4	0	2	3.9	CN(CCCN1c2ccccc2CCc2c1cccc2)C	None
	357	2013	None	42	Human	Functional	pIC50	=	8.1	8.1	-19	30	NoneNone	Drug Central	280	4	0	2	3.9	CN(CCCN1c2ccccc2CCc2c1cccc2)C	None
	3696	2013	None	42	Human	Functional	pIC50	=	8.1	8.1	-19	30	NoneNone	Drug Central	280	4	0	2	3.9	CN(CCCN1c2ccccc2CCc2c1cccc2)C	None
	CHEMBL11	2013	None	42	Human	Functional	pIC50	=	8.1	8.1	-19	30	NoneNone	Drug Central	280	4	0	2	3.9	CN(CCCN1c2ccccc2CCc2c1cccc2)C	None
	DB00458	2013	None	42	Human	Functional	pIC50	=	8.1	8.1	-19	30	NoneNone	Drug Central	280	4	0	2	3.9	CN(CCCN1c2ccccc2CCc2c1cccc2)C	None
	2337	3256	None	51	Human	Functional	pIC50	=	8.1	8.1	-1	29	NoneNone	Drug Central	383	5	1	6	2.9	OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2	None
	50	3256	None	51	Human	Functional	pIC50	=	8.1	8.1	-1	29	NoneNone	Drug Central	383	5	1	6	2.9	OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2	None
	5002	3256	None	51	Human	Functional	pIC50	=	8.1	8.1	-1	29	NoneNone	Drug Central	383	5	1	6	2.9	OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2	None
	5002.0	3256	None	51	Human	Functional	pIC50	=	8.1	8.1	-1	29	NoneNone	Drug Central	383	5	1	6	2.9	OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2	None
	CHEMBL716	3256	None	51	Human	Functional	pIC50	=	8.1	8.1	-1	29	NoneNone	Drug Central	383	5	1	6	2.9	OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2	None
	DB01224	3256	None	51	Human	Functional	pIC50	=	8.1	8.1	-1	29	NoneNone	Drug Central	383	5	1	6	2.9	OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2	None
	10103	3416	None	40	Human	Functional	pIC50	=	8.1	8.1	28	2	Inhibitory concentration against histamine H1 receptorInhibitory concentration against histamine H1 receptor	Drug Central	415	2	0	3	5.6	Cc1cncc(c1)CN1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1	None
	133017	3416	None	40	Human	Functional	pIC50	=	8.1	8.1	28	2	Inhibitory concentration against histamine H1 receptorInhibitory concentration against histamine H1 receptor	Drug Central	415	2	0	3	5.6	Cc1cncc(c1)CN1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1	None
	133017.0	3416	None	40	Human	Functional	pIC50	=	8.1	8.1	28	2	Inhibitory concentration against histamine H1 receptorInhibitory concentration against histamine H1 receptor	Drug Central	415	2	0	3	5.6	Cc1cncc(c1)CN1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1	None
	2413	3416	None	40	Human	Functional	pIC50	=	8.1	8.1	28	2	Inhibitory concentration against histamine H1 receptorInhibitory concentration against histamine H1 receptor	Drug Central	415	2	0	3	5.6	Cc1cncc(c1)CN1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1	None
	CHEMBL91397	3416	None	40	Human	Functional	pIC50	=	8.1	8.1	28	2	Inhibitory concentration against histamine H1 receptorInhibitory concentration against histamine H1 receptor	Drug Central	415	2	0	3	5.6	Cc1cncc(c1)CN1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1	None
	DB11614	3416	None	40	Human	Functional	pIC50	=	8.1	8.1	28	2	Inhibitory concentration against histamine H1 receptorInhibitory concentration against histamine H1 receptor	Drug Central	415	2	0	3	5.6	Cc1cncc(c1)CN1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1	None
	1027	1576	None	51	Guinea pig	Functional	pIC50	=	8.1	8.1	6	7	Potency against histamine H1 receptor on guinea pig ileumPotency against histamine H1 receptor on guinea pig ileum	Drug Central	249	0	2	1	2.7	N=C1NCC2N1c1ccccc1Cc1c2cccc1	None
	3241	1576	None	51	Guinea pig	Functional	pIC50	=	8.1	8.1	6	7	Potency against histamine H1 receptor on guinea pig ileumPotency against histamine H1 receptor on guinea pig ileum	Drug Central	249	0	2	1	2.7	N=C1NCC2N1c1ccccc1Cc1c2cccc1	None
	3241.0	1576	None	51	Guinea pig	Functional	pIC50	=	8.1	8.1	6	7	Potency against histamine H1 receptor on guinea pig ileumPotency against histamine H1 receptor on guinea pig ileum	Drug Central	249	0	2	1	2.7	N=C1NCC2N1c1ccccc1Cc1c2cccc1	None
	7176	1576	None	51	Guinea pig	Functional	pIC50	=	8.1	8.1	6	7	Potency against histamine H1 receptor on guinea pig ileumPotency against histamine H1 receptor on guinea pig ileum	Drug Central	249	0	2	1	2.7	N=C1NCC2N1c1ccccc1Cc1c2cccc1	None
	CHEMBL1106	1576	None	51	Guinea pig	Functional	pIC50	=	8.1	8.1	6	7	Potency against histamine H1 receptor on guinea pig ileumPotency against histamine H1 receptor on guinea pig ileum	Drug Central	249	0	2	1	2.7	N=C1NCC2N1c1ccccc1Cc1c2cccc1	None
	DB00751	1576	None	51	Guinea pig	Functional	pIC50	=	8.1	8.1	6	7	Potency against histamine H1 receptor on guinea pig ileumPotency against histamine H1 receptor on guinea pig ileum	Drug Central	249	0	2	1	2.7	N=C1NCC2N1c1ccccc1Cc1c2cccc1	None
	1224	1432	None	51	Guinea pig	Functional	pIC50	=	8.1	8.1	85	22	Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum	Drug Central	255	6	0	2	3.4	CN(CCOC(c1ccccc1)c1ccccc1)C	None
	3100	1432	None	51	Guinea pig	Functional	pIC50	=	8.1	8.1	85	22	Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum	Drug Central	255	6	0	2	3.4	CN(CCOC(c1ccccc1)c1ccccc1)C	None
	3100.0	1432	None	51	Guinea pig	Functional	pIC50	=	8.1	8.1	85	22	Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum	Drug Central	255	6	0	2	3.4	CN(CCOC(c1ccccc1)c1ccccc1)C	None
	8980	1432	None	51	Guinea pig	Functional	pIC50	=	8.1	8.1	85	22	Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum	Drug Central	255	6	0	2	3.4	CN(CCOC(c1ccccc1)c1ccccc1)C	None
	916	1432	None	51	Guinea pig	Functional	pIC50	=	8.1	8.1	85	22	Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum	Drug Central	255	6	0	2	3.4	CN(CCOC(c1ccccc1)c1ccccc1)C	None
	CHEMBL657	1432	None	51	Guinea pig	Functional	pIC50	=	8.1	8.1	85	22	Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum	Drug Central	255	6	0	2	3.4	CN(CCOC(c1ccccc1)c1ccccc1)C	None
	DB01075	1432	None	51	Guinea pig	Functional	pIC50	=	8.1	8.1	85	22	Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileumAntihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum	Drug Central	255	6	0	2	3.4	CN(CCOC(c1ccccc1)c1ccccc1)C	None
	2995	206863	None	31	Rat	Functional	pIC50	=	8.0	8.0	2	18	Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor	Drug Central	266	4	1	2	3.5	CNCCCN1c2ccccc2CCc2ccccc21	None
	2995.0	206863	None	31	Rat	Functional	pIC50	=	8.0	8.0	2	18	Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor	Drug Central	266	4	1	2	3.5	CNCCCN1c2ccccc2CCc2ccccc21	None
	CHEMBL1696	206863	None	31	Rat	Functional	pIC50	=	8.0	8.0	2	18	Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor	Drug Central	266	4	1	2	3.5	CNCCCN1c2ccccc2CCc2ccccc21	None
	CHEMBL72	206863	None	31	Rat	Functional	pIC50	=	8.0	8.0	2	18	Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor	Drug Central	266	4	1	2	3.5	CNCCCN1c2ccccc2CCc2ccccc21	None
	DB01151	206863	None	31	Rat	Functional	pIC50	=	8.0	8.0	2	18	Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor	Drug Central	266	4	1	2	3.5	CNCCCN1c2ccccc2CCc2ccccc21	None
	2398	954	None	43	Rat	Functional	pIC50	=	8.0	8.0	2	36	Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor	Drug Central	314	4	0	2	4.5	CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C	None
	2801	954	None	43	Rat	Functional	pIC50	=	8.0	8.0	2	36	Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor	Drug Central	314	4	0	2	4.5	CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C	None
	2801.0	954	None	43	Rat	Functional	pIC50	=	8.0	8.0	2	36	Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor	Drug Central	314	4	0	2	4.5	CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C	None
	701	954	None	43	Rat	Functional	pIC50	=	8.0	8.0	2	36	Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor	Drug Central	314	4	0	2	4.5	CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C	None
	CHEMBL415	954	None	43	Rat	Functional	pIC50	=	8.0	8.0	2	36	Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor	Drug Central	314	4	0	2	4.5	CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C	None
	DB01242	954	None	43	Rat	Functional	pIC50	=	8.0	8.0	2	36	Compound tested for its inhibitory activity against Histamine H1 receptorCompound tested for its inhibitory activity against Histamine H1 receptor	Drug Central	314	4	0	2	4.5	CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C	None
	4223	3992	None	57	Human	Functional	pIC50	=	6.5	6.5	-199	17	UnclassifiedUnclassified	Guide to Pharmacology	441	7	2	5	4.0	N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2	15341484
	6918314	3992	None	57	Human	Functional	pIC50	=	6.5	6.5	-199	17	UnclassifiedUnclassified	Guide to Pharmacology	441	7	2	5	4.0	N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2	15341484
	6918314.0	3992	None	57	Human	Functional	pIC50	=	6.5	6.5	-199	17	UnclassifiedUnclassified	Guide to Pharmacology	441	7	2	5	4.0	N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2	15341484
	7427	3992	None	57	Human	Functional	pIC50	=	6.5	6.5	-199	17	UnclassifiedUnclassified	Guide to Pharmacology	441	7	2	5	4.0	N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2	15341484
	CHEMBL439849	3992	None	57	Human	Functional	pIC50	=	6.5	6.5	-199	17	UnclassifiedUnclassified	Guide to Pharmacology	441	7	2	5	4.0	N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2	15341484
	DB06684	3992	None	57	Human	Functional	pIC50	=	6.5	6.5	-199	17	UnclassifiedUnclassified	Guide to Pharmacology	441	7	2	5	4.0	N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2	15341484
	2762	3863	None	23	Human	Functional	pIC50	=	7.4	7.4	100	9	UnclassifiedUnclassified	Guide to Pharmacology	255	6	0	3	2.7	CN(CCN(c1ccccn1)Cc1ccccc1)C	14667234
	5587	3863	None	23	Human	Functional	pIC50	=	7.4	7.4	100	9	UnclassifiedUnclassified	Guide to Pharmacology	255	6	0	3	2.7	CN(CCN(c1ccccn1)Cc1ccccc1)C	14667234
	5587.0	3863	None	23	Human	Functional	pIC50	=	7.4	7.4	100	9	UnclassifiedUnclassified	Guide to Pharmacology	255	6	0	3	2.7	CN(CCN(c1ccccn1)Cc1ccccc1)C	14667234
	7318	3863	None	23	Human	Functional	pIC50	=	7.4	7.4	100	9	UnclassifiedUnclassified	Guide to Pharmacology	255	6	0	3	2.7	CN(CCN(c1ccccn1)Cc1ccccc1)C	14667234
	CHEMBL1241	3863	None	23	Human	Functional	pIC50	=	7.4	7.4	100	9	UnclassifiedUnclassified	Guide to Pharmacology	255	6	0	3	2.7	CN(CCN(c1ccccn1)Cc1ccccc1)C	14667234
	DB00792	3863	None	23	Human	Functional	pIC50	=	7.4	7.4	100	9	UnclassifiedUnclassified	Guide to Pharmacology	255	6	0	3	2.7	CN(CCN(c1ccccn1)Cc1ccccc1)C	14667234
	10103	3416	None	40	Human	Functional	pIC50	=	8.4	8.4	28	2	UnclassifiedUnclassified	Guide to Pharmacology	415	2	0	3	5.6	Cc1cncc(c1)CN1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1	16220969
	133017	3416	None	40	Human	Functional	pIC50	=	8.4	8.4	28	2	UnclassifiedUnclassified	Guide to Pharmacology	415	2	0	3	5.6	Cc1cncc(c1)CN1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1	16220969
	133017.0	3416	None	40	Human	Functional	pIC50	=	8.4	8.4	28	2	UnclassifiedUnclassified	Guide to Pharmacology	415	2	0	3	5.6	Cc1cncc(c1)CN1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1	16220969
	2413	3416	None	40	Human	Functional	pIC50	=	8.4	8.4	28	2	UnclassifiedUnclassified	Guide to Pharmacology	415	2	0	3	5.6	Cc1cncc(c1)CN1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1	16220969
	CHEMBL91397	3416	None	40	Human	Functional	pIC50	=	8.4	8.4	28	2	UnclassifiedUnclassified	Guide to Pharmacology	415	2	0	3	5.6	Cc1cncc(c1)CN1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1	16220969
	DB11614	3416	None	40	Human	Functional	pIC50	=	8.4	8.4	28	2	UnclassifiedUnclassified	Guide to Pharmacology	415	2	0	3	5.6	Cc1cncc(c1)CN1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1	16220969

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Ligands (move mouse cursor over ligand name to see structure)					Receptor	Activity									Chemical information
Sel. page	Common name	GPCRdb ID	Reference ligand	Vendors	Species	Assay Type	Activity Type	Activity Relation	Activity Value	p-value (-log)	Fold selectivity	Tested GPCRs	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI
	3158	56283	None	21	Human	Binding	pAC50	=	9	9.0	40	20	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	279	3	0	2	4.0	CN(C)CCC=C1c2ccccc2COc2ccccc21	10.1038/s41467-023-40064-9
	3158.0	56283	None	21	Human	Binding	pAC50	=	9	9.0	40	20	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	279	3	0	2	4.0	CN(C)CCC=C1c2ccccc2COc2ccccc21	10.1038/s41467-023-40064-9
	CHEMBL1628227	56283	None	21	Human	Binding	pAC50	=	9	9.0	40	20	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	279	3	0	2	4.0	CN(C)CCC=C1c2ccccc2COc2ccccc21	10.1038/s41467-023-40064-9
	DB01142	56283	None	21	Human	Binding	pAC50	=	9	9.0	40	20	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	279	3	0	2	4.0	CN(C)CCC=C1c2ccccc2COc2ccccc21	10.1038/s41467-023-40064-9
	135	2532	None	33	Human	Binding	pAC50	=	8.7	8.7	-1	57	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	264	0	0	2	3.1	CN1CCN2C(C1)c1ccccc1Cc1c2cccc1	10.1038/s41467-023-40064-9
	1796	2532	None	33	Human	Binding	pAC50	=	8.7	8.7	-1	57	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	264	0	0	2	3.1	CN1CCN2C(C1)c1ccccc1Cc1c2cccc1	10.1038/s41467-023-40064-9
	4184	2532	None	33	Human	Binding	pAC50	=	8.7	8.7	-1	57	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	264	0	0	2	3.1	CN1CCN2C(C1)c1ccccc1Cc1c2cccc1	10.1038/s41467-023-40064-9
	4184.0	2532	None	33	Human	Binding	pAC50	=	8.7	8.7	-1	57	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	264	0	0	2	3.1	CN1CCN2C(C1)c1ccccc1Cc1c2cccc1	10.1038/s41467-023-40064-9
	CHEMBL6437	2532	None	33	Human	Binding	pAC50	=	8.7	8.7	-1	57	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	264	0	0	2	3.1	CN1CCN2C(C1)c1ccccc1Cc1c2cccc1	10.1038/s41467-023-40064-9
	DB06148	2532	None	33	Human	Binding	pAC50	=	8.7	8.7	-1	57	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	264	0	0	2	3.1	CN1CCN2C(C1)c1ccccc1Cc1c2cccc1	10.1038/s41467-023-40064-9
	3121	7887	None	64	Human	Binding	pAC50	=	7	7.0	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	144	5	1	1	2.3	CCCC(CCC)C(=O)O	10.1038/s41467-023-40064-9
	CHEMBL109	7887	None	64	Human	Binding	pAC50	=	7	7.0	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	144	5	1	1	2.3	CCCC(CCC)C(=O)O	10.1038/s41467-023-40064-9
	CHEMBL433	7887	None	64	Human	Binding	pAC50	=	7	7.0	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	144	5	1	1	2.3	CCCC(CCC)C(=O)O	10.1038/s41467-023-40064-9
	213	3853	None	34	Human	Binding	pAC50	=	6	6.0	-4	43	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	371	5	0	6	2.4	Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2	10.1038/s41467-023-40064-9
	2717	3853	None	34	Human	Binding	pAC50	=	6	6.0	-4	43	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	371	5	0	6	2.4	Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2	10.1038/s41467-023-40064-9
	5533	3853	None	34	Human	Binding	pAC50	=	6	6.0	-4	43	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	371	5	0	6	2.4	Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2	10.1038/s41467-023-40064-9
	5533.0	3853	None	34	Human	Binding	pAC50	=	6	6.0	-4	43	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	371	5	0	6	2.4	Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2	10.1038/s41467-023-40064-9
	CHEMBL621	3853	None	34	Human	Binding	pAC50	=	6	6.0	-4	43	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	371	5	0	6	2.4	Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2	10.1038/s41467-023-40064-9
	DB00656	3853	None	34	Human	Binding	pAC50	=	6	6.0	-4	43	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	371	5	0	6	2.4	Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2	10.1038/s41467-023-40064-9
	3689	102826	None	36	Human	Binding	pAC50	=	6	6.0	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	325	5	2	3	3.8	CC(C(O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1	10.1038/s41467-023-40064-9
	CHEMBL1372983	102826	None	36	Human	Binding	pAC50	=	6	6.0	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	325	5	2	3	3.8	CC(C(O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1	10.1038/s41467-023-40064-9
	CHEMBL305187	102826	None	36	Human	Binding	pAC50	=	6	6.0	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	325	5	2	3	3.8	CC(C(O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1	10.1038/s41467-023-40064-9
	42890	9427	None	34	Human	Binding	pAC50	=	5	5.0	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	497	3	5	10	1.0	CC(=O)[C@]1(O)Cc2c(O)c3c(c(O)c2[C@@H](O[C@H]2C[C@H](N)[C@H](O)[C@H](C)O2)C1)C(=O)c1ccccc1C3=O	10.1038/s41467-023-40064-9
	CHEMBL1117	9427	None	34	Human	Binding	pAC50	=	5	5.0	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	497	3	5	10	1.0	CC(=O)[C@]1(O)Cc2c(O)c3c(c(O)c2[C@@H](O[C@H]2C[C@H](N)[C@H](O)[C@H](C)O2)C1)C(=O)c1ccccc1C3=O	10.1038/s41467-023-40064-9
	44139752	104339	None	40	Human	Binding	pAC50	=	5	5.0	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	227	1	0	3	2.4	N#Cc1ccc([C@H]2CCc3cncn32)c(F)c1	10.1038/s41467-023-40064-9
	CHEMBL3099695	104339	None	40	Human	Binding	pAC50	=	5	5.0	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	227	1	0	3	2.4	N#Cc1ccc([C@H]2CCc3cncn32)c(F)c1	10.1038/s41467-023-40064-9
	2477	745	None	38	Human	Binding	pAC50	=	5.0	5.0	-	28	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	385	6	0	6	2.1	O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1	10.1038/s41467-023-40064-9
	2477.0	745	None	38	Human	Binding	pAC50	=	5.0	5.0	-	28	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	385	6	0	6	2.1	O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1	10.1038/s41467-023-40064-9
	36	745	None	38	Human	Binding	pAC50	=	5.0	5.0	-	28	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	385	6	0	6	2.1	O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1	10.1038/s41467-023-40064-9
	437	745	None	38	Human	Binding	pAC50	=	5.0	5.0	-	28	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	385	6	0	6	2.1	O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1	10.1038/s41467-023-40064-9
	CHEMBL49	745	None	38	Human	Binding	pAC50	=	5.0	5.0	-	28	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	385	6	0	6	2.1	O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1	10.1038/s41467-023-40064-9
	DB00490	745	None	38	Human	Binding	pAC50	=	5.0	5.0	-	28	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	385	6	0	6	2.1	O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1	10.1038/s41467-023-40064-9
	11693	1827	None	12	Human	Binding	pAC50	=	5.0	5.0	-	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	318	4	1	3	2.5	O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C	10.1038/s41467-023-40064-9
	3494	1827	None	12	Human	Binding	pAC50	=	5.0	5.0	-	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	318	4	1	3	2.5	O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C	10.1038/s41467-023-40064-9
	3494.0	1827	None	12	Human	Binding	pAC50	=	5.0	5.0	-	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	318	4	1	3	2.5	O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C	10.1038/s41467-023-40064-9
	4302	1827	None	12	Human	Binding	pAC50	=	5.0	5.0	-	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	318	4	1	3	2.5	O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C	10.1038/s41467-023-40064-9
	7459	1827	None	12	Human	Binding	pAC50	=	5.0	5.0	-	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	318	4	1	3	2.5	O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C	10.1038/s41467-023-40064-9
	9933193	1827	None	12	Human	Binding	pAC50	=	5.0	5.0	-	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	318	4	1	3	2.5	O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C	10.1038/s41467-023-40064-9
	9933193.0	1827	None	12	Human	Binding	pAC50	=	5.0	5.0	-	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	318	4	1	3	2.5	O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C	10.1038/s41467-023-40064-9
	CHEMBL1201335	1827	None	12	Human	Binding	pAC50	=	5.0	5.0	-	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	318	4	1	3	2.5	O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C	10.1038/s41467-023-40064-9
	DB00986	1827	None	12	Human	Binding	pAC50	=	5.0	5.0	-	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	318	4	1	3	2.5	O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C	10.1038/s41467-023-40064-9
	5048	3133	None	50	Human	Binding	pAC50	=	5.0	5.0	-165	10	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	295	8	0	2	4.2	Clc1ccc(cc1)CCCOCCCN1CCCCC1	10.1038/s41467-023-40064-9
	8924	3133	None	50	Human	Binding	pAC50	=	5.0	5.0	-165	10	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	295	8	0	2	4.2	Clc1ccc(cc1)CCCOCCCN1CCCCC1	10.1038/s41467-023-40064-9
	9948102	3133	None	50	Human	Binding	pAC50	=	5.0	5.0	-165	10	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	295	8	0	2	4.2	Clc1ccc(cc1)CCCOCCCN1CCCCC1	10.1038/s41467-023-40064-9
	9948102.0	3133	None	50	Human	Binding	pAC50	=	5.0	5.0	-165	10	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	295	8	0	2	4.2	Clc1ccc(cc1)CCCOCCCN1CCCCC1	10.1038/s41467-023-40064-9
	CHEMBL462605	3133	None	50	Human	Binding	pAC50	=	5.0	5.0	-165	10	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	295	8	0	2	4.2	Clc1ccc(cc1)CCCOCCCN1CCCCC1	10.1038/s41467-023-40064-9
	DB11642	3133	None	50	Human	Binding	pAC50	=	5.0	5.0	-165	10	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	295	8	0	2	4.2	Clc1ccc(cc1)CCCOCCCN1CCCCC1	10.1038/s41467-023-40064-9
	4846	27995	None	38	Human	Binding	pAC50	=	5.0	5.0	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	308	1	2	6	2.2	O=C(O)c1cc(O)c2c3nc4ccccc4oc-3cc(=O)c2n1	10.1038/s41467-023-40064-9
	CHEMBL1372341	27995	None	38	Human	Binding	pAC50	=	5.0	5.0	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	308	1	2	6	2.2	O=C(O)c1cc(O)c2c3nc4ccccc4oc-3cc(=O)c2n1	10.1038/s41467-023-40064-9
	5284632	67423	None	10	Human	Binding	pAC50	=	5.0	5.0	-	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	392	4	1	3	3.8	O=C(O[C@@H]1C[C@@H]2CC[C@H](C1)[N+]21CCCC1)C(O)(c1ccccc1)c1ccccc1	10.1038/s41467-023-40064-9
	5284632.0	67423	None	10	Human	Binding	pAC50	=	5.0	5.0	-	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	392	4	1	3	3.8	O=C(O[C@@H]1C[C@@H]2CC[C@H](C1)[N+]21CCCC1)C(O)(c1ccccc1)c1ccccc1	10.1038/s41467-023-40064-9
	CHEMBL1888176	67423	None	10	Human	Binding	pAC50	=	5.0	5.0	-	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	392	4	1	3	3.8	O=C(O[C@@H]1C[C@@H]2CC[C@H](C1)[N+]21CCCC1)C(O)(c1ccccc1)c1ccccc1	10.1038/s41467-023-40064-9
	CHEMBL3084748	67423	None	10	Human	Binding	pAC50	=	5.0	5.0	-	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	392	4	1	3	3.8	O=C(O[C@@H]1C[C@@H]2CC[C@H](C1)[N+]21CCCC1)C(O)(c1ccccc1)c1ccccc1	10.1038/s41467-023-40064-9
	DB00209	67423	None	10	Human	Binding	pAC50	=	5.0	5.0	-	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	392	4	1	3	3.8	O=C(O[C@@H]1C[C@@H]2CC[C@H](C1)[N+]21CCCC1)C(O)(c1ccccc1)c1ccccc1	10.1038/s41467-023-40064-9
	1549120	198942	None	55	Human	Binding	pAC50	=	5.0	5.0	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	319	4	1	4	2.9	CC(/C=C1\SC(=S)N(CC(=O)O)C1=O)=C\c1ccccc1	10.1038/s41467-023-40064-9
	CHEMBL56337	198942	None	55	Human	Binding	pAC50	=	5.0	5.0	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	319	4	1	4	2.9	CC(/C=C1\SC(=S)N(CC(=O)O)C1=O)=C\c1ccccc1	10.1038/s41467-023-40064-9
	2600	3779	None	53	Human	Binding	pAC50	=	7.0	7.0	1	13	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	471	8	2	3	6.4	OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O	10.1038/s41467-023-40064-9
	2608	3779	None	53	Human	Binding	pAC50	=	7.0	7.0	1	13	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	471	8	2	3	6.4	OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O	10.1038/s41467-023-40064-9
	5405	3779	None	53	Human	Binding	pAC50	=	7.0	7.0	1	13	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	471	8	2	3	6.4	OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O	10.1038/s41467-023-40064-9
	CHEMBL17157	3779	None	53	Human	Binding	pAC50	=	7.0	7.0	1	13	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	471	8	2	3	6.4	OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O	10.1038/s41467-023-40064-9
	DB00342	3779	None	53	Human	Binding	pAC50	=	7.0	7.0	1	13	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by 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
	2564	208642	None	37	Human	Binding	pAC50	=	7.0	7.0	-2	3	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	290	6	0	3	3.4	CN(C)CCOC(c1ccc(Cl)cc1)c1ccccn1	10.1038/s41467-023-40064-9
	CHEMBL864	208642	None	37	Human	Binding	pAC50	=	7.0	7.0	-2	3	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	290	6	0	3	3.4	CN(C)CCOC(c1ccc(Cl)cc1)c1ccccn1	10.1038/s41467-023-40064-9
	6337614	13001	None	38	Human	Binding	pAC50	=	6.0	6.0	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	296	1	0	2	2.7	O=C1c2cccc3c2[C@H](CCC3)CN1[C@@H]1CN2CCC1CC2	10.1038/s41467-023-40064-9
	CHEMBL1189679	13001	None	38	Human	Binding	pAC50	=	6.0	6.0	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	296	1	0	2	2.7	O=C1c2cccc3c2[C@H](CCC3)CN1[C@@H]1CN2CCC1CC2	10.1038/s41467-023-40064-9
	4260	52574	None	20	Human	Binding	pAC50	=	6.0	6.0	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	279	6	0	4	3.0	CC(=O)Oc1cc(C(C)C)c(OCCN(C)C)cc1C	10.1038/s41467-023-40064-9
	4260.0	52574	None	20	Human	Binding	pAC50	=	6.0	6.0	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	279	6	0	4	3.0	CC(=O)Oc1cc(C(C)C)c(OCCN(C)C)cc1C	10.1038/s41467-023-40064-9
	CHEMBL159226	52574	None	20	Human	Binding	pAC50	=	6.0	6.0	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	279	6	0	4	3.0	CC(=O)Oc1cc(C(C)C)c(OCCN(C)C)cc1C	10.1038/s41467-023-40064-9
	DB09205	52574	None	20	Human	Binding	pAC50	=	6.0	6.0	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	279	6	0	4	3.0	CC(=O)Oc1cc(C(C)C)c(OCCN(C)C)cc1C	10.1038/s41467-023-40064-9
	4034	55838	None	37	Human	Binding	pAC50	=	6.0	6.0	-	1	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	390	5	0	2	5.6	Cc1cccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)c1	10.1038/s41467-023-40064-9
	4034.0	55838	None	37	Human	Binding	pAC50	=	6.0	6.0	-	1	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	390	5	0	2	5.6	Cc1cccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)c1	10.1038/s41467-023-40064-9
	CHEMBL1623	55838	None	37	Human	Binding	pAC50	=	6.0	6.0	-	1	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	390	5	0	2	5.6	Cc1cccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)c1	10.1038/s41467-023-40064-9
	DB00737	55838	None	37	Human	Binding	pAC50	=	6.0	6.0	-	1	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	390	5	0	2	5.6	Cc1cccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)c1	10.1038/s41467-023-40064-9
	5656	205524	None	56	Human	Binding	pAC50	=	6.0	6.0	-79	42	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	277	5	1	3	3.0	COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1	10.1038/s41467-023-40064-9
	CHEMBL637	205524	None	56	Human	Binding	pAC50	=	6.0	6.0	-79	42	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	277	5	1	3	3.0	COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1	10.1038/s41467-023-40064-9
	214	3860	None	43	Human	Binding	pAC50	=	7.0	7.0	-43	29	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	407	4	0	4	4.9	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
	2740	3860	None	43	Human	Binding	pAC50	=	7.0	7.0	-43	29	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	407	4	0	4	4.9	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
	5566	3860	None	43	Human	Binding	pAC50	=	7.0	7.0	-43	29	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	407	4	0	4	4.9	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
	5566.0	3860	None	43	Human	Binding	pAC50	=	7.0	7.0	-43	29	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	407	4	0	4	4.9	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
	66064	3860	None	43	Human	Binding	pAC50	=	7.0	7.0	-43	29	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	407	4	0	4	4.9	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
	CHEMBL422	3860	None	43	Human	Binding	pAC50	=	7.0	7.0	-43	29	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	407	4	0	4	4.9	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
	DB00831	3860	None	43	Human	Binding	pAC50	=	7.0	7.0	-43	29	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	407	4	0	4	4.9	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
	367	3824	None	10	Human	Binding	pAC50	=	6.9	6.9	-301	9	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	392	4	1	6	2.3	O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3	10.1038/s41467-023-40064-9
	5487427	3824	None	10	Human	Binding	pAC50	=	6.9	6.9	-301	9	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	392	4	1	6	2.3	O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3	10.1038/s41467-023-40064-9
	5487427.0	3824	None	10	Human	Binding	pAC50	=	6.9	6.9	-301	9	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	392	4	1	6	2.3	O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3	10.1038/s41467-023-40064-9
	8592	3824	None	10	Human	Binding	pAC50	=	6.9	6.9	-301	9	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	392	4	1	6	2.3	O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3	10.1038/s41467-023-40064-9
	CHEMBL1900528	3824	None	10	Human	Binding	pAC50	=	6.9	6.9	-301	9	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	392	4	1	6	2.3	O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3	10.1038/s41467-023-40064-9
	CHEMBL3305968	3824	None	10	Human	Binding	pAC50	=	6.9	6.9	-301	9	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	392	4	1	6	2.3	O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3	10.1038/s41467-023-40064-9
	CHEMBL4650755	3824	None	10	Human	Binding	pAC50	=	6.9	6.9	-301	9	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	392	4	1	6	2.3	O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3	10.1038/s41467-023-40064-9
	DB01409	3824	None	10	Human	Binding	pAC50	=	6.9	6.9	-301	9	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	392	4	1	6	2.3	O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3	10.1038/s41467-023-40064-9
	2218	15289	None	20	Human	Binding	pAC50	=	5.9	5.9	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	322	8	0	2	4.4	CCN(CC)CCCN(c1ccccc1)C1Cc2ccccc2C1	10.1038/s41467-023-40064-9
	CHEMBL1213033	15289	None	20	Human	Binding	pAC50	=	5.9	5.9	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	322	8	0	2	4.4	CCN(CC)CCCN(c1ccccc1)C1Cc2ccccc2C1	10.1038/s41467-023-40064-9
	1613	2348	None	42	Human	Binding	pAC50	=	7.9	7.9	-3	44	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	327	0	0	4	3.8	CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2	10.1038/s41467-023-40064-9
	205	2348	None	42	Human	Binding	pAC50	=	7.9	7.9	-3	44	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	327	0	0	4	3.8	CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2	10.1038/s41467-023-40064-9
	3964	2348	None	42	Human	Binding	pAC50	=	7.9	7.9	-3	44	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	327	0	0	4	3.8	CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2	10.1038/s41467-023-40064-9
	3964.0	2348	None	42	Human	Binding	pAC50	=	7.9	7.9	-3	44	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	327	0	0	4	3.8	CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2	10.1038/s41467-023-40064-9
	CHEMBL831	2348	None	42	Human	Binding	pAC50	=	7.9	7.9	-3	44	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	327	0	0	4	3.8	CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2	10.1038/s41467-023-40064-9
	DB00408	2348	None	42	Human	Binding	pAC50	=	7.9	7.9	-3	44	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	327	0	0	4	3.8	CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2	10.1038/s41467-023-40064-9
	1170	1633	None	50	Human	Binding	pAC50	=	6.9	6.9	38	3	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	501	10	3	4	5.5	OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C	10.1038/s41467-023-40064-9
	3348	1633	None	50	Human	Binding	pAC50	=	6.9	6.9	38	3	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	501	10	3	4	5.5	OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C	10.1038/s41467-023-40064-9
	3348.0	1633	None	50	Human	Binding	pAC50	=	6.9	6.9	38	3	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	501	10	3	4	5.5	OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C	10.1038/s41467-023-40064-9
	4819	1633	None	50	Human	Binding	pAC50	=	6.9	6.9	38	3	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	501	10	3	4	5.5	OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C	10.1038/s41467-023-40064-9
	74685737	1633	None	50	Human	Binding	pAC50	=	6.9	6.9	38	3	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	501	10	3	4	5.5	OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C	10.1038/s41467-023-40064-9
	CHEMBL914	1633	None	50	Human	Binding	pAC50	=	6.9	6.9	38	3	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	501	10	3	4	5.5	OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C	10.1038/s41467-023-40064-9
	DB00950	1633	None	50	Human	Binding	pAC50	=	6.9	6.9	38	3	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	501	10	3	4	5.5	OC(=O)C(c1ccc(cc1)C(CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O)O)(C)C	10.1038/s41467-023-40064-9
	260	3869	None	33	Human	Binding	pAC50	=	4.9	4.9	-	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	284	2	1	3	3.0	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2	10.1038/s41467-023-40064-9
	2775	3869	None	33	Human	Binding	pAC50	=	4.9	4.9	-	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	284	2	1	3	3.0	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2	10.1038/s41467-023-40064-9
	656665	3869	None	33	Human	Binding	pAC50	=	4.9	4.9	-	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	284	2	1	3	3.0	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2	10.1038/s41467-023-40064-9
	CHEMBL56564	3869	None	33	Human	Binding	pAC50	=	4.9	4.9	-	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	284	2	1	3	3.0	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2	10.1038/s41467-023-40064-9
	DB11699	3869	None	33	Human	Binding	pAC50	=	4.9	4.9	-	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	284	2	1	3	3.0	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2	10.1038/s41467-023-40064-9
	3149	12618	None	11	Human	Binding	pAC50	=	4.9	4.9	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	334	15	0	1	6.1	CCCCCCCCCCCC[N+](C)(C)CCOc1ccccc1	10.1038/s41467-023-40064-9
	CHEMBL1187011	12618	None	11	Human	Binding	pAC50	=	4.9	4.9	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	334	15	0	1	6.1	CCCCCCCCCCCC[N+](C)(C)CCOc1ccccc1	10.1038/s41467-023-40064-9
	7029	13674	None	10	Human	Binding	pAC50	=	4.9	4.9	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	205	5	0	2	2.6	CCN(CC)C(C)C(=O)c1ccccc1	10.1038/s41467-023-40064-9
	CHEMBL1194666	13674	None	10	Human	Binding	pAC50	=	4.9	4.9	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	205	5	0	2	2.6	CCN(CC)C(C)C(=O)c1ccccc1	10.1038/s41467-023-40064-9
	11980903	14498	None	13	Human	Binding	pAC50	=	4.9	4.9	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	382	4	0	2	5.3	Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1	10.1038/s41467-023-40064-9
	22526	14498	None	13	Human	Binding	pAC50	=	4.9	4.9	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	382	4	0	2	5.3	Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1	10.1038/s41467-023-40064-9
	5281035	14498	None	13	Human	Binding	pAC50	=	4.9	4.9	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	382	4	0	2	5.3	Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1	10.1038/s41467-023-40064-9
	CHEMBL1201303	14498	None	13	Human	Binding	pAC50	=	4.9	4.9	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	382	4	0	2	5.3	Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1	10.1038/s41467-023-40064-9
	54841	205585	None	33	Human	Binding	pAC50	=	4.9	4.9	-2	30	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	255	6	1	2	3.7	CNCC[C@@H](Oc1ccccc1C)c1ccccc1	10.1038/s41467-023-40064-9
	CHEMBL641	205585	None	33	Human	Binding	pAC50	=	4.9	4.9	-2	30	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	255	6	1	2	3.7	CNCC[C@@H](Oc1ccccc1C)c1ccccc1	10.1038/s41467-023-40064-9
	10531	1420	None	13	Human	Binding	pAC50	=	4.9	4.9	-	30	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	583	4	3	6	2.1	CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O	10.1038/s41467-023-40064-9
	10531.0	1420	None	13	Human	Binding	pAC50	=	4.9	4.9	-	30	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	583	4	3	6	2.1	CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O	10.1038/s41467-023-40064-9
	121	1420	None	13	Human	Binding	pAC50	=	4.9	4.9	-	30	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	583	4	3	6	2.1	CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O	10.1038/s41467-023-40064-9
	888	1420	None	13	Human	Binding	pAC50	=	4.9	4.9	-	30	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	583	4	3	6	2.1	CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O	10.1038/s41467-023-40064-9
	CHEMBL1732	1420	None	13	Human	Binding	pAC50	=	4.9	4.9	-	30	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	583	4	3	6	2.1	CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O	10.1038/s41467-023-40064-9
	DB00320	1420	None	13	Human	Binding	pAC50	=	4.9	4.9	-	30	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by 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
	135398747	33461	None	17	Human	Binding	pAC50	=	4.9	4.9	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	137	1	1	2	0.3	C[n+]1ccccc1C=NO	10.1038/s41467-023-40064-9
	135484646	33461	None	17	Human	Binding	pAC50	=	4.9	4.9	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	137	1	1	2	0.3	C[n+]1ccccc1C=NO	10.1038/s41467-023-40064-9
	4884	33461	None	17	Human	Binding	pAC50	=	4.9	4.9	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	137	1	1	2	0.3	C[n+]1ccccc1C=NO	10.1038/s41467-023-40064-9
	CHEMBL1420	33461	None	17	Human	Binding	pAC50	=	4.9	4.9	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	137	1	1	2	0.3	C[n+]1ccccc1C=NO	10.1038/s41467-023-40064-9
	180	401	None	38	Human	Binding	pAC50	=	7.9	7.9	-1	39	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	10.1038/s41467-023-40064-9
	200	401	None	38	Human	Binding	pAC50	=	7.9	7.9	-1	39	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	10.1038/s41467-023-40064-9
	2160	401	None	38	Human	Binding	pAC50	=	7.9	7.9	-1	39	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	10.1038/s41467-023-40064-9
	2160.0	401	None	38	Human	Binding	pAC50	=	7.9	7.9	-1	39	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	10.1038/s41467-023-40064-9
	CHEMBL629	401	None	38	Human	Binding	pAC50	=	7.9	7.9	-1	39	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	10.1038/s41467-023-40064-9
	DB00321	401	None	38	Human	Binding	pAC50	=	7.9	7.9	-1	39	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	10.1038/s41467-023-40064-9
	124087	1389	None	72	Human	Binding	pAC50	=	7.9	7.9	3	15	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	310	0	1	2	4.0	Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1	10.1038/s41467-023-40064-9
	124087.0	1389	None	72	Human	Binding	pAC50	=	7.9	7.9	3	15	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	310	0	1	2	4.0	Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1	10.1038/s41467-023-40064-9
	7157	1389	None	72	Human	Binding	pAC50	=	7.9	7.9	3	15	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	310	0	1	2	4.0	Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1	10.1038/s41467-023-40064-9
	814	1389	None	72	Human	Binding	pAC50	=	7.9	7.9	3	15	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	310	0	1	2	4.0	Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1	10.1038/s41467-023-40064-9
	CHEMBL1172	1389	None	72	Human	Binding	pAC50	=	7.9	7.9	3	15	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	310	0	1	2	4.0	Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1	10.1038/s41467-023-40064-9
	DB00967	1389	None	72	Human	Binding	pAC50	=	7.9	7.9	3	15	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	310	0	1	2	4.0	Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1	10.1038/s41467-023-40064-9
	1201549	597	None	17	Human	Binding	pAC50	=	7.9	7.9	-1	20	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	307	4	0	2	4.4	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1	10.1038/s41467-023-40064-9
	1201549.0	597	None	17	Human	Binding	pAC50	=	7.9	7.9	-1	20	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	307	4	0	2	4.4	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1	10.1038/s41467-023-40064-9
	333	597	None	17	Human	Binding	pAC50	=	7.9	7.9	-1	20	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	307	4	0	2	4.4	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1	10.1038/s41467-023-40064-9
	7601	597	None	17	Human	Binding	pAC50	=	7.9	7.9	-1	20	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	307	4	0	2	4.4	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1	10.1038/s41467-023-40064-9
	CHEMBL1201203	597	None	17	Human	Binding	pAC50	=	7.9	7.9	-1	20	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	307	4	0	2	4.4	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1	10.1038/s41467-023-40064-9
	CHEMBL438151	597	None	17	Human	Binding	pAC50	=	7.9	7.9	-1	20	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	307	4	0	2	4.4	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1	10.1038/s41467-023-40064-9
	DB00245	597	None	17	Human	Binding	pAC50	=	7.9	7.9	-1	20	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	307	4	0	2	4.4	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1	10.1038/s41467-023-40064-9
	2318	154946	None	18	Human	Binding	pAC50	=	4.9	4.9	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	351	7	1	3	4.1	CC(Cc1cccc(C(F)(F)F)c1)NCCOC(=O)c1ccccc1	10.1038/s41467-023-40064-9
	CHEMBL400599	154946	None	18	Human	Binding	pAC50	=	4.9	4.9	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	351	7	1	3	4.1	CC(Cc1cccc(C(F)(F)F)c1)NCCOC(=O)c1ccccc1	10.1038/s41467-023-40064-9
	2402	3370	None	38	Human	Binding	pAC50	=	4.9	4.9	-	25	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	260	7	1	2	3.5	CCCN(CCC)CCc1cccc2c1CC(=N2)O	10.1038/s41467-023-40064-9
	5095	3370	None	38	Human	Binding	pAC50	=	4.9	4.9	-	25	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	260	7	1	2	3.5	CCCN(CCC)CCc1cccc2c1CC(=N2)O	10.1038/s41467-023-40064-9
	5095.0	3370	None	38	Human	Binding	pAC50	=	4.9	4.9	-	25	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	260	7	1	2	3.5	CCCN(CCC)CCc1cccc2c1CC(=N2)O	10.1038/s41467-023-40064-9
	7295	3370	None	38	Human	Binding	pAC50	=	4.9	4.9	-	25	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	260	7	1	2	3.5	CCCN(CCC)CCc1cccc2c1CC(=N2)O	10.1038/s41467-023-40064-9
	CHEMBL589	3370	None	38	Human	Binding	pAC50	=	4.9	4.9	-	25	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	260	7	1	2	3.5	CCCN(CCC)CCc1cccc2c1CC(=N2)O	10.1038/s41467-023-40064-9
	DB00268	3370	None	38	Human	Binding	pAC50	=	4.9	4.9	-	25	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	260	7	1	2	3.5	CCCN(CCC)CCc1cccc2c1CC(=N2)O	10.1038/s41467-023-40064-9
	2274	3173	None	38	Human	Binding	pAC50	=	6.9	6.9	-3	32	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	373	4	0	4	4.6	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2	10.1038/s41467-023-40064-9
	4917	3173	None	38	Human	Binding	pAC50	=	6.9	6.9	-3	32	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	373	4	0	4	4.6	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2	10.1038/s41467-023-40064-9
	4917.0	3173	None	38	Human	Binding	pAC50	=	6.9	6.9	-3	32	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	373	4	0	4	4.6	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2	10.1038/s41467-023-40064-9
	7279	3173	None	38	Human	Binding	pAC50	=	6.9	6.9	-3	32	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	373	4	0	4	4.6	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2	10.1038/s41467-023-40064-9
	CHEMBL728	3173	None	38	Human	Binding	pAC50	=	6.9	6.9	-3	32	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	373	4	0	4	4.6	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2	10.1038/s41467-023-40064-9
	DB00433	3173	None	38	Human	Binding	pAC50	=	6.9	6.9	-3	32	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	373	4	0	4	4.6	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2	10.1038/s41467-023-40064-9
	2995	206863	None	31	Human	Binding	pAC50	=	6.9	6.9	-14	22	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	266	4	1	2	3.5	CNCCCN1c2ccccc2CCc2ccccc21	10.1038/s41467-023-40064-9
	2995.0	206863	None	31	Human	Binding	pAC50	=	6.9	6.9	-14	22	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	266	4	1	2	3.5	CNCCCN1c2ccccc2CCc2ccccc21	10.1038/s41467-023-40064-9
	CHEMBL1696	206863	None	31	Human	Binding	pAC50	=	6.9	6.9	-14	22	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	266	4	1	2	3.5	CNCCCN1c2ccccc2CCc2ccccc21	10.1038/s41467-023-40064-9
	CHEMBL72	206863	None	31	Human	Binding	pAC50	=	6.9	6.9	-14	22	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	266	4	1	2	3.5	CNCCCN1c2ccccc2CCc2ccccc21	10.1038/s41467-023-40064-9
	DB01151	206863	None	31	Human	Binding	pAC50	=	6.9	6.9	-14	22	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	266	4	1	2	3.5	CNCCCN1c2ccccc2CCc2ccccc21	10.1038/s41467-023-40064-9
	16362	3125	None	49	Human	Binding	pAC50	=	5.9	5.9	-489	29	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	461	7	1	3	5.9	Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2	10.1038/s41467-023-40064-9
	16362.0	3125	None	49	Human	Binding	pAC50	=	5.9	5.9	-489	29	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	461	7	1	3	5.9	Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2	10.1038/s41467-023-40064-9
	2172	3125	None	49	Human	Binding	pAC50	=	5.9	5.9	-489	29	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	461	7	1	3	5.9	Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2	10.1038/s41467-023-40064-9
	90	3125	None	49	Human	Binding	pAC50	=	5.9	5.9	-489	29	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	461	7	1	3	5.9	Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2	10.1038/s41467-023-40064-9
	CHEMBL1423	3125	None	49	Human	Binding	pAC50	=	5.9	5.9	-489	29	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	461	7	1	3	5.9	Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2	10.1038/s41467-023-40064-9
	DB01100	3125	None	49	Human	Binding	pAC50	=	5.9	5.9	-489	29	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by 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
	2470	3653	None	40	Human	Binding	pAC50	=	5.9	5.9	-4570	59	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	395	6	1	4	3.2	Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1	10.1038/s41467-023-40064-9
	3300	3653	None	40	Human	Binding	pAC50	=	5.9	5.9	-4570	59	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	395	6	1	4	3.2	Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1	10.1038/s41467-023-40064-9
	5265	3653	None	40	Human	Binding	pAC50	=	5.9	5.9	-4570	59	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	395	6	1	4	3.2	Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1	10.1038/s41467-023-40064-9
	99	3653	None	40	Human	Binding	pAC50	=	5.9	5.9	-4570	59	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	395	6	1	4	3.2	Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1	10.1038/s41467-023-40064-9
	CHEMBL267930	3653	None	40	Human	Binding	pAC50	=	5.9	5.9	-4570	59	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	395	6	1	4	3.2	Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1	10.1038/s41467-023-40064-9
	10007	14490	None	22	Human	Binding	pAC50	=	4.9	4.9	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	183	2	1	1	2.6	CC(C)(N)Cc1ccc(Cl)cc1	10.1038/s41467-023-40064-9
	CHEMBL1201269	14490	None	22	Human	Binding	pAC50	=	4.9	4.9	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	183	2	1	1	2.6	CC(C)(N)Cc1ccc(Cl)cc1	10.1038/s41467-023-40064-9
	20628	96601	None	25	Human	Binding	pAC50	=	4.9	4.9	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	324	6	1	5	3.7	CN(C)CCCNc1c2ccccc2nc2cccc([N+](=O)[O-])c12	10.1038/s41467-023-40064-9
	CHEMBL26291	96601	None	25	Human	Binding	pAC50	=	4.9	4.9	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	324	6	1	5	3.7	CN(C)CCCNc1c2ccccc2nc2cccc([N+](=O)[O-])c12	10.1038/s41467-023-40064-9
	5365247	138516	None	29	Human	Binding	pAC50	=	4.9	4.9	-	1	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	316	4	0	2	3.8	CN(C)C/C=C(/c1ccc(Br)cc1)c1cccnc1	10.1038/s41467-023-40064-9
	CHEMBL37744	138516	None	29	Human	Binding	pAC50	=	4.9	4.9	-	1	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	316	4	0	2	3.8	CN(C)C/C=C(/c1ccc(Br)cc1)c1cccnc1	10.1038/s41467-023-40064-9
	21772	78430	None	26	Human	Binding	pAC50	=	7.8	7.8	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	293	4	0	1	4.5	CC(CC1c2ccccc2CCc2ccccc21)CN(C)C	10.1038/s41467-023-40064-9
	CHEMBL2110816	78430	None	26	Human	Binding	pAC50	=	7.8	7.8	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	293	4	0	1	4.5	CC(CC1c2ccccc2CCc2ccccc21)CN(C)C	10.1038/s41467-023-40064-9
	228	445	None	20	Human	Binding	pAC50	=	4.8	4.8	-	24	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	267	0	2	3	2.9	CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O	10.1038/s41467-023-40064-9
	33	445	None	20	Human	Binding	pAC50	=	4.8	4.8	-	24	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	267	0	2	3	2.9	CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O	10.1038/s41467-023-40064-9
	6005	445	None	20	Human	Binding	pAC50	=	4.8	4.8	-	24	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	267	0	2	3	2.9	CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O	10.1038/s41467-023-40064-9
	6005.0	445	None	20	Human	Binding	pAC50	=	4.8	4.8	-	24	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	267	0	2	3	2.9	CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O	10.1038/s41467-023-40064-9
	CHEMBL53	445	None	20	Human	Binding	pAC50	=	4.8	4.8	-	24	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	267	0	2	3	2.9	CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O	10.1038/s41467-023-40064-9
	DB00714	445	None	20	Human	Binding	pAC50	=	4.8	4.8	-	24	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	267	0	2	3	2.9	CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O	10.1038/s41467-023-40064-9
	2264	53206	None	25	Human	Binding	pAC50	=	4.8	4.8	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	349	2	1	4	1.5	CN1C(=O)COc2c(C(=O)NC3CN4CCC3CC4)cc(Cl)cc21	10.1038/s41467-023-40064-9
	CHEMBL1598608	53206	None	25	Human	Binding	pAC50	=	4.8	4.8	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	349	2	1	4	1.5	CN1C(=O)COc2c(C(=O)NC3CN4CCC3CC4)cc(Cl)cc21	10.1038/s41467-023-40064-9
	656603	194645	None	3	Human	Binding	pAC50	=	4.8	4.8	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	398	6	1	3	3.6	C[N@+]1(CCF)[C@@H]2CC[C@H]1C[C@@H](OC(=O)C(O)(c1ccccc1)c1ccccc1)C2	10.1038/s41467-023-40064-9
	CHEMBL5292015	194645	None	3	Human	Binding	pAC50	=	4.8	4.8	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	398	6	1	3	3.6	C[N@+]1(CCF)[C@@H]2CC[C@H]1C[C@@H](OC(=O)C(O)(c1ccccc1)c1ccccc1)C2	10.1038/s41467-023-40064-9
	55483	207555	None	29	Human	Binding	pAC50	=	4.8	4.8	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	356	13	4	4	3.6	Oc1ccc(CCNCCCCCCNCCc2ccccc2)cc1O	10.1038/s41467-023-40064-9
	CHEMBL77622	207555	None	29	Human	Binding	pAC50	=	4.8	4.8	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	356	13	4	4	3.6	Oc1ccc(CCNCCCCCCNCCc2ccccc2)cc1O	10.1038/s41467-023-40064-9
	4066	207084	None	54	Human	Binding	pAC50	=	7.8	7.8	-1	7	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	322	2	0	3	4.6	c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2	10.1038/s41467-023-40064-9
	4066.0	207084	None	54	Human	Binding	pAC50	=	7.8	7.8	-1	7	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	322	2	0	3	4.6	c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2	10.1038/s41467-023-40064-9
	CHEMBL73451	207084	None	54	Human	Binding	pAC50	=	7.8	7.8	-1	7	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	322	2	0	3	4.6	c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2	10.1038/s41467-023-40064-9
	DB01071	207084	None	54	Human	Binding	pAC50	=	7.8	7.8	-1	7	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	322	2	0	3	4.6	c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2	10.1038/s41467-023-40064-9
	156419	938	None	48	Human	Binding	pAC50	=	4.8	4.8	-	15	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	357	6	1	1	6.1	C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F	10.1038/s41467-023-40064-9
	156419.0	938	None	48	Human	Binding	pAC50	=	4.8	4.8	-	15	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	357	6	1	1	6.1	C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F	10.1038/s41467-023-40064-9
	3308	938	None	48	Human	Binding	pAC50	=	4.8	4.8	-	15	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	357	6	1	1	6.1	C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F	10.1038/s41467-023-40064-9
	647	938	None	48	Human	Binding	pAC50	=	4.8	4.8	-	15	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	357	6	1	1	6.1	C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F	10.1038/s41467-023-40064-9
	CHEMBL1201284	938	None	48	Human	Binding	pAC50	=	4.8	4.8	-	15	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	357	6	1	1	6.1	C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F	10.1038/s41467-023-40064-9
	DB01012	938	None	48	Human	Binding	pAC50	=	4.8	4.8	-	15	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	357	6	1	1	6.1	C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F	10.1038/s41467-023-40064-9
	3042	1414	None	26	Human	Binding	pAC50	=	4.8	4.8	-	15	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	309	7	0	3	4.4	CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC	10.1038/s41467-023-40064-9
	3042.0	1414	None	26	Human	Binding	pAC50	=	4.8	4.8	-	15	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	309	7	0	3	4.4	CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC	10.1038/s41467-023-40064-9
	355	1414	None	26	Human	Binding	pAC50	=	4.8	4.8	-	15	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	309	7	0	3	4.4	CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC	10.1038/s41467-023-40064-9
	868	1414	None	26	Human	Binding	pAC50	=	4.8	4.8	-	15	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	309	7	0	3	4.4	CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC	10.1038/s41467-023-40064-9
	CHEMBL1123	1414	None	26	Human	Binding	pAC50	=	4.8	4.8	-	15	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	309	7	0	3	4.4	CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC	10.1038/s41467-023-40064-9
	DB00804	1414	None	26	Human	Binding	pAC50	=	4.8	4.8	-	15	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	309	7	0	3	4.4	CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC	10.1038/s41467-023-40064-9
	2169	44861	None	29	Human	Binding	pAC50	=	4.8	4.8	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	380	9	3	6	1.4	COc1ccccc1OCCNCC(O)c1ccc(C)c(S(N)(=O)=O)c1	10.1038/s41467-023-40064-9
	CHEMBL152231	44861	None	29	Human	Binding	pAC50	=	4.8	4.8	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	380	9	3	6	1.4	COc1ccccc1OCCNCC(O)c1ccc(C)c(S(N)(=O)=O)c1	10.1038/s41467-023-40064-9
	1427	2013	None	42	Human	Binding	pAC50	=	7.8	7.8	-5	26	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	280	4	0	2	3.9	CN(CCCN1c2ccccc2CCc2c1cccc2)C	10.1038/s41467-023-40064-9
	357	2013	None	42	Human	Binding	pAC50	=	7.8	7.8	-5	26	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	280	4	0	2	3.9	CN(CCCN1c2ccccc2CCc2c1cccc2)C	10.1038/s41467-023-40064-9
	3696	2013	None	42	Human	Binding	pAC50	=	7.8	7.8	-5	26	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	280	4	0	2	3.9	CN(CCCN1c2ccccc2CCc2c1cccc2)C	10.1038/s41467-023-40064-9
	CHEMBL11	2013	None	42	Human	Binding	pAC50	=	7.8	7.8	-5	26	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	280	4	0	2	3.9	CN(CCCN1c2ccccc2CCc2c1cccc2)C	10.1038/s41467-023-40064-9
	DB00458	2013	None	42	Human	Binding	pAC50	=	7.8	7.8	-5	26	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	280	4	0	2	3.9	CN(CCCN1c2ccccc2CCc2c1cccc2)C	10.1038/s41467-023-40064-9
	40466858	16162	None	49	Human	Binding	pAC50	=	6.8	6.8	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	348	6	1	3	4.0	Cc1ccc(/C(=C\CN2CCCC2)c2cccc(/C=C/C(=O)O)n2)cc1	10.1038/s41467-023-40064-9
	5284514	16162	None	49	Human	Binding	pAC50	=	6.8	6.8	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	348	6	1	3	4.0	Cc1ccc(/C(=C\CN2CCCC2)c2cccc(/C=C/C(=O)O)n2)cc1	10.1038/s41467-023-40064-9
	5284514.0	16162	None	49	Human	Binding	pAC50	=	6.8	6.8	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	348	6	1	3	4.0	Cc1ccc(/C(=C\CN2CCCC2)c2cccc(/C=C/C(=O)O)n2)cc1	10.1038/s41467-023-40064-9
	CHEMBL1224	16162	None	49	Human	Binding	pAC50	=	6.8	6.8	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	348	6	1	3	4.0	Cc1ccc(/C(=C\CN2CCCC2)c2cccc(/C=C/C(=O)O)n2)cc1	10.1038/s41467-023-40064-9
	DB09488	16162	None	49	Human	Binding	pAC50	=	6.8	6.8	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	348	6	1	3	4.0	Cc1ccc(/C(=C\CN2CCCC2)c2cccc(/C=C/C(=O)O)n2)cc1	10.1038/s41467-023-40064-9
	5440	28732	None	28	Human	Binding	pAC50	=	6.8	6.8	-1	9	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	399	6	0	5	5.0	CCSc1ccc2c(c1)N(CCCN1CCN(C)CC1)c1ccccc1S2	10.1038/s41467-023-40064-9
	5440.0	28732	None	28	Human	Binding	pAC50	=	6.8	6.8	-1	9	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	399	6	0	5	5.0	CCSc1ccc2c(c1)N(CCCN1CCN(C)CC1)c1ccccc1S2	10.1038/s41467-023-40064-9
	CHEMBL1378	28732	None	28	Human	Binding	pAC50	=	6.8	6.8	-1	9	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	399	6	0	5	5.0	CCSc1ccc2c(c1)N(CCCN1CCN(C)CC1)c1ccccc1S2	10.1038/s41467-023-40064-9
	DB00372	28732	None	28	Human	Binding	pAC50	=	6.8	6.8	-1	9	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	399	6	0	5	5.0	CCSc1ccc2c(c1)N(CCCN1CCN(C)CC1)c1ccccc1S2	10.1038/s41467-023-40064-9
	2142	3096	None	36	Human	Binding	pAC50	=	4.8	4.8	-263	36	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	281	4	2	4	2.8	Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1	10.1038/s41467-023-40064-9
	4920903	3096	None	36	Human	Binding	pAC50	=	4.8	4.8	-263	36	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	281	4	2	4	2.8	Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1	10.1038/s41467-023-40064-9
	502	3096	None	36	Human	Binding	pAC50	=	4.8	4.8	-263	36	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	281	4	2	4	2.8	Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1	10.1038/s41467-023-40064-9
	5775	3096	None	36	Human	Binding	pAC50	=	4.8	4.8	-263	36	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	281	4	2	4	2.8	Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1	10.1038/s41467-023-40064-9
	5775.0	3096	None	36	Human	Binding	pAC50	=	4.8	4.8	-263	36	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	281	4	2	4	2.8	Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1	10.1038/s41467-023-40064-9
	CHEMBL597	3096	None	36	Human	Binding	pAC50	=	4.8	4.8	-263	36	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	281	4	2	4	2.8	Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1	10.1038/s41467-023-40064-9
	DB00692	3096	None	36	Human	Binding	pAC50	=	4.8	4.8	-263	36	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	281	4	2	4	2.8	Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1	10.1038/s41467-023-40064-9
	4632	56074	None	71	Human	Binding	pAC50	=	4.8	4.8	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	228	3	1	3	2.6	COc1ccc(C(=O)c2ccccc2)c(O)c1	10.1038/s41467-023-40064-9
	CHEMBL1625	56074	None	71	Human	Binding	pAC50	=	4.8	4.8	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	228	3	1	3	2.6	COc1ccc(C(=O)c2ccccc2)c(O)c1	10.1038/s41467-023-40064-9
	3704	78218	None	21	Human	Binding	pAC50	=	4.8	4.8	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	231	3	1	3	1.6	C1=Cc2cccc(OCC3CNCCO3)c2C1	10.1038/s41467-023-40064-9
	CHEMBL2105022	78218	None	21	Human	Binding	pAC50	=	4.8	4.8	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	231	3	1	3	1.6	C1=Cc2cccc(OCC3CNCCO3)c2C1	10.1038/s41467-023-40064-9
	4942	5720	None	27	Human	Binding	pAC50	=	4.8	4.8	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	367	7	0	4	4.0	CCCOC(C(=O)OC1CCN(C)CC1)(c1ccccc1)c1ccccc1	10.1038/s41467-023-40064-9
	4942.0	5720	None	27	Human	Binding	pAC50	=	4.8	4.8	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	367	7	0	4	4.0	CCCOC(C(=O)OC1CCN(C)CC1)(c1ccccc1)c1ccccc1	10.1038/s41467-023-40064-9
	CHEMBL1078261	5720	None	27	Human	Binding	pAC50	=	4.8	4.8	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	367	7	0	4	4.0	CCCOC(C(=O)OC1CCN(C)CC1)(c1ccccc1)c1ccccc1	10.1038/s41467-023-40064-9
	DB12278	5720	None	27	Human	Binding	pAC50	=	4.8	4.8	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	367	7	0	4	4.0	CCCOC(C(=O)OC1CCN(C)CC1)(c1ccccc1)c1ccccc1	10.1038/s41467-023-40064-9
	1971	2866	None	32	Human	Binding	pAC50	=	7.8	7.8	-1	29	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	263	3	1	1	3.8	CNCCC=C1c2ccccc2CCc2c1cccc2	10.1038/s41467-023-40064-9
	2404	2866	None	32	Human	Binding	pAC50	=	7.8	7.8	-1	29	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	263	3	1	1	3.8	CNCCC=C1c2ccccc2CCc2c1cccc2	10.1038/s41467-023-40064-9
	4543	2866	None	32	Human	Binding	pAC50	=	7.8	7.8	-1	29	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	263	3	1	1	3.8	CNCCC=C1c2ccccc2CCc2c1cccc2	10.1038/s41467-023-40064-9
	4543.0	2866	None	32	Human	Binding	pAC50	=	7.8	7.8	-1	29	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	263	3	1	1	3.8	CNCCC=C1c2ccccc2CCc2c1cccc2	10.1038/s41467-023-40064-9
	CHEMBL445	2866	None	32	Human	Binding	pAC50	=	7.8	7.8	-1	29	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	263	3	1	1	3.8	CNCCC=C1c2ccccc2CCc2c1cccc2	10.1038/s41467-023-40064-9
	DB00540	2866	None	32	Human	Binding	pAC50	=	7.8	7.8	-1	29	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	263	3	1	1	3.8	CNCCC=C1c2ccccc2CCc2c1cccc2	10.1038/s41467-023-40064-9
	1228	3866	None	24	Human	Binding	pAC50	=	7.8	7.8	-5	4	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	278	4	0	2	3.9	Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1	10.1038/s41467-023-40064-9
	2763	3866	None	24	Human	Binding	pAC50	=	7.8	7.8	-5	4	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	278	4	0	2	3.9	Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1	10.1038/s41467-023-40064-9
	5282443	3866	None	24	Human	Binding	pAC50	=	7.8	7.8	-5	4	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	278	4	0	2	3.9	Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1	10.1038/s41467-023-40064-9
	5282443.0	3866	None	24	Human	Binding	pAC50	=	7.8	7.8	-5	4	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	278	4	0	2	3.9	Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1	10.1038/s41467-023-40064-9
	CHEMBL855	3866	None	24	Human	Binding	pAC50	=	7.8	7.8	-5	4	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	278	4	0	2	3.9	Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1	10.1038/s41467-023-40064-9
	DB00427	3866	None	24	Human	Binding	pAC50	=	7.8	7.8	-5	4	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	278	4	0	2	3.9	Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1	10.1038/s41467-023-40064-9
	1605	2342	None	72	Human	Binding	pAC50	=	5.8	5.8	-2	4	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	382	1	0	3	4.9	CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1	10.1038/s41467-023-40064-9
	3957	2342	None	72	Human	Binding	pAC50	=	5.8	5.8	-2	4	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	382	1	0	3	4.9	CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1	10.1038/s41467-023-40064-9
	3957.0	2342	None	72	Human	Binding	pAC50	=	5.8	5.8	-2	4	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	382	1	0	3	4.9	CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1	10.1038/s41467-023-40064-9
	7216	2342	None	72	Human	Binding	pAC50	=	5.8	5.8	-2	4	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	382	1	0	3	4.9	CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1	10.1038/s41467-023-40064-9
	CHEMBL998	2342	None	72	Human	Binding	pAC50	=	5.8	5.8	-2	4	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	382	1	0	3	4.9	CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1	10.1038/s41467-023-40064-9
	DB00455	2342	None	72	Human	Binding	pAC50	=	5.8	5.8	-2	4	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	382	1	0	3	4.9	CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1	10.1038/s41467-023-40064-9
	30323	62505	None	35	Human	Binding	pAC50	=	4.7	4.7	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	527	4	5	11	1.0	COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(C)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1	10.1038/s41467-023-40064-9
	CHEMBL1563	62505	None	35	Human	Binding	pAC50	=	4.7	4.7	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	527	4	5	11	1.0	COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(C)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1	10.1038/s41467-023-40064-9
	CHEMBL178	62505	None	35	Human	Binding	pAC50	=	4.7	4.7	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	527	4	5	11	1.0	COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(C)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1	10.1038/s41467-023-40064-9
	2812	4781	None	63	Human	Binding	pAC50	=	4.7	4.7	-28	34	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	344	4	0	2	5.4	Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1	10.1038/s41467-023-40064-9
	CHEMBL104	4781	None	63	Human	Binding	pAC50	=	4.7	4.7	-28	34	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	344	4	0	2	5.4	Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1	10.1038/s41467-023-40064-9
	72093	35070	None	5	Human	Binding	pAC50	=	4.7	4.7	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	483	16	1	4	6.3	CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1	10.1038/s41467-023-40064-9
	CHEMBL1433361	35070	None	5	Human	Binding	pAC50	=	4.7	4.7	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	483	16	1	4	6.3	CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1	10.1038/s41467-023-40064-9
	CHEMBL2103773	35070	None	5	Human	Binding	pAC50	=	4.7	4.7	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	483	16	1	4	6.3	CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1	10.1038/s41467-023-40064-9
	5284550	41735	None	12	Human	Binding	pAC50	=	7.7	7.7	-1	9	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	295	3	0	2	4.7	CN(C)CC/C=C1\c2ccccc2CSc2ccccc21	10.1038/s41467-023-40064-9
	5284550.0	41735	None	12	Human	Binding	pAC50	=	7.7	7.7	-1	9	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	295	3	0	2	4.7	CN(C)CC/C=C1\c2ccccc2CSc2ccccc21	10.1038/s41467-023-40064-9
	CHEMBL108947	41735	None	12	Human	Binding	pAC50	=	7.7	7.7	-1	9	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	295	3	0	2	4.7	CN(C)CC/C=C1\c2ccccc2CSc2ccccc21	10.1038/s41467-023-40064-9
	CHEMBL1492500	41735	None	12	Human	Binding	pAC50	=	7.7	7.7	-1	9	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	295	3	0	2	4.7	CN(C)CC/C=C1\c2ccccc2CSc2ccccc21	10.1038/s41467-023-40064-9
	DB09167	41735	None	12	Human	Binding	pAC50	=	7.7	7.7	-1	9	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	295	3	0	2	4.7	CN(C)CC/C=C1\c2ccccc2CSc2ccccc21	10.1038/s41467-023-40064-9
	4640	78295	None	23	Human	Binding	pAC50	=	5.7	5.7	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	379	6	1	4	3.9	COc1cc2[nH]c(C)c(CCN3CCN(c4ccccc4)CC3)c2cc1OC	10.1038/s41467-023-40064-9
	CHEMBL2107011	78295	None	23	Human	Binding	pAC50	=	5.7	5.7	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	379	6	1	4	3.9	COc1cc2[nH]c(C)c(CCN3CCN(c4ccccc4)CC3)c2cc1OC	10.1038/s41467-023-40064-9
	2771	197264	None	50	Human	Binding	pAC50	=	5.7	5.7	-2	26	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	324	5	0	3	3.8	CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21	10.1038/s41467-023-40064-9
	CHEMBL1200781	197264	None	50	Human	Binding	pAC50	=	5.7	5.7	-2	26	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	324	5	0	3	3.8	CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21	10.1038/s41467-023-40064-9
	CHEMBL549	197264	None	50	Human	Binding	pAC50	=	5.7	5.7	-2	26	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	324	5	0	3	3.8	CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21	10.1038/s41467-023-40064-9
	3036780	107587	None	16	Human	Binding	pAC50	=	8.7	8.7	-11	53	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	285	0	0	2	4.3	CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1	10.1038/s41467-023-40064-9
	3036780.0	107587	None	16	Human	Binding	pAC50	=	8.7	8.7	-11	53	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	285	0	0	2	4.3	CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1	10.1038/s41467-023-40064-9
	46780481	107587	None	16	Human	Binding	pAC50	=	8.7	8.7	-11	53	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	285	0	0	2	4.3	CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1	10.1038/s41467-023-40064-9
	9903970	107587	None	16	Human	Binding	pAC50	=	8.7	8.7	-11	53	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	285	0	0	2	4.3	CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1	10.1038/s41467-023-40064-9
	9903970.0	107587	None	16	Human	Binding	pAC50	=	8.7	8.7	-11	53	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	285	0	0	2	4.3	CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1	10.1038/s41467-023-40064-9
	CHEMBL3187365	107587	None	16	Human	Binding	pAC50	=	8.7	8.7	-11	53	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	285	0	0	2	4.3	CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1	10.1038/s41467-023-40064-9
	CHEMBL3544974	107587	None	16	Human	Binding	pAC50	=	8.7	8.7	-11	53	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	285	0	0	2	4.3	CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1	10.1038/s41467-023-40064-9
	CHEMBL504548	107587	None	16	Human	Binding	pAC50	=	8.7	8.7	-11	53	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	285	0	0	2	4.3	CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1	10.1038/s41467-023-40064-9
	DB06216	107587	None	16	Human	Binding	pAC50	=	8.7	8.7	-11	53	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	285	0	0	2	4.3	CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1	10.1038/s41467-023-40064-9
	1210	918	None	42	Human	Binding	pAC50	=	7.7	7.7	-20	20	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	1213	918	None	42	Human	Binding	pAC50	=	7.7	7.7	-20	20	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	2725	918	None	42	Human	Binding	pAC50	=	7.7	7.7	-20	20	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	33036	918	None	42	Human	Binding	pAC50	=	7.7	7.7	-20	20	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	33036.0	918	None	42	Human	Binding	pAC50	=	7.7	7.7	-20	20	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	4411	918	None	42	Human	Binding	pAC50	=	7.7	7.7	-20	20	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	616	918	None	42	Human	Binding	pAC50	=	7.7	7.7	-20	20	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	6976	918	None	42	Human	Binding	pAC50	=	7.7	7.7	-20	20	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	716121	918	None	42	Human	Binding	pAC50	=	7.7	7.7	-20	20	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	CHEMBL1201353	918	None	42	Human	Binding	pAC50	=	7.7	7.7	-20	20	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	CHEMBL1554789	918	None	42	Human	Binding	pAC50	=	7.7	7.7	-20	20	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	CHEMBL505	918	None	42	Human	Binding	pAC50	=	7.7	7.7	-20	20	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	DB01114	918	None	42	Human	Binding	pAC50	=	7.7	7.7	-20	20	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	DB13679	918	None	42	Human	Binding	pAC50	=	7.7	7.7	-20	20	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	16351	102785	None	36	Human	Binding	pAC50	=	7.7	7.7	-	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	343	0	0	4	4.1	CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1	10.1038/s41467-023-40064-9
	16351.0	102785	None	36	Human	Binding	pAC50	=	7.7	7.7	-	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	343	0	0	4	4.1	CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1	10.1038/s41467-023-40064-9
	CHEMBL304902	102785	None	36	Human	Binding	pAC50	=	7.7	7.7	-	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	343	0	0	4	4.1	CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1	10.1038/s41467-023-40064-9
	DB13256	102785	None	36	Human	Binding	pAC50	=	7.7	7.7	-	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	343	0	0	4	4.1	CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1	10.1038/s41467-023-40064-9
	225609	14458	None	41	Human	Binding	pAC50	=	4.7	4.7	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	422	3	2	6	2.4	CC(=O)OCC(=O)[C@@]1(O)CC[C@H]2[C@@H]3CCC4=CC(=O)CC[C@]4(C)[C@@]3(F)[C@@H](O)C[C@@]21C	10.1038/s41467-023-40064-9
	CHEMBL1201010	14458	None	41	Human	Binding	pAC50	=	4.7	4.7	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	422	3	2	6	2.4	CC(=O)OCC(=O)[C@@]1(O)CC[C@H]2[C@@H]3CCC4=CC(=O)CC[C@]4(C)[C@@]3(F)[C@@H](O)C[C@@]21C	10.1038/s41467-023-40064-9
	216416	111644	None	40	Human	Binding	pAC50	=	4.7	4.7	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	413	6	1	3	5.7	Oc1ccc2c(c1)CC[C@H](c1ccccc1)[C@@H]2c1ccc(OCCN2CCCC2)cc1	10.1038/s41467-023-40064-9
	CHEMBL328190	111644	None	40	Human	Binding	pAC50	=	4.7	4.7	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	413	6	1	3	5.7	Oc1ccc2c(c1)CC[C@H](c1ccccc1)[C@@H]2c1ccc(OCCN2CCCC2)cc1	10.1038/s41467-023-40064-9
	2895	206050	None	27	Human	Binding	pAC50	=	7.7	7.7	-1	8	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	275	3	0	1	4.6	CN(C)CCC=C1c2ccccc2C=Cc2ccccc21	10.1038/s41467-023-40064-9
	2895.0	206050	None	27	Human	Binding	pAC50	=	7.7	7.7	-1	8	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	275	3	0	1	4.6	CN(C)CCC=C1c2ccccc2C=Cc2ccccc21	10.1038/s41467-023-40064-9
	CHEMBL669	206050	None	27	Human	Binding	pAC50	=	7.7	7.7	-1	8	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	275	3	0	1	4.6	CN(C)CCC=C1c2ccccc2C=Cc2ccccc21	10.1038/s41467-023-40064-9
	DB00924	206050	None	27	Human	Binding	pAC50	=	7.7	7.7	-1	8	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	275	3	0	1	4.6	CN(C)CCC=C1c2ccccc2C=Cc2ccccc21	10.1038/s41467-023-40064-9
	1524	2181	None	61	Human	Binding	pAC50	=	6.7	6.7	-2	51	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	395	5	1	5	2.4	Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2	10.1038/s41467-023-40064-9
	197	2181	None	61	Human	Binding	pAC50	=	6.7	6.7	-2	51	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	395	5	1	5	2.4	Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2	10.1038/s41467-023-40064-9
	3822	2181	None	61	Human	Binding	pAC50	=	6.7	6.7	-2	51	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	395	5	1	5	2.4	Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2	10.1038/s41467-023-40064-9
	3822.0	2181	None	61	Human	Binding	pAC50	=	6.7	6.7	-2	51	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	395	5	1	5	2.4	Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2	10.1038/s41467-023-40064-9
	88	2181	None	61	Human	Binding	pAC50	=	6.7	6.7	-2	51	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	395	5	1	5	2.4	Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2	10.1038/s41467-023-40064-9
	CHEMBL51	2181	None	61	Human	Binding	pAC50	=	6.7	6.7	-2	51	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	395	5	1	5	2.4	Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2	10.1038/s41467-023-40064-9
	DB12465	2181	None	61	Human	Binding	pAC50	=	6.7	6.7	-2	51	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	395	5	1	5	2.4	Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2	10.1038/s41467-023-40064-9
	2601	3780	None	25	Human	Binding	pAC50	=	5.7	5.7	-	21	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	340	3	2	2	2.9	CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC	10.1038/s41467-023-40064-9
	443951	3780	None	25	Human	Binding	pAC50	=	5.7	5.7	-	21	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	340	3	2	2	2.9	CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC	10.1038/s41467-023-40064-9
	56	3780	None	25	Human	Binding	pAC50	=	5.7	5.7	-	21	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	340	3	2	2	2.9	CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC	10.1038/s41467-023-40064-9
	CHEMBL73151	3780	None	25	Human	Binding	pAC50	=	5.7	5.7	-	21	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	340	3	2	2	2.9	CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC	10.1038/s41467-023-40064-9
	DB13399	3780	None	25	Human	Binding	pAC50	=	5.7	5.7	-	21	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	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
	6729	14491	None	33	Human	Binding	pAC50	=	5.7	5.7	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	432	5	0	2	6.5	CC(C)(C)c1ccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)cc1	10.1038/s41467-023-40064-9
	6729.0	14491	None	33	Human	Binding	pAC50	=	5.7	5.7	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	432	5	0	2	6.5	CC(C)(C)c1ccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)cc1	10.1038/s41467-023-40064-9
	CHEMBL1201271	14491	None	33	Human	Binding	pAC50	=	5.7	5.7	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	432	5	0	2	6.5	CC(C)(C)c1ccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)cc1	10.1038/s41467-023-40064-9
	DB00354	14491	None	33	Human	Binding	pAC50	=	5.7	5.7	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	432	5	0	2	6.5	CC(C)(C)c1ccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)cc1	10.1038/s41467-023-40064-9
	24826799	10802	None	64	Human	Binding	pAC50	=	4.7	4.7	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	532	4	1	6	4.5	Cc1ccc(C(=O)Nc2ccc(CN3CCN(C)CC3)c(C(F)(F)F)c2)cc1C#Cc1cnc2cccnn12	10.1038/s41467-023-40064-9
	CHEMBL1171837	10802	None	64	Human	Binding	pAC50	=	4.7	4.7	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	532	4	1	6	4.5	Cc1ccc(C(=O)Nc2ccc(CN3CCN(C)CC3)c(C(F)(F)F)c2)cc1C#Cc1cnc2cccnn12	10.1038/s41467-023-40064-9
	107771	120312	None	42	Human	Binding	pAC50	=	4.7	4.7	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	517	7	2	7	6.1	COc1ccc2nc3cc(Cl)ccc3c(Nc3cc(CN4CCCC4)c(O)c(CN4CCCC4)c3)c2n1	10.1038/s41467-023-40064-9
	CHEMBL35228	120312	None	42	Human	Binding	pAC50	=	4.7	4.7	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	517	7	2	7	6.1	COc1ccc2nc3cc(Cl)ccc3c(Nc3cc(CN4CCCC4)c(O)c(CN4CCCC4)c3)c2n1	10.1038/s41467-023-40064-9
	240	944	None	25	Human	Binding	pAC50	=	4.7	4.7	-	25	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	465	9	2	6	3.4	COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N	10.1038/s41467-023-40064-9
	2769	944	None	25	Human	Binding	pAC50	=	4.7	4.7	-	25	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	465	9	2	6	3.4	COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N	10.1038/s41467-023-40064-9
	44279790	944	None	25	Human	Binding	pAC50	=	4.7	4.7	-	25	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	465	9	2	6	3.4	COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N	10.1038/s41467-023-40064-9
	660	944	None	25	Human	Binding	pAC50	=	4.7	4.7	-	25	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	465	9	2	6	3.4	COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N	10.1038/s41467-023-40064-9
	CHEMBL1729	944	None	25	Human	Binding	pAC50	=	4.7	4.7	-	25	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	465	9	2	6	3.4	COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N	10.1038/s41467-023-40064-9
	CHEMBL560739	944	None	25	Human	Binding	pAC50	=	4.7	4.7	-	25	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	465	9	2	6	3.4	COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N	10.1038/s41467-023-40064-9
	DB00604	944	None	25	Human	Binding	pAC50	=	4.7	4.7	-	25	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	465	9	2	6	3.4	COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N	10.1038/s41467-023-40064-9
	104850	3330	None	58	Human	Binding	pAC50	=	4.7	4.7	-	6	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	462	4	1	4	5.9	Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1	10.1038/s41467-023-40064-9
	4150	3330	None	58	Human	Binding	pAC50	=	4.7	4.7	-	6	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	462	4	1	4	5.9	Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1	10.1038/s41467-023-40064-9
	743	3330	None	58	Human	Binding	pAC50	=	4.7	4.7	-	6	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	462	4	1	4	5.9	Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1	10.1038/s41467-023-40064-9
	CHEMBL111	3330	None	58	Human	Binding	pAC50	=	4.7	4.7	-	6	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	462	4	1	4	5.9	Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1	10.1038/s41467-023-40064-9
	DB06155	3330	None	58	Human	Binding	pAC50	=	4.7	4.7	-	6	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by 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
	444	209124	None	29	Human	Binding	pAC50	=	4.7	4.7	-2089	17	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	239	3	1	2	3.3	CC(NC(C)(C)C)C(=O)c1cccc(Cl)c1	10.1038/s41467-023-40064-9
	CHEMBL894	209124	None	29	Human	Binding	pAC50	=	4.7	4.7	-2089	17	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	239	3	1	2	3.3	CC(NC(C)(C)C)C(=O)c1cccc(Cl)c1	10.1038/s41467-023-40064-9
	2726	919	None	48	Human	Binding	pAC50	=	7.7	7.7	-2	72	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	10.1038/s41467-023-40064-9
	2726.0	919	None	48	Human	Binding	pAC50	=	7.7	7.7	-2	72	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	10.1038/s41467-023-40064-9
	621	919	None	48	Human	Binding	pAC50	=	7.7	7.7	-2	72	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	10.1038/s41467-023-40064-9
	83	919	None	48	Human	Binding	pAC50	=	7.7	7.7	-2	72	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	10.1038/s41467-023-40064-9
	CHEMBL71	919	None	48	Human	Binding	pAC50	=	7.7	7.7	-2	72	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	10.1038/s41467-023-40064-9
	DB00477	919	None	48	Human	Binding	pAC50	=	7.7	7.7	-2	72	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	10.1038/s41467-023-40064-9
	21722	17999	None	26	Human	Binding	pAC50	=	6.7	6.7	1	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	284	4	0	2	4.3	CN(C)CCCn1c2c(c3ccccc31)CCCCCC2	10.1038/s41467-023-40064-9
	CHEMBL126224	17999	None	26	Human	Binding	pAC50	=	6.7	6.7	1	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	284	4	0	2	4.3	CN(C)CCCn1c2c(c3ccccc31)CCCCCC2	10.1038/s41467-023-40064-9
	2200	20210	None	38	Human	Binding	pAC50	=	5.7	5.7	-	2	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	265	5	1	3	2.7	c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1	10.1038/s41467-023-40064-9
	2200.0	20210	None	38	Human	Binding	pAC50	=	5.7	5.7	-	2	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	265	5	1	3	2.7	c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1	10.1038/s41467-023-40064-9
	CHEMBL1256819	20210	None	38	Human	Binding	pAC50	=	5.7	5.7	-	2	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	265	5	1	3	2.7	c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1	10.1038/s41467-023-40064-9
	CHEMBL1305	20210	None	38	Human	Binding	pAC50	=	5.7	5.7	-	2	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	265	5	1	3	2.7	c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1	10.1038/s41467-023-40064-9
	DB08799	20210	None	38	Human	Binding	pAC50	=	5.7	5.7	-	2	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	265	5	1	3	2.7	c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1	10.1038/s41467-023-40064-9
	1164	1630	None	10	Human	Binding	pAC50	=	4.6	4.6	-	12	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	336	6	0	2	4.1	CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1	10.1038/s41467-023-40064-9
	1626	1630	None	10	Human	Binding	pAC50	=	4.6	4.6	-	12	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	336	6	0	2	4.1	CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1	10.1038/s41467-023-40064-9
	3345	1630	None	10	Human	Binding	pAC50	=	4.6	4.6	-	12	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	336	6	0	2	4.1	CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1	10.1038/s41467-023-40064-9
	3345.0	1630	None	10	Human	Binding	pAC50	=	4.6	4.6	-	12	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	336	6	0	2	4.1	CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1	10.1038/s41467-023-40064-9
	CHEMBL596	1630	None	10	Human	Binding	pAC50	=	4.6	4.6	-	12	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	336	6	0	2	4.1	CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1	10.1038/s41467-023-40064-9
	DB00813	1630	None	10	Human	Binding	pAC50	=	4.6	4.6	-	12	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	336	6	0	2	4.1	CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1	10.1038/s41467-023-40064-9
	46220502	112646	None	60	Human	Binding	pAC50	=	4.6	4.6	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	506	7	1	8	4.9	CCN1CCN(Cc2ccc(Nc3ncc(F)c(-c4cc(F)c5nc(C)n(C(C)C)c5c4)n3)nc2)CC1	10.1038/s41467-023-40064-9
	CHEMBL3301610	112646	None	60	Human	Binding	pAC50	=	4.6	4.6	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	506	7	1	8	4.9	CCN1CCN(Cc2ccc(Nc3ncc(F)c(-c4cc(F)c5nc(C)n(C(C)C)c5c4)n3)nc2)CC1	10.1038/s41467-023-40064-9
	68617	207985	None	33	Human	Binding	pAC50	=	4.6	4.6	-1023	25	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	305	2	1	1	5.2	CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21	10.1038/s41467-023-40064-9
	CHEMBL1709	207985	None	33	Human	Binding	pAC50	=	4.6	4.6	-1023	25	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	305	2	1	1	5.2	CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21	10.1038/s41467-023-40064-9
	CHEMBL809	207985	None	33	Human	Binding	pAC50	=	4.6	4.6	-1023	25	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	305	2	1	1	5.2	CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21	10.1038/s41467-023-40064-9
	176	398	None	47	Human	Binding	pAC50	=	5.6	5.6	-	31	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	10.1038/s41467-023-40064-9
	2157	398	None	47	Human	Binding	pAC50	=	5.6	5.6	-	31	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	10.1038/s41467-023-40064-9
	2157.0	398	None	47	Human	Binding	pAC50	=	5.6	5.6	-	31	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	10.1038/s41467-023-40064-9
	2566	398	None	47	Human	Binding	pAC50	=	5.6	5.6	-	31	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	10.1038/s41467-023-40064-9
	CHEMBL633	398	None	47	Human	Binding	pAC50	=	5.6	5.6	-	31	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	10.1038/s41467-023-40064-9
	DB01118	398	None	47	Human	Binding	pAC50	=	5.6	5.6	-	31	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by 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
	2381	663	None	30	Human	Binding	pAC50	=	4.6	4.6	-	9	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	311	5	1	2	4.0	OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1	10.1038/s41467-023-40064-9
	2381.0	663	None	30	Human	Binding	pAC50	=	4.6	4.6	-	9	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	311	5	1	2	4.0	OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1	10.1038/s41467-023-40064-9
	374	663	None	30	Human	Binding	pAC50	=	4.6	4.6	-	9	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	311	5	1	2	4.0	OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1	10.1038/s41467-023-40064-9
	7128	663	None	30	Human	Binding	pAC50	=	4.6	4.6	-	9	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	311	5	1	2	4.0	OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1	10.1038/s41467-023-40064-9
	CHEMBL1101	663	None	30	Human	Binding	pAC50	=	4.6	4.6	-	9	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	311	5	1	2	4.0	OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1	10.1038/s41467-023-40064-9
	DB00810	663	None	30	Human	Binding	pAC50	=	4.6	4.6	-	9	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	311	5	1	2	4.0	OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1	10.1038/s41467-023-40064-9
	2267	559	None	45	Human	Binding	pAC50	=	7.6	7.6	10	20	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	381	3	0	4	4.3	CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2	10.1038/s41467-023-40064-9
	2267.0	559	None	45	Human	Binding	pAC50	=	7.6	7.6	10	20	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	381	3	0	4	4.3	CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2	10.1038/s41467-023-40064-9
	271	559	None	45	Human	Binding	pAC50	=	7.6	7.6	10	20	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	381	3	0	4	4.3	CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2	10.1038/s41467-023-40064-9
	7121	559	None	45	Human	Binding	pAC50	=	7.6	7.6	10	20	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	381	3	0	4	4.3	CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2	10.1038/s41467-023-40064-9
	CHEMBL639	559	None	45	Human	Binding	pAC50	=	7.6	7.6	10	20	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	381	3	0	4	4.3	CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2	10.1038/s41467-023-40064-9
	DB00972	559	None	45	Human	Binding	pAC50	=	7.6	7.6	10	20	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	381	3	0	4	4.3	CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2	10.1038/s41467-023-40064-9
	2865	4143	None	47	Human	Binding	pAC50	=	6.6	6.6	-58	53	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	412	4	1	5	3.8	O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2	10.1038/s41467-023-40064-9
	59	4143	None	47	Human	Binding	pAC50	=	6.6	6.6	-58	53	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	412	4	1	5	3.8	O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2	10.1038/s41467-023-40064-9
	60854	4143	None	47	Human	Binding	pAC50	=	6.6	6.6	-58	53	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	412	4	1	5	3.8	O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2	10.1038/s41467-023-40064-9
	60854.0	4143	None	47	Human	Binding	pAC50	=	6.6	6.6	-58	53	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	412	4	1	5	3.8	O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2	10.1038/s41467-023-40064-9
	CHEMBL708	4143	None	47	Human	Binding	pAC50	=	6.6	6.6	-58	53	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	412	4	1	5	3.8	O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2	10.1038/s41467-023-40064-9
	DB00246	4143	None	47	Human	Binding	pAC50	=	6.6	6.6	-58	53	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	412	4	1	5	3.8	O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2	10.1038/s41467-023-40064-9
	65709	59901	None	35	Human	Binding	pAC50	=	4.6	4.6	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	365	8	0	5	3.3	CCN(CC)CCn1c(=O)c(Cc2ccc(OC)cc2)nc2ccccc21	10.1038/s41467-023-40064-9
	CHEMBL1729803	59901	None	35	Human	Binding	pAC50	=	4.6	4.6	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	365	8	0	5	3.3	CCN(CC)CCn1c(=O)c(Cc2ccc(OC)cc2)nc2ccccc21	10.1038/s41467-023-40064-9
	71481097	120574	None	38	Human	Binding	pAC50	=	4.6	4.6	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	443	5	2	7	3.4	O=C(/C=C\n1cnc(-c2cc(C(F)(F)F)cc(C(F)(F)F)c2)n1)NNc1cnccn1	10.1038/s41467-023-40064-9
	CHEMBL3545185	120574	None	38	Human	Binding	pAC50	=	4.6	4.6	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	443	5	2	7	3.4	O=C(/C=C\n1cnc(-c2cc(C(F)(F)F)cc(C(F)(F)F)c2)n1)NNc1cnccn1	10.1038/s41467-023-40064-9
	2337	3256	None	51	Human	Binding	pAC50	=	7.6	7.6	1	62	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	383	5	1	6	2.9	OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2	10.1038/s41467-023-40064-9
	50	3256	None	51	Human	Binding	pAC50	=	7.6	7.6	1	62	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	383	5	1	6	2.9	OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2	10.1038/s41467-023-40064-9
	5002	3256	None	51	Human	Binding	pAC50	=	7.6	7.6	1	62	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	383	5	1	6	2.9	OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2	10.1038/s41467-023-40064-9
	5002.0	3256	None	51	Human	Binding	pAC50	=	7.6	7.6	1	62	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	383	5	1	6	2.9	OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2	10.1038/s41467-023-40064-9
	CHEMBL716	3256	None	51	Human	Binding	pAC50	=	7.6	7.6	1	62	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	383	5	1	6	2.9	OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2	10.1038/s41467-023-40064-9
	DB01224	3256	None	51	Human	Binding	pAC50	=	7.6	7.6	1	62	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	383	5	1	6	2.9	OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2	10.1038/s41467-023-40064-9
	150	2509	None	14	Human	Binding	pAC50	=	5.6	5.6	-	15	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	339	4	3	3	1.9	CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO	10.1038/s41467-023-40064-9
	1764	2509	None	14	Human	Binding	pAC50	=	5.6	5.6	-	15	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	339	4	3	3	1.9	CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO	10.1038/s41467-023-40064-9
	8226	2509	None	14	Human	Binding	pAC50	=	5.6	5.6	-	15	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	339	4	3	3	1.9	CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO	10.1038/s41467-023-40064-9
	8226.0	2509	None	14	Human	Binding	pAC50	=	5.6	5.6	-	15	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	339	4	3	3	1.9	CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO	10.1038/s41467-023-40064-9
	CHEMBL1201356	2509	None	14	Human	Binding	pAC50	=	5.6	5.6	-	15	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	339	4	3	3	1.9	CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO	10.1038/s41467-023-40064-9
	DB00353	2509	None	14	Human	Binding	pAC50	=	5.6	5.6	-	15	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	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
	2389	3331	None	72	Human	Binding	pAC50	=	6.6	6.6	-45	67	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	10.1038/s41467-023-40064-9
	5073	3331	None	72	Human	Binding	pAC50	=	6.6	6.6	-45	67	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	10.1038/s41467-023-40064-9
	5073.0	3331	None	72	Human	Binding	pAC50	=	6.6	6.6	-45	67	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	10.1038/s41467-023-40064-9
	96	3331	None	72	Human	Binding	pAC50	=	6.6	6.6	-45	67	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	10.1038/s41467-023-40064-9
	CHEMBL85	3331	None	72	Human	Binding	pAC50	=	6.6	6.6	-45	67	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	10.1038/s41467-023-40064-9
	DB00734	3331	None	72	Human	Binding	pAC50	=	6.6	6.6	-45	67	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	10.1038/s41467-023-40064-9
	4832	55436	None	14	Human	Binding	pAC50	=	4.6	4.6	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	354	5	1	3	3.1	CC[N+]1(C)CCCC(OC(=O)C(O)(c2ccccc2)c2ccccc2)C1	10.1038/s41467-023-40064-9
	CHEMBL1619528	55436	None	14	Human	Binding	pAC50	=	4.6	4.6	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	354	5	1	3	3.1	CC[N+]1(C)CCCC(OC(=O)C(O)(c2ccccc2)c2ccccc2)C1	10.1038/s41467-023-40064-9
	2324	77126	None	16	Human	Binding	pAC50	=	4.6	4.6	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	505	7	1	8	4.2	COC(=O)C1=C(C)NC(C)=C(C(=O)OC2CCCN(Cc3ccccc3)C2)C1c1cccc([N+](=O)[O-])c1	10.1038/s41467-023-40064-9
	CHEMBL2074972	77126	None	16	Human	Binding	pAC50	=	4.6	4.6	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	505	7	1	8	4.2	COC(=O)C1=C(C)NC(C)=C(C(=O)OC2CCCN(Cc3ccccc3)C2)C1c1cccc([N+](=O)[O-])c1	10.1038/s41467-023-40064-9
	68867	78202	None	29	Human	Binding	pAC50	=	4.6	4.6	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	402	7	2	6	3.1	CCOc1cc(N)c([N+](=O)[O-])cc1C(=O)NC1CCN(CC2CC=CCC2)CC1	10.1038/s41467-023-40064-9
	68867.0	78202	None	29	Human	Binding	pAC50	=	4.6	4.6	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	402	7	2	6	3.1	CCOc1cc(N)c([N+](=O)[O-])cc1C(=O)NC1CCN(CC2CC=CCC2)CC1	10.1038/s41467-023-40064-9
	CHEMBL2104523	78202	None	29	Human	Binding	pAC50	=	4.6	4.6	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	402	7	2	6	3.1	CCOc1cc(N)c([N+](=O)[O-])cc1C(=O)NC1CCN(CC2CC=CCC2)CC1	10.1038/s41467-023-40064-9
	DB08810	78202	None	29	Human	Binding	pAC50	=	4.6	4.6	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	402	7	2	6	3.1	CCOc1cc(N)c([N+](=O)[O-])cc1C(=O)NC1CCN(CC2CC=CCC2)CC1	10.1038/s41467-023-40064-9
	146570	43468	None	43	Human	Binding	pAC50	=	5.6	5.6	-1	4	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	324	5	0	3	3.8	CN(C)CCC[C@@]1(c2ccc(F)cc2)OCc2cc(C#N)ccc21	10.1038/s41467-023-40064-9
	CHEMBL1508	43468	None	43	Human	Binding	pAC50	=	5.6	5.6	-1	4	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	324	5	0	3	3.8	CN(C)CCC[C@@]1(c2ccc(F)cc2)OCc2cc(C#N)ccc21	10.1038/s41467-023-40064-9
	1212	1662	None	37	Human	Binding	pAC50	=	7.6	7.6	-41	65	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
	204	1662	None	37	Human	Binding	pAC50	=	7.6	7.6	-41	65	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
	3372	1662	None	37	Human	Binding	pAC50	=	7.6	7.6	-41	65	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
	3372.0	1662	None	37	Human	Binding	pAC50	=	7.6	7.6	-41	65	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
	CHEMBL726	1662	None	37	Human	Binding	pAC50	=	7.6	7.6	-41	65	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
	DB00623	1662	None	37	Human	Binding	pAC50	=	7.6	7.6	-41	65	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
	5311507	194927	None	32	Human	Binding	pAC50	=	7.6	7.6	-	1	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	400	5	1	4	4.2	OCCN1CCN(CC/C=C2/c3ccccc3Sc3ccc(Cl)cc32)CC1	10.1038/s41467-023-40064-9
	5311507.0	194927	None	32	Human	Binding	pAC50	=	7.6	7.6	-	1	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	400	5	1	4	4.2	OCCN1CCN(CC/C=C2/c3ccccc3Sc3ccc(Cl)cc32)CC1	10.1038/s41467-023-40064-9
	CHEMBL53904	194927	None	32	Human	Binding	pAC50	=	7.6	7.6	-	1	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	400	5	1	4	4.2	OCCN1CCN(CC/C=C2/c3ccccc3Sc3ccc(Cl)cc32)CC1	10.1038/s41467-023-40064-9
	DB01624	194927	None	32	Human	Binding	pAC50	=	7.6	7.6	-	1	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	400	5	1	4	4.2	OCCN1CCN(CC/C=C2/c3ccccc3Sc3ccc(Cl)cc32)CC1	10.1038/s41467-023-40064-9
	55645	84404	None	3	Human	Binding	pAC50	=	5.6	5.6	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	395	7	2	4	2.1	CCCN1CC(NS(=O)(=O)N(CC)CC)CC2Cc3c(O)cccc3CC21	10.1038/s41467-023-40064-9
	55645.0	84404	None	3	Human	Binding	pAC50	=	5.6	5.6	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	395	7	2	4	2.1	CCCN1CC(NS(=O)(=O)N(CC)CC)CC2Cc3c(O)cccc3CC21	10.1038/s41467-023-40064-9
	CHEMBL2218861	84404	None	3	Human	Binding	pAC50	=	5.6	5.6	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	395	7	2	4	2.1	CCCN1CC(NS(=O)(=O)N(CC)CC)CC2Cc3c(O)cccc3CC21	10.1038/s41467-023-40064-9
	11658860	2344	None	24	Human	Binding	pAC50	=	4.6	4.6	-	3	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	195	0	1	1	2.6	Clc1ccc2c(c1)[C@@H](C)CNCC2	10.1038/s41467-023-40064-9
	2941	2344	None	24	Human	Binding	pAC50	=	4.6	4.6	-	3	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	195	0	1	1	2.6	Clc1ccc2c(c1)[C@@H](C)CNCC2	10.1038/s41467-023-40064-9
	4374	2344	None	24	Human	Binding	pAC50	=	4.6	4.6	-	3	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	195	0	1	1	2.6	Clc1ccc2c(c1)[C@@H](C)CNCC2	10.1038/s41467-023-40064-9
	CHEMBL360328	2344	None	24	Human	Binding	pAC50	=	4.6	4.6	-	3	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	195	0	1	1	2.6	Clc1ccc2c(c1)[C@@H](C)CNCC2	10.1038/s41467-023-40064-9
	DB04871	2344	None	24	Human	Binding	pAC50	=	4.6	4.6	-	3	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	195	0	1	1	2.6	Clc1ccc2c(c1)[C@@H](C)CNCC2	10.1038/s41467-023-40064-9
	4046	2483	None	21	Human	Binding	pAC50	=	4.6	4.6	-	2	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	378	2	2	3	4.4	OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1	10.1038/s41467-023-40064-9
	4252	2483	None	21	Human	Binding	pAC50	=	4.6	4.6	-	2	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	378	2	2	3	4.4	OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1	10.1038/s41467-023-40064-9
	CHEMBL416956	2483	None	21	Human	Binding	pAC50	=	4.6	4.6	-	2	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	378	2	2	3	4.4	OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1	10.1038/s41467-023-40064-9
	DB00358	2483	None	21	Human	Binding	pAC50	=	4.6	4.6	-	2	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	378	2	2	3	4.4	OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1	10.1038/s41467-023-40064-9
	104870	98934	None	37	Human	Binding	pAC50	=	4.6	4.6	-	21	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	209	2	1	4	1.3	C=CCN1CCc2nc(N)sc2CC1	10.1038/s41467-023-40064-9
	5374	98934	None	37	Human	Binding	pAC50	=	4.6	4.6	-	21	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	209	2	1	4	1.3	C=CCN1CCc2nc(N)sc2CC1	10.1038/s41467-023-40064-9
	CHEMBL279085	98934	None	37	Human	Binding	pAC50	=	4.6	4.6	-	21	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	209	2	1	4	1.3	C=CCN1CCc2nc(N)sc2CC1	10.1038/s41467-023-40064-9
	3081361	93987	None	66	Human	Binding	pAC50	=	6.6	6.6	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	474	5	1	5	4.4	COc1cc2/c(=N/c3ccc(Br)cc3F)nc[nH]c2cc1OCC1CCN(C)CC1	10.1038/s41467-023-40064-9
	CHEMBL24828	93987	None	66	Human	Binding	pAC50	=	6.6	6.6	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	474	5	1	5	4.4	COc1cc2/c(=N/c3ccc(Br)cc3F)nc[nH]c2cc1OCC1CCN(C)CC1	10.1038/s41467-023-40064-9
	2540	4402	None	68	Human	Binding	pAC50	=	4.5	4.5	-	4	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	610	10	1	11	6.3	CCOc1nc2cccc(C(=O)OC(C)OC(=O)OC3CCCCC3)c2n1Cc1ccc(-c2ccccc2-c2nn[nH]n2)cc1	10.1038/s41467-023-40064-9
	CHEMBL1014	4402	None	68	Human	Binding	pAC50	=	4.5	4.5	-	4	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	610	10	1	11	6.3	CCOc1nc2cccc(C(=O)OC(C)OC(=O)OC3CCCCC3)c2n1Cc1ccc(-c2ccccc2-c2nn[nH]n2)cc1	10.1038/s41467-023-40064-9
	6127	14505	None	4	Human	Binding	pAC50	=	5.5	5.5	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	278	2	0	0	4.4	C[N+]1(C)CCC(=C(c2ccccc2)c2ccccc2)CC1	10.1038/s41467-023-40064-9
	6127.0	14505	None	4	Human	Binding	pAC50	=	5.5	5.5	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	278	2	0	0	4.4	C[N+]1(C)CCC(=C(c2ccccc2)c2ccccc2)CC1	10.1038/s41467-023-40064-9
	CHEMBL1201340	14505	None	4	Human	Binding	pAC50	=	5.5	5.5	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	278	2	0	0	4.4	C[N+]1(C)CCC(=C(c2ccccc2)c2ccccc2)CC1	10.1038/s41467-023-40064-9
	DB13720	14505	None	4	Human	Binding	pAC50	=	5.5	5.5	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	278	2	0	0	4.4	C[N+]1(C)CCC(=C(c2ccccc2)c2ccccc2)CC1	10.1038/s41467-023-40064-9
	179	400	None	72	Human	Binding	pAC50	=	4.5	4.5	-4365	50	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	369	7	2	6	1.3	CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC	10.1038/s41467-023-40064-9
	2159	400	None	72	Human	Binding	pAC50	=	4.5	4.5	-4365	50	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	369	7	2	6	1.3	CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC	10.1038/s41467-023-40064-9
	2159.0	400	None	72	Human	Binding	pAC50	=	4.5	4.5	-4365	50	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	369	7	2	6	1.3	CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC	10.1038/s41467-023-40064-9
	963	400	None	72	Human	Binding	pAC50	=	4.5	4.5	-4365	50	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	369	7	2	6	1.3	CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC	10.1038/s41467-023-40064-9
	CHEMBL243712	400	None	72	Human	Binding	pAC50	=	4.5	4.5	-4365	50	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	369	7	2	6	1.3	CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC	10.1038/s41467-023-40064-9
	DB06288	400	None	72	Human	Binding	pAC50	=	4.5	4.5	-4365	50	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	369	7	2	6	1.3	CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC	10.1038/s41467-023-40064-9
	131411	15398	None	50	Human	Binding	pAC50	=	4.5	4.5	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	476	7	1	6	5.2	CCOC(=O)c1c(CSc2ccccc2)n(C)c2cc(Br)c(O)c(CN(C)C)c12	10.1038/s41467-023-40064-9
	28446253	15398	None	50	Human	Binding	pAC50	=	4.5	4.5	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	476	7	1	6	5.2	CCOC(=O)c1c(CSc2ccccc2)n(C)c2cc(Br)c(O)c(CN(C)C)c12	10.1038/s41467-023-40064-9
	CHEMBL1214598	15398	None	50	Human	Binding	pAC50	=	4.5	4.5	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	476	7	1	6	5.2	CCOC(=O)c1c(CSc2ccccc2)n(C)c2cc(Br)c(O)c(CN(C)C)c12	10.1038/s41467-023-40064-9
	CHEMBL2103737	78169	None	0	Human	Binding	pAC50	=	4.5	4.5	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL		None	None	None		None	10.1038/s41467-023-40064-9
	4528	98179	None	50	Human	Binding	pAC50	=	4.5	4.5	-1	9	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	238	1	1	2	2.8	CN1Cc2c(N)cccc2C(c2ccccc2)C1	10.1038/s41467-023-40064-9
	CHEMBL273575	98179	None	50	Human	Binding	pAC50	=	4.5	4.5	-1	9	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	238	1	1	2	2.8	CN1Cc2c(N)cccc2C(c2ccccc2)C1	10.1038/s41467-023-40064-9
	2284	3182	None	26	Human	Binding	pAC50	=	8.5	8.5	1	28	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	284	4	0	3	4.2	CN(CCCN1c2ccccc2Sc2c1cccc2)C	10.1038/s41467-023-40064-9
	4926	3182	None	26	Human	Binding	pAC50	=	8.5	8.5	1	28	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	284	4	0	3	4.2	CN(CCCN1c2ccccc2Sc2c1cccc2)C	10.1038/s41467-023-40064-9
	7281	3182	None	26	Human	Binding	pAC50	=	8.5	8.5	1	28	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	284	4	0	3	4.2	CN(CCCN1c2ccccc2Sc2c1cccc2)C	10.1038/s41467-023-40064-9
	CHEMBL564	3182	None	26	Human	Binding	pAC50	=	8.5	8.5	1	28	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	284	4	0	3	4.2	CN(CCCN1c2ccccc2Sc2c1cccc2)C	10.1038/s41467-023-40064-9
	DB00420	3182	None	26	Human	Binding	pAC50	=	8.5	8.5	1	28	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	284	4	0	3	4.2	CN(CCCN1c2ccccc2Sc2c1cccc2)C	10.1038/s41467-023-40064-9
	26987	949	None	27	Human	Binding	pAC50	=	8.5	8.5	16	21	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	343	6	0	2	5.1	Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C	10.1038/s41467-023-40064-9
	26987.0	949	None	27	Human	Binding	pAC50	=	8.5	8.5	16	21	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	343	6	0	2	5.1	Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C	10.1038/s41467-023-40064-9
	6063	949	None	27	Human	Binding	pAC50	=	8.5	8.5	16	21	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	343	6	0	2	5.1	Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C	10.1038/s41467-023-40064-9
	671	949	None	27	Human	Binding	pAC50	=	8.5	8.5	16	21	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	343	6	0	2	5.1	Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C	10.1038/s41467-023-40064-9
	CHEMBL1626	949	None	27	Human	Binding	pAC50	=	8.5	8.5	16	21	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	343	6	0	2	5.1	Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C	10.1038/s41467-023-40064-9
	DB00283	949	None	27	Human	Binding	pAC50	=	8.5	8.5	16	21	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	343	6	0	2	5.1	Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C	10.1038/s41467-023-40064-9
	2782	32008	None	48	Human	Binding	pAC50	=	8.5	8.5	-	1	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	325	4	0	3	4.3	Clc1ccc(Cn2c(CN3CCCC3)nc3ccccc32)cc1	10.1038/s41467-023-40064-9
	CHEMBL1407943	32008	None	48	Human	Binding	pAC50	=	8.5	8.5	-	1	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	325	4	0	3	4.3	Clc1ccc(Cn2c(CN3CCCC3)nc3ccccc32)cc1	10.1038/s41467-023-40064-9
	CHEMBL3216363	32008	None	48	Human	Binding	pAC50	=	8.5	8.5	-	1	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	325	4	0	3	4.3	Clc1ccc(Cn2c(CN3CCCC3)nc3ccccc32)cc1	10.1038/s41467-023-40064-9
	2136	3095	None	24	Human	Binding	pAC50	=	5.5	5.5	-	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	303	8	0	2	4.2	ClCCN(C(COc1ccccc1)C)Cc1ccccc1	10.1038/s41467-023-40064-9
	4768	3095	None	24	Human	Binding	pAC50	=	5.5	5.5	-	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	303	8	0	2	4.2	ClCCN(C(COc1ccccc1)C)Cc1ccccc1	10.1038/s41467-023-40064-9
	4768.0	3095	None	24	Human	Binding	pAC50	=	5.5	5.5	-	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	303	8	0	2	4.2	ClCCN(C(COc1ccccc1)C)Cc1ccccc1	10.1038/s41467-023-40064-9
	7268	3095	None	24	Human	Binding	pAC50	=	5.5	5.5	-	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	303	8	0	2	4.2	ClCCN(C(COc1ccccc1)C)Cc1ccccc1	10.1038/s41467-023-40064-9
	CHEMBL753	3095	None	24	Human	Binding	pAC50	=	5.5	5.5	-	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	303	8	0	2	4.2	ClCCN(C(COc1ccccc1)C)Cc1ccccc1	10.1038/s41467-023-40064-9
	DB00925	3095	None	24	Human	Binding	pAC50	=	5.5	5.5	-	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	303	8	0	2	4.2	ClCCN(C(COc1ccccc1)C)Cc1ccccc1	10.1038/s41467-023-40064-9
	4614	5393	None	62	Human	Binding	pAC50	=	6.5	6.5	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	293	5	1	3	4.0	O=C(O)CCc1nc(-c2ccccc2)c(-c2ccccc2)o1	10.1038/s41467-023-40064-9
	CHEMBL1071	5393	None	62	Human	Binding	pAC50	=	6.5	6.5	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	293	5	1	3	4.0	O=C(O)CCc1nc(-c2ccccc2)c(-c2ccccc2)o1	10.1038/s41467-023-40064-9
	1224	1432	None	51	Human	Binding	pAC50	=	7.5	7.5	-2	13	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	255	6	0	2	3.4	CN(CCOC(c1ccccc1)c1ccccc1)C	10.1038/s41467-023-40064-9
	3100	1432	None	51	Human	Binding	pAC50	=	7.5	7.5	-2	13	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	255	6	0	2	3.4	CN(CCOC(c1ccccc1)c1ccccc1)C	10.1038/s41467-023-40064-9
	3100.0	1432	None	51	Human	Binding	pAC50	=	7.5	7.5	-2	13	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	255	6	0	2	3.4	CN(CCOC(c1ccccc1)c1ccccc1)C	10.1038/s41467-023-40064-9
	8980	1432	None	51	Human	Binding	pAC50	=	7.5	7.5	-2	13	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	255	6	0	2	3.4	CN(CCOC(c1ccccc1)c1ccccc1)C	10.1038/s41467-023-40064-9
	916	1432	None	51	Human	Binding	pAC50	=	7.5	7.5	-2	13	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	255	6	0	2	3.4	CN(CCOC(c1ccccc1)c1ccccc1)C	10.1038/s41467-023-40064-9
	CHEMBL657	1432	None	51	Human	Binding	pAC50	=	7.5	7.5	-2	13	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	255	6	0	2	3.4	CN(CCOC(c1ccccc1)c1ccccc1)C	10.1038/s41467-023-40064-9
	DB01075	1432	None	51	Human	Binding	pAC50	=	7.5	7.5	-2	13	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	255	6	0	2	3.4	CN(CCOC(c1ccccc1)c1ccccc1)C	10.1038/s41467-023-40064-9
	1210	918	None	42	Human	Binding	pAC50	=	7.5	7.5	-20	20	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	1213	918	None	42	Human	Binding	pAC50	=	7.5	7.5	-20	20	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	2725	918	None	42	Human	Binding	pAC50	=	7.5	7.5	-20	20	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	33036	918	None	42	Human	Binding	pAC50	=	7.5	7.5	-20	20	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	33036.0	918	None	42	Human	Binding	pAC50	=	7.5	7.5	-20	20	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	4411	918	None	42	Human	Binding	pAC50	=	7.5	7.5	-20	20	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	616	918	None	42	Human	Binding	pAC50	=	7.5	7.5	-20	20	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	6976	918	None	42	Human	Binding	pAC50	=	7.5	7.5	-20	20	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	716121	918	None	42	Human	Binding	pAC50	=	7.5	7.5	-20	20	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	CHEMBL1201353	918	None	42	Human	Binding	pAC50	=	7.5	7.5	-20	20	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	CHEMBL1554789	918	None	42	Human	Binding	pAC50	=	7.5	7.5	-20	20	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	CHEMBL505	918	None	42	Human	Binding	pAC50	=	7.5	7.5	-20	20	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	DB01114	918	None	42	Human	Binding	pAC50	=	7.5	7.5	-20	20	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	DB13679	918	None	42	Human	Binding	pAC50	=	7.5	7.5	-20	20	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	1547484	940	None	51	Human	Binding	pAC50	=	6.5	6.5	-1	20	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	368	6	0	2	5.1	c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1	10.1038/s41467-023-40064-9
	1547484.0	940	None	51	Human	Binding	pAC50	=	6.5	6.5	-1	20	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	368	6	0	2	5.1	c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1	10.1038/s41467-023-40064-9
	654	940	None	51	Human	Binding	pAC50	=	6.5	6.5	-1	20	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	368	6	0	2	5.1	c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1	10.1038/s41467-023-40064-9
	9072	940	None	51	Human	Binding	pAC50	=	6.5	6.5	-1	20	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	368	6	0	2	5.1	c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1	10.1038/s41467-023-40064-9
	CHEMBL43064	940	None	51	Human	Binding	pAC50	=	6.5	6.5	-1	20	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	368	6	0	2	5.1	c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1	10.1038/s41467-023-40064-9
	DB00568	940	None	51	Human	Binding	pAC50	=	6.5	6.5	-1	20	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	368	6	0	2	5.1	c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1	10.1038/s41467-023-40064-9
	9429	204590	None	44	Human	Binding	pAC50	=	6.5	6.5	-	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	446	6	0	6	3.2	CN1CCN(CCCN2c3ccccc3Sc3ccc(S(=O)(=O)N(C)C)cc32)CC1	10.1038/s41467-023-40064-9
	9429.0	204590	None	44	Human	Binding	pAC50	=	6.5	6.5	-	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	446	6	0	6	3.2	CN1CCN(CCCN2c3ccccc3Sc3ccc(S(=O)(=O)N(C)C)cc32)CC1	10.1038/s41467-023-40064-9
	CHEMBL609109	204590	None	44	Human	Binding	pAC50	=	6.5	6.5	-	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	446	6	0	6	3.2	CN1CCN(CCCN2c3ccccc3Sc3ccc(S(=O)(=O)N(C)C)cc32)CC1	10.1038/s41467-023-40064-9
	DB01622	204590	None	44	Human	Binding	pAC50	=	6.5	6.5	-	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	446	6	0	6	3.2	CN1CCN(CCCN2c3ccccc3Sc3ccc(S(=O)(=O)N(C)C)cc32)CC1	10.1038/s41467-023-40064-9
	5329102	194838	None	50	Human	Binding	pAC50	=	5.5	5.5	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	398	7	3	3	3.3	CCN(CC)CCNC(=O)c1c(C)[nH]c(/C=C2\C(=O)Nc3ccc(F)cc32)c1C	10.1038/s41467-023-40064-9
	CHEMBL535	194838	None	50	Human	Binding	pAC50	=	5.5	5.5	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	398	7	3	3	3.3	CCN(CC)CCNC(=O)c1c(C)[nH]c(/C=C2\C(=O)Nc3ccc(F)cc32)c1C	10.1038/s41467-023-40064-9
	154417	23189	None	39	Human	Binding	pAC50	=	5.5	5.5	-	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	289	4	1	4	1.9	CN1[C@@H]2CC[C@H]1C[C@@H](OC(=O)[C@H](CO)c1ccccc1)C2	10.1038/s41467-023-40064-9
	CHEMBL1331216	23189	None	39	Human	Binding	pAC50	=	5.5	5.5	-	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	289	4	1	4	1.9	CN1[C@@H]2CC[C@H]1C[C@@H](OC(=O)[C@H](CO)c1ccccc1)C2	10.1038/s41467-023-40064-9
	4940	14476	None	26	Human	Binding	pAC50	=	7.5	7.5	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	340	5	0	4	4.8	CCC(=O)c1ccc2c(c1)N(CC(C)N(C)C)c1ccccc1S2	10.1038/s41467-023-40064-9
	CHEMBL1201210	14476	None	26	Human	Binding	pAC50	=	7.5	7.5	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	340	5	0	4	4.8	CCC(=O)c1ccc2c(c1)N(CC(C)N(C)C)c1ccccc1S2	10.1038/s41467-023-40064-9
	1385580	29284	None	49	Human	Binding	pAC50	=	7.5	7.5	-1	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	426	7	1	4	4.1	O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1	10.1038/s41467-023-40064-9
	4615	29284	None	49	Human	Binding	pAC50	=	7.5	7.5	-1	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	426	7	1	4	4.1	O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1	10.1038/s41467-023-40064-9
	4615.0	29284	None	49	Human	Binding	pAC50	=	7.5	7.5	-1	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	426	7	1	4	4.1	O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1	10.1038/s41467-023-40064-9
	CHEMBL13828	29284	None	49	Human	Binding	pAC50	=	7.5	7.5	-1	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	426	7	1	4	4.1	O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1	10.1038/s41467-023-40064-9
	DB12877	29284	None	49	Human	Binding	pAC50	=	7.5	7.5	-1	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	426	7	1	4	4.1	O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1	10.1038/s41467-023-40064-9
	19675	51685	None	37	Human	Binding	pAC50	=	7.5	7.5	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	410	7	1	5	5.0	CC(=O)c1ccc2c(c1)N(CCCN1CCC(CCO)CC1)c1ccccc1S2	10.1038/s41467-023-40064-9
	CHEMBL1584	51685	None	37	Human	Binding	pAC50	=	7.5	7.5	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	410	7	1	5	5.0	CC(=O)c1ccc2c(c1)N(CCCN1CCC(CCO)CC1)c1ccccc1S2	10.1038/s41467-023-40064-9
	65700	78289	None	22	Human	Binding	pAC50	=	6.5	6.5	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	238	1	1	2	3.3	CNC1Cc2ccccc2N(C)c2ccccc21	10.1038/s41467-023-40064-9
	CHEMBL2106919	78289	None	22	Human	Binding	pAC50	=	6.5	6.5	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	238	1	1	2	3.3	CNC1Cc2ccccc2N(C)c2ccccc21	10.1038/s41467-023-40064-9
	212	3806	None	35	Human	Binding	pAC50	=	7.4	7.4	-5	25	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	443	5	0	5	3.5	CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C	10.1038/s41467-023-40064-9
	2639	3806	None	35	Human	Binding	pAC50	=	7.4	7.4	-5	25	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	443	5	0	5	3.5	CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C	10.1038/s41467-023-40064-9
	941651	3806	None	35	Human	Binding	pAC50	=	7.4	7.4	-5	25	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	443	5	0	5	3.5	CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C	10.1038/s41467-023-40064-9
	941651.0	3806	None	35	Human	Binding	pAC50	=	7.4	7.4	-5	25	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	443	5	0	5	3.5	CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C	10.1038/s41467-023-40064-9
	CHEMBL1201	3806	None	35	Human	Binding	pAC50	=	7.4	7.4	-5	25	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	443	5	0	5	3.5	CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C	10.1038/s41467-023-40064-9
	DB01623	3806	None	35	Human	Binding	pAC50	=	7.4	7.4	-5	25	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by 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
	25382	9159	None	27	Human	Binding	pAC50	=	7.4	7.4	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	291	3	0	1	4.7	CN(C)CCC=C1c2ccccc2C(C)(C)c2ccccc21	10.1038/s41467-023-40064-9
	CHEMBL110094	9159	None	27	Human	Binding	pAC50	=	7.4	7.4	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	291	3	0	1	4.7	CN(C)CCC=C1c2ccccc2C(C)(C)c2ccccc21	10.1038/s41467-023-40064-9
	4008	7228	None	58	Human	Binding	pAC50	=	5.4	5.4	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	610	10	1	9	5.0	COC(=O)C1=C(C)NC(C)=C(C(=O)OCCN2CCN(C(c3ccccc3)c3ccccc3)CC2)C1c1cccc([N+](=O)[O-])c1	10.1038/s41467-023-40064-9
	CHEMBL1085699	7228	None	58	Human	Binding	pAC50	=	5.4	5.4	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	610	10	1	9	5.0	COC(=O)C1=C(C)NC(C)=C(C(=O)OCCN2CCN(C(c3ccccc3)c3ccccc3)CC2)C1c1cccc([N+](=O)[O-])c1	10.1038/s41467-023-40064-9
	1400	1957	None	46	Human	Binding	pAC50	=	7.4	7.4	2	3	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	374	8	1	4	3.1	OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1	10.1038/s41467-023-40064-9
	3658	1957	None	46	Human	Binding	pAC50	=	7.4	7.4	2	3	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	374	8	1	4	3.1	OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1	10.1038/s41467-023-40064-9
	3658.0	1957	None	46	Human	Binding	pAC50	=	7.4	7.4	2	3	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	374	8	1	4	3.1	OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1	10.1038/s41467-023-40064-9
	7199	1957	None	46	Human	Binding	pAC50	=	7.4	7.4	2	3	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	374	8	1	4	3.1	OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1	10.1038/s41467-023-40064-9
	91513	1957	None	46	Human	Binding	pAC50	=	7.4	7.4	2	3	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	374	8	1	4	3.1	OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1	10.1038/s41467-023-40064-9
	CHEMBL896	1957	None	46	Human	Binding	pAC50	=	7.4	7.4	2	3	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	374	8	1	4	3.1	OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1	10.1038/s41467-023-40064-9
	DB00557	1957	None	46	Human	Binding	pAC50	=	7.4	7.4	2	3	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	374	8	1	4	3.1	OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1	10.1038/s41467-023-40064-9
	3151	1462	None	65	Human	Binding	pAC50	=	5.4	5.4	-41	26	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	425	5	2	5	3.4	Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2	10.1038/s41467-023-40064-9
	3151.0	1462	None	65	Human	Binding	pAC50	=	5.4	5.4	-41	26	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	425	5	2	5	3.4	Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2	10.1038/s41467-023-40064-9
	945	1462	None	65	Human	Binding	pAC50	=	5.4	5.4	-41	26	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	425	5	2	5	3.4	Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2	10.1038/s41467-023-40064-9
	965	1462	None	65	Human	Binding	pAC50	=	5.4	5.4	-41	26	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	425	5	2	5	3.4	Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2	10.1038/s41467-023-40064-9
	CHEMBL219916	1462	None	65	Human	Binding	pAC50	=	5.4	5.4	-41	26	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	425	5	2	5	3.4	Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2	10.1038/s41467-023-40064-9
	DB01184	1462	None	65	Human	Binding	pAC50	=	5.4	5.4	-41	26	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	425	5	2	5	3.4	Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2	10.1038/s41467-023-40064-9
	CHEMBL4743867	216518	None	10	Human	Binding	pAC50	=	8.3	8.3	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL		None	None	None		OCCN1CCN(CCC=C2c3ccccc3Sc3ccc(C(F)(F)F)cc32)CC1	10.1038/s41467-023-40064-9
	135398737	958	None	57	Human	Binding	pAC50	=	8.3	8.3	2	91	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	10.1038/s41467-023-40064-9
	135398737.0	958	None	57	Human	Binding	pAC50	=	8.3	8.3	2	91	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	10.1038/s41467-023-40064-9
	38	958	None	57	Human	Binding	pAC50	=	8.3	8.3	2	91	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	10.1038/s41467-023-40064-9
	722	958	None	57	Human	Binding	pAC50	=	8.3	8.3	2	91	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	10.1038/s41467-023-40064-9
	CHEMBL42	958	None	57	Human	Binding	pAC50	=	8.3	8.3	2	91	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	10.1038/s41467-023-40064-9
	DB00363	958	None	57	Human	Binding	pAC50	=	8.3	8.3	2	91	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	10.1038/s41467-023-40064-9
	2220	3134	None	58	Human	Binding	pAC50	=	8.3	8.3	-	13	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	295	0	0	2	4.4	CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1	10.1038/s41467-023-40064-9
	27400	3134	None	58	Human	Binding	pAC50	=	8.3	8.3	-	13	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	295	0	0	2	4.4	CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1	10.1038/s41467-023-40064-9
	27400.0	3134	None	58	Human	Binding	pAC50	=	8.3	8.3	-	13	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	295	0	0	2	4.4	CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1	10.1038/s41467-023-40064-9
	93	3134	None	58	Human	Binding	pAC50	=	8.3	8.3	-	13	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	295	0	0	2	4.4	CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1	10.1038/s41467-023-40064-9
	CHEMBL294951	3134	None	58	Human	Binding	pAC50	=	8.3	8.3	-	13	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	295	0	0	2	4.4	CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1	10.1038/s41467-023-40064-9
	DB06153	3134	None	58	Human	Binding	pAC50	=	8.3	8.3	-	13	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	295	0	0	2	4.4	CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1	10.1038/s41467-023-40064-9
	2705	3842	None	44	Human	Binding	pAC50	=	5.4	5.4	-36	11	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	325	7	1	2	5.3	Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O	10.1038/s41467-023-40064-9
	360	3842	None	44	Human	Binding	pAC50	=	5.4	5.4	-36	11	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	325	7	1	2	5.3	Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O	10.1038/s41467-023-40064-9
	443879	3842	None	44	Human	Binding	pAC50	=	5.4	5.4	-36	11	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	325	7	1	2	5.3	Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O	10.1038/s41467-023-40064-9
	443879.0	3842	None	44	Human	Binding	pAC50	=	5.4	5.4	-36	11	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	325	7	1	2	5.3	Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O	10.1038/s41467-023-40064-9
	CHEMBL1382	3842	None	44	Human	Binding	pAC50	=	5.4	5.4	-36	11	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	325	7	1	2	5.3	Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O	10.1038/s41467-023-40064-9
	DB01036	3842	None	44	Human	Binding	pAC50	=	5.4	5.4	-36	11	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by 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
	1890	2759	None	31	Human	Binding	pAC50	=	6.4	6.4	-29	26	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	469	10	0	7	3.6	CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl	10.1038/s41467-023-40064-9
	4449	2759	None	31	Human	Binding	pAC50	=	6.4	6.4	-29	26	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	469	10	0	7	3.6	CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl	10.1038/s41467-023-40064-9
	7247	2759	None	31	Human	Binding	pAC50	=	6.4	6.4	-29	26	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	469	10	0	7	3.6	CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl	10.1038/s41467-023-40064-9
	CHEMBL623	2759	None	31	Human	Binding	pAC50	=	6.4	6.4	-29	26	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	469	10	0	7	3.6	CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl	10.1038/s41467-023-40064-9
	DB01149	2759	None	31	Human	Binding	pAC50	=	6.4	6.4	-29	26	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	469	10	0	7	3.6	CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl	10.1038/s41467-023-40064-9
	209	3057	None	57	Human	Binding	pAC50	=	7.4	7.4	-11	23	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	403	6	1	5	3.9	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2	10.1038/s41467-023-40064-9
	2113	3057	None	57	Human	Binding	pAC50	=	7.4	7.4	-11	23	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	403	6	1	5	3.9	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2	10.1038/s41467-023-40064-9
	4748	3057	None	57	Human	Binding	pAC50	=	7.4	7.4	-11	23	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	403	6	1	5	3.9	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2	10.1038/s41467-023-40064-9
	4748.0	3057	None	57	Human	Binding	pAC50	=	7.4	7.4	-11	23	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	403	6	1	5	3.9	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2	10.1038/s41467-023-40064-9
	CHEMBL567	3057	None	57	Human	Binding	pAC50	=	7.4	7.4	-11	23	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	403	6	1	5	3.9	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2	10.1038/s41467-023-40064-9
	DB00850	3057	None	57	Human	Binding	pAC50	=	7.4	7.4	-11	23	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	403	6	1	5	3.9	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2	10.1038/s41467-023-40064-9
	1209	1658	None	52	Human	Binding	pAC50	=	5.4	5.4	-144	31	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	309	6	1	2	4.4	CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F	10.1038/s41467-023-40064-9
	203	1658	None	52	Human	Binding	pAC50	=	5.4	5.4	-144	31	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	309	6	1	2	4.4	CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F	10.1038/s41467-023-40064-9
	3386	1658	None	52	Human	Binding	pAC50	=	5.4	5.4	-144	31	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	309	6	1	2	4.4	CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F	10.1038/s41467-023-40064-9
	CHEMBL41	1658	None	52	Human	Binding	pAC50	=	5.4	5.4	-144	31	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	309	6	1	2	4.4	CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F	10.1038/s41467-023-40064-9
	DB00472	1658	None	52	Human	Binding	pAC50	=	5.4	5.4	-144	31	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	309	6	1	2	4.4	CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F	10.1038/s41467-023-40064-9
	242	470	None	70	Human	Binding	pAC50	=	7.4	7.4	-22	51	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	447	7	1	4	4.9	O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl	10.1038/s41467-023-40064-9
	34	470	None	70	Human	Binding	pAC50	=	7.4	7.4	-22	51	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	447	7	1	4	4.9	O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl	10.1038/s41467-023-40064-9
	60795	470	None	70	Human	Binding	pAC50	=	7.4	7.4	-22	51	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	447	7	1	4	4.9	O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl	10.1038/s41467-023-40064-9
	60795.0	470	None	70	Human	Binding	pAC50	=	7.4	7.4	-22	51	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	447	7	1	4	4.9	O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl	10.1038/s41467-023-40064-9
	CHEMBL1112	470	None	70	Human	Binding	pAC50	=	7.4	7.4	-22	51	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	447	7	1	4	4.9	O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl	10.1038/s41467-023-40064-9
	DB01238	470	None	70	Human	Binding	pAC50	=	7.4	7.4	-22	51	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	447	7	1	4	4.9	O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl	10.1038/s41467-023-40064-9
	4452	2762	None	13	Human	Binding	pAC50	=	5.4	5.4	-	18	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	387	6	2	4	3.8	COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl	10.1038/s41467-023-40064-9
	983	2762	None	13	Human	Binding	pAC50	=	5.4	5.4	-	18	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	387	6	2	4	3.8	COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl	10.1038/s41467-023-40064-9
	CHEMBL20734	2762	None	13	Human	Binding	pAC50	=	5.4	5.4	-	18	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	387	6	2	4	3.8	COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl	10.1038/s41467-023-40064-9
	2407	3372	None	50	Human	Binding	pAC50	=	5.4	5.4	-	7	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	315	6	1	3	4.3	CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1	10.1038/s41467-023-40064-9
	59227	3372	None	50	Human	Binding	pAC50	=	5.4	5.4	-	7	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	315	6	1	3	4.3	CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1	10.1038/s41467-023-40064-9
	59227.0	3372	None	50	Human	Binding	pAC50	=	5.4	5.4	-	7	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	315	6	1	3	4.3	CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1	10.1038/s41467-023-40064-9
	941	3372	None	50	Human	Binding	pAC50	=	5.4	5.4	-	7	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	315	6	1	3	4.3	CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1	10.1038/s41467-023-40064-9
	CHEMBL1303	3372	None	50	Human	Binding	pAC50	=	5.4	5.4	-	7	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	315	6	1	3	4.3	CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1	10.1038/s41467-023-40064-9
	DB05271	3372	None	50	Human	Binding	pAC50	=	5.4	5.4	-	7	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	315	6	1	3	4.3	CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1	10.1038/s41467-023-40064-9
	5639	98949	None	48	Human	Binding	pAC50	=	5.4	5.4	-	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	387	7	1	8	0.7	COc1ccccc1N1CCN(CCCNc2cc(=O)n(C)c(=O)n2C)CC1	10.1038/s41467-023-40064-9
	CHEMBL279229	98949	None	48	Human	Binding	pAC50	=	5.4	5.4	-	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	387	7	1	8	0.7	COc1ccccc1N1CCN(CCCNc2cc(=O)n(C)c(=O)n2C)CC1	10.1038/s41467-023-40064-9
	3294	2006	None	61	Human	Binding	pAC50	=	7.4	7.4	-14	44	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	426	8	0	6	4.8	COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C	10.1038/s41467-023-40064-9
	71360	2006	None	61	Human	Binding	pAC50	=	7.4	7.4	-14	44	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	426	8	0	6	4.8	COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C	10.1038/s41467-023-40064-9
	71360.0	2006	None	61	Human	Binding	pAC50	=	7.4	7.4	-14	44	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	426	8	0	6	4.8	COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C	10.1038/s41467-023-40064-9
	87	2006	None	61	Human	Binding	pAC50	=	7.4	7.4	-14	44	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	426	8	0	6	4.8	COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C	10.1038/s41467-023-40064-9
	CHEMBL14376	2006	None	61	Human	Binding	pAC50	=	7.4	7.4	-14	44	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	426	8	0	6	4.8	COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C	10.1038/s41467-023-40064-9
	DB04946	2006	None	61	Human	Binding	pAC50	=	7.4	7.4	-14	44	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	426	8	0	6	4.8	COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C	10.1038/s41467-023-40064-9
	134	2514	None	19	Human	Binding	pAC50	=	5.4	5.4	-933	67	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	353	4	2	4	1.9	CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO	10.1038/s41467-023-40064-9
	1775	2514	None	19	Human	Binding	pAC50	=	5.4	5.4	-933	67	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	353	4	2	4	1.9	CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO	10.1038/s41467-023-40064-9
	9681	2514	None	19	Human	Binding	pAC50	=	5.4	5.4	-933	67	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	353	4	2	4	1.9	CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO	10.1038/s41467-023-40064-9
	9681.0	2514	None	19	Human	Binding	pAC50	=	5.4	5.4	-933	67	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	353	4	2	4	1.9	CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO	10.1038/s41467-023-40064-9
	CHEMBL1065	2514	None	19	Human	Binding	pAC50	=	5.4	5.4	-933	67	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	353	4	2	4	1.9	CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO	10.1038/s41467-023-40064-9
	DB00247	2514	None	19	Human	Binding	pAC50	=	5.4	5.4	-933	67	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by 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
	11434515	261	None	6	Human	Binding	pAC50	=	5.4	5.4	-	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	484	9	1	6	4.7	O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2	10.1038/s41467-023-40064-9
	11434515.0	261	None	6	Human	Binding	pAC50	=	5.4	5.4	-	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	484	9	1	6	4.7	O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2	10.1038/s41467-023-40064-9
	11519741	261	None	6	Human	Binding	pAC50	=	5.4	5.4	-	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	484	9	1	6	4.7	O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2	10.1038/s41467-023-40064-9
	4484	261	None	6	Human	Binding	pAC50	=	5.4	5.4	-	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	484	9	1	6	4.7	O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2	10.1038/s41467-023-40064-9
	7449	261	None	6	Human	Binding	pAC50	=	5.4	5.4	-	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	484	9	1	6	4.7	O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2	10.1038/s41467-023-40064-9
	CHEMBL1194325	261	None	6	Human	Binding	pAC50	=	5.4	5.4	-	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	484	9	1	6	4.7	O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2	10.1038/s41467-023-40064-9
	DB08897	261	None	6	Human	Binding	pAC50	=	5.4	5.4	-	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	484	9	1	6	4.7	O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2	10.1038/s41467-023-40064-9
	4756	16656	None	34	Human	Binding	pAC50	=	5.4	5.4	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	213	2	2	5	2.7	Nc1ccc(/N=N/c2ccccc2)c(N)n1	10.1038/s41467-023-40064-9
	CHEMBL1201022	16656	None	34	Human	Binding	pAC50	=	5.4	5.4	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	213	2	2	5	2.7	Nc1ccc(/N=N/c2ccccc2)c(N)n1	10.1038/s41467-023-40064-9
	CHEMBL1242	16656	None	34	Human	Binding	pAC50	=	5.4	5.4	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	213	2	2	5	2.7	Nc1ccc(/N=N/c2ccccc2)c(N)n1	10.1038/s41467-023-40064-9
	3949	100668	None	35	Human	Binding	pAC50	=	5.4	5.4	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	468	8	0	5	4.9	COc1ccc(CN2CCN(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)c(OC)c1OC	10.1038/s41467-023-40064-9
	CHEMBL29188	100668	None	35	Human	Binding	pAC50	=	5.4	5.4	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	468	8	0	5	4.9	COc1ccc(CN2CCN(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)c(OC)c1OC	10.1038/s41467-023-40064-9
	29566	78233	None	53	Human	Binding	pAC50	=	5.3	5.3	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	284	2	2	6	-2.7	O=S1(=O)CCN(CN2CCS(=O)(=O)NC2)CN1	10.1038/s41467-023-40064-9
	CHEMBL2105420	78233	None	53	Human	Binding	pAC50	=	5.3	5.3	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	284	2	2	6	-2.7	O=S1(=O)CCN(CN2CCS(=O)(=O)NC2)CN1	10.1038/s41467-023-40064-9
	17676	7074	None	25	Human	Binding	pAC50	=	7.3	7.3	-	3	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	411	7	1	6	3.5	CC(=O)c1ccc2c(c1)N(CCCN1CCN(CCO)CC1)c1ccccc1S2	10.1038/s41467-023-40064-9
	17676.0	7074	None	25	Human	Binding	pAC50	=	7.3	7.3	-	3	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	411	7	1	6	3.5	CC(=O)c1ccc2c(c1)N(CCCN1CCN(CCO)CC1)c1ccccc1S2	10.1038/s41467-023-40064-9
	5281082	7074	None	25	Human	Binding	pAC50	=	7.3	7.3	-	3	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	411	7	1	6	3.5	CC(=O)c1ccc2c(c1)N(CCCN1CCN(CCO)CC1)c1ccccc1S2	10.1038/s41467-023-40064-9
	CHEMBL1085	7074	None	25	Human	Binding	pAC50	=	7.3	7.3	-	3	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	411	7	1	6	3.5	CC(=O)c1ccc2c(c1)N(CCCN1CCN(CCO)CC1)c1ccccc1S2	10.1038/s41467-023-40064-9
	DB01063	7074	None	25	Human	Binding	pAC50	=	7.3	7.3	-	3	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	411	7	1	6	3.5	CC(=O)c1ccc2c(c1)N(CCCN1CCN(CCO)CC1)c1ccccc1S2	10.1038/s41467-023-40064-9
	19910	37419	None	62	Human	Binding	pAC50	=	5.3	5.3	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	190	1	1	4	1.8	O=[N+]([O-])c1ccc(O)c2ncccc12	10.1038/s41467-023-40064-9
	CHEMBL1454910	37419	None	62	Human	Binding	pAC50	=	5.3	5.3	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	190	1	1	4	1.8	O=[N+]([O-])c1ccc(O)c2ncccc12	10.1038/s41467-023-40064-9
	4976	206037	None	20	Human	Binding	pAC50	=	7.3	7.3	-1	11	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	263	4	1	1	4.3	CNCCCC1c2ccccc2C=Cc2ccccc21	10.1038/s41467-023-40064-9
	CHEMBL668	206037	None	20	Human	Binding	pAC50	=	7.3	7.3	-1	11	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	263	4	1	1	4.3	CNCCCC1c2ccccc2C=Cc2ccccc21	10.1038/s41467-023-40064-9
	2105	3054	None	28	Human	Binding	pAC50	=	5.3	5.3	-	33	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	314	4	1	2	4.3	CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3	10.1038/s41467-023-40064-9
	47811	3054	None	28	Human	Binding	pAC50	=	5.3	5.3	-	33	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	314	4	1	2	4.3	CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3	10.1038/s41467-023-40064-9
	48	3054	None	28	Human	Binding	pAC50	=	5.3	5.3	-	33	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	314	4	1	2	4.3	CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3	10.1038/s41467-023-40064-9
	CHEMBL531	3054	None	28	Human	Binding	pAC50	=	5.3	5.3	-	33	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	314	4	1	2	4.3	CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3	10.1038/s41467-023-40064-9
	DB01186	3054	None	28	Human	Binding	pAC50	=	5.3	5.3	-	33	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by 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
	6834	208010	None	36	Human	Binding	pAC50	=	7.3	7.3	-1	2	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	318	5	0	2	3.9	CN(C)CCC(c1ccc(Br)cc1)c1ccccn1	10.1038/s41467-023-40064-9
	6834.0	208010	None	36	Human	Binding	pAC50	=	7.3	7.3	-1	2	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	318	5	0	2	3.9	CN(C)CCC(c1ccc(Br)cc1)c1ccccn1	10.1038/s41467-023-40064-9
	CHEMBL811	208010	None	36	Human	Binding	pAC50	=	7.3	7.3	-1	2	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	318	5	0	2	3.9	CN(C)CCC(c1ccc(Br)cc1)c1ccccn1	10.1038/s41467-023-40064-9
	DB00835	208010	None	36	Human	Binding	pAC50	=	7.3	7.3	-1	2	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	318	5	0	2	3.9	CN(C)CCC(c1ccc(Br)cc1)c1ccccn1	10.1038/s41467-023-40064-9
	7045767	59125	None	22	Human	Binding	pAC50	=	5.3	5.3	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	203	5	0	4	-1.2	CC(=O)O[C@H](CC(=O)[O-])C[N+](C)(C)C	10.1038/s41467-023-40064-9
	CHEMBL1697733	59125	None	22	Human	Binding	pAC50	=	5.3	5.3	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	203	5	0	4	-1.2	CC(=O)O[C@H](CC(=O)[O-])C[N+](C)(C)C	10.1038/s41467-023-40064-9
	11949652	80543	None	44	Human	Binding	pAC50	=	5.3	5.3	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	426	4	1	7	1.6	Cc1cc(N2CCN([C@@H]3CN[C@H](C(=O)N4CCSC4)C3)CC2)n(-c2ccccc2)n1	10.1038/s41467-023-40064-9
	CHEMBL2147777	80543	None	44	Human	Binding	pAC50	=	5.3	5.3	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	426	4	1	7	1.6	Cc1cc(N2CCN([C@@H]3CN[C@H](C(=O)N4CCSC4)C3)CC2)n(-c2ccccc2)n1	10.1038/s41467-023-40064-9
	44093	48945	None	59	Human	Binding	pAC50	=	6.3	6.3	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	217	3	2	3	0.6	C[C@H](CS)C(=O)N1CCC[C@H]1C(=O)O	10.1038/s41467-023-40064-9
	CHEMBL1560	48945	None	59	Human	Binding	pAC50	=	6.3	6.3	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	217	3	2	3	0.6	C[C@H](CS)C(=O)N1CCC[C@H]1C(=O)O	10.1038/s41467-023-40064-9
	2393	3334	None	46	Human	Binding	pAC50	=	5.2	5.2	-	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	269	5	1	4	1.9	CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C	10.1038/s41467-023-40064-9
	5078	3334	None	46	Human	Binding	pAC50	=	5.2	5.2	-	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	269	5	1	4	1.9	CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C	10.1038/s41467-023-40064-9
	5078.0	3334	None	46	Human	Binding	pAC50	=	5.2	5.2	-	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	269	5	1	4	1.9	CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C	10.1038/s41467-023-40064-9
	51	3334	None	46	Human	Binding	pAC50	=	5.2	5.2	-	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	269	5	1	4	1.9	CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C	10.1038/s41467-023-40064-9
	CHEMBL905	3334	None	46	Human	Binding	pAC50	=	5.2	5.2	-	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	269	5	1	4	1.9	CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C	10.1038/s41467-023-40064-9
	DB00953	3334	None	46	Human	Binding	pAC50	=	5.2	5.2	-	5	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	269	5	1	4	1.9	CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C	10.1038/s41467-023-40064-9
	16960	14493	None	19	Human	Binding	pAC50	=	8.2	8.2	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	318	5	0	2	3.9	CN(C)CC[C@@H](c1ccc(Br)cc1)c1ccccn1	10.1038/s41467-023-40064-9
	16960.0	14493	None	19	Human	Binding	pAC50	=	8.2	8.2	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	318	5	0	2	3.9	CN(C)CC[C@@H](c1ccc(Br)cc1)c1ccccn1	10.1038/s41467-023-40064-9
	CHEMBL1201287	14493	None	19	Human	Binding	pAC50	=	8.2	8.2	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	318	5	0	2	3.9	CN(C)CC[C@@H](c1ccc(Br)cc1)c1ccccn1	10.1038/s41467-023-40064-9
	DB00405	14493	None	19	Human	Binding	pAC50	=	8.2	8.2	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	318	5	0	2	3.9	CN(C)CC[C@@H](c1ccc(Br)cc1)c1ccccn1	10.1038/s41467-023-40064-9
	1816	2540	None	64	Human	Binding	pAC50	=	8.2	8.2	-3	17	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	265	0	0	3	2.5	CN1CCN2C(C1)c1ccccc1Cc1c2nccc1	10.1038/s41467-023-40064-9
	4205	2540	None	64	Human	Binding	pAC50	=	8.2	8.2	-3	17	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	265	0	0	3	2.5	CN1CCN2C(C1)c1ccccc1Cc1c2nccc1	10.1038/s41467-023-40064-9
	4205.0	2540	None	64	Human	Binding	pAC50	=	8.2	8.2	-3	17	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	265	0	0	3	2.5	CN1CCN2C(C1)c1ccccc1Cc1c2nccc1	10.1038/s41467-023-40064-9
	7241	2540	None	64	Human	Binding	pAC50	=	8.2	8.2	-3	17	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	265	0	0	3	2.5	CN1CCN2C(C1)c1ccccc1Cc1c2nccc1	10.1038/s41467-023-40064-9
	CHEMBL654	2540	None	64	Human	Binding	pAC50	=	8.2	8.2	-3	17	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	265	0	0	3	2.5	CN1CCN2C(C1)c1ccccc1Cc1c2nccc1	10.1038/s41467-023-40064-9
	DB00370	2540	None	64	Human	Binding	pAC50	=	8.2	8.2	-3	17	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	265	0	0	3	2.5	CN1CCN2C(C1)c1ccccc1Cc1c2nccc1	10.1038/s41467-023-40064-9
	19861	209982	None	33	Human	Binding	pAC50	=	8.2	8.2	-	1	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	290	0	0	2	3.7	CN1CCC(=C2c3ccccc3CCc3cccnc32)CC1	10.1038/s41467-023-40064-9
	19861.0	209982	None	33	Human	Binding	pAC50	=	8.2	8.2	-	1	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	290	0	0	2	3.7	CN1CCC(=C2c3ccccc3CCc3cccnc32)CC1	10.1038/s41467-023-40064-9
	CHEMBL946	209982	None	33	Human	Binding	pAC50	=	8.2	8.2	-	1	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	290	0	0	2	3.7	CN1CCC(=C2c3ccccc3CCc3cccnc32)CC1	10.1038/s41467-023-40064-9
	DB00719	209982	None	33	Human	Binding	pAC50	=	8.2	8.2	-	1	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	290	0	0	2	3.7	CN1CCC(=C2c3ccccc3CCc3cccnc32)CC1	10.1038/s41467-023-40064-9
	3926	209699	None	30	Human	Binding	pAC50	=	6.2	6.2	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	491	9	1	3	5.8	Cc1cccc(C)c1NC(=O)CN1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1	10.1038/s41467-023-40064-9
	CHEMBL92870	209699	None	30	Human	Binding	pAC50	=	6.2	6.2	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	491	9	1	3	5.8	Cc1cccc(C)c1NC(=O)CN1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1	10.1038/s41467-023-40064-9
	146015336	53364	None	65	Human	Binding	pAC50	=	5.2	5.2	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	252	2	2	2	2.0	O=C1N=C(O)NC1(c1ccccc1)c1ccccc1	10.1038/s41467-023-40064-9
	1775	53364	None	65	Human	Binding	pAC50	=	5.2	5.2	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	252	2	2	2	2.0	O=C1N=C(O)NC1(c1ccccc1)c1ccccc1	10.1038/s41467-023-40064-9
	CHEMBL16	53364	None	65	Human	Binding	pAC50	=	5.2	5.2	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	252	2	2	2	2.0	O=C1N=C(O)NC1(c1ccccc1)c1ccccc1	10.1038/s41467-023-40064-9
	CHEMBL1611	53364	None	65	Human	Binding	pAC50	=	5.2	5.2	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	252	2	2	2	2.0	O=C1N=C(O)NC1(c1ccccc1)c1ccccc1	10.1038/s41467-023-40064-9
	1353	1911	None	63	Human	Binding	pAC50	=	5.2	5.2	-489	85	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	10.1038/s41467-023-40064-9
	3559	1911	None	63	Human	Binding	pAC50	=	5.2	5.2	-489	85	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	10.1038/s41467-023-40064-9
	3559.0	1911	None	63	Human	Binding	pAC50	=	5.2	5.2	-489	85	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	10.1038/s41467-023-40064-9
	86	1911	None	63	Human	Binding	pAC50	=	5.2	5.2	-489	85	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	10.1038/s41467-023-40064-9
	CHEMBL54	1911	None	63	Human	Binding	pAC50	=	5.2	5.2	-489	85	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	10.1038/s41467-023-40064-9
	DB00502	1911	None	63	Human	Binding	pAC50	=	5.2	5.2	-489	85	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	10.1038/s41467-023-40064-9
	5453	206077	None	58	Human	Binding	pAC50	=	7.2	7.2	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	189	3	0	1	0.2	S=P(N1CC1)(N1CC1)N1CC1	10.1038/s41467-023-40064-9
	CHEMBL671	206077	None	58	Human	Binding	pAC50	=	7.2	7.2	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	189	3	0	1	0.2	S=P(N1CC1)(N1CC1)N1CC1	10.1038/s41467-023-40064-9
	2435	3590	None	59	Human	Binding	pAC50	=	5.2	5.2	-95	48	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	440	5	1	3	4.6	Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O	10.1038/s41467-023-40064-9
	60149	3590	None	59	Human	Binding	pAC50	=	5.2	5.2	-95	48	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	440	5	1	3	4.6	Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O	10.1038/s41467-023-40064-9
	98	3590	None	59	Human	Binding	pAC50	=	5.2	5.2	-95	48	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	440	5	1	3	4.6	Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O	10.1038/s41467-023-40064-9
	CHEMBL12713	3590	None	59	Human	Binding	pAC50	=	5.2	5.2	-95	48	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	440	5	1	3	4.6	Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O	10.1038/s41467-023-40064-9
	DB06144	3590	None	59	Human	Binding	pAC50	=	5.2	5.2	-95	48	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	440	5	1	3	4.6	Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O	10.1038/s41467-023-40064-9
	65866	94317	None	50	Human	Binding	pAC50	=	5.2	5.2	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	611	12	1	8	6.5	COC(=O)C1=C(C)NC(C)=C(C(=O)OC(C)(C)CN(C)CCC(c2ccccc2)c2ccccc2)C1c1cccc([N+](=O)[O-])c1	10.1038/s41467-023-40064-9
	CHEMBL250270	94317	None	50	Human	Binding	pAC50	=	5.2	5.2	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	611	12	1	8	6.5	COC(=O)C1=C(C)NC(C)=C(C(=O)OC(C)(C)CN(C)CCC(c2ccccc2)c2ccccc2)C1c1cccc([N+](=O)[O-])c1	10.1038/s41467-023-40064-9
	4450	178333	None	41	Human	Binding	pAC50	=	6.2	6.2	-	3	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	253	1	0	2	3.2	CN1CCOC(c2ccccc2)c2ccccc2C1	10.1038/s41467-023-40064-9
	CHEMBL465026	178333	None	41	Human	Binding	pAC50	=	6.2	6.2	-	3	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	253	1	0	2	3.2	CN1CCOC(c2ccccc2)c2ccccc2C1	10.1038/s41467-023-40064-9
	3947	208853	None	39	Human	Binding	pAC50	=	6.2	6.2	-7	15	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	418	7	0	3	5.8	CN(CCCN1c2ccccc2CCc2ccccc21)CC(=O)c1ccc(Cl)cc1	10.1038/s41467-023-40064-9
	CHEMBL87708	208853	None	39	Human	Binding	pAC50	=	6.2	6.2	-7	15	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	418	7	0	3	5.8	CN(CCCN1c2ccccc2CCc2ccccc21)CC(=O)c1ccc(Cl)cc1	10.1038/s41467-023-40064-9
	2398	954	None	43	Human	Binding	pAC50	=	7.2	7.2	-1	28	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	314	4	0	2	4.5	CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C	10.1038/s41467-023-40064-9
	2801	954	None	43	Human	Binding	pAC50	=	7.2	7.2	-1	28	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	314	4	0	2	4.5	CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C	10.1038/s41467-023-40064-9
	2801.0	954	None	43	Human	Binding	pAC50	=	7.2	7.2	-1	28	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	314	4	0	2	4.5	CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C	10.1038/s41467-023-40064-9
	701	954	None	43	Human	Binding	pAC50	=	7.2	7.2	-1	28	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	314	4	0	2	4.5	CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C	10.1038/s41467-023-40064-9
	CHEMBL415	954	None	43	Human	Binding	pAC50	=	7.2	7.2	-1	28	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	314	4	0	2	4.5	CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C	10.1038/s41467-023-40064-9
	DB01242	954	None	43	Human	Binding	pAC50	=	7.2	7.2	-1	28	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	314	4	0	2	4.5	CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C	10.1038/s41467-023-40064-9
	191	403	None	60	Human	Binding	pAC50	=	7.2	7.2	-56	28	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	313	0	1	4	3.4	Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1	10.1038/s41467-023-40064-9
	201	403	None	60	Human	Binding	pAC50	=	7.2	7.2	-56	28	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	313	0	1	4	3.4	Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1	10.1038/s41467-023-40064-9
	2170	403	None	60	Human	Binding	pAC50	=	7.2	7.2	-56	28	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	313	0	1	4	3.4	Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1	10.1038/s41467-023-40064-9
	2170.0	403	None	60	Human	Binding	pAC50	=	7.2	7.2	-56	28	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	313	0	1	4	3.4	Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1	10.1038/s41467-023-40064-9
	CHEMBL1113	403	None	60	Human	Binding	pAC50	=	7.2	7.2	-56	28	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	313	0	1	4	3.4	Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1	10.1038/s41467-023-40064-9
	DB00543	403	None	60	Human	Binding	pAC50	=	7.2	7.2	-56	28	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	313	0	1	4	3.4	Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1	10.1038/s41467-023-40064-9
	37	778	None	41	Human	Binding	pAC50	=	5.2	5.2	-	17	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	451	8	2	4	3.2	C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C	10.1038/s41467-023-40064-9
	460	778	None	41	Human	Binding	pAC50	=	5.2	5.2	-	17	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	451	8	2	4	3.2	C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C	10.1038/s41467-023-40064-9
	54746	778	None	41	Human	Binding	pAC50	=	5.2	5.2	-	17	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	451	8	2	4	3.2	C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C	10.1038/s41467-023-40064-9
	54746.0	778	None	41	Human	Binding	pAC50	=	5.2	5.2	-	17	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	451	8	2	4	3.2	C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C	10.1038/s41467-023-40064-9
	CHEMBL1201087	778	None	41	Human	Binding	pAC50	=	5.2	5.2	-	17	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	451	8	2	4	3.2	C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C	10.1038/s41467-023-40064-9
	DB00248	778	None	41	Human	Binding	pAC50	=	5.2	5.2	-	17	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	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
	5904	100446	None	26	Human	Binding	pAC50	=	5.2	5.2	-	1	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	334	4	2	4	0.9	CC1(C)S[C@@H]2[C@H](NC(=O)Cc3ccccc3)C(=O)N2[C@H]1C(=O)O	10.1038/s41467-023-40064-9
	CHEMBL1223	100446	None	26	Human	Binding	pAC50	=	5.2	5.2	-	1	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	334	4	2	4	0.9	CC1(C)S[C@@H]2[C@H](NC(=O)Cc3ccccc3)C(=O)N2[C@H]1C(=O)O	10.1038/s41467-023-40064-9
	CHEMBL29	100446	None	26	Human	Binding	pAC50	=	5.2	5.2	-	1	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	334	4	2	4	0.9	CC1(C)S[C@@H]2[C@H](NC(=O)Cc3ccccc3)C(=O)N2[C@H]1C(=O)O	10.1038/s41467-023-40064-9
	2286	3183	None	36	Human	Binding	pAC50	=	8.2	8.2	-3	29	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	10.1038/s41467-023-40064-9
	4927	3183	None	36	Human	Binding	pAC50	=	8.2	8.2	-3	29	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	10.1038/s41467-023-40064-9
	4927.0	3183	None	36	Human	Binding	pAC50	=	8.2	8.2	-3	29	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	10.1038/s41467-023-40064-9
	7282	3183	None	36	Human	Binding	pAC50	=	8.2	8.2	-3	29	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	10.1038/s41467-023-40064-9
	CHEMBL643	3183	None	36	Human	Binding	pAC50	=	8.2	8.2	-3	29	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	10.1038/s41467-023-40064-9
	DB01069	3183	None	36	Human	Binding	pAC50	=	8.2	8.2	-3	29	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	10.1038/s41467-023-40064-9
	103	4153	None	44	Human	Binding	pAC50	=	8.2	8.2	-1	53	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	331	4	0	3	4.9	CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C	10.1038/s41467-023-40064-9
	2875	4153	None	44	Human	Binding	pAC50	=	8.2	8.2	-1	53	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	331	4	0	3	4.9	CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C	10.1038/s41467-023-40064-9
	5736	4153	None	44	Human	Binding	pAC50	=	8.2	8.2	-1	53	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	331	4	0	3	4.9	CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C	10.1038/s41467-023-40064-9
	CHEMBL285802	4153	None	44	Human	Binding	pAC50	=	8.2	8.2	-1	53	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	331	4	0	3	4.9	CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C	10.1038/s41467-023-40064-9
	DB09225	4153	None	44	Human	Binding	pAC50	=	8.2	8.2	-1	53	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	331	4	0	3	4.9	CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C	10.1038/s41467-023-40064-9
	4011	82440	None	34	Human	Binding	pAC50	=	8.1	8.1	6	23	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	277	4	1	1	4.2	CNCCCC12CCC(c3ccccc31)c1ccccc12	10.1038/s41467-023-40064-9
	CHEMBL21731	82440	None	34	Human	Binding	pAC50	=	8.1	8.1	6	23	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	277	4	1	1	4.2	CNCCCC12CCC(c3ccccc31)c1ccccc12	10.1038/s41467-023-40064-9
	16363	596	None	33	Human	Binding	pAC50	=	6.1	6.1	-	6	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	381	6	1	4	3.8	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2	10.1038/s41467-023-40064-9
	16363.0	596	None	33	Human	Binding	pAC50	=	6.1	6.1	-	6	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	381	6	1	4	3.8	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2	10.1038/s41467-023-40064-9
	312	596	None	33	Human	Binding	pAC50	=	6.1	6.1	-	6	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	381	6	1	4	3.8	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2	10.1038/s41467-023-40064-9
	9215	596	None	33	Human	Binding	pAC50	=	6.1	6.1	-	6	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	381	6	1	4	3.8	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2	10.1038/s41467-023-40064-9
	CHEMBL297302	596	None	33	Human	Binding	pAC50	=	6.1	6.1	-	6	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	381	6	1	4	3.8	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2	10.1038/s41467-023-40064-9
	DB12867	596	None	33	Human	Binding	pAC50	=	6.1	6.1	-	6	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	381	6	1	4	3.8	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2	10.1038/s41467-023-40064-9
	4418	34231	None	58	Human	Binding	pAC50	=	6.1	6.1	-	6	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	392	7	1	5	3.4	COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1	10.1038/s41467-023-40064-9
	4418.0	34231	None	58	Human	Binding	pAC50	=	6.1	6.1	-	6	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	392	7	1	5	3.4	COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1	10.1038/s41467-023-40064-9
	CHEMBL142635	34231	None	58	Human	Binding	pAC50	=	6.1	6.1	-	6	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	392	7	1	5	3.4	COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1	10.1038/s41467-023-40064-9
	DB12092	34231	None	58	Human	Binding	pAC50	=	6.1	6.1	-	6	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	392	7	1	5	3.4	COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1	10.1038/s41467-023-40064-9
	4020	207608	None	20	Human	Binding	pAC50	=	5.1	5.1	-	1	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	284	1	1	3	2.6	OC1(c2ccc(Cl)cc2)c2ccccc2C2=NCCN21	10.1038/s41467-023-40064-9
	CHEMBL781	207608	None	20	Human	Binding	pAC50	=	5.1	5.1	-	1	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	284	1	1	3	2.6	OC1(c2ccc(Cl)cc2)c2ccccc2C2=NCCN21	10.1038/s41467-023-40064-9
	23480	124157	None	21	Human	Binding	pAC50	=	6.1	6.1	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	281	5	1	1	5.0	CC(CC(c1ccccc1)c1ccccc1)NC(C)(C)C	10.1038/s41467-023-40064-9
	CHEMBL363295	124157	None	21	Human	Binding	pAC50	=	6.1	6.1	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	281	5	1	1	5.0	CC(CC(c1ccccc1)c1ccccc1)NC(C)(C)C	10.1038/s41467-023-40064-9
	1222	881	None	0	Human	Binding	pAC50	=	7.1	7.1	-1	2	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	388	8	1	4	3.1	OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1	10.1038/s41467-023-40064-9
	2678	881	None	0	Human	Binding	pAC50	=	7.1	7.1	-1	2	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	388	8	1	4	3.1	OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1	10.1038/s41467-023-40064-9
	2678.0	881	None	0	Human	Binding	pAC50	=	7.1	7.1	-1	2	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	388	8	1	4	3.1	OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1	10.1038/s41467-023-40064-9
	581	881	None	0	Human	Binding	pAC50	=	7.1	7.1	-1	2	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	388	8	1	4	3.1	OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1	10.1038/s41467-023-40064-9
	CHEMBL1000	881	None	0	Human	Binding	pAC50	=	7.1	7.1	-1	2	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	388	8	1	4	3.1	OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1	10.1038/s41467-023-40064-9
	DB00341	881	None	0	Human	Binding	pAC50	=	7.1	7.1	-1	2	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	388	8	1	4	3.1	OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1	10.1038/s41467-023-40064-9
	9801	91619	None	25	Human	Binding	pAC50	=	5.1	5.1	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	329	8	1	1	5.4	CC(Cc1ccccc1)NCCC(c1ccccc1)c1ccccc1	10.1038/s41467-023-40064-9
	CHEMBL24072	91619	None	25	Human	Binding	pAC50	=	5.1	5.1	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	329	8	1	1	5.4	CC(Cc1ccccc1)NCCC(c1ccccc1)c1ccccc1	10.1038/s41467-023-40064-9
	5411	206491	None	57	Human	Binding	pAC50	=	5.1	5.1	-	2	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	264	8	1	4	2.6	CCCCNc1ccc(C(=O)OCCN(C)C)cc1	10.1038/s41467-023-40064-9
	CHEMBL698	206491	None	57	Human	Binding	pAC50	=	5.1	5.1	-	2	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	264	8	1	4	2.6	CCCCNc1ccc(C(=O)OCCN(C)C)cc1	10.1038/s41467-023-40064-9
	135398745	2914	None	65	Human	Binding	pAC50	=	8.1	8.1	1	65	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	312	1	1	5	1.7	CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C	10.1038/s41467-023-40064-9
	135398745.0	2914	None	65	Human	Binding	pAC50	=	8.1	8.1	1	65	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	312	1	1	5	1.7	CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C	10.1038/s41467-023-40064-9
	47	2914	None	65	Human	Binding	pAC50	=	8.1	8.1	1	65	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	312	1	1	5	1.7	CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C	10.1038/s41467-023-40064-9
	CHEMBL715	2914	None	65	Human	Binding	pAC50	=	8.1	8.1	1	65	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	312	1	1	5	1.7	CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C	10.1038/s41467-023-40064-9
	DB00334	2914	None	65	Human	Binding	pAC50	=	8.1	8.1	1	65	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	312	1	1	5	1.7	CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C	10.1038/s41467-023-40064-9
	2762	3863	None	23	Human	Binding	pAC50	=	7.1	7.1	-9	2	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	255	6	0	3	2.7	CN(CCN(c1ccccn1)Cc1ccccc1)C	10.1038/s41467-023-40064-9
	5587	3863	None	23	Human	Binding	pAC50	=	7.1	7.1	-9	2	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	255	6	0	3	2.7	CN(CCN(c1ccccn1)Cc1ccccc1)C	10.1038/s41467-023-40064-9
	5587.0	3863	None	23	Human	Binding	pAC50	=	7.1	7.1	-9	2	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	255	6	0	3	2.7	CN(CCN(c1ccccn1)Cc1ccccc1)C	10.1038/s41467-023-40064-9
	7318	3863	None	23	Human	Binding	pAC50	=	7.1	7.1	-9	2	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	255	6	0	3	2.7	CN(CCN(c1ccccn1)Cc1ccccc1)C	10.1038/s41467-023-40064-9
	CHEMBL1241	3863	None	23	Human	Binding	pAC50	=	7.1	7.1	-9	2	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	255	6	0	3	2.7	CN(CCN(c1ccccn1)Cc1ccccc1)C	10.1038/s41467-023-40064-9
	DB00792	3863	None	23	Human	Binding	pAC50	=	7.1	7.1	-9	2	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	255	6	0	3	2.7	CN(CCN(c1ccccn1)Cc1ccccc1)C	10.1038/s41467-023-40064-9
	2247	505	None	55	Human	Binding	pAC50	=	7.1	7.1	-4	41	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	10.1038/s41467-023-40064-9
	249	505	None	55	Human	Binding	pAC50	=	7.1	7.1	-4	41	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	10.1038/s41467-023-40064-9
	2603	505	None	55	Human	Binding	pAC50	=	7.1	7.1	-4	41	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	10.1038/s41467-023-40064-9
	CHEMBL296419	505	None	55	Human	Binding	pAC50	=	7.1	7.1	-4	41	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	10.1038/s41467-023-40064-9
	DB00637	505	None	55	Human	Binding	pAC50	=	7.1	7.1	-4	41	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	10.1038/s41467-023-40064-9
	9417	133581	None	40	Human	Binding	pAC50	=	7.1	7.1	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	363	6	1	4	3.3	OCCN1CCN(CCCN2c3ccccc3C=Cc3ccccc32)CC1	10.1038/s41467-023-40064-9
	CHEMBL1524185	133581	None	40	Human	Binding	pAC50	=	7.1	7.1	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	363	6	1	4	3.3	OCCN1CCN(CCCN2c3ccccc3C=Cc3ccccc32)CC1	10.1038/s41467-023-40064-9
	CHEMBL370753	133581	None	40	Human	Binding	pAC50	=	7.1	7.1	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	363	6	1	4	3.3	OCCN1CCN(CCCN2c3ccccc3C=Cc3ccccc32)CC1	10.1038/s41467-023-40064-9
	11291	98850	None	21	Human	Binding	pAC50	=	5.1	5.1	-	2	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	261	1	0	1	3.9	CN1CCC2=C(C1)C(c1ccccc1)c1ccccc12	10.1038/s41467-023-40064-9
	11291.0	98850	None	21	Human	Binding	pAC50	=	5.1	5.1	-	2	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	261	1	0	1	3.9	CN1CCC2=C(C1)C(c1ccccc1)c1ccccc12	10.1038/s41467-023-40064-9
	CHEMBL278398	98850	None	21	Human	Binding	pAC50	=	5.1	5.1	-	2	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	261	1	0	1	3.9	CN1CCC2=C(C1)C(c1ccccc1)c1ccccc12	10.1038/s41467-023-40064-9
	DB01619	98850	None	21	Human	Binding	pAC50	=	5.1	5.1	-	2	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	261	1	0	1	3.9	CN1CCC2=C(C1)C(c1ccccc1)c1ccccc12	10.1038/s41467-023-40064-9
	2712	916	None	18	Human	Binding	pAC50	=	5.1	5.1	-5	4	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	299	1	1	3	3.0	CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl	10.1038/s41467-023-40064-9
	3370	916	None	18	Human	Binding	pAC50	=	5.1	5.1	-5	4	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	299	1	1	3	3.0	CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl	10.1038/s41467-023-40064-9
	594	916	None	18	Human	Binding	pAC50	=	5.1	5.1	-5	4	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	299	1	1	3	3.0	CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl	10.1038/s41467-023-40064-9
	CHEMBL451	916	None	18	Human	Binding	pAC50	=	5.1	5.1	-5	4	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	299	1	1	3	3.0	CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl	10.1038/s41467-023-40064-9
	DB00475	916	None	18	Human	Binding	pAC50	=	5.1	5.1	-5	4	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	299	1	1	3	3.0	CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl	10.1038/s41467-023-40064-9
	1193	1656	None	64	Human	Binding	pAC50	=	7.1	7.1	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	281	3	2	2	4.1	OC(=O)c1ccccc1Nc1cccc(c1)C(F)(F)F	10.1038/s41467-023-40064-9
	2447	1656	None	64	Human	Binding	pAC50	=	7.1	7.1	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	281	3	2	2	4.1	OC(=O)c1ccccc1Nc1cccc(c1)C(F)(F)F	10.1038/s41467-023-40064-9
	3371	1656	None	64	Human	Binding	pAC50	=	7.1	7.1	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	281	3	2	2	4.1	OC(=O)c1ccccc1Nc1cccc(c1)C(F)(F)F	10.1038/s41467-023-40064-9
	CHEMBL23588	1656	None	64	Human	Binding	pAC50	=	7.1	7.1	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	281	3	2	2	4.1	OC(=O)c1ccccc1Nc1cccc(c1)C(F)(F)F	10.1038/s41467-023-40064-9
	DB02266	1656	None	64	Human	Binding	pAC50	=	7.1	7.1	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	281	3	2	2	4.1	OC(=O)c1ccccc1Nc1cccc(c1)C(F)(F)F	10.1038/s41467-023-40064-9
	135564886	14499	None	5	Human	Binding	pAC50	=	5.1	5.1	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	752	14	1	6	8.7	CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21	10.1038/s41467-023-40064-9
	135673376	14499	None	5	Human	Binding	pAC50	=	5.1	5.1	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	752	14	1	6	8.7	CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21	10.1038/s41467-023-40064-9
	137157436	14499	None	5	Human	Binding	pAC50	=	5.1	5.1	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	752	14	1	6	8.7	CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21	10.1038/s41467-023-40064-9
	145948239	14499	None	5	Human	Binding	pAC50	=	5.1	5.1	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	752	14	1	6	8.7	CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21	10.1038/s41467-023-40064-9
	71587099	14499	None	5	Human	Binding	pAC50	=	5.1	5.1	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	752	14	1	6	8.7	CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21	10.1038/s41467-023-40064-9
	CHEMBL1201304	14499	None	5	Human	Binding	pAC50	=	5.1	5.1	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	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
	1222	1664	None	37	Human	Binding	pAC50	=	6.1	6.1	-17	32	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	475	7	1	3	5.3	Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1	10.1038/s41467-023-40064-9
	3396	1664	None	37	Human	Binding	pAC50	=	6.1	6.1	-17	32	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	475	7	1	3	5.3	Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1	10.1038/s41467-023-40064-9
	3396.0	1664	None	37	Human	Binding	pAC50	=	6.1	6.1	-17	32	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	475	7	1	3	5.3	Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1	10.1038/s41467-023-40064-9
	85	1664	None	37	Human	Binding	pAC50	=	6.1	6.1	-17	32	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	475	7	1	3	5.3	Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1	10.1038/s41467-023-40064-9
	CHEMBL46516	1664	None	37	Human	Binding	pAC50	=	6.1	6.1	-17	32	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	475	7	1	3	5.3	Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1	10.1038/s41467-023-40064-9
	DB04842	1664	None	37	Human	Binding	pAC50	=	6.1	6.1	-17	32	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	475	7	1	3	5.3	Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1	10.1038/s41467-023-40064-9
	3180	14479	None	25	Human	Binding	pAC50	=	5.1	5.1	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	289	8	0	3	3.9	CCCCOc1ccc(C(=O)CCN2CCCCC2)cc1	10.1038/s41467-023-40064-9
	CHEMBL1201217	14479	None	25	Human	Binding	pAC50	=	5.1	5.1	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	289	8	0	3	3.9	CCCCOc1ccc(C(=O)CCN2CCCCC2)cc1	10.1038/s41467-023-40064-9
	2794	19387	None	54	Human	Binding	pAC50	=	5.1	5.1	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	472	4	1	4	7.5	CC(C)/N=c1\cc2n(-c3ccc(Cl)cc3)c3ccccc3nc-2cc1Nc1ccc(Cl)cc1	10.1038/s41467-023-40064-9
	CHEMBL1292	19387	None	54	Human	Binding	pAC50	=	5.1	5.1	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	472	4	1	4	7.5	CC(C)/N=c1\cc2n(-c3ccc(Cl)cc3)c3ccccc3nc-2cc1Nc1ccc(Cl)cc1	10.1038/s41467-023-40064-9
	5284616	161721	None	39	Human	Binding	pAC50	=	6.1	6.1	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	914	6	3	13	6.2	CO[C@H]1C[C@@H]2CC[C@@H](C)[C@@](O)(O2)C(=O)C(=O)N2CCCC[C@H]2C(=O)O[C@H]([C@H](C)C[C@@H]2CC[C@@H](O)[C@H](OC)C2)CC(=O)[C@H](C)/C=C(\C)[C@@H](O)[C@@H](OC)C(=O)[C@H](C)C[C@H](C)/C=C/C=C/C=C/1C	10.1038/s41467-023-40064-9
	CHEMBL413	161721	None	39	Human	Binding	pAC50	=	6.1	6.1	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	914	6	3	13	6.2	CO[C@H]1C[C@@H]2CC[C@@H](C)[C@@](O)(O2)C(=O)C(=O)N2CCCC[C@H]2C(=O)O[C@H]([C@H](C)C[C@@H]2CC[C@@H](O)[C@H](OC)C2)CC(=O)[C@H](C)/C=C(\C)[C@@H](O)[C@@H](OC)C(=O)[C@H](C)C[C@H](C)/C=C/C=C/C=C/1C	10.1038/s41467-023-40064-9
	2351	4301	None	35	Human	Binding	pAC50	=	5.1	5.1	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	366	10	0	3	4.8	CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1	10.1038/s41467-023-40064-9
	CHEMBL1008	4301	None	35	Human	Binding	pAC50	=	5.1	5.1	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	366	10	0	3	4.8	CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1	10.1038/s41467-023-40064-9
	CHEMBL1257078	4301	None	35	Human	Binding	pAC50	=	5.1	5.1	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	366	10	0	3	4.8	CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1	10.1038/s41467-023-40064-9
	213046	2385	None	44	Human	Binding	pAC50	=	5.1	5.1	-	8	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	492	5	0	6	4.3	O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1	10.1038/s41467-023-40064-9
	213046.0	2385	None	44	Human	Binding	pAC50	=	5.1	5.1	-	8	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	492	5	0	6	4.3	O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1	10.1038/s41467-023-40064-9
	4168	2385	None	44	Human	Binding	pAC50	=	5.1	5.1	-	8	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	492	5	0	6	4.3	O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1	10.1038/s41467-023-40064-9
	7461	2385	None	44	Human	Binding	pAC50	=	5.1	5.1	-	8	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	492	5	0	6	4.3	O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1	10.1038/s41467-023-40064-9
	CHEMBL1237021	2385	None	44	Human	Binding	pAC50	=	5.1	5.1	-	8	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	492	5	0	6	4.3	O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1	10.1038/s41467-023-40064-9
	DB08815	2385	None	44	Human	Binding	pAC50	=	5.1	5.1	-	8	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	492	5	0	6	4.3	O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1	10.1038/s41467-023-40064-9
	135398735	137055	None	20	Human	Binding	pAC50	=	5.1	5.1	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	822	4	6	15	4.3	CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c(/C=N/N5CCN(C)CC5)c(O)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C	10.1038/s41467-023-40064-9
	136262914	137055	None	20	Human	Binding	pAC50	=	5.1	5.1	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	822	4	6	15	4.3	CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c(/C=N/N5CCN(C)CC5)c(O)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C	10.1038/s41467-023-40064-9
	CHEMBL374478	137055	None	20	Human	Binding	pAC50	=	5.1	5.1	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	822	4	6	15	4.3	CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c(/C=N/N5CCN(C)CC5)c(O)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C	10.1038/s41467-023-40064-9
	202	1508	None	46	Human	Binding	pAC50	=	5.1	5.1	-1	33	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	297	6	1	3	4.6	CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2	10.1038/s41467-023-40064-9
	60835	1508	None	46	Human	Binding	pAC50	=	5.1	5.1	-1	33	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	297	6	1	3	4.6	CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2	10.1038/s41467-023-40064-9
	972	1508	None	46	Human	Binding	pAC50	=	5.1	5.1	-1	33	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	297	6	1	3	4.6	CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2	10.1038/s41467-023-40064-9
	CHEMBL1175	1508	None	46	Human	Binding	pAC50	=	5.1	5.1	-1	33	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	297	6	1	3	4.6	CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2	10.1038/s41467-023-40064-9
	DB00476	1508	None	46	Human	Binding	pAC50	=	5.1	5.1	-1	33	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	297	6	1	3	4.6	CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2	10.1038/s41467-023-40064-9
	2335	11852	None	18	Human	Binding	pAC50	=	5.1	5.1	-	12	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	412	11	0	2	6.1	CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1	10.1038/s41467-023-40064-9
	8478	11852	None	18	Human	Binding	pAC50	=	5.1	5.1	-	12	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	412	11	0	2	6.1	CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1	10.1038/s41467-023-40064-9
	CHEMBL1182210	11852	None	18	Human	Binding	pAC50	=	5.1	5.1	-	12	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	412	11	0	2	6.1	CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1	10.1038/s41467-023-40064-9
	CHEMBL221753	11852	None	18	Human	Binding	pAC50	=	5.1	5.1	-	12	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	412	11	0	2	6.1	CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1	10.1038/s41467-023-40064-9
	3547	141460	None	43	Human	Binding	pAC50	=	5.0	5.0	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	291	2	1	4	1.2	O=S(=O)(c1cccc2cnccc12)N1CCCNCC1	10.1038/s41467-023-40064-9
	CHEMBL38380	141460	None	43	Human	Binding	pAC50	=	5.0	5.0	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	291	2	1	4	1.2	O=S(=O)(c1cccc2cnccc12)N1CCCNCC1	10.1038/s41467-023-40064-9
	CHEMBL541388	141460	None	43	Human	Binding	pAC50	=	5.0	5.0	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	291	2	1	4	1.2	O=S(=O)(c1cccc2cnccc12)N1CCCNCC1	10.1038/s41467-023-40064-9
	2179	167616	None	49	Human	Binding	pAC50	=	5.0	5.0	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	393	5	2	5	4.5	COc1cc(NS(C)(=O)=O)ccc1Nc1c2ccccc2nc2ccccc12	10.1038/s41467-023-40064-9
	CHEMBL1256655	167616	None	49	Human	Binding	pAC50	=	5.0	5.0	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	393	5	2	5	4.5	COc1cc(NS(C)(=O)=O)ccc1Nc1c2ccccc2nc2ccccc12	10.1038/s41467-023-40064-9
	CHEMBL43	167616	None	49	Human	Binding	pAC50	=	5.0	5.0	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	393	5	2	5	4.5	COc1cc(NS(C)(=O)=O)ccc1Nc1c2ccccc2nc2ccccc12	10.1038/s41467-023-40064-9
	100	3805	None	44	Human	Binding	pAC50	=	7.0	7.0	-7	55	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	10.1038/s41467-023-40064-9
	2637	3805	None	44	Human	Binding	pAC50	=	7.0	7.0	-7	55	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	10.1038/s41467-023-40064-9
	5452	3805	None	44	Human	Binding	pAC50	=	7.0	7.0	-7	55	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	10.1038/s41467-023-40064-9
	CHEMBL479	3805	None	44	Human	Binding	pAC50	=	7.0	7.0	-7	55	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	10.1038/s41467-023-40064-9
	DB00679	3805	None	44	Human	Binding	pAC50	=	7.0	7.0	-7	55	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	10.1038/s41467-023-40064-9
	2448	99377	None	50	Human	Binding	pAC50	=	5.0	5.0	-4	17	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	419	6	1	3	4.5	O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1	10.1038/s41467-023-40064-9
	2448.0	99377	None	50	Human	Binding	pAC50	=	5.0	5.0	-4	17	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	419	6	1	3	4.5	O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1	10.1038/s41467-023-40064-9
	CHEMBL28218	99377	None	50	Human	Binding	pAC50	=	5.0	5.0	-4	17	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	419	6	1	3	4.5	O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1	10.1038/s41467-023-40064-9
	DB12401	99377	None	50	Human	Binding	pAC50	=	5.0	5.0	-4	17	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	419	6	1	3	4.5	O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1	10.1038/s41467-023-40064-9
	4642	42000	None	22	Human	Binding	pAC50	=	6	6.0	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	344	5	1	5	2.7	CN1CCCN=C1COC(=O)C(O)(c1ccccc1)C1CCCCC1	10.1038/s41467-023-40064-9
	4642.0	42000	None	22	Human	Binding	pAC50	=	6	6.0	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	344	5	1	5	2.7	CN1CCCN=C1COC(=O)C(O)(c1ccccc1)C1CCCCC1	10.1038/s41467-023-40064-9
	CHEMBL1495	42000	None	22	Human	Binding	pAC50	=	6	6.0	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	344	5	1	5	2.7	CN1CCCN=C1COC(=O)C(O)(c1ccccc1)C1CCCCC1	10.1038/s41467-023-40064-9
	DB00383	42000	None	22	Human	Binding	pAC50	=	6	6.0	-	0	Binding affinity towards human HRH1 in an in vitro assay measured by filtrationBinding affinity towards human HRH1 in an in vitro assay measured by filtration	ChEMBL	344	5	1	5	2.7	CN1CCCN=C1COC(=O)C(O)(c1ccccc1)C1CCCCC1	10.1038/s41467-023-40064-9
	135398737	958	None	57	Human	Binding	pEC50	=	9.4	9.4	2	91	Inverse agonist activity at human histamine H1 receptor by R-SAT assayInverse agonist activity at human histamine H1 receptor by R-SAT assay	ChEMBL	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	nan
	135398737.0	958	None	57	Human	Binding	pEC50	=	9.4	9.4	2	91	Inverse agonist activity at human histamine H1 receptor by R-SAT assayInverse agonist activity at human histamine H1 receptor by R-SAT assay	ChEMBL	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	nan
	38	958	None	57	Human	Binding	pEC50	=	9.4	9.4	2	91	Inverse agonist activity at human histamine H1 receptor by R-SAT assayInverse agonist activity at human histamine H1 receptor by R-SAT assay	ChEMBL	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	nan
	722	958	None	57	Human	Binding	pEC50	=	9.4	9.4	2	91	Inverse agonist activity at human histamine H1 receptor by R-SAT assayInverse agonist activity at human histamine H1 receptor by R-SAT assay	ChEMBL	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	nan
	CHEMBL42	958	None	57	Human	Binding	pEC50	=	9.4	9.4	2	91	Inverse agonist activity at human histamine H1 receptor by R-SAT assayInverse agonist activity at human histamine H1 receptor by R-SAT assay	ChEMBL	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	nan
	DB00363	958	None	57	Human	Binding	pEC50	=	9.4	9.4	2	91	Inverse agonist activity at human histamine H1 receptor by R-SAT assayInverse agonist activity at human histamine H1 receptor by R-SAT assay	ChEMBL	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	nan
	11327353	165716	None	0	Guinea pig	Binding	pEC50	=	6.9	6.9	-	0	Effective concentration against histamine H1 receptor in guinea pig ileumEffective concentration against histamine H1 receptor in guinea pig ileum	ChEMBL	410	11	2	3	4.9	c1ccc(C(CCc2nc(CCNCCc3ccncc3)c[nH]2)c2ccccc2)cc1	10.1021/jm0309147
	CHEMBL424336	165716	None	0	Guinea pig	Binding	pEC50	=	6.9	6.9	-	0	Effective concentration against histamine H1 receptor in guinea pig ileumEffective concentration against histamine H1 receptor in guinea pig ileum	ChEMBL	410	11	2	3	4.9	c1ccc(C(CCc2nc(CCNCCc3ccncc3)c[nH]2)c2ccccc2)cc1	10.1021/jm0309147
	11201079	46232	None	0	Guinea pig	Binding	pEC50	=	6.9	6.9	-	0	Effective concentration against histamine H1 receptor in guinea pig ileumEffective concentration against histamine H1 receptor in guinea pig ileum	ChEMBL	424	12	2	3	5.3	c1ccc(C(CCc2nc(CCNCCCc3cccnc3)c[nH]2)c2ccccc2)cc1	10.1021/jm0309147
	CHEMBL153474	46232	None	0	Guinea pig	Binding	pEC50	=	6.9	6.9	-	0	Effective concentration against histamine H1 receptor in guinea pig ileumEffective concentration against histamine H1 receptor in guinea pig ileum	ChEMBL	424	12	2	3	5.3	c1ccc(C(CCc2nc(CCNCCCc3cccnc3)c[nH]2)c2ccccc2)cc1	10.1021/jm0309147
	11235688	119916	None	0	Guinea pig	Binding	pEC50	=	6.9	6.9	-	1	Effective concentration against histamine H1 receptor in guinea pig ileumEffective concentration against histamine H1 receptor in guinea pig ileum	ChEMBL	427	13	3	3	5.1	c1ccc(C(CCc2nc(CCNCCCCc3c[nH]cn3)c[nH]2)c2ccccc2)cc1	10.1021/jm0309147
	CHEMBL348656	119916	None	0	Guinea pig	Binding	pEC50	=	6.9	6.9	-	1	Effective concentration against histamine H1 receptor in guinea pig ileumEffective concentration against histamine H1 receptor in guinea pig ileum	ChEMBL	427	13	3	3	5.1	c1ccc(C(CCc2nc(CCNCCCCc3c[nH]cn3)c[nH]2)c2ccccc2)cc1	10.1021/jm0309147
	42625384	169876	None	0	Human	Binding	pEC50	=	4.9	4.9	-	1	Agonist activity at human H1 receptor expressed in insect Sf9 cells co-expressing RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H1 receptor expressed in insect Sf9 cells co-expressing RGS4 assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	209	4	3	2	-0.2	CC(=O)/N=C(\N)NCCCc1c[nH]cn1	10.1021/jm9000693
	CHEMBL443896	169876	None	0	Human	Binding	pEC50	=	4.9	4.9	-	1	Agonist activity at human H1 receptor expressed in insect Sf9 cells co-expressing RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H1 receptor expressed in insect Sf9 cells co-expressing RGS4 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
	1204	1932	None	74	Human	Binding	pEC50	=	7.9	7.9	-501	24	Inhibition of human Histamine H1 receptor using [3H]pyrilamineInhibition of human Histamine H1 receptor using [3H]pyrilamine	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm020415q
	1247	1932	None	74	Human	Binding	pEC50	=	7.9	7.9	-501	24	Inhibition of human Histamine H1 receptor using [3H]pyrilamineInhibition of human Histamine H1 receptor using [3H]pyrilamine	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm020415q
	1375	1932	None	74	Human	Binding	pEC50	=	7.9	7.9	-501	24	Inhibition of human Histamine H1 receptor using [3H]pyrilamineInhibition of human Histamine H1 receptor using [3H]pyrilamine	ChEMBL	111	2

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Main reference

Ligand source activities (1 row/activity)