Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
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name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Potency)
# tested GPCRs
(Potency)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
56953889 81641 0 None 120 2 Guinea pig 9.6 pEC50 = 9.6 Functional
Agonist activity at H2R in spontaneously beating guinea pig right atrium assessed as increase in heart rateAgonist activity at H2R in spontaneously beating guinea pig right atrium assessed as increase in heart rate
ChEMBL 564 15 6 8 2.1 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/jm201128q
CHEMBL2165630 81641 0 None 120 2 Guinea pig 9.6 pEC50 = 9.6 Functional
Agonist activity at H2R in spontaneously beating guinea pig right atrium assessed as increase in heart rateAgonist activity at H2R in spontaneously beating guinea pig right atrium assessed as increase in heart rate
ChEMBL 564 15 6 8 2.1 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/jm201128q
56954000 81643 0 None 10 2 Guinea pig 9.4 pEC50 = 9.4 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 592 17 6 8 2.9 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/jm201128q
CHEMBL2165632 81643 0 None 10 2 Guinea pig 9.4 pEC50 = 9.4 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 592 17 6 8 2.9 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/jm201128q
56954515 81639 0 None 5 4 Guinea pig 9.3 pEC50 = 9.3 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 546 17 6 6 2.3 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm201128q
CHEMBL2165628 81639 0 None 5 4 Guinea pig 9.3 pEC50 = 9.3 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 546 17 6 6 2.3 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm201128q
56954515 81639 0 None 5 4 Guinea pig 9.3 pEC50 = 9.3 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 546 17 6 6 2.3 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm201128q
CHEMBL2165628 81639 0 None 5 4 Guinea pig 9.3 pEC50 = 9.3 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 546 17 6 6 2.3 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm201128q
56954322 81654 0 None 2 4 Guinea pig 9.2 pEC50 = 9.2 Functional
Agonist activity at H2R in spontaneously beating guinea pig right atrium assessed as increase in heart rateAgonist activity at H2R in spontaneously beating guinea pig right atrium assessed as increase in heart rate
ChEMBL 500 17 6 4 1.7 N/C(=N\C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1 10.1021/jm201128q
CHEMBL2165642 81654 0 None 2 4 Guinea pig 9.2 pEC50 = 9.2 Functional
Agonist activity at H2R in spontaneously beating guinea pig right atrium assessed as increase in heart rateAgonist activity at H2R in spontaneously beating guinea pig right atrium assessed as increase in heart rate
ChEMBL 500 17 6 4 1.7 N/C(=N\C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1 10.1021/jm201128q
56953889 81641 0 None 120 2 Guinea pig 9.2 pEC50 = 9.2 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 564 15 6 8 2.1 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/jm201128q
CHEMBL2165630 81641 0 None 120 2 Guinea pig 9.2 pEC50 = 9.2 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 564 15 6 8 2.1 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/jm201128q
56953889 81641 0 None 120 2 Guinea pig 9.2 pEC50 = 9.2 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 564 15 6 8 2.1 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/jm201128q
CHEMBL2165630 81641 0 None 120 2 Guinea pig 9.2 pEC50 = 9.2 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 564 15 6 8 2.1 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/jm201128q
56953998 81642 0 None 29 2 Guinea pig 9.1 pEC50 = 9.1 Functional
Agonist activity at H2R in spontaneously beating guinea pig right atrium assessed as increase in heart rateAgonist activity at H2R in spontaneously beating guinea pig right atrium assessed as increase in heart rate
ChEMBL 578 16 6 8 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/jm201128q
CHEMBL2165631 81642 0 None 29 2 Guinea pig 9.1 pEC50 = 9.1 Functional
Agonist activity at H2R in spontaneously beating guinea pig right atrium assessed as increase in heart rateAgonist activity at H2R in spontaneously beating guinea pig right atrium assessed as increase in heart rate
ChEMBL 578 16 6 8 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/jm201128q
168281746 192270 0 None 9 3 Guinea pig 9.0 pEC50 = 9.0 Functional
Agonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beatAgonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beat
ChEMBL 365 6 4 5 1.6 CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5184911 192270 0 None 9 3 Guinea pig 9.0 pEC50 = 9.0 Functional
Agonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beatAgonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beat
ChEMBL 365 6 4 5 1.6 CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5221974 192270 0 None 9 3 Guinea pig 9.0 pEC50 = 9.0 Functional
Agonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beatAgonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beat
ChEMBL 365 6 4 5 1.6 CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1 10.1021/acs.jmedchem.1c00692
56954000 81643 0 None 10 2 Guinea pig 9.0 pEC50 = 9 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 592 17 6 8 2.9 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/jm201128q
CHEMBL2165632 81643 0 None 10 2 Guinea pig 9.0 pEC50 = 9 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 592 17 6 8 2.9 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/jm201128q
56954322 81654 0 None 2 4 Guinea pig 8.9 pEC50 = 8.9 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 500 17 6 4 1.7 N/C(=N\C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1 10.1021/jm201128q
CHEMBL2165642 81654 0 None 2 4 Guinea pig 8.9 pEC50 = 8.9 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 500 17 6 4 1.7 N/C(=N\C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1 10.1021/jm201128q
56954000 81643 0 None 10 2 Guinea pig 8.9 pEC50 = 8.9 Functional
Agonist activity at H2R in spontaneously beating guinea pig right atrium assessed as increase in heart rateAgonist activity at H2R in spontaneously beating guinea pig right atrium assessed as increase in heart rate
ChEMBL 592 17 6 8 2.9 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/jm201128q
CHEMBL2165632 81643 0 None 10 2 Guinea pig 8.9 pEC50 = 8.9 Functional
Agonist activity at H2R in spontaneously beating guinea pig right atrium assessed as increase in heart rateAgonist activity at H2R in spontaneously beating guinea pig right atrium assessed as increase in heart rate
ChEMBL 592 17 6 8 2.9 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/jm201128q
168295528 192419 0 None 12 10 Guinea pig 8.9 pEC50 = 8.9 Functional
Agonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beatAgonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beat
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5206565 192419 0 None 12 10 Guinea pig 8.9 pEC50 = 8.9 Functional
Agonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beatAgonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beat
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222872 192419 0 None 12 10 Guinea pig 8.9 pEC50 = 8.9 Functional
Agonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beatAgonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beat
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
56954129 81647 0 None 22 2 Guinea pig 8.9 pEC50 = 8.9 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 536 15 6 8 1.5 N/C(=N\C(=O)CCCCCCC(=O)/N=C(\N)NCCCc1cnc(N)s1)NCCCc1cnc(N)s1 10.1021/jm201128q
CHEMBL2165636 81647 0 None 22 2 Guinea pig 8.9 pEC50 = 8.9 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 536 15 6 8 1.5 N/C(=N\C(=O)CCCCCCC(=O)/N=C(\N)NCCCc1cnc(N)s1)NCCCc1cnc(N)s1 10.1021/jm201128q
164611474 184860 0 None - 1 Guinea pig 8.0 pEC50 = 8 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 366 6 4 5 2.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1cccs1 10.1016/j.ejmech.2021.113190
CHEMBL4861704 184860 0 None - 1 Guinea pig 8.0 pEC50 = 8 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 366 6 4 5 2.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1cccs1 10.1016/j.ejmech.2021.113190
56954517 81640 0 None 14 2 Guinea pig 8.0 pEC50 = 8.0 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 502 17 6 6 0.5 N/C(=N\C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1ncn[nH]1)NCCCc1ncn[nH]1 10.1021/jm201128q
CHEMBL2165629 81640 0 None 14 2 Guinea pig 8.0 pEC50 = 8.0 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 502 17 6 6 0.5 N/C(=N\C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1ncn[nH]1)NCCCc1ncn[nH]1 10.1021/jm201128q
164620678 185427 0 None - 1 Guinea pig 8.0 pEC50 = 8.0 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 374 7 4 4 2.7 CCC(NC(=O)/N=C(\N)NCCCc1sc(N)nc1C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4870510 185427 0 None - 1 Guinea pig 8.0 pEC50 = 8.0 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 374 7 4 4 2.7 CCC(NC(=O)/N=C(\N)NCCCc1sc(N)nc1C)c1ccccc1 10.1016/j.ejmech.2021.113190
168294449 192406 0 None 50 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 367 7 4 5 1.9 CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1 10.1021/acs.jmedchem.1c00692
CHEMBL5204599 192406 0 None 50 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 367 7 4 5 1.9 CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1 10.1021/acs.jmedchem.1c00692
CHEMBL5222793 192406 0 None 50 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 367 7 4 5 1.9 CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1 10.1021/acs.jmedchem.1c00692
56954318 81652 0 None 7 3 Guinea pig 8.0 pEC50 = 8.0 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 444 13 6 4 0.1 N/C(=N\C(=O)CCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1 10.1021/jm201128q
CHEMBL2165640 81652 0 None 7 3 Guinea pig 8.0 pEC50 = 8.0 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 444 13 6 4 0.1 N/C(=N\C(=O)CCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1 10.1021/jm201128q
25149814 184732 0 None - 1 Guinea pig 7.0 pEC50 = 7 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 291 6 4 3 2.0 N=C(NCCCc1c[nH]cn1)NC(=O)CC1CCCCC1 10.1021/jm800841w
CHEMBL485958 184732 0 None - 1 Guinea pig 7.0 pEC50 = 7 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 291 6 4 3 2.0 N=C(NCCCc1c[nH]cn1)NC(=O)CC1CCCCC1 10.1021/jm800841w
CHEMBL5093461 213767 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis
ChEMBL None None None CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2nnc(N)s2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1016/j.bmcl.2021.128388
CHEMBL5095884 213767 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis
ChEMBL None None None CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2nnc(N)s2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1016/j.bmcl.2021.128388
164611342 184495 0 None -1 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 346 6 4 4 1.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCc1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4856005 184495 0 None -1 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 346 6 4 4 1.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCc1ccccc1 10.1016/j.ejmech.2021.113190
155559319 174281 0 None 13 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay
ChEMBL 239 1 1 3 3.2 CC1CCCc2c(-c3ccccc3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
CHEMBL4563363 174281 0 None 13 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay
ChEMBL 239 1 1 3 3.2 CC1CCCc2c(-c3ccccc3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
1204 1893 114 None -14 11 Guinea pig 6.0 pEC50 = 6 Functional
Agonist activity at H2R in spontaneously beating guinea pig right atrium assessed as increase in heart rateAgonist activity at H2R in spontaneously beating guinea pig right atrium assessed as increase in heart rate
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm201128q
1247 1893 114 None -14 11 Guinea pig 6.0 pEC50 = 6 Functional
Agonist activity at H2R in spontaneously beating guinea pig right atrium assessed as increase in heart rateAgonist activity at H2R in spontaneously beating guinea pig right atrium assessed as increase in heart rate
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm201128q
1375 1893 114 None -14 11 Guinea pig 6.0 pEC50 = 6 Functional
Agonist activity at H2R in spontaneously beating guinea pig right atrium assessed as increase in heart rateAgonist activity at H2R in spontaneously beating guinea pig right atrium assessed as increase in heart rate
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm201128q
774 1893 114 None -14 11 Guinea pig 6.0 pEC50 = 6 Functional
Agonist activity at H2R in spontaneously beating guinea pig right atrium assessed as increase in heart rateAgonist activity at H2R in spontaneously beating guinea pig right atrium assessed as increase in heart rate
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm201128q
CHEMBL90 1893 114 None -14 11 Guinea pig 6.0 pEC50 = 6 Functional
Agonist activity at H2R in spontaneously beating guinea pig right atrium assessed as increase in heart rateAgonist activity at H2R in spontaneously beating guinea pig right atrium assessed as increase in heart rate
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm201128q
DB05381 1893 114 None -14 11 Guinea pig 6.0 pEC50 = 6 Functional
Agonist activity at H2R in spontaneously beating guinea pig right atrium assessed as increase in heart rateAgonist activity at H2R in spontaneously beating guinea pig right atrium assessed as increase in heart rate
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm201128q
1204 1893 114 None -14 11 Guinea pig 6.0 pEC50 = 6 Functional
Agonist activity at histamine H2 receptor in guinea pig atrium assessed as increase in heart rateAgonist activity at histamine H2 receptor in guinea pig atrium assessed as increase in heart rate
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm9000693
1247 1893 114 None -14 11 Guinea pig 6.0 pEC50 = 6 Functional
Agonist activity at histamine H2 receptor in guinea pig atrium assessed as increase in heart rateAgonist activity at histamine H2 receptor in guinea pig atrium assessed as increase in heart rate
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm9000693
1375 1893 114 None -14 11 Guinea pig 6.0 pEC50 = 6 Functional
Agonist activity at histamine H2 receptor in guinea pig atrium assessed as increase in heart rateAgonist activity at histamine H2 receptor in guinea pig atrium assessed as increase in heart rate
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm9000693
774 1893 114 None -14 11 Guinea pig 6.0 pEC50 = 6 Functional
Agonist activity at histamine H2 receptor in guinea pig atrium assessed as increase in heart rateAgonist activity at histamine H2 receptor in guinea pig atrium assessed as increase in heart rate
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm9000693
CHEMBL90 1893 114 None -14 11 Guinea pig 6.0 pEC50 = 6 Functional
Agonist activity at histamine H2 receptor in guinea pig atrium assessed as increase in heart rateAgonist activity at histamine H2 receptor in guinea pig atrium assessed as increase in heart rate
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm9000693
DB05381 1893 114 None -14 11 Guinea pig 6.0 pEC50 = 6 Functional
Agonist activity at histamine H2 receptor in guinea pig atrium assessed as increase in heart rateAgonist activity at histamine H2 receptor in guinea pig atrium assessed as increase in heart rate
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm9000693
1204 1893 114 None -14 11 Guinea pig 6.0 pEC50 = 6 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm800841w
1247 1893 114 None -14 11 Guinea pig 6.0 pEC50 = 6 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm800841w
1375 1893 114 None -14 11 Guinea pig 6.0 pEC50 = 6 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm800841w
774 1893 114 None -14 11 Guinea pig 6.0 pEC50 = 6 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm800841w
CHEMBL90 1893 114 None -14 11 Guinea pig 6.0 pEC50 = 6 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm800841w
DB05381 1893 114 None -14 11 Guinea pig 6.0 pEC50 = 6 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm800841w
1204 1893 114 None -14 11 Guinea pig 6.0 pEC50 = 6 Functional
Agonist activity at histamine H2 receptor in spontaneously beating guinea pig atriumAgonist activity at histamine H2 receptor in spontaneously beating guinea pig atrium
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.03.082
1247 1893 114 None -14 11 Guinea pig 6.0 pEC50 = 6 Functional
Agonist activity at histamine H2 receptor in spontaneously beating guinea pig atriumAgonist activity at histamine H2 receptor in spontaneously beating guinea pig atrium
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.03.082
1375 1893 114 None -14 11 Guinea pig 6.0 pEC50 = 6 Functional
Agonist activity at histamine H2 receptor in spontaneously beating guinea pig atriumAgonist activity at histamine H2 receptor in spontaneously beating guinea pig atrium
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.03.082
774 1893 114 None -14 11 Guinea pig 6.0 pEC50 = 6 Functional
Agonist activity at histamine H2 receptor in spontaneously beating guinea pig atriumAgonist activity at histamine H2 receptor in spontaneously beating guinea pig atrium
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.03.082
CHEMBL90 1893 114 None -14 11 Guinea pig 6.0 pEC50 = 6 Functional
Agonist activity at histamine H2 receptor in spontaneously beating guinea pig atriumAgonist activity at histamine H2 receptor in spontaneously beating guinea pig atrium
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.03.082
DB05381 1893 114 None -14 11 Guinea pig 6.0 pEC50 = 6 Functional
Agonist activity at histamine H2 receptor in spontaneously beating guinea pig atriumAgonist activity at histamine H2 receptor in spontaneously beating guinea pig atrium
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.03.082
46887042 8659 0 None -15 5 Guinea pig 7.0 pEC50 = 7.0 Functional
Agonist activity at histamine H2 receptor in spontaneously beating guinea pig atriumAgonist activity at histamine H2 receptor in spontaneously beating guinea pig atrium
ChEMBL 319 7 4 3 2.6 C[C@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)C1CCCCC1 10.1016/j.bmcl.2010.03.082
CHEMBL1096430 8659 0 None -15 5 Guinea pig 7.0 pEC50 = 7.0 Functional
Agonist activity at histamine H2 receptor in spontaneously beating guinea pig atriumAgonist activity at histamine H2 receptor in spontaneously beating guinea pig atrium
ChEMBL 319 7 4 3 2.6 C[C@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)C1CCCCC1 10.1016/j.bmcl.2010.03.082
46887077 8900 0 None 1 2 Guinea pig 7.0 pEC50 = 7.0 Functional
Agonist activity at histamine H2 receptor in spontaneously beating guinea pig atriumAgonist activity at histamine H2 receptor in spontaneously beating guinea pig atrium
ChEMBL 359 7 4 5 2.8 Cc1nc(N)sc1CCCNC(=N)NC(=O)C[C@@H](C)c1ccccc1 10.1016/j.bmcl.2010.03.082
CHEMBL1098441 8900 0 None 1 2 Guinea pig 7.0 pEC50 = 7.0 Functional
Agonist activity at histamine H2 receptor in spontaneously beating guinea pig atriumAgonist activity at histamine H2 receptor in spontaneously beating guinea pig atrium
ChEMBL 359 7 4 5 2.8 Cc1nc(N)sc1CCCNC(=N)NC(=O)C[C@@H](C)c1ccccc1 10.1016/j.bmcl.2010.03.082
25150702 178287 0 None - 1 Guinea pig 6.0 pEC50 = 6.0 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 361 7 4 3 2.8 N=C(NCCCc1c[nH]cn1)NC(=O)C(c1ccccc1)c1ccccc1 10.1021/jm800841w
CHEMBL469748 178287 0 None - 1 Guinea pig 6.0 pEC50 = 6.0 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 361 7 4 3 2.8 N=C(NCCCc1c[nH]cn1)NC(=O)C(c1ccccc1)c1ccccc1 10.1021/jm800841w
168290815 192361 0 None -23 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay
ChEMBL 327 9 4 5 1.2 CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5200771 192361 0 None -23 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay
ChEMBL 327 9 4 5 1.2 CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222529 192361 0 None -23 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay
ChEMBL 327 9 4 5 1.2 CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
42625304 178512 0 None -77 5 Guinea pig 7.0 pEC50 = 7.0 Functional
Agonist activity at histamine H2 receptor in guinea pig atrium assessed as increase in heart rateAgonist activity at histamine H2 receptor in guinea pig atrium assessed as increase in heart rate
ChEMBL 237 5 3 2 0.4 CC(C)C(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL471724 178512 0 None -77 5 Guinea pig 7.0 pEC50 = 7.0 Functional
Agonist activity at histamine H2 receptor in guinea pig atrium assessed as increase in heart rateAgonist activity at histamine H2 receptor in guinea pig atrium assessed as increase in heart rate
ChEMBL 237 5 3 2 0.4 CC(C)C(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL5083588 213748 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C 10.1016/j.bmcl.2021.128388
CHEMBL5095633 213748 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C 10.1016/j.bmcl.2021.128388
164622259 185138 0 None - 1 Guinea pig 7.9 pEC50 = 7.9 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 336 6 4 5 1.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCc1ccco1 10.1016/j.ejmech.2021.113190
CHEMBL4865965 185138 0 None - 1 Guinea pig 7.9 pEC50 = 7.9 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 336 6 4 5 1.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCc1ccco1 10.1016/j.ejmech.2021.113190
1204 1893 114 None -61 11 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitment
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2021.128388
1247 1893 114 None -61 11 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitment
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2021.128388
1375 1893 114 None -61 11 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitment
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2021.128388
774 1893 114 None -61 11 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitment
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2021.128388
CHEMBL90 1893 114 None -61 11 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitment
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2021.128388
DB05381 1893 114 None -61 11 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitment
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2021.128388
CHEMBL5075713 213743 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitment
ChEMBL None None None CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2c[nH]cn2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1016/j.bmcl.2021.128388
CHEMBL5095559 213743 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitment
ChEMBL None None None CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2c[nH]cn2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1016/j.bmcl.2021.128388
1204 1893 114 None -61 11 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
1247 1893 114 None -61 11 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
1375 1893 114 None -61 11 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
774 1893 114 None -61 11 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
CHEMBL90 1893 114 None -61 11 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
DB05381 1893 114 None -61 11 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
17873053 9376 0 None - 1 Guinea pig 5.9 pEC50 = 5.9 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 271 5 4 3 1.3 N=C(NCCCc1c[nH]cn1)NC(=O)c1ccccc1 10.1021/jm800841w
CHEMBL111988 9376 0 None - 1 Guinea pig 5.9 pEC50 = 5.9 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 271 5 4 3 1.3 N=C(NCCCc1c[nH]cn1)NC(=O)c1ccccc1 10.1021/jm800841w
164619208 185070 0 None - 1 Guinea pig 7.9 pEC50 = 7.9 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 378 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccccc1F 10.1016/j.ejmech.2021.113190
CHEMBL4864852 185070 0 None - 1 Guinea pig 7.9 pEC50 = 7.9 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 378 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccccc1F 10.1016/j.ejmech.2021.113190
164622886 185350 0 None - 1 Guinea pig 7.9 pEC50 = 7.9 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 374 7 4 4 2.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC[C@@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4869389 185350 0 None - 1 Guinea pig 7.9 pEC50 = 7.9 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 374 7 4 4 2.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC[C@@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
168268853 192173 0 None -1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting method
ChEMBL 389 8 4 5 1.9 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5180504 192173 0 None -1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting method
ChEMBL 389 8 4 5 1.9 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5221353 192173 0 None -1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting method
ChEMBL 389 8 4 5 1.9 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
46887041 8657 0 None -5 5 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay
ChEMBL 313 7 4 3 2.2 C[C@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)c1ccccc1 10.1016/j.bmcl.2010.03.082
CHEMBL1096428 8657 0 None -5 5 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay
ChEMBL 313 7 4 3 2.2 C[C@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)c1ccccc1 10.1016/j.bmcl.2010.03.082
CHEMBL5092267 213571 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCC[n+]1c(C)cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc1C 10.1016/j.bmcl.2021.128388
CHEMBL5075713 213743 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis
ChEMBL None None None CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2c[nH]cn2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1016/j.bmcl.2021.128388
CHEMBL5095559 213743 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis
ChEMBL None None None CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2c[nH]cn2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1016/j.bmcl.2021.128388
1204 1893 114 None -14 11 Guinea pig 5.9 pEC50 = 5.9 Functional
Agonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.03.082
1247 1893 114 None -14 11 Guinea pig 5.9 pEC50 = 5.9 Functional
Agonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.03.082
1375 1893 114 None -14 11 Guinea pig 5.9 pEC50 = 5.9 Functional
Agonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.03.082
774 1893 114 None -14 11 Guinea pig 5.9 pEC50 = 5.9 Functional
Agonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.03.082
CHEMBL90 1893 114 None -14 11 Guinea pig 5.9 pEC50 = 5.9 Functional
Agonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.03.082
DB05381 1893 114 None -14 11 Guinea pig 5.9 pEC50 = 5.9 Functional
Agonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.03.082
1204 1893 114 None -14 11 Guinea pig 5.9 pEC50 = 5.9 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm201128q
1247 1893 114 None -14 11 Guinea pig 5.9 pEC50 = 5.9 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm201128q
1375 1893 114 None -14 11 Guinea pig 5.9 pEC50 = 5.9 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm201128q
774 1893 114 None -14 11 Guinea pig 5.9 pEC50 = 5.9 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm201128q
CHEMBL90 1893 114 None -14 11 Guinea pig 5.9 pEC50 = 5.9 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm201128q
DB05381 1893 114 None -14 11 Guinea pig 5.9 pEC50 = 5.9 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm201128q
1204 1893 114 None -61 11 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm900526h
1247 1893 114 None -61 11 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm900526h
1375 1893 114 None -61 11 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm900526h
774 1893 114 None -61 11 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm900526h
CHEMBL90 1893 114 None -61 11 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm900526h
DB05381 1893 114 None -61 11 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm900526h
1204 1893 114 None -61 11 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
1247 1893 114 None -61 11 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
1375 1893 114 None -61 11 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
774 1893 114 None -61 11 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
CHEMBL90 1893 114 None -61 11 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
DB05381 1893 114 None -61 11 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
44482302 5535 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay
ChEMBL 321 6 4 4 1.2 Cc1ccc(S(=O)(=O)NC(=N)NCCCc2c[nH]cn2)cc1 10.1021/jm900526h
CHEMBL1077596 5535 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay
ChEMBL 321 6 4 4 1.2 Cc1ccc(S(=O)(=O)NC(=N)NCCCc2c[nH]cn2)cc1 10.1021/jm900526h
44481217 5702 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay
ChEMBL 335 8 4 4 1.0 N=C(NCCCc1c[nH]cn1)NS(=O)(=O)CCc1ccccc1 10.1021/jm900526h
CHEMBL1078747 5702 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay
ChEMBL 335 8 4 4 1.0 N=C(NCCCc1c[nH]cn1)NS(=O)(=O)CCc1ccccc1 10.1021/jm900526h
CHEMBL5090859 213499 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCCC[n+]1c(C)cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc1C 10.1016/j.bmcl.2021.128388
1204 1893 114 None -61 11 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.03.082
1247 1893 114 None -61 11 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.03.082
1375 1893 114 None -61 11 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.03.082
774 1893 114 None -61 11 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.03.082
CHEMBL90 1893 114 None -61 11 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.03.082
DB05381 1893 114 None -61 11 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.03.082
1204 1893 114 None -61 11 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm201128q
1247 1893 114 None -61 11 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm201128q
1375 1893 114 None -61 11 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm201128q
774 1893 114 None -61 11 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm201128q
CHEMBL90 1893 114 None -61 11 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm201128q
DB05381 1893 114 None -61 11 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm201128q
CHEMBL5083588 213748 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitment
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C 10.1016/j.bmcl.2021.128388
CHEMBL5095633 213748 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitment
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C 10.1016/j.bmcl.2021.128388
168268853 192173 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay
ChEMBL 389 8 4 5 1.9 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5180504 192173 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay
ChEMBL 389 8 4 5 1.9 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5221353 192173 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay
ChEMBL 389 8 4 5 1.9 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5077939 213755 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)O)c3ccccc3C2(C)C)c2cc(S(=O)(=O)[O-])ccc2C1(C)C 10.1016/j.bmcl.2021.128388
CHEMBL5095769 213755 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)O)c3ccccc3C2(C)C)c2cc(S(=O)(=O)[O-])ccc2C1(C)C 10.1016/j.bmcl.2021.128388
13170764 174497 0 None 2 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay
ChEMBL 255 2 1 4 2.6 COc1ccc(-c2nc(N)nc3c2CCCC3)cc1 10.1021/acs.jmedchem.9b00241
CHEMBL4568452 174497 0 None 2 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay
ChEMBL 255 2 1 4 2.6 COc1ccc(-c2nc(N)nc3c2CCCC3)cc1 10.1021/acs.jmedchem.9b00241
46887080 8445 0 None -1 2 Guinea pig 7.9 pEC50 = 7.9 Functional
Agonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay
ChEMBL 365 7 4 5 3.2 Cc1nc(N)sc1CCCNC(=N)NC(=O)C[C@@H](C)C1CCCCC1 10.1016/j.bmcl.2010.03.082
CHEMBL1094452 8445 0 None -1 2 Guinea pig 7.9 pEC50 = 7.9 Functional
Agonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay
ChEMBL 365 7 4 5 3.2 Cc1nc(N)sc1CCCNC(=N)NC(=O)C[C@@H](C)C1CCCCC1 10.1016/j.bmcl.2010.03.082
168294449 192406 0 None 50 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting method
ChEMBL 367 7 4 5 1.9 CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1 10.1021/acs.jmedchem.1c00692
CHEMBL5204599 192406 0 None 50 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting method
ChEMBL 367 7 4 5 1.9 CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1 10.1021/acs.jmedchem.1c00692
CHEMBL5222793 192406 0 None 50 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting method
ChEMBL 367 7 4 5 1.9 CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1 10.1021/acs.jmedchem.1c00692
56954513 81657 0 None -3 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 578 17 6 8 2.6 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1cnc(N)s1 10.1021/jm201128q
CHEMBL2165645 81657 0 None -3 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 578 17 6 8 2.6 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1cnc(N)s1 10.1021/jm201128q
CHEMBL5092102 213562 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis
ChEMBL None None None NCCCCCCCCNC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1016/j.bmcl.2021.128388
164611757 184310 0 None 3 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 402 8 4 4 2.8 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1 10.1016/j.ejmech.2021.113190
CHEMBL4853107 184310 0 None 3 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 402 8 4 4 2.8 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1 10.1016/j.ejmech.2021.113190
168294449 192406 0 None 50 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay
ChEMBL 367 7 4 5 1.9 CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1 10.1021/acs.jmedchem.1c00692
CHEMBL5204599 192406 0 None 50 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay
ChEMBL 367 7 4 5 1.9 CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1 10.1021/acs.jmedchem.1c00692
CHEMBL5222793 192406 0 None 50 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay
ChEMBL 367 7 4 5 1.9 CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1 10.1021/acs.jmedchem.1c00692
25149429 185372 0 None - 1 Guinea pig 6.9 pEC50 = 6.9 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 305 6 4 3 2.2 CC(C(=O)NC(=N)NCCCc1c[nH]cn1)C1CCCCC1 10.1021/jm800841w
CHEMBL486964 185372 0 None - 1 Guinea pig 6.9 pEC50 = 6.9 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 305 6 4 3 2.2 CC(C(=O)NC(=N)NCCCc1c[nH]cn1)C1CCCCC1 10.1021/jm800841w
168295528 192419 0 None -12 10 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5206565 192419 0 None -12 10 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222872 192419 0 None -12 10 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5085542 213189 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCC[n+]1c(C)cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc1C 10.1016/j.bmcl.2021.128388
13170764 174497 0 None 2 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay
ChEMBL 255 2 1 4 2.6 COc1ccc(-c2nc(N)nc3c2CCCC3)cc1 10.1021/acs.jmedchem.9b00241
CHEMBL4568452 174497 0 None 2 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay
ChEMBL 255 2 1 4 2.6 COc1ccc(-c2nc(N)nc3c2CCCC3)cc1 10.1021/acs.jmedchem.9b00241
46887115 8411 0 None -1 4 Guinea pig 7.9 pEC50 = 7.9 Functional
Agonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay
ChEMBL 365 7 4 5 3.2 Cc1nc(N)sc1CCCNC(=N)NC(=O)C[C@H](C)C1CCCCC1 10.1016/j.bmcl.2010.03.082
CHEMBL1094144 8411 0 None -1 4 Guinea pig 7.9 pEC50 = 7.9 Functional
Agonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay
ChEMBL 365 7 4 5 3.2 Cc1nc(N)sc1CCCNC(=N)NC(=O)C[C@H](C)C1CCCCC1 10.1016/j.bmcl.2010.03.082
168268853 192173 0 None 1 2 Guinea pig 7.8 pEC50 = 7.8 Functional
Agonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assayAgonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assay
ChEMBL 389 8 4 5 1.9 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5180504 192173 0 None 1 2 Guinea pig 7.8 pEC50 = 7.8 Functional
Agonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assayAgonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assay
ChEMBL 389 8 4 5 1.9 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5221353 192173 0 None 1 2 Guinea pig 7.8 pEC50 = 7.8 Functional
Agonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assayAgonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assay
ChEMBL 389 8 4 5 1.9 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
1204 1893 114 None -61 11 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2021.128388
1247 1893 114 None -61 11 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2021.128388
1375 1893 114 None -61 11 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2021.128388
774 1893 114 None -61 11 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2021.128388
CHEMBL90 1893 114 None -61 11 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2021.128388
DB05381 1893 114 None -61 11 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2021.128388
44481489 5622 0 None -18 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay
ChEMBL 310 8 3 3 2.0 N#C/N=C(\NCCCc1ccccc1)NCCCc1c[nH]cn1 10.1021/jm900526h
CHEMBL1078210 5622 0 None -18 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay
ChEMBL 310 8 3 3 2.0 N#C/N=C(\NCCCc1ccccc1)NCCCc1c[nH]cn1 10.1021/jm900526h
CHEMBL5088914 213776 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C 10.1016/j.bmcl.2021.128388
CHEMBL5095949 213776 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C 10.1016/j.bmcl.2021.128388
164608941 183791 0 None - 1 Guinea pig 6.8 pEC50 = 6.8 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 390 7 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NC[C@@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4845733 183791 0 None - 1 Guinea pig 6.8 pEC50 = 6.8 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 390 7 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NC[C@@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
164628701 185875 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 338 5 4 4 1.9 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC1CCCCC1 10.1016/j.ejmech.2021.113190
CHEMBL4876743 185875 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 338 5 4 4 1.9 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC1CCCCC1 10.1016/j.ejmech.2021.113190
164626370 185881 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 338 6 4 4 1.8 CCCCCCNC(=O)/N=C(\N)NC1CCc2nc(N)sc2C1 10.1016/j.ejmech.2021.113190
CHEMBL4876799 185881 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 338 6 4 4 1.8 CCCCCCNC(=O)/N=C(\N)NC1CCc2nc(N)sc2C1 10.1016/j.ejmech.2021.113190
71458814 81658 0 None 1 2 Guinea pig 7.8 pEC50 = 7.8 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 345 7 3 4 2.0 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCc1ccccc1 10.1021/jm201128q
CHEMBL2165646 81658 0 None 1 2 Guinea pig 7.8 pEC50 = 7.8 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 345 7 3 4 2.0 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCc1ccccc1 10.1021/jm201128q
164614549 184350 0 None 1 4 Guinea pig 7.8 pEC50 = 7.8 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 340 9 4 4 2.2 CCCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1016/j.ejmech.2021.113190
CHEMBL4853668 184350 0 None 1 4 Guinea pig 7.8 pEC50 = 7.8 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 340 9 4 4 2.2 CCCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1016/j.ejmech.2021.113190
25149335 183633 0 None -5 4 Guinea pig 7.8 pEC50 = 7.8 Functional
Agonist activity at histamine H2 receptor in guinea pig atrium assessed as increase in heart rateAgonist activity at histamine H2 receptor in guinea pig atrium assessed as increase in heart rate
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1021/jm9000693
CHEMBL483406 183633 0 None -5 4 Guinea pig 7.8 pEC50 = 7.8 Functional
Agonist activity at histamine H2 receptor in guinea pig atrium assessed as increase in heart rateAgonist activity at histamine H2 receptor in guinea pig atrium assessed as increase in heart rate
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1021/jm9000693
25149335 183633 0 None -5 4 Guinea pig 7.8 pEC50 = 7.8 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1021/jm800841w
CHEMBL483406 183633 0 None -5 4 Guinea pig 7.8 pEC50 = 7.8 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1021/jm800841w
56954517 81640 0 None -14 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 502 17 6 6 0.5 N/C(=N\C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1ncn[nH]1)NCCCc1ncn[nH]1 10.1021/jm201128q
CHEMBL2165629 81640 0 None -14 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 502 17 6 6 0.5 N/C(=N\C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1ncn[nH]1)NCCCc1ncn[nH]1 10.1021/jm201128q
164614645 184539 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 402 8 4 4 3.0 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(c1ccccc1)C(C)C 10.1016/j.ejmech.2021.113190
CHEMBL4856572 184539 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 402 8 4 4 3.0 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(c1ccccc1)C(C)C 10.1016/j.ejmech.2021.113190
1204 1893 114 None -61 11 Human 5.8 pEC50 = 5.8 Functional
Antagonist activity at Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins in presence of histamine by GTPgammaS binding assayAntagonist activity at Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins in presence of histamine by GTPgammaS binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acsmedchemlett.0c00033
1247 1893 114 None -61 11 Human 5.8 pEC50 = 5.8 Functional
Antagonist activity at Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins in presence of histamine by GTPgammaS binding assayAntagonist activity at Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins in presence of histamine by GTPgammaS binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acsmedchemlett.0c00033
1375 1893 114 None -61 11 Human 5.8 pEC50 = 5.8 Functional
Antagonist activity at Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins in presence of histamine by GTPgammaS binding assayAntagonist activity at Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins in presence of histamine by GTPgammaS binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acsmedchemlett.0c00033
774 1893 114 None -61 11 Human 5.8 pEC50 = 5.8 Functional
Antagonist activity at Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins in presence of histamine by GTPgammaS binding assayAntagonist activity at Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins in presence of histamine by GTPgammaS binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acsmedchemlett.0c00033
CHEMBL90 1893 114 None -61 11 Human 5.8 pEC50 = 5.8 Functional
Antagonist activity at Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins in presence of histamine by GTPgammaS binding assayAntagonist activity at Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins in presence of histamine by GTPgammaS binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acsmedchemlett.0c00033
DB05381 1893 114 None -61 11 Human 5.8 pEC50 = 5.8 Functional
Antagonist activity at Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins in presence of histamine by GTPgammaS binding assayAntagonist activity at Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins in presence of histamine by GTPgammaS binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acsmedchemlett.0c00033
168290235 192356 0 None 3 10 Guinea pig 7.8 pEC50 = 7.8 Functional
Agonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assayAgonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assay
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5201074 192356 0 None 3 10 Guinea pig 7.8 pEC50 = 7.8 Functional
Agonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assayAgonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assay
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222491 192356 0 None 3 10 Guinea pig 7.8 pEC50 = 7.8 Functional
Agonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assayAgonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assay
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
56954002 81644 0 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 620 19 6 8 3.7 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/jm201128q
CHEMBL2165633 81644 0 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 620 19 6 8 3.7 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/jm201128q
46887077 8900 0 None 1 2 Guinea pig 7.8 pEC50 = 7.8 Functional
Agonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay
ChEMBL 359 7 4 5 2.8 Cc1nc(N)sc1CCCNC(=N)NC(=O)C[C@@H](C)c1ccccc1 10.1016/j.bmcl.2010.03.082
CHEMBL1098441 8900 0 None 1 2 Guinea pig 7.8 pEC50 = 7.8 Functional
Agonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay
ChEMBL 359 7 4 5 2.8 Cc1nc(N)sc1CCCNC(=N)NC(=O)C[C@@H](C)c1ccccc1 10.1016/j.bmcl.2010.03.082
44414337 79714 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human H2RAgonist activity at human H2R
ChEMBL 945 24 3 9 8.3 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCC/N=C(\NC#N)NCCCOc3cccc(CN4CCCCC4)c3)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1016/j.bmcl.2006.05.039
CHEMBL213357 79714 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human H2RAgonist activity at human H2R
ChEMBL 945 24 3 9 8.3 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCC/N=C(\NC#N)NCCCOc3cccc(CN4CCCCC4)c3)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1016/j.bmcl.2006.05.039
90667237 108974 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
ChEMBL 356 9 3 4 2.8 Cc1nc(CCCCN/C(=N\C#N)NCCSc2ccccc2)c[nH]1 10.1039/C3MD00245D
CHEMBL3220638 108974 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
ChEMBL 356 9 3 4 2.8 Cc1nc(CCCCN/C(=N\C#N)NCCSc2ccccc2)c[nH]1 10.1039/C3MD00245D
25149712 178398 0 None -66 4 Guinea pig 6.8 pEC50 = 6.8 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 299 7 4 3 1.6 N=C(NCCCc1c[nH]cn1)NC(=O)CCc1ccccc1 10.1021/jm800841w
CHEMBL470790 178398 0 None -66 4 Guinea pig 6.8 pEC50 = 6.8 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 299 7 4 3 1.6 N=C(NCCCc1c[nH]cn1)NC(=O)CCc1ccccc1 10.1021/jm800841w
164622190 185024 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 360 7 4 4 1.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCc1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4864067 185024 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 360 7 4 4 1.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCc1ccccc1 10.1016/j.ejmech.2021.113190
119570 3098 90 None -128 7 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/acs.jmedchem.1c00692
2233 3098 90 None -128 7 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/acs.jmedchem.1c00692
953 3098 90 None -128 7 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/acs.jmedchem.1c00692
CHEMBL301265 3098 90 None -128 7 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/acs.jmedchem.1c00692
DB00413 3098 90 None -128 7 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/acs.jmedchem.1c00692
164627189 185729 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 298 6 4 4 1.0 CCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1016/j.ejmech.2021.113190
CHEMBL4874758 185729 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 298 6 4 4 1.0 CCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1016/j.ejmech.2021.113190
164610892 184605 0 None 4 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 394 8 4 4 3.2 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CC1CCCCC1 10.1016/j.ejmech.2021.113190
CHEMBL4857560 184605 0 None 4 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 394 8 4 4 3.2 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CC1CCCCC1 10.1016/j.ejmech.2021.113190
164620139 185196 0 None - 1 Guinea pig 6.8 pEC50 = 6.8 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 436 8 4 4 3.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4866734 185196 0 None - 1 Guinea pig 6.8 pEC50 = 6.8 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 436 8 4 4 3.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2021.113190
164612037 184785 0 None -30 12 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1016/j.ejmech.2021.113190
CHEMBL4860528 184785 0 None -30 12 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1016/j.ejmech.2021.113190
164627189 185729 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 298 6 4 4 1.0 CCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1016/j.ejmech.2021.113190
CHEMBL4874758 185729 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 298 6 4 4 1.0 CCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1016/j.ejmech.2021.113190
46887042 8659 0 None -6 5 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay
ChEMBL 319 7 4 3 2.6 C[C@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)C1CCCCC1 10.1016/j.bmcl.2010.03.082
CHEMBL1096430 8659 0 None -6 5 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay
ChEMBL 319 7 4 3 2.6 C[C@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)C1CCCCC1 10.1016/j.bmcl.2010.03.082
42626109 179178 0 None -9 3 Guinea pig 6.7 pEC50 = 6.7 Functional
Agonist activity at histamine H2 receptor in guinea pig atrium assessed as increase in heart rateAgonist activity at histamine H2 receptor in guinea pig atrium assessed as increase in heart rate
ChEMBL 324 6 4 2 1.5 N/C(=N\C(=O)Cc1c[nH]c2ccccc12)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL474447 179178 0 None -9 3 Guinea pig 6.7 pEC50 = 6.7 Functional
Agonist activity at histamine H2 receptor in guinea pig atrium assessed as increase in heart rateAgonist activity at histamine H2 receptor in guinea pig atrium assessed as increase in heart rate
ChEMBL 324 6 4 2 1.5 N/C(=N\C(=O)Cc1c[nH]c2ccccc12)NCCCc1c[nH]cn1 10.1021/jm9000693
25149425 187613 0 None - 1 Guinea pig 6.7 pEC50 = 6.7 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 285 6 4 3 1.2 N=C(NCCCc1c[nH]cn1)NC(=O)Cc1ccccc1 10.1021/jm800841w
CHEMBL499092 187613 0 None - 1 Guinea pig 6.7 pEC50 = 6.7 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 285 6 4 3 1.2 N=C(NCCCc1c[nH]cn1)NC(=O)Cc1ccccc1 10.1021/jm800841w
42625386 177768 0 None -117 5 Guinea pig 6.7 pEC50 = 6.7 Functional
Agonist activity at histamine H2 receptor in guinea pig atrium assessed as increase in heart rateAgonist activity at histamine H2 receptor in guinea pig atrium assessed as increase in heart rate
ChEMBL 237 6 3 2 0.6 CCCC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL465170 177768 0 None -117 5 Guinea pig 6.7 pEC50 = 6.7 Functional
Agonist activity at histamine H2 receptor in guinea pig atrium assessed as increase in heart rateAgonist activity at histamine H2 receptor in guinea pig atrium assessed as increase in heart rate
ChEMBL 237 6 3 2 0.6 CCCC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL5094663 213720 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](C)c3ccccc3C2(C)C)c2ccccc2C1(C)C 10.1016/j.bmcl.2021.128388
46887042 8659 0 None -15 5 Guinea pig 7.7 pEC50 = 7.7 Functional
Agonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay
ChEMBL 319 7 4 3 2.6 C[C@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)C1CCCCC1 10.1016/j.bmcl.2010.03.082
CHEMBL1096430 8659 0 None -15 5 Guinea pig 7.7 pEC50 = 7.7 Functional
Agonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay
ChEMBL 319 7 4 3 2.6 C[C@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)C1CCCCC1 10.1016/j.bmcl.2010.03.082
56954425 81655 0 None 1 3 Guinea pig 7.7 pEC50 = 7.7 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 584 23 6 4 4.0 N/C(=N\C(=O)CCCCCCCCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1 10.1021/jm201128q
CHEMBL2165643 81655 0 None 1 3 Guinea pig 7.7 pEC50 = 7.7 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 584 23 6 4 4.0 N/C(=N\C(=O)CCCCCCCCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1 10.1021/jm201128q
1226 1980 16 None 1 2 Guinea pig 7.7 pEC50 = 7.7 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C 10.1021/jm800841w
41376 1980 16 None 1 2 Guinea pig 7.7 pEC50 = 7.7 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C 10.1021/jm800841w
CHEMBL12608 1980 16 None 1 2 Guinea pig 7.7 pEC50 = 7.7 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C 10.1021/jm800841w
168273640 192193 0 None 4 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 568 15 8 10 -0.1 N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5176229 192193 0 None 4 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 568 15 8 10 -0.1 N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221444 192193 0 None 4 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 568 15 8 10 -0.1 N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
168295541 192428 0 None -8 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 347 6 4 5 1.4 C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5208845 192428 0 None -8 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 347 6 4 5 1.4 C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222926 192428 0 None -8 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 347 6 4 5 1.4 C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1 10.1021/acs.jmedchem.1c00692
126688 400 28 None -1 3 Guinea pig 6.7 pEC50 = 6.7 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 157 2 2 4 0.5 NCCc1sc(nc1C)N 10.1021/jm201128q
4025 400 28 None -1 3 Guinea pig 6.7 pEC50 = 6.7 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 157 2 2 4 0.5 NCCc1sc(nc1C)N 10.1021/jm201128q
CHEMBL293762 400 28 None -1 3 Guinea pig 6.7 pEC50 = 6.7 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 157 2 2 4 0.5 NCCc1sc(nc1C)N 10.1021/jm201128q
CHEMBL5094663 213720 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitment
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](C)c3ccccc3C2(C)C)c2ccccc2C1(C)C 10.1016/j.bmcl.2021.128388
126688 400 28 None 1 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 157 2 2 4 0.5 NCCc1sc(nc1C)N 10.1021/jm201128q
4025 400 28 None 1 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 157 2 2 4 0.5 NCCc1sc(nc1C)N 10.1021/jm201128q
CHEMBL293762 400 28 None 1 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 157 2 2 4 0.5 NCCc1sc(nc1C)N 10.1021/jm201128q
CHEMBL5092102 213562 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL None None None NCCCCCCCCNC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1016/j.bmcl.2021.128388
44481214 5644 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay
ChEMBL 314 7 4 2 1.2 NC(=O)/N=C(/NCCCc1ccccc1)NCCc1c[nH]cn1 10.1021/jm900526h
CHEMBL1078358 5644 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay
ChEMBL 314 7 4 2 1.2 NC(=O)/N=C(/NCCCc1ccccc1)NCCc1c[nH]cn1 10.1021/jm900526h
168295528 192419 0 None 12 10 Guinea pig 8.7 pEC50 = 8.7 Functional
Agonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assayAgonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assay
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5206565 192419 0 None 12 10 Guinea pig 8.7 pEC50 = 8.7 Functional
Agonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assayAgonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assay
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222872 192419 0 None 12 10 Guinea pig 8.7 pEC50 = 8.7 Functional
Agonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assayAgonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assay
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
168290815 192361 0 None 23 3 Guinea pig 8.6 pEC50 = 8.6 Functional
Agonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assayAgonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assay
ChEMBL 327 9 4 5 1.2 CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5200771 192361 0 None 23 3 Guinea pig 8.6 pEC50 = 8.6 Functional
Agonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assayAgonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assay
ChEMBL 327 9 4 5 1.2 CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222529 192361 0 None 23 3 Guinea pig 8.6 pEC50 = 8.6 Functional
Agonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assayAgonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assay
ChEMBL 327 9 4 5 1.2 CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
56953887 81659 0 None 22 2 Guinea pig 8.6 pEC50 = 8.6 Functional
Agonist activity at H2R in spontaneously beating guinea pig right atrium assessed as increase in heart rateAgonist activity at H2R in spontaneously beating guinea pig right atrium assessed as increase in heart rate
ChEMBL 536 13 6 8 1.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/jm201128q
CHEMBL2165647 81659 0 None 22 2 Guinea pig 8.6 pEC50 = 8.6 Functional
Agonist activity at H2R in spontaneously beating guinea pig right atrium assessed as increase in heart rateAgonist activity at H2R in spontaneously beating guinea pig right atrium assessed as increase in heart rate
ChEMBL 536 13 6 8 1.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/jm201128q
56953887 81659 0 None 22 2 Guinea pig 8.6 pEC50 = 8.6 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 536 13 6 8 1.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/jm201128q
CHEMBL2165647 81659 0 None 22 2 Guinea pig 8.6 pEC50 = 8.6 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 536 13 6 8 1.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/jm201128q
56954002 81644 0 None -1 2 Guinea pig 8.6 pEC50 = 8.6 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 620 19 6 8 3.7 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/jm201128q
CHEMBL2165633 81644 0 None -1 2 Guinea pig 8.6 pEC50 = 8.6 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 620 19 6 8 3.7 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/jm201128q
56953998 81642 0 None 29 2 Guinea pig 8.6 pEC50 = 8.6 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 578 16 6 8 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/jm201128q
CHEMBL2165631 81642 0 None 29 2 Guinea pig 8.6 pEC50 = 8.6 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 578 16 6 8 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/jm201128q
168295541 192428 0 None 8 3 Guinea pig 8.5 pEC50 = 8.5 Functional
Agonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beatAgonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beat
ChEMBL 347 6 4 5 1.4 C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5208845 192428 0 None 8 3 Guinea pig 8.5 pEC50 = 8.5 Functional
Agonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beatAgonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beat
ChEMBL 347 6 4 5 1.4 C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222926 192428 0 None 8 3 Guinea pig 8.5 pEC50 = 8.5 Functional
Agonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beatAgonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beat
ChEMBL 347 6 4 5 1.4 C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1 10.1021/acs.jmedchem.1c00692
46887080 8445 0 None 1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay
ChEMBL 365 7 4 5 3.2 Cc1nc(N)sc1CCCNC(=N)NC(=O)C[C@@H](C)C1CCCCC1 10.1016/j.bmcl.2010.03.082
CHEMBL1094452 8445 0 None 1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay
ChEMBL 365 7 4 5 3.2 Cc1nc(N)sc1CCCNC(=N)NC(=O)C[C@@H](C)C1CCCCC1 10.1016/j.bmcl.2010.03.082
71458814 81658 0 None -1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 345 7 3 4 2.0 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCc1ccccc1 10.1021/jm201128q
CHEMBL2165646 81658 0 None -1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 345 7 3 4 2.0 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCc1ccccc1 10.1021/jm201128q
56954231 81650 0 None - 1 Guinea pig 6.7 pEC50 = 6.7 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 732 29 6 8 7.0 N/C(=N\C(=O)CCCCCCCCCCCCCCCCCCCCC(=O)/N=C(\N)NCCCc1cnc(N)s1)NCCCc1cnc(N)s1 10.1021/jm201128q
CHEMBL2165639 81650 0 None - 1 Guinea pig 6.7 pEC50 = 6.7 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 732 29 6 8 7.0 N/C(=N\C(=O)CCCCCCCCCCCCCCCCCCCCC(=O)/N=C(\N)NCCCc1cnc(N)s1)NCCCc1cnc(N)s1 10.1021/jm201128q
1202 3890 1 None - 1 Guinea pig 6.7 pEC50 = 6.7 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 411 8 3 3 3.3 O=C(CC(c1ccc(cc1)F)c1ccc(cc1)F)NC(=NCCCc1cnc[nH]1)N 10.1021/jm800841w
25150704 3890 1 None - 1 Guinea pig 6.7 pEC50 = 6.7 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 411 8 3 3 3.3 O=C(CC(c1ccc(cc1)F)c1ccc(cc1)F)NC(=NCCCc1cnc[nH]1)N 10.1021/jm800841w
CHEMBL513883 3890 1 None - 1 Guinea pig 6.7 pEC50 = 6.7 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 411 8 3 3 3.3 O=C(CC(c1ccc(cc1)F)c1ccc(cc1)F)NC(=NCCCc1cnc[nH]1)N 10.1021/jm800841w
CHEMBL5076746 213739 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(N)(=O)=O)c3ccccc3C2(C)C)c2cc(S(=O)(=O)[O-])ccc2C1(C)C 10.1016/j.bmcl.2021.128388
CHEMBL5095519 213739 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(N)(=O)=O)c3ccccc3C2(C)C)c2cc(S(=O)(=O)[O-])ccc2C1(C)C 10.1016/j.bmcl.2021.128388
CHEMBL5075106 213741 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)O)c3ccccc3C2(C)C)c2cc(S(=O)(=O)[O-])ccc2C1(C)C 10.1016/j.bmcl.2021.128388
CHEMBL5095549 213741 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)O)c3ccccc3C2(C)C)c2cc(S(=O)(=O)[O-])ccc2C1(C)C 10.1016/j.bmcl.2021.128388
56954227 81648 0 None -4 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 564 17 6 8 2.3 N/C(=N\C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1cnc(N)s1)NCCCc1cnc(N)s1 10.1021/jm201128q
CHEMBL2165637 81648 0 None -4 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 564 17 6 8 2.3 N/C(=N\C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1cnc(N)s1)NCCCc1cnc(N)s1 10.1021/jm201128q
164608815 183862 0 None 3 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 380 7 4 4 2.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1 10.1016/j.ejmech.2021.113190
CHEMBL4846638 183862 0 None 3 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 380 7 4 4 2.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1 10.1016/j.ejmech.2021.113190
155544816 174451 0 None 2 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay
ChEMBL 269 2 1 4 2.9 COc1ccc(-c2nc(N)nc3c2CC(C)CC3)cc1 10.1021/acs.jmedchem.9b00241
CHEMBL4567405 174451 0 None 2 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay
ChEMBL 269 2 1 4 2.9 COc1ccc(-c2nc(N)nc3c2CC(C)CC3)cc1 10.1021/acs.jmedchem.9b00241
56954318 81652 0 None -19 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 444 13 6 4 0.1 N/C(=N\C(=O)CCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1 10.1021/jm201128q
CHEMBL2165640 81652 0 None -19 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 444 13 6 4 0.1 N/C(=N\C(=O)CCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1 10.1021/jm201128q
164627774 185973 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 344 3 4 4 1.4 N/C(=N\C(=O)NCc1ccccc1)NC1CCc2nc(N)sc2C1 10.1016/j.ejmech.2021.113190
CHEMBL4878215 185973 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 344 3 4 4 1.4 N/C(=N\C(=O)NCc1ccccc1)NC1CCc2nc(N)sc2C1 10.1016/j.ejmech.2021.113190
155544816 174451 0 None 2 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay
ChEMBL 269 2 1 4 2.9 COc1ccc(-c2nc(N)nc3c2CC(C)CC3)cc1 10.1021/acs.jmedchem.9b00241
CHEMBL4567405 174451 0 None 2 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay
ChEMBL 269 2 1 4 2.9 COc1ccc(-c2nc(N)nc3c2CC(C)CC3)cc1 10.1021/acs.jmedchem.9b00241
46887076 8855 0 None 1 2 Guinea pig 7.7 pEC50 = 7.7 Functional
Agonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay
ChEMBL 359 7 4 5 2.8 Cc1nc(N)sc1CCCNC(=N)NC(=O)CC(C)c1ccccc1 10.1016/j.bmcl.2010.03.082
CHEMBL1098110 8855 0 None 1 2 Guinea pig 7.7 pEC50 = 7.7 Functional
Agonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay
ChEMBL 359 7 4 5 2.8 Cc1nc(N)sc1CCCNC(=N)NC(=O)CC(C)c1ccccc1 10.1016/j.bmcl.2010.03.082
164618508 185340 0 None - 1 Guinea pig 7.7 pEC50 = 7.7 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 374 6 4 4 2.7 Cc1ccc(C(C)NC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1 10.1016/j.ejmech.2021.113190
CHEMBL4869194 185340 0 None - 1 Guinea pig 7.7 pEC50 = 7.7 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 374 6 4 4 2.7 Cc1ccc(C(C)NC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1 10.1016/j.ejmech.2021.113190
164611807 184391 0 None - 1 Guinea pig 6.7 pEC50 = 6.7 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 376 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)N[C@@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4854278 184391 0 None - 1 Guinea pig 6.7 pEC50 = 6.7 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 376 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)N[C@@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
164608815 183862 0 None 3 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 380 7 4 4 2.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1 10.1016/j.ejmech.2021.113190
CHEMBL4846638 183862 0 None 3 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 380 7 4 4 2.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1 10.1016/j.ejmech.2021.113190
164614907 183991 0 None - 1 Guinea pig 7.6 pEC50 = 7.6 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 378 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(F)cc1 10.1016/j.ejmech.2021.113190
CHEMBL4848697 183991 0 None - 1 Guinea pig 7.6 pEC50 = 7.6 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 378 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(F)cc1 10.1016/j.ejmech.2021.113190
164622330 185270 0 None 9 3 Guinea pig 7.6 pEC50 = 7.6 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 360 6 4 4 2.3 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)N[C@@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4867962 185270 0 None 9 3 Guinea pig 7.6 pEC50 = 7.6 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 360 6 4 4 2.3 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)N[C@@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
46830167 8658 0 None -13 5 Guinea pig 7.6 pEC50 = 7.6 Functional
Agonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay
ChEMBL 313 7 4 3 2.2 C[C@@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)c1ccccc1 10.1016/j.bmcl.2010.03.082
CHEMBL1096429 8658 0 None -13 5 Guinea pig 7.6 pEC50 = 7.6 Functional
Agonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay
ChEMBL 313 7 4 3 2.2 C[C@@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)c1ccccc1 10.1016/j.bmcl.2010.03.082
168286426 192314 0 None 5 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 403 10 4 5 2.3 CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5198795 192314 0 None 5 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 403 10 4 5 2.3 CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222241 192314 0 None 5 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 403 10 4 5 2.3 CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
164609493 183844 0 None -23 4 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 350 6 4 5 1.9 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccco1 10.1016/j.ejmech.2021.113190
CHEMBL4846380 183844 0 None -23 4 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 350 6 4 5 1.9 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccco1 10.1016/j.ejmech.2021.113190
168292954 192385 0 None 7 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay
ChEMBL 388 8 4 4 2.5 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5202592 192385 0 None 7 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay
ChEMBL 388 8 4 4 2.5 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222660 192385 0 None 7 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay
ChEMBL 388 8 4 4 2.5 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
168294767 192407 0 None -6 11 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5207281 192407 0 None -6 11 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222802 192407 0 None -6 11 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5075106 213741 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)O)c3ccccc3C2(C)C)c2cc(S(=O)(=O)[O-])ccc2C1(C)C 10.1016/j.bmcl.2021.128388
CHEMBL5095549 213741 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)O)c3ccccc3C2(C)C)c2cc(S(=O)(=O)[O-])ccc2C1(C)C 10.1016/j.bmcl.2021.128388
164622153 184976 0 None - 1 Guinea pig 7.6 pEC50 = 7.6 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 394 6 4 4 3.0 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(Cl)cc1 10.1016/j.ejmech.2021.113190
CHEMBL4863347 184976 0 None - 1 Guinea pig 7.6 pEC50 = 7.6 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 394 6 4 4 3.0 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(Cl)cc1 10.1016/j.ejmech.2021.113190
56954425 81655 0 None -1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 584 23 6 4 4.0 N/C(=N\C(=O)CCCCCCCCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1 10.1021/jm201128q
CHEMBL2165643 81655 0 None -1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 584 23 6 4 4.0 N/C(=N\C(=O)CCCCCCCCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1 10.1021/jm201128q
155523256 170169 0 None -3 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay
ChEMBL 269 2 1 4 3.2 COc1cccc(-c2nc(N)nc3c2CCCC3C)c1 10.1021/acs.jmedchem.9b00241
CHEMBL4452406 170169 0 None -3 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay
ChEMBL 269 2 1 4 3.2 COc1cccc(-c2nc(N)nc3c2CCCC3C)c1 10.1021/acs.jmedchem.9b00241
168295541 192428 0 None 8 3 Guinea pig 7.6 pEC50 = 7.6 Functional
Agonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assayAgonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assay
ChEMBL 347 6 4 5 1.4 C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5208845 192428 0 None 8 3 Guinea pig 7.6 pEC50 = 7.6 Functional
Agonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assayAgonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assay
ChEMBL 347 6 4 5 1.4 C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222926 192428 0 None 8 3 Guinea pig 7.6 pEC50 = 7.6 Functional
Agonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assayAgonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assay
ChEMBL 347 6 4 5 1.4 C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1 10.1021/acs.jmedchem.1c00692
46830167 8658 0 None -13 5 Guinea pig 7.6 pEC50 = 7.6 Functional
Agonist activity at histamine H2 receptor in spontaneously beating guinea pig atriumAgonist activity at histamine H2 receptor in spontaneously beating guinea pig atrium
ChEMBL 313 7 4 3 2.2 C[C@@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)c1ccccc1 10.1016/j.bmcl.2010.03.082
CHEMBL1096429 8658 0 None -13 5 Guinea pig 7.6 pEC50 = 7.6 Functional
Agonist activity at histamine H2 receptor in spontaneously beating guinea pig atriumAgonist activity at histamine H2 receptor in spontaneously beating guinea pig atrium
ChEMBL 313 7 4 3 2.2 C[C@@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)c1ccccc1 10.1016/j.bmcl.2010.03.082
164610648 184245 0 None - 1 Guinea pig 7.6 pEC50 = 7.6 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 374 7 4 4 2.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4852212 184245 0 None - 1 Guinea pig 7.6 pEC50 = 7.6 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 374 7 4 4 2.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
56954125 81645 0 None 5 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 676 23 6 8 5.3 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCCCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/jm201128q
CHEMBL2165634 81645 0 None 5 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 676 23 6 8 5.3 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCCCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/jm201128q
168290235 192356 0 None -3 10 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5201074 192356 0 None -3 10 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222491 192356 0 None -3 10 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
168294767 192407 0 None -6 11 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting method
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5207281 192407 0 None -6 11 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting method
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222802 192407 0 None -6 11 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting method
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
155523256 170169 0 None -3 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay
ChEMBL 269 2 1 4 3.2 COc1cccc(-c2nc(N)nc3c2CCCC3C)c1 10.1021/acs.jmedchem.9b00241
CHEMBL4452406 170169 0 None -3 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay
ChEMBL 269 2 1 4 3.2 COc1cccc(-c2nc(N)nc3c2CCCC3C)c1 10.1021/acs.jmedchem.9b00241
1204 1893 114 None -14 11 Guinea pig 6.6 pEC50 = 6.6 Functional
Agonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assayAgonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
1247 1893 114 None -14 11 Guinea pig 6.6 pEC50 = 6.6 Functional
Agonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assayAgonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
1375 1893 114 None -14 11 Guinea pig 6.6 pEC50 = 6.6 Functional
Agonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assayAgonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
774 1893 114 None -14 11 Guinea pig 6.6 pEC50 = 6.6 Functional
Agonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assayAgonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
CHEMBL90 1893 114 None -14 11 Guinea pig 6.6 pEC50 = 6.6 Functional
Agonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assayAgonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
DB05381 1893 114 None -14 11 Guinea pig 6.6 pEC50 = 6.6 Functional
Agonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assayAgonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
CHEMBL5092267 213571 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCC[n+]1c(C)cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc1C 10.1016/j.bmcl.2021.128388
164609017 183833 0 None -6 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 416 10 4 4 3.2 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CCCc1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4846201 183833 0 None -6 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 416 10 4 4 3.2 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CCCc1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL5093461 213767 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL None None None CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2nnc(N)s2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1016/j.bmcl.2021.128388
CHEMBL5095884 213767 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL None None None CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2nnc(N)s2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1016/j.bmcl.2021.128388
164626153 185786 0 None 2 4 Guinea pig 7.6 pEC50 = 7.6 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 378 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1cccc(F)c1 10.1016/j.ejmech.2021.113190
CHEMBL4875600 185786 0 None 2 4 Guinea pig 7.6 pEC50 = 7.6 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 378 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1cccc(F)c1 10.1016/j.ejmech.2021.113190
164617783 183997 0 None -2 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 388 8 4 4 2.8 CCC(CNC(=O)/N=C(\N)NCCCc1sc(N)nc1C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4848815 183997 0 None -2 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 388 8 4 4 2.8 CCC(CNC(=O)/N=C(\N)NCCCc1sc(N)nc1C)c1ccccc1 10.1016/j.ejmech.2021.113190
56954002 81644 0 None -1 2 Guinea pig 6.6 pEC50 = 6.6 Functional
Agonist activity at H2R in spontaneously beating guinea pig right atrium assessed as increase in heart rateAgonist activity at H2R in spontaneously beating guinea pig right atrium assessed as increase in heart rate
ChEMBL 620 19 6 8 3.7 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/jm201128q
CHEMBL2165633 81644 0 None -1 2 Guinea pig 6.6 pEC50 = 6.6 Functional
Agonist activity at H2R in spontaneously beating guinea pig right atrium assessed as increase in heart rateAgonist activity at H2R in spontaneously beating guinea pig right atrium assessed as increase in heart rate
ChEMBL 620 19 6 8 3.7 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/jm201128q
46887078 8901 0 None -1 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay
ChEMBL 359 7 4 5 2.8 Cc1nc(N)sc1CCCNC(=N)NC(=O)C[C@H](C)c1ccccc1 10.1016/j.bmcl.2010.03.082
CHEMBL1098442 8901 0 None -1 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay
ChEMBL 359 7 4 5 2.8 Cc1nc(N)sc1CCCNC(=N)NC(=O)C[C@H](C)c1ccccc1 10.1016/j.bmcl.2010.03.082
25149521 178464 0 None -1 3 Guinea pig 7.6 pEC50 = 7.6 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 375 8 4 3 3.2 N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1ccccc1 10.1021/jm800841w
CHEMBL471413 178464 0 None -1 3 Guinea pig 7.6 pEC50 = 7.6 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 375 8 4 3 3.2 N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1ccccc1 10.1021/jm800841w
46887115 8411 0 None 1 4 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay
ChEMBL 365 7 4 5 3.2 Cc1nc(N)sc1CCCNC(=N)NC(=O)C[C@H](C)C1CCCCC1 10.1016/j.bmcl.2010.03.082
CHEMBL1094144 8411 0 None 1 4 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay
ChEMBL 365 7 4 5 3.2 Cc1nc(N)sc1CCCNC(=N)NC(=O)C[C@H](C)C1CCCCC1 10.1016/j.bmcl.2010.03.082
164617783 183997 0 None -2 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 388 8 4 4 2.8 CCC(CNC(=O)/N=C(\N)NCCCc1sc(N)nc1C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4848815 183997 0 None -2 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 388 8 4 4 2.8 CCC(CNC(=O)/N=C(\N)NCCCc1sc(N)nc1C)c1ccccc1 10.1016/j.ejmech.2021.113190
164611342 184495 0 None -1 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 346 6 4 4 1.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCc1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4856005 184495 0 None -1 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 346 6 4 4 1.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCc1ccccc1 10.1016/j.ejmech.2021.113190
164620704 185491 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 416 8 4 4 3.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)c1ccc(C(C)C)cc1 10.1016/j.ejmech.2021.113190
CHEMBL4871482 185491 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 416 8 4 4 3.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)c1ccc(C(C)C)cc1 10.1016/j.ejmech.2021.113190
168295541 192428 0 None -8 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay
ChEMBL 347 6 4 5 1.4 C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5208845 192428 0 None -8 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay
ChEMBL 347 6 4 5 1.4 C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222926 192428 0 None -8 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay
ChEMBL 347 6 4 5 1.4 C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1 10.1021/acs.jmedchem.1c00692
168286426 192314 0 None 5 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay
ChEMBL 403 10 4 5 2.3 CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5198795 192314 0 None 5 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay
ChEMBL 403 10 4 5 2.3 CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222241 192314 0 None 5 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay
ChEMBL 403 10 4 5 2.3 CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
1269 121 33 None -67 6 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1021/jm900526h
37463 121 33 None -67 6 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1021/jm900526h
CHEMBL275443 121 33 None -67 6 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1021/jm900526h
164624107 185130 0 None 8 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 402 9 4 4 2.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CCc1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4865765 185130 0 None 8 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 402 9 4 4 2.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CCc1ccccc1 10.1016/j.ejmech.2021.113190
56954320 81653 0 None 1 4 Guinea pig 8.5 pEC50 = 8.5 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 472 15 6 4 0.9 N/C(=N\C(=O)CCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1 10.1021/jm201128q
CHEMBL2165641 81653 0 None 1 4 Guinea pig 8.5 pEC50 = 8.5 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 472 15 6 4 0.9 N/C(=N\C(=O)CCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1 10.1021/jm201128q
168295528 192419 0 None -12 10 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5206565 192419 0 None -12 10 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222872 192419 0 None -12 10 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
56954513 81657 0 None 3 2 Guinea pig 8.5 pEC50 = 8.5 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 578 17 6 8 2.6 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1cnc(N)s1 10.1021/jm201128q
CHEMBL2165645 81657 0 None 3 2 Guinea pig 8.5 pEC50 = 8.5 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 578 17 6 8 2.6 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1cnc(N)s1 10.1021/jm201128q
1200 3888 1 None - 1 Guinea pig 7.5 pEC50 = 7.5 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 335 8 4 5 0.7 O=C(NC(=NCCCc1cnc[nH]1)N)CSCc1nc[nH]c1C 10.1021/jm800841w
25149519 3888 1 None - 1 Guinea pig 7.5 pEC50 = 7.5 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 335 8 4 5 0.7 O=C(NC(=NCCCc1cnc[nH]1)N)CSCc1nc[nH]c1C 10.1021/jm800841w
CHEMBL513056 3888 1 None - 1 Guinea pig 7.5 pEC50 = 7.5 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 335 8 4 5 0.7 O=C(NC(=NCCCc1cnc[nH]1)N)CSCc1nc[nH]c1C 10.1021/jm800841w
56954129 81647 0 None -22 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 536 15 6 8 1.5 N/C(=N\C(=O)CCCCCCC(=O)/N=C(\N)NCCCc1cnc(N)s1)NCCCc1cnc(N)s1 10.1021/jm201128q
CHEMBL2165636 81647 0 None -22 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 536 15 6 8 1.5 N/C(=N\C(=O)CCCCCCC(=O)/N=C(\N)NCCCc1cnc(N)s1)NCCCc1cnc(N)s1 10.1021/jm201128q
164614645 184539 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 402 8 4 4 3.0 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(c1ccccc1)C(C)C 10.1016/j.ejmech.2021.113190
CHEMBL4856572 184539 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 402 8 4 4 3.0 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(c1ccccc1)C(C)C 10.1016/j.ejmech.2021.113190
42625303 180174 0 None -190 7 Guinea pig 6.5 pEC50 = 6.5 Functional
Agonist activity at histamine H2 receptor in guinea pig atrium assessed as increase in heart rateAgonist activity at histamine H2 receptor in guinea pig atrium assessed as increase in heart rate
ChEMBL 223 5 3 2 0.2 CCC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL475621 180174 0 None -190 7 Guinea pig 6.5 pEC50 = 6.5 Functional
Agonist activity at histamine H2 receptor in guinea pig atrium assessed as increase in heart rateAgonist activity at histamine H2 receptor in guinea pig atrium assessed as increase in heart rate
ChEMBL 223 5 3 2 0.2 CCC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
164610892 184605 0 None 4 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 394 8 4 4 3.2 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CC1CCCCC1 10.1016/j.ejmech.2021.113190
CHEMBL4857560 184605 0 None 4 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 394 8 4 4 3.2 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CC1CCCCC1 10.1016/j.ejmech.2021.113190
25149609 178551 0 None - 1 Guinea pig 6.5 pEC50 = 6.5 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 443 8 4 3 4.5 N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccc(Cl)cc1)c1ccc(Cl)cc1 10.1021/jm800841w
CHEMBL472054 178551 0 None - 1 Guinea pig 6.5 pEC50 = 6.5 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 443 8 4 3 4.5 N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccc(Cl)cc1)c1ccc(Cl)cc1 10.1021/jm800841w
155565842 175033 0 None -5 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay
ChEMBL 317 1 1 3 3.9 CC1CCCc2c(-c3cccc(Br)c3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
CHEMBL4580450 175033 0 None -5 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay
ChEMBL 317 1 1 3 3.9 CC1CCCc2c(-c3cccc(Br)c3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
1269 121 33 None -67 6 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assay
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
37463 121 33 None -67 6 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assay
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL275443 121 33 None -67 6 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assay
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
168290235 192356 0 None -3 10 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5201074 192356 0 None -3 10 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222491 192356 0 None -3 10 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
46887043 8660 0 None -3 5 Guinea pig 7.5 pEC50 = 7.5 Functional
Agonist activity at histamine H2 receptor in spontaneously beating guinea pig atriumAgonist activity at histamine H2 receptor in spontaneously beating guinea pig atrium
ChEMBL 319 7 4 3 2.6 C[C@@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)C1CCCCC1 10.1016/j.bmcl.2010.03.082
CHEMBL1096431 8660 0 None -3 5 Guinea pig 7.5 pEC50 = 7.5 Functional
Agonist activity at histamine H2 receptor in spontaneously beating guinea pig atriumAgonist activity at histamine H2 receptor in spontaneously beating guinea pig atrium
ChEMBL 319 7 4 3 2.6 C[C@@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)C1CCCCC1 10.1016/j.bmcl.2010.03.082
1199 2916 0 None - 1 Guinea pig 7.5 pEC50 = 7.5 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as 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 2916 0 None - 1 Guinea pig 7.5 pEC50 = 7.5 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as 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 2916 0 None - 1 Guinea pig 7.5 pEC50 = 7.5 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 394 8 3 4 2.5 NC(=NCCCc1[nH]cnc1)NC(=O)CC(c1ccccn1)c1ccc(cc1)F 10.1021/jm800841w
CHEMBL5094083 213682 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis
ChEMBL None None None C=C(/N=C(\C)NCCCc1nnc(N)s1)NCCCCCCCCN 10.1016/j.bmcl.2021.128388
56954127 81646 0 None - 1 Guinea pig 6.5 pEC50 = 6.5 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 760 29 6 8 7.6 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCCCCCCCCCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/jm201128q
CHEMBL2165635 81646 0 None - 1 Guinea pig 6.5 pEC50 = 6.5 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 760 29 6 8 7.6 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCCCCCCCCCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/jm201128q
164627020 185816 0 None -8 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 422 7 4 4 3.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4876025 185816 0 None -8 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 422 7 4 4 3.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL5075713 213743 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL None None None CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2c[nH]cn2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1016/j.bmcl.2021.128388
CHEMBL5095559 213743 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL None None None CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2c[nH]cn2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1016/j.bmcl.2021.128388
CHEMBL5093461 213767 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitment
ChEMBL None None None CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2nnc(N)s2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1016/j.bmcl.2021.128388
CHEMBL5095884 213767 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitment
ChEMBL None None None CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2nnc(N)s2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1016/j.bmcl.2021.128388
CHEMBL5083588 213748 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C 10.1016/j.bmcl.2021.128388
CHEMBL5095633 213748 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C 10.1016/j.bmcl.2021.128388
164610421 184668 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 332 5 4 4 2.1 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)Nc1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4858567 184668 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 332 5 4 4 2.1 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)Nc1ccccc1 10.1016/j.ejmech.2021.113190
44588146 175330 0 None - 1 Guinea pig 5.5 pEC50 = 5.5 Functional
Antagonist activity at histamine H2 receptor in guinea pig atrium assessed as changes in rate of spontaneous beatAntagonist activity at histamine H2 receptor in guinea pig atrium assessed as changes in rate of spontaneous beat
ChEMBL 380 13 0 2 6.6 CCCN(CCC)Cc1ccc(-c2ccc(CN(CCC)CCC)cc2)cc1 10.1016/j.bmc.2008.10.029
CHEMBL458718 175330 0 None - 1 Guinea pig 5.5 pEC50 = 5.5 Functional
Antagonist activity at histamine H2 receptor in guinea pig atrium assessed as changes in rate of spontaneous beatAntagonist activity at histamine H2 receptor in guinea pig atrium assessed as changes in rate of spontaneous beat
ChEMBL 380 13 0 2 6.6 CCCN(CCC)Cc1ccc(-c2ccc(CN(CCC)CCC)cc2)cc1 10.1016/j.bmc.2008.10.029
56954125 81645 0 None -5 2 Guinea pig 7.5 pEC50 = 7.5 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 676 23 6 8 5.3 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCCCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/jm201128q
CHEMBL2165634 81645 0 None -5 2 Guinea pig 7.5 pEC50 = 7.5 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 676 23 6 8 5.3 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCCCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/jm201128q
56954427 81656 0 None 12 2 Guinea pig 7.5 pEC50 = 7.5 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 669 29 6 4 6.4 N/C(=N\C(=O)CCCCCCCCCCCCCCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1 10.1021/jm201128q
CHEMBL2165644 81656 0 None 12 2 Guinea pig 7.5 pEC50 = 7.5 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 669 29 6 4 6.4 N/C(=N\C(=O)CCCCCCCCCCCCCCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1 10.1021/jm201128q
164614841 184682 0 None - 1 Guinea pig 7.5 pEC50 = 7.5 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 388 7 4 4 3.0 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(c1ccccc1)C(C)C 10.1016/j.ejmech.2021.113190
CHEMBL4858849 184682 0 None - 1 Guinea pig 7.5 pEC50 = 7.5 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 388 7 4 4 3.0 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(c1ccccc1)C(C)C 10.1016/j.ejmech.2021.113190
168273640 192193 0 None 4 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting method
ChEMBL 568 15 8 10 -0.1 N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5176229 192193 0 None 4 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting method
ChEMBL 568 15 8 10 -0.1 N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221444 192193 0 None 4 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting method
ChEMBL 568 15 8 10 -0.1 N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
164620704 185491 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 416 8 4 4 3.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)c1ccc(C(C)C)cc1 10.1016/j.ejmech.2021.113190
CHEMBL4871482 185491 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 416 8 4 4 3.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)c1ccc(C(C)C)cc1 10.1016/j.ejmech.2021.113190
164624107 185130 0 None 8 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 402 9 4 4 2.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CCc1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4865765 185130 0 None 8 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 402 9 4 4 2.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CCc1ccccc1 10.1016/j.ejmech.2021.113190
42625223 179335 0 None -323 4 Guinea pig 5.5 pEC50 = 5.5 Functional
Agonist activity at histamine H2 receptor in guinea pig atrium assessed as increase in heart rateAgonist activity at histamine H2 receptor in guinea pig atrium assessed as increase in heart rate
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 179335 0 None -323 4 Guinea pig 5.5 pEC50 = 5.5 Functional
Agonist activity at histamine H2 receptor in guinea pig atrium assessed as increase in heart rateAgonist activity at histamine H2 receptor in guinea pig atrium assessed as increase in heart rate
ChEMBL 395 8 4 3 1.4 CN(CCC(=O)/N=C(\N)NCCCc1c[nH]cn1)C(=O)c1cc2ccccc2[nH]1 10.1021/jm9000693
155567151 175269 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay
ChEMBL 245 1 1 3 3.5 CC1CCCc2c1nc(N)nc2C1CCCCC1 10.1021/acs.jmedchem.9b00241
CHEMBL4585616 175269 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay
ChEMBL 245 1 1 3 3.5 CC1CCCc2c1nc(N)nc2C1CCCCC1 10.1021/acs.jmedchem.9b00241
155567151 175269 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay
ChEMBL 245 1 1 3 3.5 CC1CCCc2c1nc(N)nc2C1CCCCC1 10.1021/acs.jmedchem.9b00241
CHEMBL4585616 175269 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay
ChEMBL 245 1 1 3 3.5 CC1CCCc2c1nc(N)nc2C1CCCCC1 10.1021/acs.jmedchem.9b00241
25149706 178374 0 None - 1 Guinea pig 5.4 pEC50 = 5.4 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 299 6 4 3 1.8 CC(C(=O)NC(=N)NCCCc1c[nH]cn1)c1ccccc1 10.1021/jm800841w
CHEMBL470564 178374 0 None - 1 Guinea pig 5.4 pEC50 = 5.4 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 299 6 4 3 1.8 CC(C(=O)NC(=N)NCCCc1c[nH]cn1)c1ccccc1 10.1021/jm800841w
25149515 185238 0 None - 1 Guinea pig 6.4 pEC50 = 6.4 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 319 8 4 3 2.7 N=C(NCCCc1c[nH]cn1)NC(=O)CCCC1CCCCC1 10.1021/jm800841w
CHEMBL486746 185238 0 None - 1 Guinea pig 6.4 pEC50 = 6.4 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 319 8 4 3 2.7 N=C(NCCCc1c[nH]cn1)NC(=O)CCCC1CCCCC1 10.1021/jm800841w
164616851 184357 0 None -4 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 376 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)N[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4853772 184357 0 None -4 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 376 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)N[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
164618283 183951 0 None - 1 Guinea pig 7.4 pEC50 = 7.4 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 390 7 4 5 2.4 COc1ccc(C(C)NC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1 10.1016/j.ejmech.2021.113190
CHEMBL4848026 183951 0 None - 1 Guinea pig 7.4 pEC50 = 7.4 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 390 7 4 5 2.4 COc1ccc(C(C)NC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1 10.1016/j.ejmech.2021.113190
25149613 178611 0 None 2 3 Guinea pig 7.4 pEC50 = 7.4 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 382 8 4 5 2.7 N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1nccs1 10.1021/jm800841w
CHEMBL472441 178611 0 None 2 3 Guinea pig 7.4 pEC50 = 7.4 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 382 8 4 5 2.7 N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1nccs1 10.1021/jm800841w
25149337 187791 0 None - 1 Guinea pig 7.4 pEC50 = 7.4 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 314 7 4 4 1.6 CC(CC(=O)NC(=N)NCCCc1c[nH]cn1)c1ccccn1 10.1021/jm800841w
CHEMBL501589 187791 0 None - 1 Guinea pig 7.4 pEC50 = 7.4 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 314 7 4 4 1.6 CC(CC(=O)NC(=N)NCCCc1c[nH]cn1)c1ccccn1 10.1021/jm800841w
25149708 187842 0 None -17 4 Guinea pig 7.4 pEC50 = 7.4 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 319 7 4 4 2.2 CC(CC(=O)NC(=N)NCCCc1c[nH]cn1)c1cccs1 10.1021/jm800841w
CHEMBL502339 187842 0 None -17 4 Guinea pig 7.4 pEC50 = 7.4 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 319 7 4 4 2.2 CC(CC(=O)NC(=N)NCCCc1c[nH]cn1)c1cccs1 10.1021/jm800841w
168290235 192356 0 None 3 10 Guinea pig 7.4 pEC50 = 7.4 Functional
Agonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beatAgonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beat
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5201074 192356 0 None 3 10 Guinea pig 7.4 pEC50 = 7.4 Functional
Agonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beatAgonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beat
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222491 192356 0 None 3 10 Guinea pig 7.4 pEC50 = 7.4 Functional
Agonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beatAgonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beat
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
25149710 178550 0 None - 1 Guinea pig 7.4 pEC50 = 7.4 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 320 7 4 5 1.6 CC(CC(=O)NC(=N)NCCCc1c[nH]cn1)c1nccs1 10.1021/jm800841w
CHEMBL472039 178550 0 None - 1 Guinea pig 7.4 pEC50 = 7.4 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 320 7 4 5 1.6 CC(CC(=O)NC(=N)NCCCc1c[nH]cn1)c1nccs1 10.1021/jm800841w
164614549 184350 0 None -3 4 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 340 9 4 4 2.2 CCCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1016/j.ejmech.2021.113190
CHEMBL4853668 184350 0 None -3 4 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 340 9 4 4 2.2 CCCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1016/j.ejmech.2021.113190
44482300 5701 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay
ChEMBL 342 9 4 2 2.0 NC(=O)/N=C(/NCCCCc1ccccc1)NCCCc1c[nH]cn1 10.1021/jm900526h
CHEMBL1078746 5701 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay
ChEMBL 342 9 4 2 2.0 NC(=O)/N=C(/NCCCCc1ccccc1)NCCCc1c[nH]cn1 10.1021/jm900526h
1204 1893 114 None -61 11 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2021.128388
1247 1893 114 None -61 11 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2021.128388
1375 1893 114 None -61 11 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2021.128388
774 1893 114 None -61 11 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2021.128388
CHEMBL90 1893 114 None -61 11 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2021.128388
DB05381 1893 114 None -61 11 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2021.128388
1204 1893 114 None -61 11 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2021.113190
1247 1893 114 None -61 11 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2021.113190
1375 1893 114 None -61 11 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2021.113190
774 1893 114 None -61 11 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2021.113190
CHEMBL90 1893 114 None -61 11 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2021.113190
DB05381 1893 114 None -61 11 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2021.113190
1204 1893 114 None -61 11 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
1247 1893 114 None -61 11 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
1375 1893 114 None -61 11 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
774 1893 114 None -61 11 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
CHEMBL90 1893 114 None -61 11 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
DB05381 1893 114 None -61 11 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
164628701 185875 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 338 5 4 4 1.9 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC1CCCCC1 10.1016/j.ejmech.2021.113190
CHEMBL4876743 185875 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 338 5 4 4 1.9 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC1CCCCC1 10.1016/j.ejmech.2021.113190
CHEMBL5087637 213769 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C 10.1016/j.bmcl.2021.128388
CHEMBL5095891 213769 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C 10.1016/j.bmcl.2021.128388
44481487 6015 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay
ChEMBL 302 7 3 3 2.3 N#C/N=C(/NCCCC1CCCCC1)NCCc1c[nH]cn1 10.1021/jm900526h
CHEMBL1080772 6015 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay
ChEMBL 302 7 3 3 2.3 N#C/N=C(/NCCCC1CCCCC1)NCCc1c[nH]cn1 10.1021/jm900526h
164627020 185816 0 None 8 2 Guinea pig 7.4 pEC50 = 7.4 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 422 7 4 4 3.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4876025 185816 0 None 8 2 Guinea pig 7.4 pEC50 = 7.4 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 422 7 4 4 3.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2021.113190
46887078 8901 0 None 1 2 Guinea pig 7.4 pEC50 = 7.4 Functional
Agonist activity at histamine H2 receptor in spontaneously beating guinea pig atriumAgonist activity at histamine H2 receptor in spontaneously beating guinea pig atrium
ChEMBL 359 7 4 5 2.8 Cc1nc(N)sc1CCCNC(=N)NC(=O)C[C@H](C)c1ccccc1 10.1016/j.bmcl.2010.03.082
CHEMBL1098442 8901 0 None 1 2 Guinea pig 7.4 pEC50 = 7.4 Functional
Agonist activity at histamine H2 receptor in spontaneously beating guinea pig atriumAgonist activity at histamine H2 receptor in spontaneously beating guinea pig atrium
ChEMBL 359 7 4 5 2.8 Cc1nc(N)sc1CCCNC(=N)NC(=O)C[C@H](C)c1ccccc1 10.1016/j.bmcl.2010.03.082
25149331 188801 0 None - 1 Guinea pig 6.4 pEC50 = 6.4 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 491 10 4 5 3.7 N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccc(F)c(F)c1)c1nccn1Cc1ccccc1 10.1021/jm800841w
CHEMBL513039 188801 0 None - 1 Guinea pig 6.4 pEC50 = 6.4 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 491 10 4 5 3.7 N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccc(F)c(F)c1)c1nccn1Cc1ccccc1 10.1021/jm800841w
59868 93707 56 None - 1 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 211 3 2 4 1.6 CCCN[C@@H]1CCc2nc(N)sc2C1 10.1016/j.ejmech.2021.113190
CHEMBL249420 93707 56 None - 1 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 211 3 2 4 1.6 CCCN[C@@H]1CCc2nc(N)sc2C1 10.1016/j.ejmech.2021.113190
168294767 192407 0 None 6 11 Guinea pig 8.4 pEC50 = 8.4 Functional
Agonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assayAgonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assay
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5207281 192407 0 None 6 11 Guinea pig 8.4 pEC50 = 8.4 Functional
Agonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assayAgonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assay
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222802 192407 0 None 6 11 Guinea pig 8.4 pEC50 = 8.4 Functional
Agonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assayAgonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assay
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
168290815 192361 0 None 23 3 Guinea pig 8.3 pEC50 = 8.3 Functional
Agonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beatAgonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beat
ChEMBL 327 9 4 5 1.2 CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5200771 192361 0 None 23 3 Guinea pig 8.3 pEC50 = 8.3 Functional
Agonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beatAgonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beat
ChEMBL 327 9 4 5 1.2 CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222529 192361 0 None 23 3 Guinea pig 8.3 pEC50 = 8.3 Functional
Agonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beatAgonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beat
ChEMBL 327 9 4 5 1.2 CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
168273745 192196 0 None 4 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 332 6 4 4 1.5 N/C(=N\C(=O)NCc1ccccc1)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5178472 192196 0 None 4 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 332 6 4 4 1.5 N/C(=N\C(=O)NCc1ccccc1)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221451 192196 0 None 4 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 332 6 4 4 1.5 N/C(=N\C(=O)NCc1ccccc1)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
168273640 192193 0 None 4 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay
ChEMBL 568 15 8 10 -0.1 N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5176229 192193 0 None 4 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay
ChEMBL 568 15 8 10 -0.1 N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221444 192193 0 None 4 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay
ChEMBL 568 15 8 10 -0.1 N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5075713 213743 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitment
ChEMBL None None None CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2c[nH]cn2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1016/j.bmcl.2021.128388
CHEMBL5095559 213743 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitment
ChEMBL None None None CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2c[nH]cn2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1016/j.bmcl.2021.128388
44482299 5645 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay
ChEMBL 328 8 4 2 1.6 NC(=O)/N=C(/NCCCc1ccccc1)NCCCc1c[nH]cn1 10.1021/jm900526h
CHEMBL1078359 5645 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay
ChEMBL 328 8 4 2 1.6 NC(=O)/N=C(/NCCCc1ccccc1)NCCCc1c[nH]cn1 10.1021/jm900526h
164627774 185973 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 344 3 4 4 1.4 N/C(=N\C(=O)NCc1ccccc1)NC1CCc2nc(N)sc2C1 10.1016/j.ejmech.2021.113190
CHEMBL4878215 185973 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 344 3 4 4 1.4 N/C(=N\C(=O)NCc1ccccc1)NC1CCc2nc(N)sc2C1 10.1016/j.ejmech.2021.113190
56953998 81642 0 None -29 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 578 16 6 8 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/jm201128q
CHEMBL2165631 81642 0 None -29 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 578 16 6 8 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/jm201128q
164622190 185024 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 360 7 4 4 1.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCc1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4864067 185024 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 360 7 4 4 1.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCc1ccccc1 10.1016/j.ejmech.2021.113190
164609729 184505 0 None -6 4 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 360 6 4 4 2.3 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)N[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4856059 184505 0 None -6 4 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 360 6 4 4 2.3 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)N[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
25149811 185370 0 None - 1 Guinea pig 6.3 pEC50 = 6.3 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 327 9 4 3 2.4 N=C(NCCCc1c[nH]cn1)NC(=O)CCCCc1ccccc1 10.1021/jm800841w
CHEMBL486963 185370 0 None - 1 Guinea pig 6.3 pEC50 = 6.3 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 327 9 4 3 2.4 N=C(NCCCc1c[nH]cn1)NC(=O)CCCCc1ccccc1 10.1021/jm800841w
164611143 184123 0 None - 1 Guinea pig 7.3 pEC50 = 7.3 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 414 6 4 4 2.9 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(c1ccccc1)C(F)(F)F 10.1016/j.ejmech.2021.113190
CHEMBL4850448 184123 0 None - 1 Guinea pig 7.3 pEC50 = 7.3 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 414 6 4 4 2.9 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(c1ccccc1)C(F)(F)F 10.1016/j.ejmech.2021.113190
25149431 184845 0 None - 1 Guinea pig 7.3 pEC50 = 7.3 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 277 5 4 3 1.6 N=C(NCCCc1c[nH]cn1)NC(=O)C1CCCCC1 10.1021/jm800841w
CHEMBL486153 184845 0 None - 1 Guinea pig 7.3 pEC50 = 7.3 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 277 5 4 3 1.6 N=C(NCCCc1c[nH]cn1)NC(=O)C1CCCCC1 10.1021/jm800841w
56953889 81641 0 None -120 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 564 15 6 8 2.1 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/jm201128q
CHEMBL2165630 81641 0 None -120 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 564 15 6 8 2.1 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/jm201128q
46887076 8855 0 None 1 2 Guinea pig 7.3 pEC50 = 7.3 Functional
Agonist activity at histamine H2 receptor in spontaneously beating guinea pig atriumAgonist activity at histamine H2 receptor in spontaneously beating guinea pig atrium
ChEMBL 359 7 4 5 2.8 Cc1nc(N)sc1CCCNC(=N)NC(=O)CC(C)c1ccccc1 10.1016/j.bmcl.2010.03.082
CHEMBL1098110 8855 0 None 1 2 Guinea pig 7.3 pEC50 = 7.3 Functional
Agonist activity at histamine H2 receptor in spontaneously beating guinea pig atriumAgonist activity at histamine H2 receptor in spontaneously beating guinea pig atrium
ChEMBL 359 7 4 5 2.8 Cc1nc(N)sc1CCCNC(=N)NC(=O)CC(C)c1ccccc1 10.1016/j.bmcl.2010.03.082
168273745 192196 0 None 4 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay
ChEMBL 332 6 4 4 1.5 N/C(=N\C(=O)NCc1ccccc1)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5178472 192196 0 None 4 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay
ChEMBL 332 6 4 4 1.5 N/C(=N\C(=O)NCc1ccccc1)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221451 192196 0 None 4 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay
ChEMBL 332 6 4 4 1.5 N/C(=N\C(=O)NCc1ccccc1)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
164612760 184125 0 None - 1 Guinea pig 6.3 pEC50 = 6.3 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 390 7 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NC[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4850490 184125 0 None - 1 Guinea pig 6.3 pEC50 = 6.3 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 390 7 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NC[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
42625224 180172 0 None -16 2 Guinea pig 6.3 pEC50 = 6.3 Functional
Agonist activity at histamine H2 receptor in guinea pig atrium assessed as increase in heart rateAgonist activity at histamine H2 receptor in guinea pig atrium assessed as increase in heart rate
ChEMBL 395 9 5 3 1.5 N/C(=N\C(=O)CCCNC(=O)c1cc2ccccc2[nH]1)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL475620 180172 0 None -16 2 Guinea pig 6.3 pEC50 = 6.3 Functional
Agonist activity at histamine H2 receptor in guinea pig atrium assessed as increase in heart rateAgonist activity at histamine H2 receptor in guinea pig atrium assessed as increase in heart rate
ChEMBL 395 9 5 3 1.5 N/C(=N\C(=O)CCCNC(=O)c1cc2ccccc2[nH]1)NCCCc1c[nH]cn1 10.1021/jm9000693
56954227 81648 0 None 4 2 Guinea pig 8.3 pEC50 = 8.3 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 564 17 6 8 2.3 N/C(=N\C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1cnc(N)s1)NCCCc1cnc(N)s1 10.1021/jm201128q
CHEMBL2165637 81648 0 None 4 2 Guinea pig 8.3 pEC50 = 8.3 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 564 17 6 8 2.3 N/C(=N\C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1cnc(N)s1)NCCCc1cnc(N)s1 10.1021/jm201128q
168294767 192407 0 None 6 11 Guinea pig 8.3 pEC50 = 8.3 Functional
Agonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beatAgonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beat
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5207281 192407 0 None 6 11 Guinea pig 8.3 pEC50 = 8.3 Functional
Agonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beatAgonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beat
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222802 192407 0 None 6 11 Guinea pig 8.3 pEC50 = 8.3 Functional
Agonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beatAgonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beat
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
164612037 184785 0 None 2 12 Guinea pig 8.2 pEC50 = 8.2 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1016/j.ejmech.2021.113190
CHEMBL4860528 184785 0 None 2 12 Guinea pig 8.2 pEC50 = 8.2 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1016/j.ejmech.2021.113190
168294767 192407 0 None -6 11 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5207281 192407 0 None -6 11 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222802 192407 0 None -6 11 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
46887076 8855 0 None -1 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay
ChEMBL 359 7 4 5 2.8 Cc1nc(N)sc1CCCNC(=N)NC(=O)CC(C)c1ccccc1 10.1016/j.bmcl.2010.03.082
CHEMBL1098110 8855 0 None -1 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay
ChEMBL 359 7 4 5 2.8 Cc1nc(N)sc1CCCNC(=N)NC(=O)CC(C)c1ccccc1 10.1016/j.bmcl.2010.03.082
25149246 188876 0 None - 1 Guinea pig 7.3 pEC50 = 7.3 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as 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 188876 0 None - 1 Guinea pig 7.3 pEC50 = 7.3 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as 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
CHEMBL5094663 213720 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](C)c3ccccc3C2(C)C)c2ccccc2C1(C)C 10.1016/j.bmcl.2021.128388
25149611 178586 0 None - 1 Guinea pig 7.3 pEC50 = 7.3 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 376 8 4 4 2.6 N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1ccccn1 10.1021/jm800841w
CHEMBL472272 178586 0 None - 1 Guinea pig 7.3 pEC50 = 7.3 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 376 8 4 4 2.6 N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1ccccn1 10.1021/jm800841w
CHEMBL5094663 213720 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitment
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](C)c3ccccc3C2(C)C)c2ccccc2C1(C)C 10.1016/j.bmcl.2021.128388
155542256 172505 0 None -1 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay
ChEMBL 257 5 1 4 3.1 CCCCc1cc(-c2ccc(OC)cc2)nc(N)n1 10.1021/acs.jmedchem.9b00241
CHEMBL4519923 172505 0 None -1 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay
ChEMBL 257 5 1 4 3.1 CCCCc1cc(-c2ccc(OC)cc2)nc(N)n1 10.1021/acs.jmedchem.9b00241
168297879 191740 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at histamine H2 receptor (unknown origin)Agonist activity at histamine H2 receptor (unknown origin)
ChEMBL 640 18 5 9 4.9 CCOC(=O)C1=C(C)NC(CSCCCCCNC(=N)NCCCc2ccc[nH]2)=C(C(=O)OCC)C1c1cccc([N+](=O)[O-])c1 10.1016/j.bmc.2022.116706
CHEMBL5207008 191740 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at histamine H2 receptor (unknown origin)Agonist activity at histamine H2 receptor (unknown origin)
ChEMBL 640 18 5 9 4.9 CCOC(=O)C1=C(C)NC(CSCCCCCNC(=N)NCCCc2ccc[nH]2)=C(C(=O)OCC)C1c1cccc([N+](=O)[O-])c1 10.1016/j.bmc.2022.116706
164610421 184668 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 332 5 4 4 2.1 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)Nc1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4858567 184668 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 332 5 4 4 2.1 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)Nc1ccccc1 10.1016/j.ejmech.2021.113190
155542256 172505 0 None -1 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay
ChEMBL 257 5 1 4 3.1 CCCCc1cc(-c2ccc(OC)cc2)nc(N)n1 10.1021/acs.jmedchem.9b00241
CHEMBL4519923 172505 0 None -1 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay
ChEMBL 257 5 1 4 3.1 CCCCc1cc(-c2ccc(OC)cc2)nc(N)n1 10.1021/acs.jmedchem.9b00241
155544839 174361 0 None 2 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay
ChEMBL 284 2 1 5 3.1 CC1CCCc2c(-c3ccc([N+](=O)[O-])cc3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
CHEMBL4565419 174361 0 None 2 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay
ChEMBL 284 2 1 5 3.1 CC1CCCc2c(-c3ccc([N+](=O)[O-])cc3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
46887077 8900 0 None -1 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay
ChEMBL 359 7 4 5 2.8 Cc1nc(N)sc1CCCNC(=N)NC(=O)C[C@@H](C)c1ccccc1 10.1016/j.bmcl.2010.03.082
CHEMBL1098441 8900 0 None -1 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay
ChEMBL 359 7 4 5 2.8 Cc1nc(N)sc1CCCNC(=N)NC(=O)C[C@@H](C)c1ccccc1 10.1016/j.bmcl.2010.03.082
25149240 188762 0 None - 1 Guinea pig 7.3 pEC50 = 7.3 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 411 8 4 3 3.5 N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1ccc(F)c(F)c1 10.1021/jm800841w
CHEMBL512716 188762 0 None - 1 Guinea pig 7.3 pEC50 = 7.3 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 411 8 4 3 3.5 N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1ccc(F)c(F)c1 10.1021/jm800841w
155544839 174361 0 None 2 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay
ChEMBL 284 2 1 5 3.1 CC1CCCc2c(-c3ccc([N+](=O)[O-])cc3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
CHEMBL4565419 174361 0 None 2 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay
ChEMBL 284 2 1 5 3.1 CC1CCCc2c(-c3ccc([N+](=O)[O-])cc3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
164627241 185837 0 None - 1 Guinea pig 7.3 pEC50 = 7.3 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 438 6 4 4 3.1 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(Br)cc1 10.1016/j.ejmech.2021.113190
CHEMBL4876267 185837 0 None - 1 Guinea pig 7.3 pEC50 = 7.3 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 438 6 4 4 3.1 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(Br)cc1 10.1016/j.ejmech.2021.113190
25149607 178288 0 None - 1 Guinea pig 7.3 pEC50 = 7.3 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 393 8 4 3 3.3 N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1ccc(F)cc1 10.1021/jm800841w
CHEMBL469749 178288 0 None - 1 Guinea pig 7.3 pEC50 = 7.3 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 393 8 4 3 3.3 N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1ccc(F)cc1 10.1021/jm800841w
56954125 81645 0 None -5 2 Guinea pig 6.3 pEC50 = 6.3 Functional
Agonist activity at H2R in spontaneously beating guinea pig right atrium assessed as increase in heart rateAgonist activity at H2R in spontaneously beating guinea pig right atrium assessed as increase in heart rate
ChEMBL 676 23 6 8 5.3 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCCCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/jm201128q
CHEMBL2165634 81645 0 None -5 2 Guinea pig 6.3 pEC50 = 6.3 Functional
Agonist activity at H2R in spontaneously beating guinea pig right atrium assessed as increase in heart rateAgonist activity at H2R in spontaneously beating guinea pig right atrium assessed as increase in heart rate
ChEMBL 676 23 6 8 5.3 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCCCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/jm201128q
1204 1893 114 None -61 11 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitment
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2021.128388
1247 1893 114 None -61 11 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitment
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2021.128388
1375 1893 114 None -61 11 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitment
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2021.128388
774 1893 114 None -61 11 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitment
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2021.128388
CHEMBL90 1893 114 None -61 11 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitment
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2021.128388
DB05381 1893 114 None -61 11 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitment
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2021.128388
25149427 185369 0 None - 1 Guinea pig 7.3 pEC50 = 7.3 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 313 8 4 3 2.0 N=C(NCCCc1c[nH]cn1)NC(=O)CCCc1ccccc1 10.1021/jm800841w
CHEMBL486962 185369 0 None - 1 Guinea pig 7.3 pEC50 = 7.3 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 313 8 4 3 2.0 N=C(NCCCc1c[nH]cn1)NC(=O)CCCc1ccccc1 10.1021/jm800841w
56954320 81653 0 None -17 4 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 472 15 6 4 0.9 N/C(=N\C(=O)CCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1 10.1021/jm201128q
CHEMBL2165641 81653 0 None -17 4 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 472 15 6 4 0.9 N/C(=N\C(=O)CCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1 10.1021/jm201128q
168278471 192236 0 None 2 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay
ChEMBL 312 8 4 4 1.5 CCCCCNC(=O)/N=C(\N)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5183205 192236 0 None 2 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay
ChEMBL 312 8 4 4 1.5 CCCCCNC(=O)/N=C(\N)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221757 192236 0 None 2 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay
ChEMBL 312 8 4 4 1.5 CCCCCNC(=O)/N=C(\N)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5087637 213769 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C 10.1016/j.bmcl.2021.128388
CHEMBL5095891 213769 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C 10.1016/j.bmcl.2021.128388
46887080 8445 0 None -1 2 Guinea pig 7.2 pEC50 = 7.2 Functional
Agonist activity at histamine H2 receptor in spontaneously beating guinea pig atriumAgonist activity at histamine H2 receptor in spontaneously beating guinea pig atrium
ChEMBL 365 7 4 5 3.2 Cc1nc(N)sc1CCCNC(=N)NC(=O)C[C@@H](C)C1CCCCC1 10.1016/j.bmcl.2010.03.082
CHEMBL1094452 8445 0 None -1 2 Guinea pig 7.2 pEC50 = 7.2 Functional
Agonist activity at histamine H2 receptor in spontaneously beating guinea pig atriumAgonist activity at histamine H2 receptor in spontaneously beating guinea pig atrium
ChEMBL 365 7 4 5 3.2 Cc1nc(N)sc1CCCNC(=N)NC(=O)C[C@@H](C)C1CCCCC1 10.1016/j.bmcl.2010.03.082
56953887 81659 0 None -22 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 536 13 6 8 1.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/jm201128q
CHEMBL2165647 81659 0 None -22 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 536 13 6 8 1.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/jm201128q
56954229 81649 0 None 1 2 Guinea pig 7.2 pEC50 = 7.2 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 648 23 6 8 4.7 N/C(=N\C(=O)CCCCCCCCCCCCCCC(=O)/N=C(\N)NCCCc1cnc(N)s1)NCCCc1cnc(N)s1 10.1021/jm201128q
CHEMBL2165638 81649 0 None 1 2 Guinea pig 7.2 pEC50 = 7.2 Functional
Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 648 23 6 8 4.7 N/C(=N\C(=O)CCCCCCCCCCCCCCC(=O)/N=C(\N)NCCCc1cnc(N)s1)NCCCc1cnc(N)s1 10.1021/jm201128q
168278471 192236 0 None 2 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 312 8 4 4 1.5 CCCCCNC(=O)/N=C(\N)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5183205 192236 0 None 2 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 312 8 4 4 1.5 CCCCCNC(=O)/N=C(\N)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221757 192236 0 None 2 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 312 8 4 4 1.5 CCCCCNC(=O)/N=C(\N)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
168290815 192361 0 None -23 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 327 9 4 5 1.2 CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5200771 192361 0 None -23 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 327 9 4 5 1.2 CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222529 192361 0 None -23 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 327 9 4 5 1.2 CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
56954322 81654 0 None -7 4 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 500 17 6 4 1.7 N/C(=N\C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1 10.1021/jm201128q
CHEMBL2165642 81654 0 None -7 4 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 500 17 6 4 1.7 N/C(=N\C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1 10.1021/jm201128q
46887043 8660 0 None -1 5 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay
ChEMBL 319 7 4 3 2.6 C[C@@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)C1CCCCC1 10.1016/j.bmcl.2010.03.082
CHEMBL1096431 8660 0 None -1 5 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay
ChEMBL 319 7 4 3 2.6 C[C@@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)C1CCCCC1 10.1016/j.bmcl.2010.03.082
168281746 192270 0 None 9 3 Guinea pig 8.2 pEC50 = 8.2 Functional
Agonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assayAgonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assay
ChEMBL 365 6 4 5 1.6 CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5184911 192270 0 None 9 3 Guinea pig 8.2 pEC50 = 8.2 Functional
Agonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assayAgonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assay
ChEMBL 365 6 4 5 1.6 CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5221974 192270 0 None 9 3 Guinea pig 8.2 pEC50 = 8.2 Functional
Agonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assayAgonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assay
ChEMBL 365 6 4 5 1.6 CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1 10.1021/acs.jmedchem.1c00692
164611757 184310 0 None 3 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 402 8 4 4 2.8 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1 10.1016/j.ejmech.2021.113190
CHEMBL4853107 184310 0 None 3 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 402 8 4 4 2.8 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1 10.1016/j.ejmech.2021.113190
25149433 185384 2 None - 1 Guinea pig 7.2 pEC50 = 7.2 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 305 7 4 3 2.3 N=C(NCCCc1c[nH]cn1)NC(=O)CCC1CCCCC1 10.1021/jm800841w
CHEMBL486974 185384 2 None - 1 Guinea pig 7.2 pEC50 = 7.2 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 305 7 4 3 2.3 N=C(NCCCc1c[nH]cn1)NC(=O)CCC1CCCCC1 10.1021/jm800841w
168268853 192173 0 None -1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 389 8 4 5 1.9 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5180504 192173 0 None -1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 389 8 4 5 1.9 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5221353 192173 0 None -1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 389 8 4 5 1.9 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
126688 400 28 None -1 3 Guinea pig 6.2 pEC50 = 6.2 Functional
Agonist activity at H2R in spontaneously beating guinea pig right atrium assessed as increase in heart rateAgonist activity at H2R in spontaneously beating guinea pig right atrium assessed as increase in heart rate
ChEMBL 157 2 2 4 0.5 NCCc1sc(nc1C)N 10.1021/jm201128q
4025 400 28 None -1 3 Guinea pig 6.2 pEC50 = 6.2 Functional
Agonist activity at H2R in spontaneously beating guinea pig right atrium assessed as increase in heart rateAgonist activity at H2R in spontaneously beating guinea pig right atrium assessed as increase in heart rate
ChEMBL 157 2 2 4 0.5 NCCc1sc(nc1C)N 10.1021/jm201128q
CHEMBL293762 400 28 None -1 3 Guinea pig 6.2 pEC50 = 6.2 Functional
Agonist activity at H2R in spontaneously beating guinea pig right atrium assessed as increase in heart rateAgonist activity at H2R in spontaneously beating guinea pig right atrium assessed as increase in heart rate
ChEMBL 157 2 2 4 0.5 NCCc1sc(nc1C)N 10.1021/jm201128q
CHEMBL5083588 213748 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitment
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C 10.1016/j.bmcl.2021.128388
CHEMBL5095633 213748 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitment
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C 10.1016/j.bmcl.2021.128388
25149712 178398 0 None -25 4 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assay
ChEMBL 299 7 4 3 1.6 N=C(NCCCc1c[nH]cn1)NC(=O)CCc1ccccc1 10.1016/j.bmcl.2010.10.041
CHEMBL470790 178398 0 None -25 4 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assay
ChEMBL 299 7 4 3 1.6 N=C(NCCCc1c[nH]cn1)NC(=O)CCc1ccccc1 10.1016/j.bmcl.2010.10.041
25149335 183633 0 None -26 4 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assay
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1016/j.bmcl.2010.10.041
CHEMBL483406 183633 0 None -26 4 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assay
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1016/j.bmcl.2010.10.041
CHEMBL5093461 213767 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitment
ChEMBL None None None CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2nnc(N)s2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1016/j.bmcl.2021.128388
CHEMBL5095884 213767 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitment
ChEMBL None None None CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2nnc(N)s2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1016/j.bmcl.2021.128388
164626153 185786 0 None -2 4 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 378 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1cccc(F)c1 10.1016/j.ejmech.2021.113190
CHEMBL4875600 185786 0 None -2 4 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 378 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1cccc(F)c1 10.1016/j.ejmech.2021.113190
1201 3889 1 None - 1 Guinea pig 6.2 pEC50 = 6.2 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 361 7 3 3 2.6 O=C(CC(c1ccccc1)c1ccccc1)NC(=NCCc1cnc[nH]1)N 10.1021/jm800841w
25150700 3889 1 None - 1 Guinea pig 6.2 pEC50 = 6.2 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 361 7 3 3 2.6 O=C(CC(c1ccccc1)c1ccccc1)NC(=NCCc1cnc[nH]1)N 10.1021/jm800841w
CHEMBL499301 3889 1 None - 1 Guinea pig 6.2 pEC50 = 6.2 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 361 7 3 3 2.6 O=C(CC(c1ccccc1)c1ccccc1)NC(=NCCc1cnc[nH]1)N 10.1021/jm800841w
44482299 5645 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay
ChEMBL 328 8 4 2 1.6 NC(=O)/N=C(/NCCCc1ccccc1)NCCCc1c[nH]cn1 10.1021/jm900526h
CHEMBL1078359 5645 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay
ChEMBL 328 8 4 2 1.6 NC(=O)/N=C(/NCCCc1ccccc1)NCCCc1c[nH]cn1 10.1021/jm900526h
25149333 172086 0 None - 1 Guinea pig 5.2 pEC50 = 5.2 Functional
Antagonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as inhibition of histamine-induced positive chronotropic activity
ChEMBL 313 7 4 3 2.2 CC(CCNC(=N)NC(=O)CCc1c[nH]cn1)c1ccccc1 10.1021/jm800841w
CHEMBL449828 172086 0 None - 1 Guinea pig 5.2 pEC50 = 5.2 Functional
Antagonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as inhibition of histamine-induced positive chronotropic activityAntagonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as inhibition of histamine-induced positive chronotropic activity
ChEMBL 313 7 4 3 2.2 CC(CCNC(=N)NC(=O)CCc1c[nH]cn1)c1ccccc1 10.1021/jm800841w
1204 1893 114 None -61 11 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human H2 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H2 receptor expressed in 293-EBNA cells by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0603318
1247 1893 114 None -61 11 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human H2 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H2 receptor expressed in 293-EBNA cells by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0603318
1375 1893 114 None -61 11 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human H2 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H2 receptor expressed in 293-EBNA cells by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0603318
774 1893 114 None -61 11 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human H2 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H2 receptor expressed in 293-EBNA cells by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0603318
CHEMBL90 1893 114 None -61 11 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human H2 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H2 receptor expressed in 293-EBNA cells by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0603318
DB05381 1893 114 None -61 11 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human H2 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H2 receptor expressed in 293-EBNA cells by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0603318
164610289 184540 0 None - 1 Guinea pig 7.2 pEC50 = 7.2 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 438 7 4 4 3.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NC(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4856602 184540 0 None - 1 Guinea pig 7.2 pEC50 = 7.2 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 438 7 4 4 3.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NC(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2021.113190
11956130 185373 0 None - 1 Guinea pig 7.2 pEC50 = 7.2 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 319 7 4 3 2.6 CC(CC(=O)NC(=N)NCCCc1c[nH]cn1)C1CCCCC1 10.1021/jm800841w
CHEMBL486965 185373 0 None - 1 Guinea pig 7.2 pEC50 = 7.2 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 319 7 4 3 2.6 CC(CC(=O)NC(=N)NCCCc1c[nH]cn1)C1CCCCC1 10.1021/jm800841w
CHEMBL5076746 213739 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(N)(=O)=O)c3ccccc3C2(C)C)c2cc(S(=O)(=O)[O-])ccc2C1(C)C 10.1016/j.bmcl.2021.128388
CHEMBL5095519 213739 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(N)(=O)=O)c3ccccc3C2(C)C)c2cc(S(=O)(=O)[O-])ccc2C1(C)C 10.1016/j.bmcl.2021.128388
CHEMBL5088914 213776 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C 10.1016/j.bmcl.2021.128388
CHEMBL5095949 213776 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C 10.1016/j.bmcl.2021.128388
46887079 8409 0 None -2 4 Guinea pig 7.2 pEC50 = 7.2 Functional
Agonist activity at histamine H2 receptor in spontaneously beating guinea pig atriumAgonist activity at histamine H2 receptor in spontaneously beating guinea pig atrium
ChEMBL 365 7 4 5 3.2 Cc1nc(N)sc1CCCNC(=N)NC(=O)CC(C)C1CCCCC1 10.1016/j.bmcl.2010.03.082
CHEMBL1094142 8409 0 None -2 4 Guinea pig 7.2 pEC50 = 7.2 Functional
Agonist activity at histamine H2 receptor in spontaneously beating guinea pig atriumAgonist activity at histamine H2 receptor in spontaneously beating guinea pig atrium
ChEMBL 365 7 4 5 3.2 Cc1nc(N)sc1CCCNC(=N)NC(=O)CC(C)C1CCCCC1 10.1016/j.bmcl.2010.03.082
CHEMBL5085542 213189 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCC[n+]1c(C)cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc1C 10.1016/j.bmcl.2021.128388
1204 1893 114 None -14 11 Guinea pig 6.2 pEC50 = 6.2 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2021.113190
1247 1893 114 None -14 11 Guinea pig 6.2 pEC50 = 6.2 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2021.113190
1375 1893 114 None -14 11 Guinea pig 6.2 pEC50 = 6.2 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2021.113190
774 1893 114 None -14 11 Guinea pig 6.2 pEC50 = 6.2 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2021.113190
CHEMBL90 1893 114 None -14 11 Guinea pig 6.2 pEC50 = 6.2 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2021.113190
DB05381 1893 114 None -14 11 Guinea pig 6.2 pEC50 = 6.2 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2021.113190
1204 1893 114 None -14 11 Guinea pig 6.2 pEC50 = 6.2 Functional
Agonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beatAgonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beat
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
1247 1893 114 None -14 11 Guinea pig 6.2 pEC50 = 6.2 Functional
Agonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beatAgonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beat
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
1375 1893 114 None -14 11 Guinea pig 6.2 pEC50 = 6.2 Functional
Agonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beatAgonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beat
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
774 1893 114 None -14 11 Guinea pig 6.2 pEC50 = 6.2 Functional
Agonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beatAgonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beat
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
CHEMBL90 1893 114 None -14 11 Guinea pig 6.2 pEC50 = 6.2 Functional
Agonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beatAgonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beat
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
DB05381 1893 114 None -14 11 Guinea pig 6.2 pEC50 = 6.2 Functional
Agonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beatAgonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beat
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
CHEMBL5092102 213562 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitment
ChEMBL None None None NCCCCCCCCNC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1016/j.bmcl.2021.128388
46887079 8409 0 None -2 4 Guinea pig 8.1 pEC50 = 8.1 Functional
Agonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay
ChEMBL 365 7 4 5 3.2 Cc1nc(N)sc1CCCNC(=N)NC(=O)CC(C)C1CCCCC1 10.1016/j.bmcl.2010.03.082
CHEMBL1094142 8409 0 None -2 4 Guinea pig 8.1 pEC50 = 8.1 Functional
Agonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay
ChEMBL 365 7 4 5 3.2 Cc1nc(N)sc1CCCNC(=N)NC(=O)CC(C)C1CCCCC1 10.1016/j.bmcl.2010.03.082
164609729 184505 0 None 2 4 Guinea pig 8.1 pEC50 = 8.1 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 360 6 4 4 2.3 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)N[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4856059 184505 0 None 2 4 Guinea pig 8.1 pEC50 = 8.1 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 360 6 4 4 2.3 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)N[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL5094083 213682 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitment
ChEMBL None None None C=C(/N=C(\C)NCCCc1nnc(N)s1)NCCCCCCCCN 10.1016/j.bmcl.2021.128388
56954515 81639 0 None -14 4 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 546 17 6 6 2.3 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm201128q
CHEMBL2165628 81639 0 None -14 4 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 546 17 6 6 2.3 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm201128q
46887043 8660 0 None -3 5 Guinea pig 8.1 pEC50 = 8.1 Functional
Agonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay
ChEMBL 319 7 4 3 2.6 C[C@@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)C1CCCCC1 10.1016/j.bmcl.2010.03.082
CHEMBL1096431 8660 0 None -3 5 Guinea pig 8.1 pEC50 = 8.1 Functional
Agonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay
ChEMBL 319 7 4 3 2.6 C[C@@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)C1CCCCC1 10.1016/j.bmcl.2010.03.082
46887078 8901 0 None 1 2 Guinea pig 8.1 pEC50 = 8.1 Functional
Agonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay
ChEMBL 359 7 4 5 2.8 Cc1nc(N)sc1CCCNC(=N)NC(=O)C[C@H](C)c1ccccc1 10.1016/j.bmcl.2010.03.082
CHEMBL1098442 8901 0 None 1 2 Guinea pig 8.1 pEC50 = 8.1 Functional
Agonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay
ChEMBL 359 7 4 5 2.8 Cc1nc(N)sc1CCCNC(=N)NC(=O)C[C@H](C)c1ccccc1 10.1016/j.bmcl.2010.03.082
56954000 81643 0 None -10 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 592 17 6 8 2.9 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/jm201128q
CHEMBL2165632 81643 0 None -10 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 592 17 6 8 2.9 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/jm201128q
CHEMBL5078202 213750 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1 10.1016/j.bmcl.2021.128388
CHEMBL5095695 213750 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1 10.1016/j.bmcl.2021.128388
164621681 184988 0 None - 1 Guinea pig 6.1 pEC50 = 6.1 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 444 7 4 5 3.2 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(OC(F)(F)F)cc1 10.1016/j.ejmech.2021.113190
CHEMBL4863523 184988 0 None - 1 Guinea pig 6.1 pEC50 = 6.1 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 444 7 4 5 3.2 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(OC(F)(F)F)cc1 10.1016/j.ejmech.2021.113190
44480707 5671 0 None -5 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay
ChEMBL 328 8 3 4 2.2 N#C/N=C(/NCCCc1c[nH]cn1)NCCSc1ccccc1 10.1021/jm900526h
CHEMBL1078529 5671 0 None -5 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay
ChEMBL 328 8 3 4 2.2 N#C/N=C(/NCCCc1c[nH]cn1)NCCSc1ccccc1 10.1021/jm900526h
46887041 8657 0 None -3 5 Guinea pig 7.1 pEC50 = 7.1 Functional
Agonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay
ChEMBL 313 7 4 3 2.2 C[C@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)c1ccccc1 10.1016/j.bmcl.2010.03.082
CHEMBL1096428 8657 0 None -3 5 Guinea pig 7.1 pEC50 = 7.1 Functional
Agonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay
ChEMBL 313 7 4 3 2.2 C[C@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)c1ccccc1 10.1016/j.bmcl.2010.03.082
168281746 192270 0 None -9 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay
ChEMBL 365 6 4 5 1.6 CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5184911 192270 0 None -9 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay
ChEMBL 365 6 4 5 1.6 CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5221974 192270 0 None -9 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay
ChEMBL 365 6 4 5 1.6 CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1 10.1021/acs.jmedchem.1c00692
155525816 170477 0 None 7 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay
ChEMBL 257 1 1 3 3.3 CC1CCCc2c(-c3ccc(F)cc3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
CHEMBL4456972 170477 0 None 7 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay
ChEMBL 257 1 1 3 3.3 CC1CCCc2c(-c3ccc(F)cc3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
CHEMBL5077939 213755 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)O)c3ccccc3C2(C)C)c2cc(S(=O)(=O)[O-])ccc2C1(C)C 10.1016/j.bmcl.2021.128388
CHEMBL5095769 213755 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)O)c3ccccc3C2(C)C)c2cc(S(=O)(=O)[O-])ccc2C1(C)C 10.1016/j.bmcl.2021.128388
42625221 188987 0 None -10 3 Guinea pig 7.1 pEC50 = 7.1 Functional
Agonist activity at histamine H2 receptor in guinea pig atrium assessed as increase in heart rateAgonist activity at histamine H2 receptor in guinea pig atrium assessed as increase in heart rate
ChEMBL 338 7 4 2 1.9 N/C(=N\C(=O)CCc1c[nH]c2ccccc12)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL514641 188987 0 None -10 3 Guinea pig 7.1 pEC50 = 7.1 Functional
Agonist activity at histamine H2 receptor in guinea pig atrium assessed as increase in heart rateAgonist activity at histamine H2 receptor in guinea pig atrium assessed as increase in heart rate
ChEMBL 338 7 4 2 1.9 N/C(=N\C(=O)CCc1c[nH]c2ccccc12)NCCCc1c[nH]cn1 10.1021/jm9000693
168292954 192385 0 None 7 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 388 8 4 4 2.5 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5202592 192385 0 None 7 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 388 8 4 4 2.5 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222660 192385 0 None 7 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 388 8 4 4 2.5 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
155553964 174874 0 None 11 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay
ChEMBL 273 1 1 3 3.8 CC1CCCc2c(-c3ccc(Cl)cc3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
CHEMBL4576986 174874 0 None 11 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay
ChEMBL 273 1 1 3 3.8 CC1CCCc2c(-c3ccc(Cl)cc3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
25149242 178585 0 None - 1 Guinea pig 6.1 pEC50 = 6.1 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 531 8 4 3 4.7 N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccc(Br)cc1)c1ccc(Br)cc1 10.1021/jm800841w
CHEMBL472271 178585 0 None - 1 Guinea pig 6.1 pEC50 = 6.1 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 531 8 4 3 4.7 N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccc(Br)cc1)c1ccc(Br)cc1 10.1021/jm800841w
46830167 8658 0 None -42 5 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay
ChEMBL 313 7 4 3 2.2 C[C@@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)c1ccccc1 10.1016/j.bmcl.2010.03.082
CHEMBL1096429 8658 0 None -42 5 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay
ChEMBL 313 7 4 3 2.2 C[C@@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)c1ccccc1 10.1016/j.bmcl.2010.03.082
25149521 178464 0 None -9 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assay
ChEMBL 375 8 4 3 3.2 N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2010.10.041
CHEMBL471413 178464 0 None -9 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assay
ChEMBL 375 8 4 3 3.2 N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2010.10.041
56954127 81646 0 None - 1 Guinea pig 5.1 pEC50 = 5.1 Functional
Agonist activity at H2R in spontaneously beating guinea pig right atrium assessed as increase in heart rateAgonist activity at H2R in spontaneously beating guinea pig right atrium assessed as increase in heart rate
ChEMBL 760 29 6 8 7.6 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCCCCCCCCCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/jm201128q
CHEMBL2165635 81646 0 None - 1 Guinea pig 5.1 pEC50 = 5.1 Functional
Agonist activity at H2R in spontaneously beating guinea pig right atrium assessed as increase in heart rateAgonist activity at H2R in spontaneously beating guinea pig right atrium assessed as increase in heart rate
ChEMBL 760 29 6 8 7.6 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCCCCCCCCCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/jm201128q
168281746 192270 0 None -9 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 365 6 4 5 1.6 CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5184911 192270 0 None -9 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 365 6 4 5 1.6 CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5221974 192270 0 None -9 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL 365 6 4 5 1.6 CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1 10.1021/acs.jmedchem.1c00692
155525816 170477 0 None 7 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay
ChEMBL 257 1 1 3 3.3 CC1CCCc2c(-c3ccc(F)cc3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
CHEMBL4456972 170477 0 None 7 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay
ChEMBL 257 1 1 3 3.3 CC1CCCc2c(-c3ccc(F)cc3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
155553964 174874 0 None 11 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay
ChEMBL 273 1 1 3 3.8 CC1CCCc2c(-c3ccc(Cl)cc3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
CHEMBL4576986 174874 0 None 11 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay
ChEMBL 273 1 1 3 3.8 CC1CCCc2c(-c3ccc(Cl)cc3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
42625384 169195 0 None -223 5 Guinea pig 6.1 pEC50 = 6.1 Functional
Agonist activity at histamine H2 receptor in guinea pig atrium assessed as increase in heart rateAgonist activity at histamine H2 receptor in guinea pig atrium assessed as increase in heart rate
ChEMBL 209 4 3 2 -0.2 CC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL443896 169195 0 None -223 5 Guinea pig 6.1 pEC50 = 6.1 Functional
Agonist activity at histamine H2 receptor in guinea pig atrium assessed as increase in heart rateAgonist activity at histamine H2 receptor in guinea pig atrium assessed as increase in heart rate
ChEMBL 209 4 3 2 -0.2 CC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
155565842 175033 0 None -5 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay
ChEMBL 317 1 1 3 3.9 CC1CCCc2c(-c3cccc(Br)c3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
CHEMBL4580450 175033 0 None -5 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay
ChEMBL 317 1 1 3 3.9 CC1CCCc2c(-c3cccc(Br)c3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
164614549 184350 0 None -3 4 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 340 9 4 4 2.2 CCCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1016/j.ejmech.2021.113190
CHEMBL4853668 184350 0 None -3 4 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 340 9 4 4 2.2 CCCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1016/j.ejmech.2021.113190
59868 93707 56 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 211 3 2 4 1.6 CCCN[C@@H]1CCc2nc(N)sc2C1 10.1016/j.ejmech.2021.113190
CHEMBL249420 93707 56 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 211 3 2 4 1.6 CCCN[C@@H]1CCc2nc(N)sc2C1 10.1016/j.ejmech.2021.113190
155532722 171209 0 None 3 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay
ChEMBL 253 1 1 3 3.5 Cc1ccc(-c2nc(N)nc3c2CCCC3C)cc1 10.1021/acs.jmedchem.9b00241
CHEMBL4467878 171209 0 None 3 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay
ChEMBL 253 1 1 3 3.5 Cc1ccc(-c2nc(N)nc3c2CCCC3C)cc1 10.1021/acs.jmedchem.9b00241
164616851 184357 0 None 1 4 Guinea pig 7.1 pEC50 = 7.1 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 376 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)N[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4853772 184357 0 None 1 4 Guinea pig 7.1 pEC50 = 7.1 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 376 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)N[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL5090859 213499 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCCC[n+]1c(C)cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc1C 10.1016/j.bmcl.2021.128388
155532722 171209 0 None 3 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay
ChEMBL 253 1 1 3 3.5 Cc1ccc(-c2nc(N)nc3c2CCCC3C)cc1 10.1021/acs.jmedchem.9b00241
CHEMBL4467878 171209 0 None 3 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay
ChEMBL 253 1 1 3 3.5 Cc1ccc(-c2nc(N)nc3c2CCCC3C)cc1 10.1021/acs.jmedchem.9b00241
44481758 5623 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay
ChEMBL 324 9 3 3 2.4 N#C/N=C(\NCCCCc1ccccc1)NCCCc1c[nH]cn1 10.1021/jm900526h
CHEMBL1078212 5623 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay
ChEMBL 324 9 3 3 2.4 N#C/N=C(\NCCCCc1ccccc1)NCCCc1c[nH]cn1 10.1021/jm900526h
46887079 8409 0 None 2 4 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay
ChEMBL 365 7 4 5 3.2 Cc1nc(N)sc1CCCNC(=N)NC(=O)CC(C)C1CCCCC1 10.1016/j.bmcl.2010.03.082
CHEMBL1094142 8409 0 None 2 4 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay
ChEMBL 365 7 4 5 3.2 Cc1nc(N)sc1CCCNC(=N)NC(=O)CC(C)C1CCCCC1 10.1016/j.bmcl.2010.03.082
164609493 183844 0 None 10 4 Guinea pig 8.0 pEC50 = 8.0 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 350 6 4 5 1.9 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccco1 10.1016/j.ejmech.2021.113190
CHEMBL4846380 183844 0 None 10 4 Guinea pig 8.0 pEC50 = 8.0 Functional
Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidineAgonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine
ChEMBL 350 6 4 5 1.9 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccco1 10.1016/j.ejmech.2021.113190
1221 472 9 None - 1 Guinea pig 8.0 pEC50 = 8.0 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 380 9 3 3 3.0 NC(=NCCCc1[nH]cnc1)NCCC(c1ccccn1)c1ccc(cc1)F 10.1021/jm800841w
65895 472 9 None - 1 Guinea pig 8.0 pEC50 = 8.0 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 380 9 3 3 3.0 NC(=NCCCc1[nH]cnc1)NCCC(c1ccccn1)c1ccc(cc1)F 10.1021/jm800841w
CHEMBL293802 472 9 None - 1 Guinea pig 8.0 pEC50 = 8.0 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 380 9 3 3 3.0 NC(=NCCCc1[nH]cnc1)NCCC(c1ccccn1)c1ccc(cc1)F 10.1021/jm800841w
44414337 79714 0 None 1 2 Guinea pig 7.1 pEC50 = 7.1 Functional
Agonist activity at guinea pig H2RAgonist activity at guinea pig H2R
ChEMBL 945 24 3 9 8.3 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCC/N=C(\NC#N)NCCCOc3cccc(CN4CCCCC4)c3)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1016/j.bmcl.2006.05.039
CHEMBL213357 79714 0 None 1 2 Guinea pig 7.1 pEC50 = 7.1 Functional
Agonist activity at guinea pig H2RAgonist activity at guinea pig H2R
ChEMBL 945 24 3 9 8.3 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCC/N=C(\NC#N)NCCCOc3cccc(CN4CCCCC4)c3)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1016/j.bmcl.2006.05.039
46887115 8411 0 None -1 4 Guinea pig 7.0 pEC50 = 7.0 Functional
Agonist activity at histamine H2 receptor in spontaneously beating guinea pig atriumAgonist activity at histamine H2 receptor in spontaneously beating guinea pig atrium
ChEMBL 365 7 4 5 3.2 Cc1nc(N)sc1CCCNC(=N)NC(=O)C[C@H](C)C1CCCCC1 10.1016/j.bmcl.2010.03.082
CHEMBL1094144 8411 0 None -1 4 Guinea pig 7.0 pEC50 = 7.0 Functional
Agonist activity at histamine H2 receptor in spontaneously beating guinea pig atriumAgonist activity at histamine H2 receptor in spontaneously beating guinea pig atrium
ChEMBL 365 7 4 5 3.2 Cc1nc(N)sc1CCCNC(=N)NC(=O)C[C@H](C)C1CCCCC1 10.1016/j.bmcl.2010.03.082
46887041 8657 0 None -3 5 Guinea pig 7.0 pEC50 = 7.0 Functional
Agonist activity at histamine H2 receptor in spontaneously beating guinea pig atriumAgonist activity at histamine H2 receptor in spontaneously beating guinea pig atrium
ChEMBL 313 7 4 3 2.2 C[C@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)c1ccccc1 10.1016/j.bmcl.2010.03.082
CHEMBL1096428 8657 0 None -3 5 Guinea pig 7.0 pEC50 = 7.0 Functional
Agonist activity at histamine H2 receptor in spontaneously beating guinea pig atriumAgonist activity at histamine H2 receptor in spontaneously beating guinea pig atrium
ChEMBL 313 7 4 3 2.2 C[C@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)c1ccccc1 10.1016/j.bmcl.2010.03.082
56954229 81649 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 648 23 6 8 4.7 N/C(=N\C(=O)CCCCCCCCCCCCCCC(=O)/N=C(\N)NCCCc1cnc(N)s1)NCCCc1cnc(N)s1 10.1021/jm201128q
CHEMBL2165638 81649 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
ChEMBL 648 23 6 8 4.7 N/C(=N\C(=O)CCCCCCCCCCCCCCC(=O)/N=C(\N)NCCCc1cnc(N)s1)NCCCc1cnc(N)s1 10.1021/jm201128q
CHEMBL5094083 213682 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay
ChEMBL None None None C=C(/N=C(\C)NCCCc1nnc(N)s1)NCCCCCCCCN 10.1016/j.bmcl.2021.128388
168268853 192173 0 None 1 2 Guinea pig 7.0 pEC50 = 7.0 Functional
Agonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beatAgonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beat
ChEMBL 389 8 4 5 1.9 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5180504 192173 0 None 1 2 Guinea pig 7.0 pEC50 = 7.0 Functional
Agonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beatAgonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beat
ChEMBL 389 8 4 5 1.9 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5221353 192173 0 None 1 2 Guinea pig 7.0 pEC50 = 7.0 Functional
Agonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beatAgonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beat
ChEMBL 389 8 4 5 1.9 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
155559319 174281 0 None 13 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay
ChEMBL 239 1 1 3 3.2 CC1CCCc2c(-c3ccccc3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
CHEMBL4563363 174281 0 None 13 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay
ChEMBL 239 1 1 3 3.2 CC1CCCc2c(-c3ccccc3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
1198 3887 1 None - 1 Guinea pig 7.0 pEC50 = 7.0 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 401 8 4 4 2.0 O=C(CC(c1ccc(c(c1)F)F)c1ncc[nH]1)NC(=NCCCc1cnc[nH]1)N 10.1021/jm800841w
25149704 3887 1 None - 1 Guinea pig 7.0 pEC50 = 7.0 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 401 8 4 4 2.0 O=C(CC(c1ccc(c(c1)F)F)c1ncc[nH]1)NC(=NCCCc1cnc[nH]1)N 10.1021/jm800841w
CHEMBL470563 3887 1 None - 1 Guinea pig 7.0 pEC50 = 7.0 Functional
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityAgonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
ChEMBL 401 8 4 4 2.0 O=C(CC(c1ccc(c(c1)F)F)c1ncc[nH]1)NC(=NCCCc1cnc[nH]1)N 10.1021/jm800841w
1204 1893 114 None -61 11 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2021.113190
1247 1893 114 None -61 11 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2021.113190
1375 1893 114 None -61 11 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2021.113190
774 1893 114 None -61 11 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2021.113190
CHEMBL90 1893 114 None -61 11 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2021.113190
DB05381 1893 114 None -61 11 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2021.113190
10446940 13764 6 None - 1 Guinea pig 5.9 pIC50 = 5.9 Functional
Compound was tested for H2 receptor antagonistic activity against histamine stimulated chronotropic response in isolated guinea pig right atriumCompound was tested for H2 receptor antagonistic activity against histamine stimulated chronotropic response in isolated guinea pig right atrium
ChEMBL 290 4 3 5 0.7 CC(=O)NCc1cccc(-c2csc(N=C(N)N)n2)n1 10.1021/jm00027a007
CHEMBL1196182 13764 6 None - 1 Guinea pig 5.9 pIC50 = 5.9 Functional
Compound was tested for H2 receptor antagonistic activity against histamine stimulated chronotropic response in isolated guinea pig right atriumCompound was tested for H2 receptor antagonistic activity against histamine stimulated chronotropic response in isolated guinea pig right atrium
ChEMBL 290 4 3 5 0.7 CC(=O)NCc1cccc(-c2csc(N=C(N)N)n2)n1 10.1021/jm00027a007
CHEMBL556048 13764 6 None - 1 Guinea pig 5.9 pIC50 = 5.9 Functional
Compound was tested for H2 receptor antagonistic activity against histamine stimulated chronotropic response in isolated guinea pig right atriumCompound was tested for H2 receptor antagonistic activity against histamine stimulated chronotropic response in isolated guinea pig right atrium
ChEMBL 290 4 3 5 0.7 CC(=O)NCc1cccc(-c2csc(N=C(N)N)n2)n1 10.1021/jm00027a007
3158 55959 21 None -2754 21 Guinea pig 5.8 pIC50 = 5.8 Functional
Inhibitory activity against brain adenylate cyclase Histamine H2 receptorInhibitory activity against brain adenylate cyclase Histamine H2 receptor
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1021/jm9910369
CHEMBL1628227 55959 21 None -2754 21 Guinea pig 5.8 pIC50 = 5.8 Functional
Inhibitory activity against brain adenylate cyclase Histamine H2 receptorInhibitory activity against brain adenylate cyclase Histamine H2 receptor
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1021/jm9910369
1427 1974 50 None -2454 11 Guinea pig 5.7 pIC50 = 5.7 Functional
Inhibitory activity against brain adenylate cyclase Histamine H2 receptorInhibitory activity against brain adenylate cyclase Histamine H2 receptor
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1021/jm9910369
357 1974 50 None -2454 11 Guinea pig 5.7 pIC50 = 5.7 Functional
Inhibitory activity against brain adenylate cyclase Histamine H2 receptorInhibitory activity against brain adenylate cyclase Histamine H2 receptor
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1021/jm9910369
3696 1974 50 None -2454 11 Guinea pig 5.7 pIC50 = 5.7 Functional
Inhibitory activity against brain adenylate cyclase Histamine H2 receptorInhibitory activity against brain adenylate cyclase Histamine H2 receptor
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1021/jm9910369
CHEMBL11 1974 50 None -2454 11 Guinea pig 5.7 pIC50 = 5.7 Functional
Inhibitory activity against brain adenylate cyclase Histamine H2 receptorInhibitory activity against brain adenylate cyclase Histamine H2 receptor
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1021/jm9910369
DB00458 1974 50 None -2454 11 Guinea pig 5.7 pIC50 = 5.7 Functional
Inhibitory activity against brain adenylate cyclase Histamine H2 receptorInhibitory activity against brain adenylate cyclase Histamine H2 receptor
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1021/jm9910369
13048194 26754 0 None - 1 Guinea pig 4.7 pIC50 = 4.7 Functional
In vitro antihistamine activity by activation of 4-methylhistamine mediated by Histamine H2 receptorIn vitro antihistamine activity by activation of 4-methylhistamine mediated by Histamine H2 receptor
ChEMBL 270 0 0 3 3.1 CN1CCN2c3ccccc3Cc3ccsc3C2C1 10.1021/jm00362a006
CHEMBL13645 26754 0 None - 1 Guinea pig 4.7 pIC50 = 4.7 Functional
In vitro antihistamine activity by activation of 4-methylhistamine mediated by Histamine H2 receptorIn vitro antihistamine activity by activation of 4-methylhistamine mediated by Histamine H2 receptor
ChEMBL 270 0 0 3 3.1 CN1CCN2c3ccccc3Cc3ccsc3C2C1 10.1021/jm00362a006
1129 1584 89 None -7 3 Guinea pig 6.5 pIC50 = 6.5 Functional
Compound was tested for H2 receptor antagonistic activity against histamine stimulated chronotropic response in isolated guinea pig right atriumCompound was tested for H2 receptor antagonistic activity against histamine stimulated chronotropic response in isolated guinea pig right atrium
ChEMBL 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N 10.1021/jm00027a007
3325 1584 89 None -7 3 Guinea pig 6.5 pIC50 = 6.5 Functional
Compound was tested for H2 receptor antagonistic activity against histamine stimulated chronotropic response in isolated guinea pig right atriumCompound was tested for H2 receptor antagonistic activity against histamine stimulated chronotropic response in isolated guinea pig right atrium
ChEMBL 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N 10.1021/jm00027a007
5353622 1584 89 None -7 3 Guinea pig 6.5 pIC50 = 6.5 Functional
Compound was tested for H2 receptor antagonistic activity against histamine stimulated chronotropic response in isolated guinea pig right atriumCompound was tested for H2 receptor antagonistic activity against histamine stimulated chronotropic response in isolated guinea pig right atrium
ChEMBL 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N 10.1021/jm00027a007
5702160 1584 89 None -7 3 Guinea pig 6.5 pIC50 = 6.5 Functional
Compound was tested for H2 receptor antagonistic activity against histamine stimulated chronotropic response in isolated guinea pig right atriumCompound was tested for H2 receptor antagonistic activity against histamine stimulated chronotropic response in isolated guinea pig right atrium
ChEMBL 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N 10.1021/jm00027a007
7074 1584 89 None -7 3 Guinea pig 6.5 pIC50 = 6.5 Functional
Compound was tested for H2 receptor antagonistic activity against histamine stimulated chronotropic response in isolated guinea pig right atriumCompound was tested for H2 receptor antagonistic activity against histamine stimulated chronotropic response in isolated guinea pig right atrium
ChEMBL 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N 10.1021/jm00027a007
CHEMBL902 1584 89 None -7 3 Guinea pig 6.5 pIC50 = 6.5 Functional
Compound was tested for H2 receptor antagonistic activity against histamine stimulated chronotropic response in isolated guinea pig right atriumCompound was tested for H2 receptor antagonistic activity against histamine stimulated chronotropic response in isolated guinea pig right atrium
ChEMBL 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N 10.1021/jm00027a007
DB00927 1584 89 None -7 3 Guinea pig 6.5 pIC50 = 6.5 Functional
Compound was tested for H2 receptor antagonistic activity against histamine stimulated chronotropic response in isolated guinea pig right atriumCompound was tested for H2 receptor antagonistic activity against histamine stimulated chronotropic response in isolated guinea pig right atrium
ChEMBL 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N 10.1021/jm00027a007
5039 62838 13 None 2 3 Guinea pig 5.5 pIC50 = 5.5 Functional
Compound was tested for H2 receptor antagonistic activity against histamine stimulated chronotropic response in isolated guinea pig right atriumCompound was tested for H2 receptor antagonistic activity against histamine stimulated chronotropic response in isolated guinea pig right atrium
ChEMBL 314 10 2 7 1.5 CNC(=C[N+](=O)[O-])NCCSCc1ccc(CN(C)C)o1 10.1021/jm00027a007
CHEMBL1790041 62838 13 None 2 3 Guinea pig 5.5 pIC50 = 5.5 Functional
Compound was tested for H2 receptor antagonistic activity against histamine stimulated chronotropic response in isolated guinea pig right atriumCompound was tested for H2 receptor antagonistic activity against histamine stimulated chronotropic response in isolated guinea pig right atrium
ChEMBL 314 10 2 7 1.5 CNC(=C[N+](=O)[O-])NCCSCc1ccc(CN(C)C)o1 10.1021/jm00027a007
135 2486 38 None -794 31 Guinea pig 5.4 pIC50 = 5.4 Functional
In vitro antihistamine activity by activation of 4-methylhistamine mediated by Histamine H2 receptorIn vitro antihistamine activity by activation of 4-methylhistamine mediated by Histamine H2 receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm00362a006
1796 2486 38 None -794 31 Guinea pig 5.4 pIC50 = 5.4 Functional
In vitro antihistamine activity by activation of 4-methylhistamine mediated by Histamine H2 receptorIn vitro antihistamine activity by activation of 4-methylhistamine mediated by Histamine H2 receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm00362a006
4184 2486 38 None -794 31 Guinea pig 5.4 pIC50 = 5.4 Functional
In vitro antihistamine activity by activation of 4-methylhistamine mediated by Histamine H2 receptorIn vitro antihistamine activity by activation of 4-methylhistamine mediated by Histamine H2 receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm00362a006
CHEMBL6437 2486 38 None -794 31 Guinea pig 5.4 pIC50 = 5.4 Functional
In vitro antihistamine activity by activation of 4-methylhistamine mediated by Histamine H2 receptorIn vitro antihistamine activity by activation of 4-methylhistamine mediated by Histamine H2 receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm00362a006
DB06148 2486 38 None -794 31 Guinea pig 5.4 pIC50 = 5.4 Functional
In vitro antihistamine activity by activation of 4-methylhistamine mediated by Histamine H2 receptorIn vitro antihistamine activity by activation of 4-methylhistamine mediated by Histamine H2 receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm00362a006
2995 202690 49 None -1412 7 Guinea pig 5.4 pIC50 = 5.4 Functional
Inhibitory activity against brain adenylate cyclase Histamine H2 receptorInhibitory activity against brain adenylate cyclase Histamine H2 receptor
ChEMBL 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 10.1021/jm9910369
CHEMBL1696 202690 49 None -1412 7 Guinea pig 5.4 pIC50 = 5.4 Functional
Inhibitory activity against brain adenylate cyclase Histamine H2 receptorInhibitory activity against brain adenylate cyclase Histamine H2 receptor
ChEMBL 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 10.1021/jm9910369
CHEMBL72 202690 49 None -1412 7 Guinea pig 5.4 pIC50 = 5.4 Functional
Inhibitory activity against brain adenylate cyclase Histamine H2 receptorInhibitory activity against brain adenylate cyclase Histamine H2 receptor
ChEMBL 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 10.1021/jm9910369
180 397 50 None -1412 27 Guinea pig 6.2 pIC50 = 6.2 Functional
Inhibitory activity against brain adenylate cyclase Histamine H2 receptorInhibitory activity against brain adenylate cyclase Histamine H2 receptor
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1021/jm9910369
200 397 50 None -1412 27 Guinea pig 6.2 pIC50 = 6.2 Functional
Inhibitory activity against brain adenylate cyclase Histamine H2 receptorInhibitory activity against brain adenylate cyclase Histamine H2 receptor
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1021/jm9910369
2160 397 50 None -1412 27 Guinea pig 6.2 pIC50 = 6.2 Functional
Inhibitory activity against brain adenylate cyclase Histamine H2 receptorInhibitory activity against brain adenylate cyclase Histamine H2 receptor
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1021/jm9910369
CHEMBL629 397 50 None -1412 27 Guinea pig 6.2 pIC50 = 6.2 Functional
Inhibitory activity against brain adenylate cyclase Histamine H2 receptorInhibitory activity against brain adenylate cyclase Histamine H2 receptor
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1021/jm9910369
DB00321 397 50 None -1412 27 Guinea pig 6.2 pIC50 = 6.2 Functional
Inhibitory activity against brain adenylate cyclase Histamine H2 receptorInhibitory activity against brain adenylate cyclase Histamine H2 receptor
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1021/jm9910369
4543 169972 36 None -9549 26 Guinea pig 5.2 pIC50 = 5.2 Functional
Inhibitory activity against brain adenylate cyclase Histamine H2 receptorInhibitory activity against brain adenylate cyclase Histamine H2 receptor
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 10.1021/jm9910369
CHEMBL1201156 169972 36 None -9549 26 Guinea pig 5.2 pIC50 = 5.2 Functional
Inhibitory activity against brain adenylate cyclase Histamine H2 receptorInhibitory activity against brain adenylate cyclase Histamine H2 receptor
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 10.1021/jm9910369
CHEMBL445 169972 36 None -9549 26 Guinea pig 5.2 pIC50 = 5.2 Functional
Inhibitory activity against brain adenylate cyclase Histamine H2 receptorInhibitory activity against brain adenylate cyclase Histamine H2 receptor
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 10.1021/jm9910369
2801 161313 56 None -524 25 Guinea pig 6.1 pIC50 = 6.1 Functional
Inhibitory activity against brain adenylate cyclase Histamine H2 receptorInhibitory activity against brain adenylate cyclase Histamine H2 receptor
ChEMBL 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 10.1021/jm9910369
CHEMBL1200710 161313 56 None -524 25 Guinea pig 6.1 pIC50 = 6.1 Functional
Inhibitory activity against brain adenylate cyclase Histamine H2 receptorInhibitory activity against brain adenylate cyclase Histamine H2 receptor
ChEMBL 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 10.1021/jm9910369
CHEMBL415 161313 56 None -524 25 Guinea pig 6.1 pIC50 = 6.1 Functional
Inhibitory activity against brain adenylate cyclase Histamine H2 receptorInhibitory activity against brain adenylate cyclase Histamine H2 receptor
ChEMBL 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 10.1021/jm9910369
13048195 26744 0 None - 1 Guinea pig 5.1 pIC50 = 5.1 Functional
In vitro antihistamine activity by activation of 4-methylhistamine mediated by Histamine H2 receptorIn vitro antihistamine activity by activation of 4-methylhistamine mediated by Histamine H2 receptor
ChEMBL 270 0 0 3 3.1 CN1CCN2c3ccccc3Cc3sccc3C2C1 10.1021/jm00362a006
CHEMBL13644 26744 0 None - 1 Guinea pig 5.1 pIC50 = 5.1 Functional
In vitro antihistamine activity by activation of 4-methylhistamine mediated by Histamine H2 receptorIn vitro antihistamine activity by activation of 4-methylhistamine mediated by Histamine H2 receptor
ChEMBL 270 0 0 3 3.1 CN1CCN2c3ccccc3Cc3sccc3C2C1 10.1021/jm00362a006
135 2486 38 None -794 31 Guinea pig 6.1 pIC50 = 6.1 Functional
Inhibitory activity against brain adenylate cyclase Histamine H2 receptorInhibitory activity against brain adenylate cyclase Histamine H2 receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm9910369
1796 2486 38 None -794 31 Guinea pig 6.1 pIC50 = 6.1 Functional
Inhibitory activity against brain adenylate cyclase Histamine H2 receptorInhibitory activity against brain adenylate cyclase Histamine H2 receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm9910369
4184 2486 38 None -794 31 Guinea pig 6.1 pIC50 = 6.1 Functional
Inhibitory activity against brain adenylate cyclase Histamine H2 receptorInhibitory activity against brain adenylate cyclase Histamine H2 receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm9910369
CHEMBL6437 2486 38 None -794 31 Guinea pig 6.1 pIC50 = 6.1 Functional
Inhibitory activity against brain adenylate cyclase Histamine H2 receptorInhibitory activity against brain adenylate cyclase Histamine H2 receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm9910369
DB06148 2486 38 None -794 31 Guinea pig 6.1 pIC50 = 6.1 Functional
Inhibitory activity against brain adenylate cyclase Histamine H2 receptorInhibitory activity against brain adenylate cyclase Histamine H2 receptor
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm9910369
10416230 174697 0 None - 0 Guinea pig 8.0 pKd = 8.0 Functional
Histamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atriumHistamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atrium
ChEMBL 605 18 3 10 5.4 N#CN/C(=N\CCCCCCCCNc1ccc([N+](=O)[O-])c2nonc12)NCCCOc1cccc(CN2CCCCC2)c1 10.1016/s0960-894x(03)00235-x
CHEMBL45728 174697 0 None - 0 Guinea pig 8.0 pKd = 8.0 Functional
Histamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atriumHistamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atrium
ChEMBL 605 18 3 10 5.4 N#CN/C(=N\CCCCCCCCNc1ccc([N+](=O)[O-])c2nonc12)NCCCOc1cccc(CN2CCCCC2)c1 10.1016/s0960-894x(03)00235-x
44281005 116218 0 None - 3 Rat 6.0 pKd = 6 Functional
Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.
ChEMBL 787 17 4 8 6.4 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CCOC(=O)NCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1 10.1016/S0960-894X(96)00249-1
CHEMBL33743 116218 0 None - 3 Rat 6.0 pKd = 6 Functional
Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.
ChEMBL 787 17 4 8 6.4 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CCOC(=O)NCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1 10.1016/S0960-894X(96)00249-1
CHEMBL432671 167521 0 None - 3 Rat 6.0 pKd = 6 Functional
Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.
ChEMBL 784 15 7 12 3.1 CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCNC(=O)CC(=O)NCCSCc3csc(C=C(N)N)n3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
44280028 98707 0 None - 3 Rat 6.0 pKd = 6 Functional
Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats
ChEMBL 768 17 6 9 4.3 CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCCCCC(=O)NCCSCc3csc(N=C(N)N)n3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00248-X
CHEMBL281318 98707 0 None - 3 Rat 6.0 pKd = 6 Functional
Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats
ChEMBL 768 17 6 9 4.3 CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCCCCC(=O)NCCSCc3csc(N=C(N)N)n3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00248-X
9896825 102491 0 None - 3 Rat 6.0 pKd = 6 Functional
Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats
ChEMBL 742 14 6 10 2.9 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCC(=O)NCCSCc4csc(N=C(N)N)n4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL30656 102491 0 None - 3 Rat 6.0 pKd = 6 Functional
Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats
ChEMBL 742 14 6 10 2.9 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCC(=O)NCCSCc4csc(N=C(N)N)n4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
1231 922 112 None -11 4 Guinea pig 6.0 pKd = 6 Functional
Histamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atriumHistamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atrium
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/s0960-894x(03)00235-x
2756 922 112 None -11 4 Guinea pig 6.0 pKd = 6 Functional
Histamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atriumHistamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atrium
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/s0960-894x(03)00235-x
645 922 112 None -11 4 Guinea pig 6.0 pKd = 6 Functional
Histamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atriumHistamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atrium
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/s0960-894x(03)00235-x
CHEMBL30 922 112 None -11 4 Guinea pig 6.0 pKd = 6 Functional
Histamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atriumHistamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atrium
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/s0960-894x(03)00235-x
DB00501 922 112 None -11 4 Guinea pig 6.0 pKd = 6 Functional
Histamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atriumHistamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atrium
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/s0960-894x(03)00235-x
11413171 11989 0 None - 1 Guinea pig 5.0 pKd = 5 Functional
Functional H2 receptor antagonistic activity in vitro assay on the isolated spontaneously beating guinea-pig right atriumFunctional H2 receptor antagonistic activity in vitro assay on the isolated spontaneously beating guinea-pig right atrium
ChEMBL 210 9 1 2 2.9 CCCCCCOCCCc1c[nH]cn1 10.1021/jm031065q
CHEMBL1184057 11989 0 None - 1 Guinea pig 5.0 pKd = 5 Functional
Functional H2 receptor antagonistic activity in vitro assay on the isolated spontaneously beating guinea-pig right atriumFunctional H2 receptor antagonistic activity in vitro assay on the isolated spontaneously beating guinea-pig right atrium
ChEMBL 210 9 1 2 2.9 CCCCCCOCCCc1c[nH]cn1 10.1021/jm031065q
CHEMBL330688 11989 0 None - 1 Guinea pig 5.0 pKd = 5 Functional
Functional H2 receptor antagonistic activity in vitro assay on the isolated spontaneously beating guinea-pig right atriumFunctional H2 receptor antagonistic activity in vitro assay on the isolated spontaneously beating guinea-pig right atrium
ChEMBL 210 9 1 2 2.9 CCCCCCOCCCc1c[nH]cn1 10.1021/jm031065q
44292730 182785 0 None - 0 Guinea pig 5.0 pKd = 5 Functional
Histamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atriumHistamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atrium
ChEMBL 746 15 5 9 5.2 N#CN/C(=N\CCCCNC(=O)c1ccc(C(=O)O)c(C2c3ccc(O)cc3OC3=CC(=O)C=CC32)c1)NCCCOc1cccc(CN2CCCCC2)c1 10.1016/s0960-894x(03)00235-x
CHEMBL47979 182785 0 None - 0 Guinea pig 5.0 pKd = 5 Functional
Histamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atriumHistamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atrium
ChEMBL 746 15 5 9 5.2 N#CN/C(=N\CCCCNC(=O)c1ccc(C(=O)O)c(C2c3ccc(O)cc3OC3=CC(=O)C=CC32)c1)NCCCOc1cccc(CN2CCCCC2)c1 10.1016/s0960-894x(03)00235-x
13499385 13699 0 None - 0 Guinea pig 4.0 pKd = 4 Functional
Antagonistic activity against H2 receptor in guinea pig.Antagonistic activity against H2 receptor in guinea pig.
ChEMBL 195 5 3 2 0.3 C/N=C(\N)NCCCCc1c[nH]cn1 10.1021/jm00148a007
CHEMBL1195762 13699 0 None - 0 Guinea pig 4.0 pKd = 4 Functional
Antagonistic activity against H2 receptor in guinea pig.Antagonistic activity against H2 receptor in guinea pig.
ChEMBL 195 5 3 2 0.3 C/N=C(\N)NCCCCc1c[nH]cn1 10.1021/jm00148a007
CHEMBL555309 13699 0 None - 0 Guinea pig 4.0 pKd = 4 Functional
Antagonistic activity against H2 receptor in guinea pig.Antagonistic activity against H2 receptor in guinea pig.
ChEMBL 195 5 3 2 0.3 C/N=C(\N)NCCCCc1c[nH]cn1 10.1021/jm00148a007
15179485 186162 0 None - 0 Guinea pig 6.0 pKd = 6.0 Functional
Histamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atriumHistamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atrium
ChEMBL 358 9 3 5 1.4 N#CN/C(=N\CCN)NCCCOc1cccc(CN2CCCCC2)c1 10.1016/s0960-894x(03)00235-x
CHEMBL48885 186162 0 None - 0 Guinea pig 6.0 pKd = 6.0 Functional
Histamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atriumHistamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atrium
ChEMBL 358 9 3 5 1.4 N#CN/C(=N\CCN)NCCCOc1cccc(CN2CCCCC2)c1 10.1016/s0960-894x(03)00235-x
13499391 103300 0 None - 0 Guinea pig 5.0 pKd = 5.0 Functional
Antagonistic activity against H2 receptor in guinea pig.Antagonistic activity against H2 receptor in guinea pig.
ChEMBL 230 5 2 4 0.9 C/N=C(\N)NCCSCc1nccs1 10.1021/jm00148a007
CHEMBL1744353 103300 0 None - 0 Guinea pig 5.0 pKd = 5.0 Functional
Antagonistic activity against H2 receptor in guinea pig.Antagonistic activity against H2 receptor in guinea pig.
ChEMBL 230 5 2 4 0.9 C/N=C(\N)NCCSCc1nccs1 10.1021/jm00148a007
CHEMBL30893 103300 0 None - 0 Guinea pig 5.0 pKd = 5.0 Functional
Antagonistic activity against H2 receptor in guinea pig.Antagonistic activity against H2 receptor in guinea pig.
ChEMBL 230 5 2 4 0.9 C/N=C(\N)NCCSCc1nccs1 10.1021/jm00148a007
134179 11129 13 None - 0 Guinea pig 8.0 pKd = 8.0 Functional
Histamine H2 receptor antagonism on the right atrium of the guinea pigHistamine H2 receptor antagonism on the right atrium of the guinea pig
ChEMBL 242 3 2 2 3.3 CC(C)(C)/N=C/Nc1ccc(-c2c[nH]cn2)cc1 10.1021/jm00110a004
CHEMBL1178963 11129 13 None - 0 Guinea pig 8.0 pKd = 8.0 Functional
Histamine H2 receptor antagonism on the right atrium of the guinea pigHistamine H2 receptor antagonism on the right atrium of the guinea pig
ChEMBL 242 3 2 2 3.3 CC(C)(C)/N=C/Nc1ccc(-c2c[nH]cn2)cc1 10.1021/jm00110a004
CHEMBL51541 11129 13 None - 0 Guinea pig 8.0 pKd = 8.0 Functional
Histamine H2 receptor antagonism on the right atrium of the guinea pigHistamine H2 receptor antagonism on the right atrium of the guinea pig
ChEMBL 242 3 2 2 3.3 CC(C)(C)/N=C/Nc1ccc(-c2c[nH]cn2)cc1 10.1021/jm00110a004
20449709 12135 0 None - 0 Guinea pig 8.0 pKd = 8.0 Functional
Histamine H2 receptor antagonism on the right atrium of the guinea pigHistamine H2 receptor antagonism on the right atrium of the guinea pig
ChEMBL 242 6 2 2 3.1 CCCCN/C=N/c1ccc(-c2c[nH]cn2)cc1 10.1021/jm00110a004
CHEMBL1184647 12135 0 None - 0 Guinea pig 8.0 pKd = 8.0 Functional
Histamine H2 receptor antagonism on the right atrium of the guinea pigHistamine H2 receptor antagonism on the right atrium of the guinea pig
ChEMBL 242 6 2 2 3.1 CCCCN/C=N/c1ccc(-c2c[nH]cn2)cc1 10.1021/jm00110a004
CHEMBL362059 12135 0 None - 0 Guinea pig 8.0 pKd = 8.0 Functional
Histamine H2 receptor antagonism on the right atrium of the guinea pigHistamine H2 receptor antagonism on the right atrium of the guinea pig
ChEMBL 242 6 2 2 3.1 CCCCN/C=N/c1ccc(-c2c[nH]cn2)cc1 10.1021/jm00110a004
71263 102665 16 None - 0 Guinea pig 7.9 pKd = 7.9 Functional
Antagonistic activity of guinea pig Histamine H2 receptor expressed as pA2 at pH 7.8Antagonistic activity of guinea pig Histamine H2 receptor expressed as pA2 at pH 7.8
ChEMBL 228 4 2 2 2.9 CC(C)/N=C/Nc1ccc(-c2c[nH]cn2)cc1 10.1021/jm00384a036
CHEMBL308005 102665 16 None - 0 Guinea pig 7.9 pKd = 7.9 Functional
Antagonistic activity of guinea pig Histamine H2 receptor expressed as pA2 at pH 7.8Antagonistic activity of guinea pig Histamine H2 receptor expressed as pA2 at pH 7.8
ChEMBL 228 4 2 2 2.9 CC(C)/N=C/Nc1ccc(-c2c[nH]cn2)cc1 10.1021/jm00384a036
CHEMBL50020 102665 16 None - 0 Guinea pig 7.9 pKd = 7.9 Functional
Antagonistic activity of guinea pig Histamine H2 receptor expressed as pA2 at pH 7.8Antagonistic activity of guinea pig Histamine H2 receptor expressed as pA2 at pH 7.8
ChEMBL 228 4 2 2 2.9 CC(C)/N=C/Nc1ccc(-c2c[nH]cn2)cc1 10.1021/jm00384a036
13499361 13466 0 None - 0 Guinea pig 5.9 pKd = 5.9 Functional
Antagonistic activity against H2 receptor in guinea pig.Antagonistic activity against H2 receptor in guinea pig.
ChEMBL 335 10 4 4 1.6 Cc1[nH]cnc1CSCC/N=C(\N)NCCCCc1c[nH]cn1 10.1021/jm00148a007
CHEMBL1194112 13466 0 None - 0 Guinea pig 5.9 pKd = 5.9 Functional
Antagonistic activity against H2 receptor in guinea pig.Antagonistic activity against H2 receptor in guinea pig.
ChEMBL 335 10 4 4 1.6 Cc1[nH]cnc1CSCC/N=C(\N)NCCCCc1c[nH]cn1 10.1021/jm00148a007
CHEMBL545625 13466 0 None - 0 Guinea pig 5.9 pKd = 5.9 Functional
Antagonistic activity against H2 receptor in guinea pig.Antagonistic activity against H2 receptor in guinea pig.
ChEMBL 335 10 4 4 1.6 Cc1[nH]cnc1CSCC/N=C(\N)NCCCCc1c[nH]cn1 10.1021/jm00148a007
13499407 103654 0 None - 0 Guinea pig 5.9 pKd = 5.9 Functional
Antagonistic activity against H2 receptor in guinea pig.Antagonistic activity against H2 receptor in guinea pig.
ChEMBL 338 9 4 4 2.2 Cc1[nH]cnc1CSCC/N=C(\S)NCCCc1c[nH]cn1 10.1021/jm00148a007
CHEMBL30946 103654 0 None - 0 Guinea pig 5.9 pKd = 5.9 Functional
Antagonistic activity against H2 receptor in guinea pig.Antagonistic activity against H2 receptor in guinea pig.
ChEMBL 338 9 4 4 2.2 Cc1[nH]cnc1CSCC/N=C(\S)NCCCc1c[nH]cn1 10.1021/jm00148a007
134176 11127 11 None - 0 Guinea pig 5.9 pKd = 5.9 Functional
Histamine H2 receptor antagonism on the right atrium of the guinea pigHistamine H2 receptor antagonism on the right atrium of the guinea pig
ChEMBL 200 3 2 2 2.1 C/N=C\Nc1ccc(-c2c[nH]cn2)cc1 10.1021/jm00110a004
CHEMBL1178945 11127 11 None - 0 Guinea pig 5.9 pKd = 5.9 Functional
Histamine H2 receptor antagonism on the right atrium of the guinea pigHistamine H2 receptor antagonism on the right atrium of the guinea pig
ChEMBL 200 3 2 2 2.1 C/N=C\Nc1ccc(-c2c[nH]cn2)cc1 10.1021/jm00110a004
CHEMBL50960 11127 11 None - 0 Guinea pig 5.9 pKd = 5.9 Functional
Histamine H2 receptor antagonism on the right atrium of the guinea pigHistamine H2 receptor antagonism on the right atrium of the guinea pig
ChEMBL 200 3 2 2 2.1 C/N=C\Nc1ccc(-c2c[nH]cn2)cc1 10.1021/jm00110a004
44281078 99269 0 None - 3 Rat 5.9 pKd = 5.9 Functional
Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.
ChEMBL 773 16 4 8 5.9 CN1C(=O)[C@H](NC(=O)Nc2cccc(CCOC(=O)NCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
CHEMBL284975 99269 0 None - 3 Rat 5.9 pKd = 5.9 Functional
Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.
ChEMBL 773 16 4 8 5.9 CN1C(=O)[C@H](NC(=O)Nc2cccc(CCOC(=O)NCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
44280714 99558 0 None - 3 Rat 5.9 pKd = 5.9 Functional
Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats
ChEMBL 726 14 6 9 3.2 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCC(=O)NCCSCc3csc(N=C(N)N)n3)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL286908 99558 0 None - 3 Rat 5.9 pKd = 5.9 Functional
Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats
ChEMBL 726 14 6 9 3.2 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCC(=O)NCCSCc3csc(N=C(N)N)n3)C2=O)c1 10.1016/S0960-894X(96)00248-X
13499387 12923 0 None - 0 Guinea pig 4.9 pKd = 4.9 Functional
Antagonistic activity against H2 receptor in guinea pig.Antagonistic activity against H2 receptor in guinea pig.
ChEMBL 181 4 3 2 -0.1 C/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm00148a007
CHEMBL1190014 12923 0 None - 0 Guinea pig 4.9 pKd = 4.9 Functional
Antagonistic activity against H2 receptor in guinea pig.Antagonistic activity against H2 receptor in guinea pig.
ChEMBL 181 4 3 2 -0.1 C/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm00148a007
CHEMBL540005 12923 0 None - 0 Guinea pig 4.9 pKd = 4.9 Functional
Antagonistic activity against H2 receptor in guinea pig.Antagonistic activity against H2 receptor in guinea pig.
ChEMBL 181 4 3 2 -0.1 C/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm00148a007
10403687 2465 2 None - 2 Guinea pig 4.9 pKd = 4.9 Functional
Compound was evaluated for its antagonist affinity towards Histamine H2 receptor of guinea pigCompound was evaluated for its antagonist affinity towards Histamine H2 receptor of guinea pig
ChEMBL 319 8 2 2 3.9 CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
1205 2465 2 None - 2 Guinea pig 4.9 pKd = 4.9 Functional
Compound was evaluated for its antagonist affinity towards Histamine H2 receptor of guinea pigCompound was evaluated for its antagonist affinity towards Histamine H2 receptor of guinea pig
ChEMBL 319 8 2 2 3.9 CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
CHEMBL275035 2465 2 None - 2 Guinea pig 4.9 pKd = 4.9 Functional
Compound was evaluated for its antagonist affinity towards Histamine H2 receptor of guinea pigCompound was evaluated for its antagonist affinity towards Histamine H2 receptor of guinea pig
ChEMBL 319 8 2 2 3.9 CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
20449717 11128 0 None - 0 Guinea pig 7.9 pKd = 7.9 Functional
Histamine H2 receptor antagonism on the right atrium of the guinea pigHistamine H2 receptor antagonism on the right atrium of the guinea pig
ChEMBL 242 5 2 2 3.1 CCC(C)N/C=N/c1ccc(-c2c[nH]cn2)cc1 10.1021/jm00110a004
CHEMBL1178962 11128 0 None - 0 Guinea pig 7.9 pKd = 7.9 Functional
Histamine H2 receptor antagonism on the right atrium of the guinea pigHistamine H2 receptor antagonism on the right atrium of the guinea pig
ChEMBL 242 5 2 2 3.1 CCC(C)N/C=N/c1ccc(-c2c[nH]cn2)cc1 10.1021/jm00110a004
CHEMBL51540 11128 0 None - 0 Guinea pig 7.9 pKd = 7.9 Functional
Histamine H2 receptor antagonism on the right atrium of the guinea pigHistamine H2 receptor antagonism on the right atrium of the guinea pig
ChEMBL 242 5 2 2 3.1 CCC(C)N/C=N/c1ccc(-c2c[nH]cn2)cc1 10.1021/jm00110a004
44281291 99351 0 None - 0 Rat 7.8 pKd = 7.8 Functional
Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.
ChEMBL 433 11 2 5 3.9 CC(C)(C)OC(=O)NCCCC(=O)NCCCOc1cccc(CN2CCCCC2)c1 10.1016/S0960-894X(96)00249-1
CHEMBL285556 99351 0 None - 0 Rat 7.8 pKd = 7.8 Functional
Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.
ChEMBL 433 11 2 5 3.9 CC(C)(C)OC(=O)NCCCC(=O)NCCCOc1cccc(CN2CCCCC2)c1 10.1016/S0960-894X(96)00249-1
13637167 9236 21 None - 0 Guinea pig 4.8 pKd = 4.8 Functional
Compound is evaluated for histamine H2 receptor agonistic activity in guinea pig cerebral cortex using [3H]tiotidine as radioligandCompound is evaluated for histamine H2 receptor agonistic activity in guinea pig cerebral cortex using [3H]tiotidine as radioligand
ChEMBL 143 2 2 4 0.2 NCCc1cnc(N)s1 10.1021/jm00095a021
CHEMBL111215 9236 21 None - 0 Guinea pig 4.8 pKd = 4.8 Functional
Compound is evaluated for histamine H2 receptor agonistic activity in guinea pig cerebral cortex using [3H]tiotidine as radioligandCompound is evaluated for histamine H2 receptor agonistic activity in guinea pig cerebral cortex using [3H]tiotidine as radioligand
ChEMBL 143 2 2 4 0.2 NCCc1cnc(N)s1 10.1021/jm00095a021
3037827 102661 5 None - 0 Guinea pig 6.8 pKd = 6.8 Functional
Histamine H2 receptor antagonistic activity at a concentration of 1 uM on the isolated guinea pig right atrium.Histamine H2 receptor antagonistic activity at a concentration of 1 uM on the isolated guinea pig right atrium.
ChEMBL 629 12 3 6 4.4 N#CN/C(=N\CCNC(=O)c1ccc(N=[N+]=[N-])c(I)c1)NCCCOc1cccc(CN2CCCCC2)c1 10.1021/jm00090a013
CHEMBL307952 102661 5 None - 0 Guinea pig 6.8 pKd = 6.8 Functional
Histamine H2 receptor antagonistic activity at a concentration of 1 uM on the isolated guinea pig right atrium.Histamine H2 receptor antagonistic activity at a concentration of 1 uM on the isolated guinea pig right atrium.
ChEMBL 629 12 3 6 4.4 N#CN/C(=N\CCNC(=O)c1ccc(N=[N+]=[N-])c(I)c1)NCCCOc1cccc(CN2CCCCC2)c1 10.1021/jm00090a013
44281292 114283 0 None - 3 Rat 6.8 pKd = 6.8 Functional
Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.
ChEMBL 816 17 5 9 5.0 CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCCNC(=O)CC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
CHEMBL33398 114283 0 None - 3 Rat 6.8 pKd = 6.8 Functional
Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.
ChEMBL 816 17 5 9 5.0 CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCCNC(=O)CC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
44280143 102385 0 None - 0 Guinea pig 5.8 pKd = 5.8 Functional
Antagonistic activity against H2 receptor in guinea pig.Antagonistic activity against H2 receptor in guinea pig.
ChEMBL 599 12 3 11 2.2 CC1=NN(c2ccc([N+](=O)[O-])cc2)C(=O)C1[N+](=O)[O-].Cc1[nH]cnc1CSCC/N=C(\N)NCCCc1cn(C)cn1 10.1021/jm00148a007
CHEMBL30578 102385 0 None - 0 Guinea pig 5.8 pKd = 5.8 Functional
Antagonistic activity against H2 receptor in guinea pig.Antagonistic activity against H2 receptor in guinea pig.
ChEMBL 599 12 3 11 2.2 CC1=NN(c2ccc([N+](=O)[O-])cc2)C(=O)C1[N+](=O)[O-].Cc1[nH]cnc1CSCC/N=C(\N)NCCCc1cn(C)cn1 10.1021/jm00148a007
11276413 11951 0 None - 0 Guinea pig 4.8 pKd = 4.8 Functional
Functional H2 receptor antagonistic activity in vitro assay on the isolated spontaneously beating guinea-pig right atriumFunctional H2 receptor antagonistic activity in vitro assay on the isolated spontaneously beating guinea-pig right atrium
ChEMBL 236 7 1 2 3.3 c1nc(CCCOCCC2CCCCC2)c[nH]1 10.1021/jm031065q
CHEMBL1183700 11951 0 None - 0 Guinea pig 4.8 pKd = 4.8 Functional
Functional H2 receptor antagonistic activity in vitro assay on the isolated spontaneously beating guinea-pig right atriumFunctional H2 receptor antagonistic activity in vitro assay on the isolated spontaneously beating guinea-pig right atrium
ChEMBL 236 7 1 2 3.3 c1nc(CCCOCCC2CCCCC2)c[nH]1 10.1021/jm031065q
CHEMBL313803 11951 0 None - 0 Guinea pig 4.8 pKd = 4.8 Functional
Functional H2 receptor antagonistic activity in vitro assay on the isolated spontaneously beating guinea-pig right atriumFunctional H2 receptor antagonistic activity in vitro assay on the isolated spontaneously beating guinea-pig right atrium
ChEMBL 236 7 1 2 3.3 c1nc(CCCOCCC2CCCCC2)c[nH]1 10.1021/jm031065q
10659856 11277 0 None - 0 Guinea pig 4.8 pKd = 4.8 Functional
Histamine H2-receptor activity on isolated spontaneously beating guinea pig atriumHistamine H2-receptor activity on isolated spontaneously beating guinea pig atrium
ChEMBL 273 7 1 4 2.8 CO/N=C(\C)c1ccc(OCCCc2c[nH]cn2)cc1 10.1021/jm000971p
CHEMBL112753 11277 0 None - 0 Guinea pig 4.8 pKd = 4.8 Functional
Histamine H2-receptor activity on isolated spontaneously beating guinea pig atriumHistamine H2-receptor activity on isolated spontaneously beating guinea pig atrium
ChEMBL 273 7 1 4 2.8 CO/N=C(\C)c1ccc(OCCCc2c[nH]cn2)cc1 10.1021/jm000971p
CHEMBL1180075 11277 0 None - 0 Guinea pig 4.8 pKd = 4.8 Functional
Histamine H2-receptor activity on isolated spontaneously beating guinea pig atriumHistamine H2-receptor activity on isolated spontaneously beating guinea pig atrium
ChEMBL 273 7 1 4 2.8 CO/N=C(\C)c1ccc(OCCCc2c[nH]cn2)cc1 10.1021/jm000971p
15179507 202469 0 None - 0 Guinea pig 7.8 pKd = 7.8 Functional
Histamine H2 receptor antagonistic activity at a concentration of 1 uM on the isolated guinea pig right atrium.Histamine H2 receptor antagonistic activity at a concentration of 1 uM on the isolated guinea pig right atrium.
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 202469 0 None - 0 Guinea pig 7.8 pKd = 7.8 Functional
Histamine H2 receptor antagonistic activity at a concentration of 1 uM on the isolated guinea pig right atrium.Histamine H2 receptor antagonistic activity at a concentration of 1 uM on the isolated guinea pig right atrium.
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
129817 13069 17 None - 0 Guinea pig 4.8 pKd = 4.8 Functional
Antagonistic activity against H2 receptor in guinea pig.Antagonistic activity against H2 receptor in guinea pig.
ChEMBL 227 5 4 3 0.7 CNC(=N)NCCSCc1nc[nH]c1C 10.1021/jm00148a007
CHEMBL1191048 13069 17 None - 0 Guinea pig 4.8 pKd = 4.8 Functional
Antagonistic activity against H2 receptor in guinea pig.Antagonistic activity against H2 receptor in guinea pig.
ChEMBL 227 5 4 3 0.7 CNC(=N)NCCSCc1nc[nH]c1C 10.1021/jm00148a007
CHEMBL542087 13069 17 None - 0 Guinea pig 4.8 pKd = 4.8 Functional
Antagonistic activity against H2 receptor in guinea pig.Antagonistic activity against H2 receptor in guinea pig.
ChEMBL 227 5 4 3 0.7 CNC(=N)NCCSCc1nc[nH]c1C 10.1021/jm00148a007
5039 62838 13 None 2 3 Guinea pig 6.8 pKd = 6.8 Functional
Histamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atriumHistamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atrium
ChEMBL 314 10 2 7 1.5 CNC(=C[N+](=O)[O-])NCCSCc1ccc(CN(C)C)o1 10.1016/s0960-894x(03)00235-x
CHEMBL1790041 62838 13 None 2 3 Guinea pig 6.8 pKd = 6.8 Functional
Histamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atriumHistamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atrium
ChEMBL 314 10 2 7 1.5 CNC(=C[N+](=O)[O-])NCCSCc1ccc(CN(C)C)o1 10.1016/s0960-894x(03)00235-x
71263 102665 16 None - 0 Guinea pig 7.8 pKd = 7.8 Functional
Antagonistic activity of guinea pig Histamine H2 receptor expressed as pA2 at pH 7.4Antagonistic activity of guinea pig Histamine H2 receptor expressed as pA2 at pH 7.4
ChEMBL 228 4 2 2 2.9 CC(C)/N=C/Nc1ccc(-c2c[nH]cn2)cc1 10.1021/jm00384a036
CHEMBL308005 102665 16 None - 0 Guinea pig 7.8 pKd = 7.8 Functional
Antagonistic activity of guinea pig Histamine H2 receptor expressed as pA2 at pH 7.4Antagonistic activity of guinea pig Histamine H2 receptor expressed as pA2 at pH 7.4
ChEMBL 228 4 2 2 2.9 CC(C)/N=C/Nc1ccc(-c2c[nH]cn2)cc1 10.1021/jm00384a036
CHEMBL50020 102665 16 None - 0 Guinea pig 7.8 pKd = 7.8 Functional
Antagonistic activity of guinea pig Histamine H2 receptor expressed as pA2 at pH 7.4Antagonistic activity of guinea pig Histamine H2 receptor expressed as pA2 at pH 7.4
ChEMBL 228 4 2 2 2.9 CC(C)/N=C/Nc1ccc(-c2c[nH]cn2)cc1 10.1021/jm00384a036
90660592 55914 0 None - 0 Guinea pig 4.8 pKd = 4.8 Functional
Antagonistic activity against H2 receptor in guinea pig was evaluatedAntagonistic activity against H2 receptor in guinea pig was evaluated
ChEMBL 353 9 4 3 1.3 C/[S+]=C(/NCCCc1c[nH]cn1)NCCSCc1[nH]cnc1C 10.1021/jm00148a007
CHEMBL1626721 55914 0 None - 0 Guinea pig 4.8 pKd = 4.8 Functional
Antagonistic activity against H2 receptor in guinea pig was evaluatedAntagonistic activity against H2 receptor in guinea pig was evaluated
ChEMBL 353 9 4 3 1.3 C/[S+]=C(/NCCCc1c[nH]cn1)NCCSCc1[nH]cnc1C 10.1021/jm00148a007
CHEMBL1626961 55914 0 None - 0 Guinea pig 4.8 pKd = 4.8 Functional
Antagonistic activity against H2 receptor in guinea pig was evaluatedAntagonistic activity against H2 receptor in guinea pig was evaluated
ChEMBL 353 9 4 3 1.3 C/[S+]=C(/NCCCc1c[nH]cn1)NCCSCc1[nH]cnc1C 10.1021/jm00148a007
1129 1584 89 None -7 3 Guinea pig 7.7 pKd = 7.7 Functional
Histamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atriumHistamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atrium
ChEMBL 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N 10.1016/s0960-894x(03)00235-x
3325 1584 89 None -7 3 Guinea pig 7.7 pKd = 7.7 Functional
Histamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atriumHistamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atrium
ChEMBL 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N 10.1016/s0960-894x(03)00235-x
5353622 1584 89 None -7 3 Guinea pig 7.7 pKd = 7.7 Functional
Histamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atriumHistamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atrium
ChEMBL 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N 10.1016/s0960-894x(03)00235-x
5702160 1584 89 None -7 3 Guinea pig 7.7 pKd = 7.7 Functional
Histamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atriumHistamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atrium
ChEMBL 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N 10.1016/s0960-894x(03)00235-x
7074 1584 89 None -7 3 Guinea pig 7.7 pKd = 7.7 Functional
Histamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atriumHistamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atrium
ChEMBL 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N 10.1016/s0960-894x(03)00235-x
CHEMBL902 1584 89 None -7 3 Guinea pig 7.7 pKd = 7.7 Functional
Histamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atriumHistamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atrium
ChEMBL 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N 10.1016/s0960-894x(03)00235-x
DB00927 1584 89 None -7 3 Guinea pig 7.7 pKd = 7.7 Functional
Histamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atriumHistamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atrium
ChEMBL 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N 10.1016/s0960-894x(03)00235-x
44292729 182271 0 None - 0 Guinea pig 6.7 pKd = 6.7 Functional
Histamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atriumHistamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atrium
ChEMBL 563 11 3 6 4.6 N#CN/C(=N\CCNC(=O)c1c2ccccc2nc2ccccc12)NCCCOc1cccc(CN2CCCCC2)c1 10.1016/s0960-894x(03)00235-x
CHEMBL47917 182271 0 None - 0 Guinea pig 6.7 pKd = 6.7 Functional
Histamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atriumHistamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atrium
ChEMBL 563 11 3 6 4.6 N#CN/C(=N\CCNC(=O)c1c2ccccc2nc2ccccc12)NCCCOc1cccc(CN2CCCCC2)c1 10.1016/s0960-894x(03)00235-x
44292744 100038 0 None - 0 Guinea pig 5.7 pKd = 5.7 Functional
Histamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atriumHistamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atrium
ChEMBL 638 13 2 8 5.2 CC(=O)c1ccc2n(c1=O)[C@H](COC(=O)CCC(=O)NCCCOc1cccc(CN3CCCCC3)c1)Cc1c-2[nH]c2ccccc12 10.1016/s0960-894x(03)00235-x
CHEMBL291192 100038 0 None - 0 Guinea pig 5.7 pKd = 5.7 Functional
Histamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atriumHistamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atrium
ChEMBL 638 13 2 8 5.2 CC(=O)c1ccc2n(c1=O)[C@H](COC(=O)CCC(=O)NCCCOc1cccc(CN3CCCCC3)c1)Cc1c-2[nH]c2ccccc12 10.1016/s0960-894x(03)00235-x
44292619 100649 0 None - 0 Guinea pig 5.7 pKd = 5.7 Functional
Histamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atriumHistamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atrium
ChEMBL 591 13 3 7 3.7 CN(C)c1cccc2c(S(=O)(=O)NCC/N=C(\NC#N)NCCCOc3cccc(CN4CCCCC4)c3)cccc12 10.1016/s0960-894x(03)00235-x
CHEMBL295252 100649 0 None - 0 Guinea pig 5.7 pKd = 5.7 Functional
Histamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atriumHistamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atrium
ChEMBL 591 13 3 7 3.7 CN(C)c1cccc2c(S(=O)(=O)NCC/N=C(\NC#N)NCCCOc3cccc(CN4CCCCC4)c3)cccc12 10.1016/s0960-894x(03)00235-x
CHEMBL286835 99544 0 None - 0 Rat 5.7 pKd = 5.7 Functional
Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.
ChEMBL 755 14 6 11 4.5 Cc1cccc(NC(=O)N[C@@H]2N=C(c3cccc(OC(=O)NCCCC(=O)NCCSCc4csc(C=C(N)N)n4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00249-1
11218373 11987 2 None - 0 Guinea pig 5.7 pKd = 5.7 Functional
Functional H2 receptor antagonistic activity in vitro assay on the isolated spontaneously beating guinea-pig right atriumFunctional H2 receptor antagonistic activity in vitro assay on the isolated spontaneously beating guinea-pig right atrium
ChEMBL 224 10 1 2 3.3 CCCCCCCOCCCc1c[nH]cn1 10.1021/jm031065q
CHEMBL1184028 11987 2 None - 0 Guinea pig 5.7 pKd = 5.7 Functional
Functional H2 receptor antagonistic activity in vitro assay on the isolated spontaneously beating guinea-pig right atriumFunctional H2 receptor antagonistic activity in vitro assay on the isolated spontaneously beating guinea-pig right atrium
ChEMBL 224 10 1 2 3.3 CCCCCCCOCCCc1c[nH]cn1 10.1021/jm031065q
CHEMBL329116 11987 2 None - 0 Guinea pig 5.7 pKd = 5.7 Functional
Functional H2 receptor antagonistic activity in vitro assay on the isolated spontaneously beating guinea-pig right atriumFunctional H2 receptor antagonistic activity in vitro assay on the isolated spontaneously beating guinea-pig right atrium
ChEMBL 224 10 1 2 3.3 CCCCCCCOCCCc1c[nH]cn1 10.1021/jm031065q
11791817 97838 0 None - 2 Guinea pig 4.7 pKd = 4.7 Functional
Compound was evaluated for its antagonist affinity towards Histamine H2 receptor of guinea pigCompound was evaluated for its antagonist affinity towards Histamine H2 receptor of guinea pig
ChEMBL 345 9 2 2 4.5 c1ccc(C(CCc2nc(CCNC3CC3)c[nH]2)c2ccccc2)cc1 10.1021/jm991056a
CHEMBL274831 97838 0 None - 2 Guinea pig 4.7 pKd = 4.7 Functional
Compound was evaluated for its antagonist affinity towards Histamine H2 receptor of guinea pigCompound was evaluated for its antagonist affinity towards Histamine H2 receptor of guinea pig
ChEMBL 345 9 2 2 4.5 c1ccc(C(CCc2nc(CCNC3CC3)c[nH]2)c2ccccc2)cc1 10.1021/jm991056a
10730975 11984 0 None - 0 Guinea pig 4.7 pKd = 4.7 Functional
Histamine H2-receptor activity on isolated spontaneously beating guinea pig atriumHistamine H2-receptor activity on isolated spontaneously beating guinea pig atrium
ChEMBL 273 6 2 4 2.9 C/C(=N\O)c1ccc(OCCCc2c[nH]cn2)c(C)c1 10.1021/jm000971p
CHEMBL1183977 11984 0 None - 0 Guinea pig 4.7 pKd = 4.7 Functional
Histamine H2-receptor activity on isolated spontaneously beating guinea pig atriumHistamine H2-receptor activity on isolated spontaneously beating guinea pig atrium
ChEMBL 273 6 2 4 2.9 C/C(=N\O)c1ccc(OCCCc2c[nH]cn2)c(C)c1 10.1021/jm000971p
CHEMBL326624 11984 0 None - 0 Guinea pig 4.7 pKd = 4.7 Functional
Histamine H2-receptor activity on isolated spontaneously beating guinea pig atriumHistamine H2-receptor activity on isolated spontaneously beating guinea pig atrium
ChEMBL 273 6 2 4 2.9 C/C(=N\O)c1ccc(OCCCc2c[nH]cn2)c(C)c1 10.1021/jm000971p
9976264 13437 0 None - 0 Guinea pig 6.7 pKd = 6.7 Functional
Antagonistic activity against H2 receptor in guinea pig.Antagonistic activity against H2 receptor in guinea pig.
ChEMBL 367 10 5 5 2.0 Cc1[nH]cnc1CSCCNC(=N)NCCSCc1nc[nH]c1C 10.1021/jm00148a007
CHEMBL1193914 13437 0 None - 0 Guinea pig 6.7 pKd = 6.7 Functional
Antagonistic activity against H2 receptor in guinea pig.Antagonistic activity against H2 receptor in guinea pig.
ChEMBL 367 10 5 5 2.0 Cc1[nH]cnc1CSCCNC(=N)NCCSCc1nc[nH]c1C 10.1021/jm00148a007
CHEMBL545393 13437 0 None - 0 Guinea pig 6.7 pKd = 6.7 Functional
Antagonistic activity against H2 receptor in guinea pig.Antagonistic activity against H2 receptor in guinea pig.
ChEMBL 367 10 5 5 2.0 Cc1[nH]cnc1CSCCNC(=N)NCCSCc1nc[nH]c1C 10.1021/jm00148a007
135564658 101730 3 None - 0 Guinea pig 7.6 pKd = 7.6 Functional
Competitive antagonism of Histamine H2 receptor in the isolated guinea pig atriumCompetitive antagonism of Histamine H2 receptor in the isolated guinea pig atrium
ChEMBL 346 7 5 9 0.9 N=C(N)Nc1nc(CSCCNc2n[s+]([O-])nc2N)cs1 10.1021/jm00345a003
5477889 101730 3 None - 0 Guinea pig 7.6 pKd = 7.6 Functional
Competitive antagonism of Histamine H2 receptor in the isolated guinea pig atriumCompetitive antagonism of Histamine H2 receptor in the isolated guinea pig atrium
ChEMBL 346 7 5 9 0.9 N=C(N)Nc1nc(CSCCNc2n[s+]([O-])nc2N)cs1 10.1021/jm00345a003
CHEMBL302907 101730 3 None - 0 Guinea pig 7.6 pKd = 7.6 Functional
Competitive antagonism of Histamine H2 receptor in the isolated guinea pig atriumCompetitive antagonism of Histamine H2 receptor in the isolated guinea pig atrium
ChEMBL 346 7 5 9 0.9 N=C(N)Nc1nc(CSCCNc2n[s+]([O-])nc2N)cs1 10.1021/jm00345a003
44293003 174684 0 None - 0 Guinea pig 7.6 pKd = 7.6 Functional
Histamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atriumHistamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atrium
ChEMBL 634 18 4 11 3.7 N#CN/C(=N\CCNC(=O)CCCCCNc1ccc([N+](=O)[O-])c2nonc12)NCCCOc1cccc(CN2CCCCC2)c1 10.1016/s0960-894x(03)00235-x
CHEMBL45725 174684 0 None - 0 Guinea pig 7.6 pKd = 7.6 Functional
Histamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atriumHistamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atrium
ChEMBL 634 18 4 11 3.7 N#CN/C(=N\CCNC(=O)CCCCCNc1ccc([N+](=O)[O-])c2nonc12)NCCCOc1cccc(CN2CCCCC2)c1 10.1016/s0960-894x(03)00235-x
1231 922 112 None - 4 Rat 6.6 pKd = 6.6 Functional
Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/S0960-894X(96)00249-1
2756 922 112 None - 4 Rat 6.6 pKd = 6.6 Functional
Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/S0960-894X(96)00249-1
645 922 112 None - 4 Rat 6.6 pKd = 6.6 Functional
Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/S0960-894X(96)00249-1
CHEMBL30 922 112 None - 4 Rat 6.6 pKd = 6.6 Functional
Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/S0960-894X(96)00249-1
DB00501 922 112 None - 4 Rat 6.6 pKd = 6.6 Functional
Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/S0960-894X(96)00249-1
44281020 116131 0 None - 3 Rat 6.6 pKd = 6.6 Functional
Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.
ChEMBL 773 16 4 8 6.2 CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
CHEMBL33698 116131 0 None - 3 Rat 6.6 pKd = 6.6 Functional
Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.
ChEMBL 773 16 4 8 6.2 CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
1231 922 112 None - 4 Rat 6.6 pKd = 6.6 Functional
Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/S0960-894X(96)00248-X
2756 922 112 None - 4 Rat 6.6 pKd = 6.6 Functional
Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/S0960-894X(96)00248-X
645 922 112 None - 4 Rat 6.6 pKd = 6.6 Functional
Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/S0960-894X(96)00248-X
CHEMBL30 922 112 None - 4 Rat 6.6 pKd = 6.6 Functional
Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/S0960-894X(96)00248-X
DB00501 922 112 None - 4 Rat 6.6 pKd = 6.6 Functional
Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/S0960-894X(96)00248-X
44279811 96464 0 None - 3 Rat 6.6 pKd = 6.6 Functional
Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats
ChEMBL 743 15 4 7 5.3 CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00248-X
CHEMBL265987 96464 0 None - 3 Rat 6.6 pKd = 6.6 Functional
Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats
ChEMBL 743 15 4 7 5.3 CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00248-X
11459067 11228 0 None - 0 Guinea pig 5.6 pKd = 5.6 Functional
Functional H2 receptor antagonistic activity in vitro assay on the isolated spontaneously beating guinea-pig right atriumFunctional H2 receptor antagonistic activity in vitro assay on the isolated spontaneously beating guinea-pig right atrium
ChEMBL 238 11 1 2 3.7 CCCCCCCCOCCCc1c[nH]cn1 10.1021/jm031065q
CHEMBL1179647 11228 0 None - 0 Guinea pig 5.6 pKd = 5.6 Functional
Functional H2 receptor antagonistic activity in vitro assay on the isolated spontaneously beating guinea-pig right atriumFunctional H2 receptor antagonistic activity in vitro assay on the isolated spontaneously beating guinea-pig right atrium
ChEMBL 238 11 1 2 3.7 CCCCCCCCOCCCc1c[nH]cn1 10.1021/jm031065q
CHEMBL91523 11228 0 None - 0 Guinea pig 5.6 pKd = 5.6 Functional
Functional H2 receptor antagonistic activity in vitro assay on the isolated spontaneously beating guinea-pig right atriumFunctional H2 receptor antagonistic activity in vitro assay on the isolated spontaneously beating guinea-pig right atrium
ChEMBL 238 11 1 2 3.7 CCCCCCCCOCCCc1c[nH]cn1 10.1021/jm031065q
19854557 119846 0 None - 0 Guinea pig 4.6 pKd = 4.6 Functional
Antagonistic activity against H2 receptor in guinea pig.Antagonistic activity against H2 receptor in guinea pig.
ChEMBL 198 4 3 3 1.2 CSC(=N)NCCCc1c[nH]cn1 10.1021/jm00148a007
CHEMBL353211 119846 0 None - 0 Guinea pig 4.6 pKd = 4.6 Functional
Antagonistic activity against H2 receptor in guinea pig.Antagonistic activity against H2 receptor in guinea pig.
ChEMBL 198 4 3 3 1.2 CSC(=N)NCCCc1c[nH]cn1 10.1021/jm00148a007
CHEMBL540256 119846 0 None - 0 Guinea pig 4.6 pKd = 4.6 Functional
Antagonistic activity against H2 receptor in guinea pig.Antagonistic activity against H2 receptor in guinea pig.
ChEMBL 198 4 3 3 1.2 CSC(=N)NCCCc1c[nH]cn1 10.1021/jm00148a007
1248 1391 27 None - 1 Guinea pig 4.6 pKd = 4.6 Functional
Compound is evaluated for histamine H2 receptor agonistic activity in guinea pig cerebral cortex using [3H]tiotidine as radioligandCompound is evaluated for histamine H2 receptor agonistic activity in guinea pig cerebral cortex using [3H]tiotidine as radioligand
ChEMBL 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1021/jm00095a021
3077 1391 27 None - 1 Guinea pig 4.6 pKd = 4.6 Functional
Compound is evaluated for histamine H2 receptor agonistic activity in guinea pig cerebral cortex using [3H]tiotidine as radioligandCompound is evaluated for histamine H2 receptor agonistic activity in guinea pig cerebral cortex using [3H]tiotidine as radioligand
ChEMBL 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1021/jm00095a021
90045 1391 27 None - 1 Guinea pig 4.6 pKd = 4.6 Functional
Compound is evaluated for histamine H2 receptor agonistic activity in guinea pig cerebral cortex using [3H]tiotidine as radioligandCompound is evaluated for histamine H2 receptor agonistic activity in guinea pig cerebral cortex using [3H]tiotidine as radioligand
ChEMBL 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1021/jm00095a021
CHEMBL12344 1391 27 None - 1 Guinea pig 4.6 pKd = 4.6 Functional
Compound is evaluated for histamine H2 receptor agonistic activity in guinea pig cerebral cortex using [3H]tiotidine as radioligandCompound is evaluated for histamine H2 receptor agonistic activity in guinea pig cerebral cortex using [3H]tiotidine as radioligand
ChEMBL 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1021/jm00095a021
10042467 1393 1 None - 2 Guinea pig 4.6 pKd = 4.6 Functional
Compound was evaluated for its antagonist affinity towards Histamine H2 receptor of guinea pigCompound was evaluated for its antagonist affinity towards Histamine H2 receptor of guinea pig
ChEMBL 333 8 1 2 4.3 CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C 10.1021/jm991056a
1203 1393 1 None - 2 Guinea pig 4.6 pKd = 4.6 Functional
Compound was evaluated for its antagonist affinity towards Histamine H2 receptor of guinea pigCompound was evaluated for its antagonist affinity towards Histamine H2 receptor of guinea pig
ChEMBL 333 8 1 2 4.3 CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C 10.1021/jm991056a
CHEMBL11553 1393 1 None - 2 Guinea pig 4.6 pKd = 4.6 Functional
Compound was evaluated for its antagonist affinity towards Histamine H2 receptor of guinea pigCompound was evaluated for its antagonist affinity towards Histamine H2 receptor of guinea pig
ChEMBL 333 8 1 2 4.3 CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C 10.1021/jm991056a
1232 2017 6 None - 0 Guinea pig 7.6 pKd = 7.6 Functional
Histamine H2 receptor antagonistic activity at a concentration of 1 uM on the isolated guinea pig right atrium.Histamine H2 receptor antagonistic activity at a concentration of 1 uM on the isolated guinea pig right atrium.
ChEMBL 603 11 4 6 3.1 N#CNC(=NCCCOc1cccc(c1)CN1CCCCC1)NCCNC(=O)c1ccc(c(c1)I)N 10.1021/jm00090a013
181461 2017 6 None - 0 Guinea pig 7.6 pKd = 7.6 Functional
Histamine H2 receptor antagonistic activity at a concentration of 1 uM on the isolated guinea pig right atrium.Histamine H2 receptor antagonistic activity at a concentration of 1 uM on the isolated guinea pig right atrium.
ChEMBL 603 11 4 6 3.1 N#CNC(=NCCCOc1cccc(c1)CN1CCCCC1)NCCNC(=O)c1ccc(c(c1)I)N 10.1021/jm00090a013
CHEMBL72193 2017 6 None - 0 Guinea pig 7.6 pKd = 7.6 Functional
Histamine H2 receptor antagonistic activity at a concentration of 1 uM on the isolated guinea pig right atrium.Histamine H2 receptor antagonistic activity at a concentration of 1 uM on the isolated guinea pig right atrium.
ChEMBL 603 11 4 6 3.1 N#CNC(=NCCCOc1cccc(c1)CN1CCCCC1)NCCNC(=O)c1ccc(c(c1)I)N 10.1021/jm00090a013
71263 102665 16 None - 0 Guinea pig 7.6 pKd = 7.6 Functional
Histamine H2 receptor antagonism on the right atrium of the guinea pigHistamine H2 receptor antagonism on the right atrium of the guinea pig
ChEMBL 228 4 2 2 2.9 CC(C)/N=C/Nc1ccc(-c2c[nH]cn2)cc1 10.1021/jm00110a004
CHEMBL308005 102665 16 None - 0 Guinea pig 7.6 pKd = 7.6 Functional
Histamine H2 receptor antagonism on the right atrium of the guinea pigHistamine H2 receptor antagonism on the right atrium of the guinea pig
ChEMBL 228 4 2 2 2.9 CC(C)/N=C/Nc1ccc(-c2c[nH]cn2)cc1 10.1021/jm00110a004
CHEMBL50020 102665 16 None - 0 Guinea pig 7.6 pKd = 7.6 Functional
Histamine H2 receptor antagonism on the right atrium of the guinea pigHistamine H2 receptor antagonism on the right atrium of the guinea pig
ChEMBL 228 4 2 2 2.9 CC(C)/N=C/Nc1ccc(-c2c[nH]cn2)cc1 10.1021/jm00110a004
42625304 178512 0 None -77 5 Guinea pig 6.5 pKd = 6.5 Functional
Antagonist activity at histamine H2 receptor in guinea pig right atrium assessed as inhibition of histamine-induced increase in heart rateAntagonist activity at histamine H2 receptor in guinea pig right atrium assessed as inhibition of histamine-induced increase in heart rate
ChEMBL 237 5 3 2 0.4 CC(C)C(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL471724 178512 0 None -77 5 Guinea pig 6.5 pKd = 6.5 Functional
Antagonist activity at histamine H2 receptor in guinea pig right atrium assessed as inhibition of histamine-induced increase in heart rateAntagonist activity at histamine H2 receptor in guinea pig right atrium assessed as inhibition of histamine-induced increase in heart rate
ChEMBL 237 5 3 2 0.4 CC(C)C(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
44294873 12265 0 None - 0 Guinea pig 7.5 pKd = 7.5 Functional
Histamine H2 receptor antagonism on the right atrium of the guinea pigHistamine H2 receptor antagonism on the right atrium of the guinea pig
ChEMBL 256 6 2 2 3.5 CCC(CC)N/C=N/c1ccc(-c2c[nH]cn2)cc1 10.1021/jm00110a004
CHEMBL1185623 12265 0 None - 0 Guinea pig 7.5 pKd = 7.5 Functional
Histamine H2 receptor antagonism on the right atrium of the guinea pigHistamine H2 receptor antagonism on the right atrium of the guinea pig
ChEMBL 256 6 2 2 3.5 CCC(CC)N/C=N/c1ccc(-c2c[nH]cn2)cc1 10.1021/jm00110a004
CHEMBL423660 12265 0 None - 0 Guinea pig 7.5 pKd = 7.5 Functional
Histamine H2 receptor antagonism on the right atrium of the guinea pigHistamine H2 receptor antagonism on the right atrium of the guinea pig
ChEMBL 256 6 2 2 3.5 CCC(CC)N/C=N/c1ccc(-c2c[nH]cn2)cc1 10.1021/jm00110a004
13499363 162635 0 None - 0 Guinea pig 6.5 pKd = 6.5 Functional
Antagonistic activity against H2 receptor in guinea pig.Antagonistic activity against H2 receptor in guinea pig.
ChEMBL 338 9 3 5 1.9 Cc1[nH]cnc1CSCC/N=C(\N)NCCCc1nccs1 10.1021/jm00148a007
CHEMBL1744352 162635 0 None - 0 Guinea pig 6.5 pKd = 6.5 Functional
Antagonistic activity against H2 receptor in guinea pig.Antagonistic activity against H2 receptor in guinea pig.
ChEMBL 338 9 3 5 1.9 Cc1[nH]cnc1CSCC/N=C(\N)NCCCc1nccs1 10.1021/jm00148a007
CHEMBL418211 162635 0 None - 0 Guinea pig 6.5 pKd = 6.5 Functional
Antagonistic activity against H2 receptor in guinea pig.Antagonistic activity against H2 receptor in guinea pig.
ChEMBL 338 9 3 5 1.9 Cc1[nH]cnc1CSCC/N=C(\N)NCCCc1nccs1 10.1021/jm00148a007
44281204 99375 0 None - 3 Rat 6.5 pKd = 6.5 Functional
Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.
ChEMBL 871 18 4 10 5.5 CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCCCN3CCN(C(=O)CNCCCOc4cccc(CN5CCCCC5)c4)CC3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
CHEMBL285719 99375 0 None - 3 Rat 6.5 pKd = 6.5 Functional
Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.
ChEMBL 871 18 4 10 5.5 CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCCCN3CCN(C(=O)CNCCCOc4cccc(CN5CCCCC5)c4)CC3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
44280741 156009 0 None - 3 Rat 6.5 pKd = 6.5 Functional
Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.
ChEMBL 759 15 4 8 5.8 CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
CHEMBL406844 156009 0 None - 3 Rat 6.5 pKd = 6.5 Functional
Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.
ChEMBL 759 15 4 8 5.8 CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
44280372 98915 0 None - 3 Rat 6.5 pKd = 6.5 Functional
Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats
ChEMBL 787 17 4 8 5.8 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL282645 98915 0 None - 3 Rat 6.5 pKd = 6.5 Functional
Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats
ChEMBL 787 17 4 8 5.8 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL282175 98850 0 None - 3 Rat 5.5 pKd = 5.5 Functional
Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.
ChEMBL 769 16 6 11 4.6 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CCOC(=O)NCCCC(=O)NCCSCc3csc(C=C(N)N)n3)C2=O)c1 10.1016/S0960-894X(96)00249-1
44280713 99557 0 None - 3 Rat 5.5 pKd = 5.5 Functional
Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats
ChEMBL 740 15 6 9 3.6 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCCC(=O)NCCSCc3csc(N=C(N)N)n3)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL286907 99557 0 None - 3 Rat 5.5 pKd = 5.5 Functional
Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats
ChEMBL 740 15 6 9 3.6 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCCC(=O)NCCSCc3csc(N=C(N)N)n3)C2=O)c1 10.1016/S0960-894X(96)00248-X
10688111 9930 0 None - 2 Guinea pig 4.5 pKd = 4.5 Functional
Compound was evaluated for its antagonist affinity towards Histamine H2 receptor of guinea pigCompound was evaluated for its antagonist affinity towards Histamine H2 receptor of guinea pig
ChEMBL 333 9 2 2 4.3 CCNCCc1c[nH]c(CCC(c2ccccc2)c2ccccc2)n1 10.1021/jm991056a
CHEMBL11515 9930 0 None - 2 Guinea pig 4.5 pKd = 4.5 Functional
Compound was evaluated for its antagonist affinity towards Histamine H2 receptor of guinea pigCompound was evaluated for its antagonist affinity towards Histamine H2 receptor of guinea pig
ChEMBL 333 9 2 2 4.3 CCNCCc1c[nH]c(CCC(c2ccccc2)c2ccccc2)n1 10.1021/jm991056a
44293001 176179 0 None - 0 Guinea pig 7.5 pKd = 7.5 Functional
Histamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atriumHistamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atrium
ChEMBL 577 16 3 10 4.6 N#CN/C(=N\CCCCCCNc1ccc([N+](=O)[O-])c2nonc12)NCCCOc1cccc(CN2CCCCC2)c1 10.1016/s0960-894x(03)00235-x
CHEMBL46043 176179 0 None - 0 Guinea pig 7.5 pKd = 7.5 Functional
Histamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atriumHistamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atrium
ChEMBL 577 16 3 10 4.6 N#CN/C(=N\CCCCCCNc1ccc([N+](=O)[O-])c2nonc12)NCCCOc1cccc(CN2CCCCC2)c1 10.1016/s0960-894x(03)00235-x
13499397 13226 0 None - 0 Guinea pig 5.5 pKd = 5.5 Functional
Antagonistic activity against H2 receptor in guinea pig.Antagonistic activity against H2 receptor in guinea pig.
ChEMBL 338 9 3 5 2.4 Cc1[nH]cnc1CSCC/N=C(\N)SCCCc1c[nH]cn1 10.1021/jm00148a007
CHEMBL1192303 13226 0 None - 0 Guinea pig 5.5 pKd = 5.5 Functional
Antagonistic activity against H2 receptor in guinea pig.Antagonistic activity against H2 receptor in guinea pig.
ChEMBL 338 9 3 5 2.4 Cc1[nH]cnc1CSCC/N=C(\N)SCCCc1c[nH]cn1 10.1021/jm00148a007
CHEMBL543520 13226 0 None - 0 Guinea pig 5.5 pKd = 5.5 Functional
Antagonistic activity against H2 receptor in guinea pig.Antagonistic activity against H2 receptor in guinea pig.
ChEMBL 338 9 3 5 2.4 Cc1[nH]cnc1CSCC/N=C(\N)SCCCc1c[nH]cn1 10.1021/jm00148a007
42625303 180174 0 None -190 7 Guinea pig 6.5 pKd = 6.5 Functional
Antagonist activity at histamine H2 receptor in guinea pig right atrium assessed as inhibition of histamine-induced increase in heart rateAntagonist activity at histamine H2 receptor in guinea pig right atrium assessed as inhibition of histamine-induced increase in heart rate
ChEMBL 223 5 3 2 0.2 CCC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL475621 180174 0 None -190 7 Guinea pig 6.5 pKd = 6.5 Functional
Antagonist activity at histamine H2 receptor in guinea pig right atrium assessed as inhibition of histamine-induced increase in heart rateAntagonist activity at histamine H2 receptor in guinea pig right atrium assessed as inhibition of histamine-induced increase in heart rate
ChEMBL 223 5 3 2 0.2 CCC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
10447834 1894 4 None - 3 Guinea pig 4.5 pKd = 4.5 Functional
Compound was evaluated for its antagonist affinity towards Histamine H2 receptor of guinea pigCompound was evaluated for its antagonist affinity towards Histamine H2 receptor of guinea pig
ChEMBL 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
4026 1894 4 None - 3 Guinea pig 4.5 pKd = 4.5 Functional
Compound was evaluated for its antagonist affinity towards Histamine H2 receptor of guinea pigCompound was evaluated for its antagonist affinity towards Histamine H2 receptor of guinea pig
ChEMBL 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
CHEMBL275507 1894 4 None - 3 Guinea pig 4.5 pKd = 4.5 Functional
Compound was evaluated for its antagonist affinity towards Histamine H2 receptor of guinea pigCompound was evaluated for its antagonist affinity towards Histamine H2 receptor of guinea pig
ChEMBL 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
42625384 169195 0 None -223 5 Guinea pig 6.4 pKd = 6.4 Functional
Antagonist activity at histamine H2 receptor in guinea pig right atrium assessed as inhibition of histamine-induced increase in heart rateAntagonist activity at histamine H2 receptor in guinea pig right atrium assessed as inhibition of histamine-induced increase in heart rate
ChEMBL 209 4 3 2 -0.2 CC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL443896 169195 0 None -223 5 Guinea pig 6.4 pKd = 6.4 Functional
Antagonist activity at histamine H2 receptor in guinea pig right atrium assessed as inhibition of histamine-induced increase in heart rateAntagonist activity at histamine H2 receptor in guinea pig right atrium assessed as inhibition of histamine-induced increase in heart rate
ChEMBL 209 4 3 2 -0.2 CC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
44293002 100706 0 None - 0 Guinea pig 7.4 pKd = 7.4 Functional
Histamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atriumHistamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atrium
ChEMBL 535 13 3 10 3.4 N#CN/C(=N\CCCNc1ccc([N+](=O)[O-])c2nonc12)NCCCOc1cccc(CN2CCCCC2)c1 10.1016/s0960-894x(03)00235-x
CHEMBL295682 100706 0 None - 0 Guinea pig 7.4 pKd = 7.4 Functional
Histamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atriumHistamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atrium
ChEMBL 535 13 3 10 3.4 N#CN/C(=N\CCCNc1ccc([N+](=O)[O-])c2nonc12)NCCCOc1cccc(CN2CCCCC2)c1 10.1016/s0960-894x(03)00235-x
1231 922 112 None -11 4 Guinea pig 6.4 pKd = 6.4 Functional
Antagonistic activity against Histamine H2 receptor expressed as the charge of receptor sensitivity was determined at pH 7.8Antagonistic activity against Histamine H2 receptor expressed as the charge of receptor sensitivity was determined at pH 7.8
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/jm00384a036
2756 922 112 None -11 4 Guinea pig 6.4 pKd = 6.4 Functional
Antagonistic activity against Histamine H2 receptor expressed as the charge of receptor sensitivity was determined at pH 7.8Antagonistic activity against Histamine H2 receptor expressed as the charge of receptor sensitivity was determined at pH 7.8
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/jm00384a036
645 922 112 None -11 4 Guinea pig 6.4 pKd = 6.4 Functional
Antagonistic activity against Histamine H2 receptor expressed as the charge of receptor sensitivity was determined at pH 7.8Antagonistic activity against Histamine H2 receptor expressed as the charge of receptor sensitivity was determined at pH 7.8
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/jm00384a036
CHEMBL30 922 112 None -11 4 Guinea pig 6.4 pKd = 6.4 Functional
Antagonistic activity against Histamine H2 receptor expressed as the charge of receptor sensitivity was determined at pH 7.8Antagonistic activity against Histamine H2 receptor expressed as the charge of receptor sensitivity was determined at pH 7.8
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/jm00384a036
DB00501 922 112 None -11 4 Guinea pig 6.4 pKd = 6.4 Functional
Antagonistic activity against Histamine H2 receptor expressed as the charge of receptor sensitivity was determined at pH 7.8Antagonistic activity against Histamine H2 receptor expressed as the charge of receptor sensitivity was determined at pH 7.8
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/jm00384a036
5105 176243 49 None - 0 Guinea pig 7.4 pKd = 7.4 Functional
Histamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atriumHistamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atrium
ChEMBL 348 9 1 5 2.1 CC(=O)OCC(=O)NCCCOc1cccc(CN2CCCCC2)c1 10.1016/s0960-894x(03)00235-x
CHEMBL46102 176243 49 None - 0 Guinea pig 7.4 pKd = 7.4 Functional
Histamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atriumHistamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atrium
ChEMBL 348 9 1 5 2.1 CC(=O)OCC(=O)NCCCOc1cccc(CN2CCCCC2)c1 10.1016/s0960-894x(03)00235-x
1231 922 112 None -11 4 Guinea pig 6.4 pKd = 6.4 Functional
Antagonistic activity against Histamine H2 receptor expressed as the charge of receptor sensitivity was determined at pH 7.4Antagonistic activity against Histamine H2 receptor expressed as the charge of receptor sensitivity was determined at pH 7.4
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/jm00384a036
2756 922 112 None -11 4 Guinea pig 6.4 pKd = 6.4 Functional
Antagonistic activity against Histamine H2 receptor expressed as the charge of receptor sensitivity was determined at pH 7.4Antagonistic activity against Histamine H2 receptor expressed as the charge of receptor sensitivity was determined at pH 7.4
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/jm00384a036
645 922 112 None -11 4 Guinea pig 6.4 pKd = 6.4 Functional
Antagonistic activity against Histamine H2 receptor expressed as the charge of receptor sensitivity was determined at pH 7.4Antagonistic activity against Histamine H2 receptor expressed as the charge of receptor sensitivity was determined at pH 7.4
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/jm00384a036
CHEMBL30 922 112 None -11 4 Guinea pig 6.4 pKd = 6.4 Functional
Antagonistic activity against Histamine H2 receptor expressed as the charge of receptor sensitivity was determined at pH 7.4Antagonistic activity against Histamine H2 receptor expressed as the charge of receptor sensitivity was determined at pH 7.4
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/jm00384a036
DB00501 922 112 None -11 4 Guinea pig 6.4 pKd = 6.4 Functional
Antagonistic activity against Histamine H2 receptor expressed as the charge of receptor sensitivity was determined at pH 7.4Antagonistic activity against Histamine H2 receptor expressed as the charge of receptor sensitivity was determined at pH 7.4
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/jm00384a036
44280740 99928 0 None - 3 Rat 6.4 pKd = 6.4 Functional
Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.
ChEMBL 787 17 4 8 6.3 CN1C(=O)[C@H](NC(=O)Nc2cccc(CCOC(=O)NCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
CHEMBL290122 99928 0 None - 3 Rat 6.4 pKd = 6.4 Functional
Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.
ChEMBL 787 17 4 8 6.3 CN1C(=O)[C@H](NC(=O)Nc2cccc(CCOC(=O)NCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
44280200 100344 0 None - 3 Rat 6.4 pKd = 6.4 Functional
Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats
ChEMBL 785 18 4 7 6.6 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL29331 100344 0 None - 3 Rat 6.4 pKd = 6.4 Functional
Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats
ChEMBL 785 18 4 7 6.6 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1 10.1016/S0960-894X(96)00248-X
44279861 102696 0 None - 3 Rat 6.4 pKd = 6.4 Functional
Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats
ChEMBL 726 14 6 9 3.1 CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCC(=O)NCCSCc3csc(N=C(N)N)n3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00248-X
CHEMBL30821 102696 0 None - 3 Rat 6.4 pKd = 6.4 Functional
Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats
ChEMBL 726 14 6 9 3.1 CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCC(=O)NCCSCc3csc(N=C(N)N)n3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00248-X
44279810 103354 0 None - 3 Rat 6.4 pKd = 6.4 Functional
Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats
ChEMBL 757 16 4 7 5.7 CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00248-X
CHEMBL30917 103354 0 None - 3 Rat 6.4 pKd = 6.4 Functional
Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats
ChEMBL 757 16 4 7 5.7 CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00248-X
44279808 98671 0 None - 3 Rat 5.4 pKd = 5.4 Functional
Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats
ChEMBL 712 13 6 9 2.9 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCC(=O)NCCSCc3csc(N=C(N)N)n3)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL281082 98671 0 None - 3 Rat 5.4 pKd = 5.4 Functional
Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats
ChEMBL 712 13 6 9 2.9 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCC(=O)NCCSCc3csc(N=C(N)N)n3)C2=O)c1 10.1016/S0960-894X(96)00248-X
10849869 9922 0 None - 0 Guinea pig 4.4 pKd = 4.4 Functional
Histamine H2-receptor activity on isolated spontaneously beating guinea pig atriumHistamine H2-receptor activity on isolated spontaneously beating guinea pig atrium
ChEMBL 273 6 2 4 2.9 C/C(=N\O)c1ccc(OCCCc2c[nH]cn2)cc1C 10.1021/jm000971p
CHEMBL115091 9922 0 None - 0 Guinea pig 4.4 pKd = 4.4 Functional
Histamine H2-receptor activity on isolated spontaneously beating guinea pig atriumHistamine H2-receptor activity on isolated spontaneously beating guinea pig atrium
ChEMBL 273 6 2 4 2.9 C/C(=N\O)c1ccc(OCCCc2c[nH]cn2)cc1C 10.1021/jm000971p
42625386 177768 0 None -117 5 Guinea pig 6.4 pKd = 6.4 Functional
Antagonist activity at histamine H2 receptor in guinea pig right atrium assessed as inhibition of histamine-induced increase in heart rateAntagonist activity at histamine H2 receptor in guinea pig right atrium assessed as inhibition of histamine-induced increase in heart rate
ChEMBL 237 6 3 2 0.6 CCCC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL465170 177768 0 None -117 5 Guinea pig 6.4 pKd = 6.4 Functional
Antagonist activity at histamine H2 receptor in guinea pig right atrium assessed as inhibition of histamine-induced increase in heart rateAntagonist activity at histamine H2 receptor in guinea pig right atrium assessed as inhibition of histamine-induced increase in heart rate
ChEMBL 237 6 3 2 0.6 CCCC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
13499383 13737 0 None - 0 Guinea pig 4.4 pKd = 4.4 Functional
Antagonistic activity against H2 receptor in guinea pig.Antagonistic activity against H2 receptor in guinea pig.
ChEMBL 213 5 3 3 0.2 C/N=C(\N)NCCSCc1c[nH]cn1 10.1021/jm00148a007
CHEMBL1195977 13737 0 None - 0 Guinea pig 4.4 pKd = 4.4 Functional
Antagonistic activity against H2 receptor in guinea pig.Antagonistic activity against H2 receptor in guinea pig.
ChEMBL 213 5 3 3 0.2 C/N=C(\N)NCCSCc1c[nH]cn1 10.1021/jm00148a007
CHEMBL555668 13737 0 None - 0 Guinea pig 4.4 pKd = 4.4 Functional
Antagonistic activity against H2 receptor in guinea pig.Antagonistic activity against H2 receptor in guinea pig.
ChEMBL 213 5 3 3 0.2 C/N=C(\N)NCCSCc1c[nH]cn1 10.1021/jm00148a007
14479829 61783 2 None - 0 Guinea pig 7.4 pKd = 7.4 Functional
Histamine H2 receptor antagonism on the right atrium of the guinea pigHistamine H2 receptor antagonism on the right atrium of the guinea pig
ChEMBL 214 4 2 2 2.5 CC/N=C/Nc1ccc(-c2c[nH]cn2)cc1 10.1021/jm00110a004
CHEMBL177683 61783 2 None - 0 Guinea pig 7.4 pKd = 7.4 Functional
Histamine H2 receptor antagonism on the right atrium of the guinea pigHistamine H2 receptor antagonism on the right atrium of the guinea pig
ChEMBL 214 4 2 2 2.5 CC/N=C/Nc1ccc(-c2c[nH]cn2)cc1 10.1021/jm00110a004
CHEMBL296826 61783 2 None - 0 Guinea pig 7.4 pKd = 7.4 Functional
Histamine H2 receptor antagonism on the right atrium of the guinea pigHistamine H2 receptor antagonism on the right atrium of the guinea pig
ChEMBL 214 4 2 2 2.5 CC/N=C/Nc1ccc(-c2c[nH]cn2)cc1 10.1021/jm00110a004
42625221 188987 0 None -10 3 Guinea pig 6.4 pKd = 6.4 Functional
Antagonist activity at histamine H2 receptor in guinea pig right atrium assessed as inhibition of histamine-induced increase in heart rateAntagonist activity at histamine H2 receptor in guinea pig right atrium assessed as inhibition of histamine-induced increase in heart rate
ChEMBL 338 7 4 2 1.9 N/C(=N\C(=O)CCc1c[nH]c2ccccc12)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL514641 188987 0 None -10 3 Guinea pig 6.4 pKd = 6.4 Functional
Antagonist activity at histamine H2 receptor in guinea pig right atrium assessed as inhibition of histamine-induced increase in heart rateAntagonist activity at histamine H2 receptor in guinea pig right atrium assessed as inhibition of histamine-induced increase in heart rate
ChEMBL 338 7 4 2 1.9 N/C(=N\C(=O)CCc1c[nH]c2ccccc12)NCCCc1c[nH]cn1 10.1021/jm9000693
44292743 175476 0 None - 0 Guinea pig 4.4 pKd = 4.4 Functional
Histamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atriumHistamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atrium
ChEMBL 718 13 5 9 4.5 N#CN/C(=N\CCNC(=O)c1ccc(C(=O)O)c(C2c3ccc(O)cc3OC3=CC(=O)C=CC32)c1)NCCCOc1cccc(CN2CCCCC2)c1 10.1016/s0960-894x(03)00235-x
CHEMBL45907 175476 0 None - 0 Guinea pig 4.4 pKd = 4.4 Functional
Histamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atriumHistamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atrium
ChEMBL 718 13 5 9 4.5 N#CN/C(=N\CCNC(=O)c1ccc(C(=O)O)c(C2c3ccc(O)cc3OC3=CC(=O)C=CC32)c1)NCCCOc1cccc(CN2CCCCC2)c1 10.1016/s0960-894x(03)00235-x
71263 102665 16 None - 0 Guinea pig 7.3 pKd = 7.3 Functional
Antagonistic activity of guinea pig Histamine H2 receptor expressed as pA2 at pH 7.0Antagonistic activity of guinea pig Histamine H2 receptor expressed as pA2 at pH 7.0
ChEMBL 228 4 2 2 2.9 CC(C)/N=C/Nc1ccc(-c2c[nH]cn2)cc1 10.1021/jm00384a036
CHEMBL308005 102665 16 None - 0 Guinea pig 7.3 pKd = 7.3 Functional
Antagonistic activity of guinea pig Histamine H2 receptor expressed as pA2 at pH 7.0Antagonistic activity of guinea pig Histamine H2 receptor expressed as pA2 at pH 7.0
ChEMBL 228 4 2 2 2.9 CC(C)/N=C/Nc1ccc(-c2c[nH]cn2)cc1 10.1021/jm00384a036
CHEMBL50020 102665 16 None - 0 Guinea pig 7.3 pKd = 7.3 Functional
Antagonistic activity of guinea pig Histamine H2 receptor expressed as pA2 at pH 7.0Antagonistic activity of guinea pig Histamine H2 receptor expressed as pA2 at pH 7.0
ChEMBL 228 4 2 2 2.9 CC(C)/N=C/Nc1ccc(-c2c[nH]cn2)cc1 10.1021/jm00384a036
20449725 11924 1 None - 0 Guinea pig 8.3 pKd = 8.3 Functional
Histamine H2 receptor antagonism on the right atrium of the guinea pigHistamine H2 receptor antagonism on the right atrium of the guinea pig
ChEMBL 242 5 2 2 3.2 CC(C)C/N=C/Nc1ccc(-c2c[nH]cn2)cc1 10.1021/jm00110a004
CHEMBL1183471 11924 1 None - 0 Guinea pig 8.3 pKd = 8.3 Functional
Histamine H2 receptor antagonism on the right atrium of the guinea pigHistamine H2 receptor antagonism on the right atrium of the guinea pig
ChEMBL 242 5 2 2 3.2 CC(C)C/N=C/Nc1ccc(-c2c[nH]cn2)cc1 10.1021/jm00110a004
CHEMBL298859 11924 1 None - 0 Guinea pig 8.3 pKd = 8.3 Functional
Histamine H2 receptor antagonism on the right atrium of the guinea pigHistamine H2 receptor antagonism on the right atrium of the guinea pig
ChEMBL 242 5 2 2 3.2 CC(C)C/N=C/Nc1ccc(-c2c[nH]cn2)cc1 10.1021/jm00110a004
135881774 99184 0 None - 0 Rat 7.3 pKd = 7.3 Functional
Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.
ChEMBL 415 10 4 8 2.0 CC(C)(C)OC(=O)NCCCC(=O)NCCSCc1csc(C=C(N)N)n1 10.1016/S0960-894X(96)00249-1
CHEMBL284374 99184 0 None - 0 Rat 7.3 pKd = 7.3 Functional
Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.
ChEMBL 415 10 4 8 2.0 CC(C)(C)OC(=O)NCCCC(=O)NCCSCc1csc(C=C(N)N)n1 10.1016/S0960-894X(96)00249-1
44281004 99604 0 None - 3 Rat 6.3 pKd = 6.3 Functional
Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.
ChEMBL 773 15 4 8 6.4 Cc1cccc(NC(=O)N[C@@H]2N=C(c3cccc(OC(=O)NCCCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00249-1
CHEMBL287295 99604 0 None - 3 Rat 6.3 pKd = 6.3 Functional
Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.
ChEMBL 773 15 4 8 6.4 Cc1cccc(NC(=O)N[C@@H]2N=C(c3cccc(OC(=O)NCCCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00249-1
44280029 95981 0 None - 3 Rat 6.3 pKd = 6.3 Functional
Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats
ChEMBL 740 15 6 9 3.5 CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCCC(=O)NCCSCc3csc(N=C(N)N)n3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00248-X
CHEMBL262125 95981 0 None - 3 Rat 6.3 pKd = 6.3 Functional
Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats
ChEMBL 740 15 6 9 3.5 CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCCC(=O)NCCSCc3csc(N=C(N)N)n3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00248-X
44280373 98916 0 None - 3 Rat 6.3 pKd = 6.3 Functional
Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats
ChEMBL 773 16 4 8 5.4 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL282646 98916 0 None - 3 Rat 6.3 pKd = 6.3 Functional
Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats
ChEMBL 773 16 4 8 5.4 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
44280388 116356 0 None - 3 Rat 6.3 pKd = 6.3 Functional
Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats
ChEMBL 759 15 4 8 5.0 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL33819 116356 0 None - 3 Rat 6.3 pKd = 6.3 Functional
Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats
ChEMBL 759 15 4 8 5.0 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
44279862 98660 0 None - 3 Rat 5.3 pKd = 5.3 Functional
Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats
ChEMBL 702 13 3 7 5.9 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL281017 98660 0 None - 3 Rat 5.3 pKd = 5.3 Functional
Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats
ChEMBL 702 13 3 7 5.9 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
44280213 101134 0 None - 3 Rat 5.3 pKd = 5.3 Functional
Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats
ChEMBL 685 12 5 9 3.7 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCSCc4csc(N=C(N)N)n4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL29888 101134 0 None - 3 Rat 5.3 pKd = 5.3 Functional
Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats
ChEMBL 685 12 5 9 3.7 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCSCc4csc(N=C(N)N)n4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
126688 400 28 None -1 3 Guinea pig 5.3 pKd = 5.3 Functional
Compound is evaluated for histamine H2 receptor agonistic activity in guinea pig cerebral cortex using [3H]tiotidine as radioligandCompound is evaluated for histamine H2 receptor agonistic activity in guinea pig cerebral cortex using [3H]tiotidine as radioligand
ChEMBL 157 2 2 4 0.5 NCCc1sc(nc1C)N 10.1021/jm00095a021
4025 400 28 None -1 3 Guinea pig 5.3 pKd = 5.3 Functional
Compound is evaluated for histamine H2 receptor agonistic activity in guinea pig cerebral cortex using [3H]tiotidine as radioligandCompound is evaluated for histamine H2 receptor agonistic activity in guinea pig cerebral cortex using [3H]tiotidine as radioligand
ChEMBL 157 2 2 4 0.5 NCCc1sc(nc1C)N 10.1021/jm00095a021
CHEMBL293762 400 28 None -1 3 Guinea pig 5.3 pKd = 5.3 Functional
Compound is evaluated for histamine H2 receptor agonistic activity in guinea pig cerebral cortex using [3H]tiotidine as radioligandCompound is evaluated for histamine H2 receptor agonistic activity in guinea pig cerebral cortex using [3H]tiotidine as radioligand
ChEMBL 157 2 2 4 0.5 NCCc1sc(nc1C)N 10.1021/jm00095a021
11436304 11217 0 None - 0 Guinea pig 5.3 pKd = 5.3 Functional
Functional H2 receptor antagonistic activity in vitro assay on the isolated spontaneously beating guinea-pig right atriumFunctional H2 receptor antagonistic activity in vitro assay on the isolated spontaneously beating guinea-pig right atrium
ChEMBL 236 8 1 2 3.3 c1nc(CCCOCCCC2CCCC2)c[nH]1 10.1021/jm031065q
CHEMBL1179594 11217 0 None - 0 Guinea pig 5.3 pKd = 5.3 Functional
Functional H2 receptor antagonistic activity in vitro assay on the isolated spontaneously beating guinea-pig right atriumFunctional H2 receptor antagonistic activity in vitro assay on the isolated spontaneously beating guinea-pig right atrium
ChEMBL 236 8 1 2 3.3 c1nc(CCCOCCCC2CCCC2)c[nH]1 10.1021/jm031065q
CHEMBL88306 11217 0 None - 0 Guinea pig 5.3 pKd = 5.3 Functional
Functional H2 receptor antagonistic activity in vitro assay on the isolated spontaneously beating guinea-pig right atriumFunctional H2 receptor antagonistic activity in vitro assay on the isolated spontaneously beating guinea-pig right atrium
ChEMBL 236 8 1 2 3.3 c1nc(CCCOCCCC2CCCC2)c[nH]1 10.1021/jm031065q
11345716 11224 0 None - 0 Guinea pig 4.3 pKd = 4.3 Functional
Functional H2 receptor antagonistic activity in vitro assay on the isolated spontaneously beating guinea-pig right atriumFunctional H2 receptor antagonistic activity in vitro assay on the isolated spontaneously beating guinea-pig right atrium
ChEMBL 250 8 1 2 3.7 c1nc(CCCOCCCC2CCCCC2)c[nH]1 10.1021/jm031065q
CHEMBL1179627 11224 0 None - 0 Guinea pig 4.3 pKd = 4.3 Functional
Functional H2 receptor antagonistic activity in vitro assay on the isolated spontaneously beating guinea-pig right atriumFunctional H2 receptor antagonistic activity in vitro assay on the isolated spontaneously beating guinea-pig right atrium
ChEMBL 250 8 1 2 3.7 c1nc(CCCOCCCC2CCCCC2)c[nH]1 10.1021/jm031065q
CHEMBL89999 11224 0 None - 0 Guinea pig 4.3 pKd = 4.3 Functional
Functional H2 receptor antagonistic activity in vitro assay on the isolated spontaneously beating guinea-pig right atriumFunctional H2 receptor antagonistic activity in vitro assay on the isolated spontaneously beating guinea-pig right atrium
ChEMBL 250 8 1 2 3.7 c1nc(CCCOCCCC2CCCCC2)c[nH]1 10.1021/jm031065q
9997754 102612 0 None - 0 Guinea pig 6.2 pKd = 6.2 Functional
Antagonistic activity against H2 receptor in guinea pig.Antagonistic activity against H2 receptor in guinea pig.
ChEMBL 346 9 4 5 1.3 Cc1[nH]cnc1CSCC/N=C(\NC#N)NCCCc1c[nH]cn1 10.1021/jm00148a007
CHEMBL30761 102612 0 None - 0 Guinea pig 6.2 pKd = 6.2 Functional
Antagonistic activity against H2 receptor in guinea pig.Antagonistic activity against H2 receptor in guinea pig.
ChEMBL 346 9 4 5 1.3 Cc1[nH]cnc1CSCC/N=C(\NC#N)NCCCc1c[nH]cn1 10.1021/jm00148a007
44281205 114307 0 None - 3 Rat 6.2 pKd = 6.2 Functional
Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.
ChEMBL 857 17 4 10 5.1 CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCCN3CCN(C(=O)CNCCCOc4cccc(CN5CCCCC5)c4)CC3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
CHEMBL33412 114307 0 None - 3 Rat 6.2 pKd = 6.2 Functional
Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.
ChEMBL 857 17 4 10 5.1 CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCCN3CCN(C(=O)CNCCCOc4cccc(CN5CCCCC5)c4)CC3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
44279809 98497 0 None - 3 Rat 6.2 pKd = 6.2 Functional
Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats
ChEMBL 785 18 4 7 6.4 CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00248-X
CHEMBL279778 98497 0 None - 3 Rat 6.2 pKd = 6.2 Functional
Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats
ChEMBL 785 18 4 7 6.4 CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00248-X
44280371 102541 0 None - 3 Rat 6.2 pKd = 6.2 Functional
Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats
ChEMBL 815 19 4 8 6.6 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCCCCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL30701 102541 0 None - 3 Rat 6.2 pKd = 6.2 Functional
Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats
ChEMBL 815 19 4 8 6.6 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCCCCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
44280214 106805 0 None - 3 Rat 6.2 pKd = 6.2 Functional
Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats
ChEMBL 770 16 6 10 3.6 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCCC(=O)NCCSCc4csc(N=C(N)N)n4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL31726 106805 0 None - 3 Rat 6.2 pKd = 6.2 Functional
Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats
ChEMBL 770 16 6 10 3.6 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCCC(=O)NCCSCc4csc(N=C(N)N)n4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
13499406 100976 0 None - 0 Guinea pig 5.2 pKd = 5.2 Functional
Antagonistic activity against H2 receptor in guinea pig.Antagonistic activity against H2 receptor in guinea pig.
ChEMBL 322 9 4 4 1.6 Cc1[nH]cnc1CSCCNC(=O)NCCCc1c[nH]cn1 10.1021/jm00148a007
CHEMBL29770 100976 0 None - 0 Guinea pig 5.2 pKd = 5.2 Functional
Antagonistic activity against H2 receptor in guinea pig.Antagonistic activity against H2 receptor in guinea pig.
ChEMBL 322 9 4 4 1.6 Cc1[nH]cnc1CSCCNC(=O)NCCCc1c[nH]cn1 10.1021/jm00148a007
44280266 98309 0 None - 3 Rat 5.2 pKd = 5.2 Functional
Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats
ChEMBL 729 14 4 7 5.0 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL278217 98309 0 None - 3 Rat 5.2 pKd = 5.2 Functional
Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats
ChEMBL 729 14 4 7 5.0 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1 10.1016/S0960-894X(96)00248-X
13499389 13000 0 None - 0 Guinea pig 4.2 pKd = 4.2 Functional
Antagonistic activity against H2 receptor in guinea pig.Antagonistic activity against H2 receptor in guinea pig.
ChEMBL 198 4 2 3 0.6 C/N=C(\N)NCCCc1nccs1 10.1021/jm00148a007
CHEMBL1190496 13000 0 None - 0 Guinea pig 4.2 pKd = 4.2 Functional
Antagonistic activity against H2 receptor in guinea pig.Antagonistic activity against H2 receptor in guinea pig.
ChEMBL 198 4 2 3 0.6 C/N=C(\N)NCCCc1nccs1 10.1021/jm00148a007
CHEMBL541027 13000 0 None - 0 Guinea pig 4.2 pKd = 4.2 Functional
Antagonistic activity against H2 receptor in guinea pig.Antagonistic activity against H2 receptor in guinea pig.
ChEMBL 198 4 2 3 0.6 C/N=C(\N)NCCCc1nccs1 10.1021/jm00148a007
11356502 11218 0 None - 0 Guinea pig 4.2 pKd = 4.2 Functional
Functional H2 receptor antagonistic activity in vitro assay on the isolated spontaneously beating guinea-pig right atriumFunctional H2 receptor antagonistic activity in vitro assay on the isolated spontaneously beating guinea-pig right atrium
ChEMBL 222 6 1 2 3.3 c1nc(COCCCC2CCCCC2)c[nH]1 10.1021/jm031065q
CHEMBL1179596 11218 0 None - 0 Guinea pig 4.2 pKd = 4.2 Functional
Functional H2 receptor antagonistic activity in vitro assay on the isolated spontaneously beating guinea-pig right atriumFunctional H2 receptor antagonistic activity in vitro assay on the isolated spontaneously beating guinea-pig right atrium
ChEMBL 222 6 1 2 3.3 c1nc(COCCCC2CCCCC2)c[nH]1 10.1021/jm031065q
CHEMBL88362 11218 0 None - 0 Guinea pig 4.2 pKd = 4.2 Functional
Functional H2 receptor antagonistic activity in vitro assay on the isolated spontaneously beating guinea-pig right atriumFunctional H2 receptor antagonistic activity in vitro assay on the isolated spontaneously beating guinea-pig right atrium
ChEMBL 222 6 1 2 3.3 c1nc(COCCCC2CCCCC2)c[nH]1 10.1021/jm031065q
44292856 100967 0 None - 0 Guinea pig 4.2 pKd = 4.2 Functional
Histamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atriumHistamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atrium
ChEMBL 718 13 5 9 4.5 N#CN/C(=N\CCNC(=O)c1ccc(C2c3ccc(O)cc3OC3=CC(=O)C=CC32)c(C(=O)O)c1)NCCCOc1cccc(CN2CCCCC2)c1 10.1016/s0960-894x(03)00235-x
CHEMBL297627 100967 0 None - 0 Guinea pig 4.2 pKd = 4.2 Functional
Histamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atriumHistamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atrium
ChEMBL 718 13 5 9 4.5 N#CN/C(=N\CCNC(=O)c1ccc(C2c3ccc(O)cc3OC3=CC(=O)C=CC32)c(C(=O)O)c1)NCCCOc1cccc(CN2CCCCC2)c1 10.1016/s0960-894x(03)00235-x
12810814 13156 0 None - 0 Guinea pig 5.2 pKd = 5.2 Functional
Antagonistic activity against H2 receptor in guinea pig.Antagonistic activity against H2 receptor in guinea pig.
ChEMBL 244 5 3 4 1.8 CSC(=N)NCCSCc1[nH]cnc1C 10.1021/jm00148a007
CHEMBL1191682 13156 0 None - 0 Guinea pig 5.2 pKd = 5.2 Functional
Antagonistic activity against H2 receptor in guinea pig.Antagonistic activity against H2 receptor in guinea pig.
ChEMBL 244 5 3 4 1.8 CSC(=N)NCCSCc1[nH]cnc1C 10.1021/jm00148a007
CHEMBL542817 13156 0 None - 0 Guinea pig 5.2 pKd = 5.2 Functional
Antagonistic activity against H2 receptor in guinea pig.Antagonistic activity against H2 receptor in guinea pig.
ChEMBL 244 5 3 4 1.8 CSC(=N)NCCSCc1[nH]cnc1C 10.1021/jm00148a007
1204 1893 114 None -14 11 Guinea pig 4.2 pKd = 4.2 Functional
Compound is evaluated for histamine H2 receptor agonistic activity in guinea pig cerebral cortex using [3H]tiotidine as radioligandCompound is evaluated for histamine H2 receptor agonistic activity in guinea pig cerebral cortex using [3H]tiotidine as radioligand
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm00095a021
1247 1893 114 None -14 11 Guinea pig 4.2 pKd = 4.2 Functional
Compound is evaluated for histamine H2 receptor agonistic activity in guinea pig cerebral cortex using [3H]tiotidine as radioligandCompound is evaluated for histamine H2 receptor agonistic activity in guinea pig cerebral cortex using [3H]tiotidine as radioligand
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm00095a021
1375 1893 114 None -14 11 Guinea pig 4.2 pKd = 4.2 Functional
Compound is evaluated for histamine H2 receptor agonistic activity in guinea pig cerebral cortex using [3H]tiotidine as radioligandCompound is evaluated for histamine H2 receptor agonistic activity in guinea pig cerebral cortex using [3H]tiotidine as radioligand
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm00095a021
774 1893 114 None -14 11 Guinea pig 4.2 pKd = 4.2 Functional
Compound is evaluated for histamine H2 receptor agonistic activity in guinea pig cerebral cortex using [3H]tiotidine as radioligandCompound is evaluated for histamine H2 receptor agonistic activity in guinea pig cerebral cortex using [3H]tiotidine as radioligand
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm00095a021
CHEMBL90 1893 114 None -14 11 Guinea pig 4.2 pKd = 4.2 Functional
Compound is evaluated for histamine H2 receptor agonistic activity in guinea pig cerebral cortex using [3H]tiotidine as radioligandCompound is evaluated for histamine H2 receptor agonistic activity in guinea pig cerebral cortex using [3H]tiotidine as radioligand
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm00095a021
DB05381 1893 114 None -14 11 Guinea pig 4.2 pKd = 4.2 Functional
Compound is evaluated for histamine H2 receptor agonistic activity in guinea pig cerebral cortex using [3H]tiotidine as radioligandCompound is evaluated for histamine H2 receptor agonistic activity in guinea pig cerebral cortex using [3H]tiotidine as radioligand
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm00095a021
44294891 11925 0 None - 0 Guinea pig 8.1 pKd = 8.1 Functional
Histamine H2 receptor antagonism on the right atrium of the guinea pigHistamine H2 receptor antagonism on the right atrium of the guinea pig
ChEMBL 256 5 2 2 3.5 CCC(C)(C)N/C=N/c1ccc(-c2c[nH]cn2)cc1 10.1021/jm00110a004
CHEMBL1183478 11925 0 None - 0 Guinea pig 8.1 pKd = 8.1 Functional
Histamine H2 receptor antagonism on the right atrium of the guinea pigHistamine H2 receptor antagonism on the right atrium of the guinea pig
ChEMBL 256 5 2 2 3.5 CCC(C)(C)N/C=N/c1ccc(-c2c[nH]cn2)cc1 10.1021/jm00110a004
CHEMBL299537 11925 0 None - 0 Guinea pig 8.1 pKd = 8.1 Functional
Histamine H2 receptor antagonism on the right atrium of the guinea pigHistamine H2 receptor antagonism on the right atrium of the guinea pig
ChEMBL 256 5 2 2 3.5 CCC(C)(C)N/C=N/c1ccc(-c2c[nH]cn2)cc1 10.1021/jm00110a004
13499375 100980 0 None - 0 Guinea pig 6.1 pKd = 6.1 Functional
Antagonistic activity against H2 receptor in guinea pig.Antagonistic activity against H2 receptor in guinea pig.
ChEMBL 370 10 3 6 2.2 Cc1[nH]cnc1CSCC/N=C(\N)NCCSCc1nccs1 10.1021/jm00148a007
CHEMBL1744351 100980 0 None - 0 Guinea pig 6.1 pKd = 6.1 Functional
Antagonistic activity against H2 receptor in guinea pig.Antagonistic activity against H2 receptor in guinea pig.
ChEMBL 370 10 3 6 2.2 Cc1[nH]cnc1CSCC/N=C(\N)NCCSCc1nccs1 10.1021/jm00148a007
CHEMBL29771 100980 0 None - 0 Guinea pig 6.1 pKd = 6.1 Functional
Antagonistic activity against H2 receptor in guinea pig.Antagonistic activity against H2 receptor in guinea pig.
ChEMBL 370 10 3 6 2.2 Cc1[nH]cnc1CSCC/N=C(\N)NCCSCc1nccs1 10.1021/jm00148a007
44280996 99270 0 None - 3 Rat 6.1 pKd = 6.1 Functional
Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.
ChEMBL 745 14 4 8 5.4 CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
CHEMBL284976 99270 0 None - 3 Rat 6.1 pKd = 6.1 Functional
Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.
ChEMBL 745 14 4 8 5.4 CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
CHEMBL285995 99417 0 None - 3 Rat 6.1 pKd = 6.1 Functional
Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.
ChEMBL 741 16 6 11 4.5 CN1C(=O)[C@H](NC(=O)Nc2cccc(CCOC(=O)NCCCNCCSCc3csc(C=C(N)N)n3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
44280215 99356 0 None - 3 Rat 6.1 pKd = 6.1 Functional
Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats
ChEMBL 756 15 6 10 3.3 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCC(=O)NCCSCc4csc(N=C(N)N)n4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL285586 99356 0 None - 3 Rat 6.1 pKd = 6.1 Functional
Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats
ChEMBL 756 15 6 10 3.3 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCC(=O)NCCSCc4csc(N=C(N)N)n4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
44280225 99488 0 None - 3 Rat 6.1 pKd = 6.1 Functional
Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats
ChEMBL 743 15 4 7 5.4 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL286475 99488 0 None - 3 Rat 6.1 pKd = 6.1 Functional
Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats
ChEMBL 743 15 4 7 5.4 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1 10.1016/S0960-894X(96)00248-X
44280224 104292 0 None - 3 Rat 6.1 pKd = 6.1 Functional
Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats
ChEMBL 757 16 4 7 5.8 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL31090 104292 0 None - 3 Rat 6.1 pKd = 6.1 Functional
Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats
ChEMBL 757 16 4 7 5.8 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1 10.1016/S0960-894X(96)00248-X
44292855 100928 0 None - 0 Guinea pig 5.1 pKd = 5.1 Functional
Histamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atriumHistamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atrium
ChEMBL 746 15 5 9 5.2 N#CN/C(=N\CCCCNC(=O)c1ccc(C2c3ccc(O)cc3OC3=CC(=O)C=CC32)c(C(=O)O)c1)NCCCOc1cccc(CN2CCCCC2)c1 10.1016/s0960-894x(03)00235-x
CHEMBL297324 100928 0 None - 0 Guinea pig 5.1 pKd = 5.1 Functional
Histamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atriumHistamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atrium
ChEMBL 746 15 5 9 5.2 N#CN/C(=N\CCCCNC(=O)c1ccc(C2c3ccc(O)cc3OC3=CC(=O)C=CC32)c(C(=O)O)c1)NCCCOc1cccc(CN2CCCCC2)c1 10.1016/s0960-894x(03)00235-x
1231 922 112 None -11 4 Guinea pig 6.0 pKd = 6.0 Functional
Antagonistic activity against Histamine H2 receptor expressed as the charge of receptor sensitivity was determined at pH 7.0Antagonistic activity against Histamine H2 receptor expressed as the charge of receptor sensitivity was determined at pH 7.0
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/jm00384a036
2756 922 112 None -11 4 Guinea pig 6.0 pKd = 6.0 Functional
Antagonistic activity against Histamine H2 receptor expressed as the charge of receptor sensitivity was determined at pH 7.0Antagonistic activity against Histamine H2 receptor expressed as the charge of receptor sensitivity was determined at pH 7.0
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/jm00384a036
645 922 112 None -11 4 Guinea pig 6.0 pKd = 6.0 Functional
Antagonistic activity against Histamine H2 receptor expressed as the charge of receptor sensitivity was determined at pH 7.0Antagonistic activity against Histamine H2 receptor expressed as the charge of receptor sensitivity was determined at pH 7.0
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/jm00384a036
CHEMBL30 922 112 None -11 4 Guinea pig 6.0 pKd = 6.0 Functional
Antagonistic activity against Histamine H2 receptor expressed as the charge of receptor sensitivity was determined at pH 7.0Antagonistic activity against Histamine H2 receptor expressed as the charge of receptor sensitivity was determined at pH 7.0
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/jm00384a036
DB00501 922 112 None -11 4 Guinea pig 6.0 pKd = 6.0 Functional
Antagonistic activity against Histamine H2 receptor expressed as the charge of receptor sensitivity was determined at pH 7.0Antagonistic activity against Histamine H2 receptor expressed as the charge of receptor sensitivity was determined at pH 7.0
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/jm00384a036
54754351 67860 0 None - 0 Human 5.5 pKi = 5.5 Functional
Antagonist activity at histamine H2 receptorAntagonist activity at histamine H2 receptor
ChEMBL 277 4 1 5 2.1 CN1CCN(c2cc(NCCC(C)(C)C)ncn2)CC1 10.1016/j.bmcl.2011.07.114
CHEMBL1915535 67860 0 None - 0 Human 5.5 pKi = 5.5 Functional
Antagonist activity at histamine H2 receptorAntagonist activity at histamine H2 receptor
ChEMBL 277 4 1 5 2.1 CN1CCN(c2cc(NCCC(C)(C)C)ncn2)CC1 10.1016/j.bmcl.2011.07.114
57395620 67859 0 None - 0 Human 5.1 pKi = 5.1 Functional
Antagonist activity at histamine H2 receptorAntagonist activity at histamine H2 receptor
ChEMBL 263 5 3 5 2.1 CC(C)(C)CCNc1cc(N[C@H]2CCNC2)ncn1 10.1016/j.bmcl.2011.07.114
CHEMBL1915534 67859 0 None - 0 Human 5.1 pKi = 5.1 Functional
Antagonist activity at histamine H2 receptorAntagonist activity at histamine H2 receptor
ChEMBL 263 5 3 5 2.1 CC(C)(C)CCNc1cc(N[C@H]2CCNC2)ncn1 10.1016/j.bmcl.2011.07.114
1204 1893 114 None -14 11 Guinea pig 8.2 pEC50 = 8.2 Functional
Agonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 minsAgonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 mins
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1893 114 None -14 11 Guinea pig 8.2 pEC50 = 8.2 Functional
Agonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 minsAgonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 mins
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1893 114 None -14 11 Guinea pig 8.2 pEC50 = 8.2 Functional
Agonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 minsAgonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 mins
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1893 114 None -14 11 Guinea pig 8.2 pEC50 = 8.2 Functional
Agonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 minsAgonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 mins
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1893 114 None -14 11 Guinea pig 8.2 pEC50 = 8.2 Functional
Agonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 minsAgonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 mins
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1893 114 None -14 11 Guinea pig 8.2 pEC50 = 8.2 Functional
Agonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 minsAgonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 mins
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
126688 400 28 None 1 3 Human 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 157 2 2 4 0.5 NCCc1sc(nc1C)N 19072936
4025 400 28 None 1 3 Human 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 157 2 2 4 0.5 NCCc1sc(nc1C)N 19072936
CHEMBL293762 400 28 None 1 3 Human 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 157 2 2 4 0.5 NCCc1sc(nc1C)N 19072936
1229 730 0 None - 1 Human 5.7 pEC50 None 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 262 5 3 2 2.0 CNC(=S)NCCCCc1cccc2c1cn[nH]2 9681472
5311293 730 0 None - 1 Human 5.7 pEC50 None 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 262 5 3 2 2.0 CNC(=S)NCCCCc1cccc2c1cn[nH]2 9681472
18381 215965 0 None 1 4 Human 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 469 4 2 6 3.2 CC1=C(C(=O)N[C@H]2[C@H]3SC(C)(C)[C@@H](N3C2=O)C(O)=O)C(=NO1)C1=C(Cl)C=CC=C1Cl None
30699 215959 0 None -1 14 Human 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 423 7 2 8 0.5 CC(=O)OCC1=C(N2[C@H](SC1)[C@H](NC(=O)CSC1=CC=NC=C1)C2=O)C(O)=O None
180 397 50 None -151 27 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 397 50 None -151 27 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 397 50 None -151 27 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 397 50 None -151 27 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 397 50 None -151 27 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
46780481 107032 18 None - 1 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 107032 18 None - 1 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 107032 18 None - 1 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 107032 18 None - 1 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None




Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Affinity)
# tested GPCRs
(Affinity)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
90667234 108972 0 None 3 2 Guinea pig 7.0 pEC50 = 7 Binding
Agonist activity at guinea pig histamine H2 receptor assessed as potentiation of cimetidine-induced response at after 30 minsAgonist activity at guinea pig histamine H2 receptor assessed as potentiation of cimetidine-induced response at after 30 mins
ChEMBL 314 7 3 3 1.4 CC(CC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1039/C3MD00245D
CHEMBL3220635 108972 0 None 3 2 Guinea pig 7.0 pEC50 = 7 Binding
Agonist activity at guinea pig histamine H2 receptor assessed as potentiation of cimetidine-induced response at after 30 minsAgonist activity at guinea pig histamine H2 receptor assessed as potentiation of cimetidine-induced response at after 30 mins
ChEMBL 314 7 3 3 1.4 CC(CC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1039/C3MD00245D
1204 1893 114 None -794 25 Guinea pig 6.0 pEC50 = 6 Binding
Agonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 minsAgonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 mins
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
1247 1893 114 None -794 25 Guinea pig 6.0 pEC50 = 6 Binding
Agonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 minsAgonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 mins
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
1375 1893 114 None -794 25 Guinea pig 6.0 pEC50 = 6 Binding
Agonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 minsAgonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 mins
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
774 1893 114 None -794 25 Guinea pig 6.0 pEC50 = 6 Binding
Agonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 minsAgonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 mins
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
CHEMBL90 1893 114 None -794 25 Guinea pig 6.0 pEC50 = 6 Binding
Agonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 minsAgonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 mins
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
DB05381 1893 114 None -794 25 Guinea pig 6.0 pEC50 = 6 Binding
Agonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 minsAgonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 mins
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
11741669 96292 0 None - 2 Guinea pig 5.0 pEC50 = 5 Binding
Tested for inhibition of histamine H2 receptor-induced rise in heart rate in guinea pig right atrium in the presence of mepyramine at a concentration of 0.3 micro MTested for inhibition of histamine H2 receptor-induced rise in heart rate in guinea pig right atrium in the presence of mepyramine at a concentration of 0.3 micro M
ChEMBL 399 11 3 3 4.3 c1ccc(C(CCc2nc(CCNCCc3cnc[nH]3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
CHEMBL264491 96292 0 None - 2 Guinea pig 5.0 pEC50 = 5 Binding
Tested for inhibition of histamine H2 receptor-induced rise in heart rate in guinea pig right atrium in the presence of mepyramine at a concentration of 0.3 micro MTested for inhibition of histamine H2 receptor-induced rise in heart rate in guinea pig right atrium in the presence of mepyramine at a concentration of 0.3 micro M
ChEMBL 399 11 3 3 4.3 c1ccc(C(CCc2nc(CCNCCc3cnc[nH]3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
25149708 187842 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Activity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay
ChEMBL 319 7 4 4 2.2 CC(CC(=O)NC(=N)NCCCc1c[nH]cn1)c1cccs1 10.1021/jm800841w
CHEMBL502339 187842 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Activity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay
ChEMBL 319 7 4 4 2.2 CC(CC(=O)NC(=N)NCCCc1c[nH]cn1)c1cccs1 10.1021/jm800841w
42625304 178512 0 None - 2 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 237 5 3 2 0.4 CC(C)C(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL471724 178512 0 None - 2 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 237 5 3 2 0.4 CC(C)C(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
25149335 183633 0 None - 1 Guinea pig 7.9 pEC50 = 7.9 Binding
Activity at guinea pig recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at guinea pig recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1021/jm800841w
CHEMBL483406 183633 0 None - 1 Guinea pig 7.9 pEC50 = 7.9 Binding
Activity at guinea pig recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at guinea pig recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1021/jm800841w
25149613 178611 0 None - 1 Human 6.9 pEC50 = 6.9 Binding
Activity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay
ChEMBL 382 8 4 5 2.7 N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1nccs1 10.1021/jm800841w
CHEMBL472441 178611 0 None - 1 Human 6.9 pEC50 = 6.9 Binding
Activity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay
ChEMBL 382 8 4 5 2.7 N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1nccs1 10.1021/jm800841w
1204 1893 114 None -794 25 Guinea pig 5.9 pEC50 = 5.9 Binding
Activity at guinea pig recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at guinea pig recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm800841w
1247 1893 114 None -794 25 Guinea pig 5.9 pEC50 = 5.9 Binding
Activity at guinea pig recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at guinea pig recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm800841w
1375 1893 114 None -794 25 Guinea pig 5.9 pEC50 = 5.9 Binding
Activity at guinea pig recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at guinea pig recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm800841w
774 1893 114 None -794 25 Guinea pig 5.9 pEC50 = 5.9 Binding
Activity at guinea pig recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at guinea pig recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm800841w
CHEMBL90 1893 114 None -794 25 Guinea pig 5.9 pEC50 = 5.9 Binding
Activity at guinea pig recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at guinea pig recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm800841w
DB05381 1893 114 None -794 25 Guinea pig 5.9 pEC50 = 5.9 Binding
Activity at guinea pig recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at guinea pig recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm800841w
1204 1893 114 None -173 25 Human 5.9 pEC50 = 5.9 Binding
Activity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm800841w
1247 1893 114 None -173 25 Human 5.9 pEC50 = 5.9 Binding
Activity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm800841w
1375 1893 114 None -173 25 Human 5.9 pEC50 = 5.9 Binding
Activity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm800841w
774 1893 114 None -173 25 Human 5.9 pEC50 = 5.9 Binding
Activity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm800841w
CHEMBL90 1893 114 None -173 25 Human 5.9 pEC50 = 5.9 Binding
Activity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm800841w
DB05381 1893 114 None -173 25 Human 5.9 pEC50 = 5.9 Binding
Activity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm800841w
1204 1893 114 None -173 25 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm9000693
1247 1893 114 None -173 25 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm9000693
1375 1893 114 None -173 25 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm9000693
774 1893 114 None -173 25 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm9000693
CHEMBL90 1893 114 None -173 25 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm9000693
DB05381 1893 114 None -173 25 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm9000693
1204 1893 114 None -173 25 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
1247 1893 114 None -173 25 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
1375 1893 114 None -173 25 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
774 1893 114 None -173 25 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
CHEMBL90 1893 114 None -173 25 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
DB05381 1893 114 None -173 25 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
46890166 7220 0 None - 2 Human 6.9 pEC50 = 6.9 Binding
Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cellsDisplacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells
ChEMBL 419 6 2 4 4.5 Cc1cc(OCCCN2CCc3nc[nH]c3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1086105 7220 0 None - 2 Human 6.9 pEC50 = 6.9 Binding
Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cellsDisplacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells
ChEMBL 419 6 2 4 4.5 Cc1cc(OCCCN2CCc3nc[nH]c3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
25149613 178611 0 None - 1 Guinea pig 7.9 pEC50 = 7.9 Binding
Activity at guinea pig recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at guinea pig recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay
ChEMBL 382 8 4 5 2.7 N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1nccs1 10.1021/jm800841w
CHEMBL472441 178611 0 None - 1 Guinea pig 7.9 pEC50 = 7.9 Binding
Activity at guinea pig recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at guinea pig recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay
ChEMBL 382 8 4 5 2.7 N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1nccs1 10.1021/jm800841w
42625386 177768 0 None - 2 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 237 6 3 2 0.6 CCCC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL465170 177768 0 None - 2 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 237 6 3 2 0.6 CCCC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
25149335 183633 0 None - 1 Guinea pig 7.8 pEC50 = 7.8 Binding
Agonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 minsAgonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 mins
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1039/C3MD00245D
CHEMBL483406 183633 0 None - 1 Guinea pig 7.8 pEC50 = 7.8 Binding
Agonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 minsAgonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 mins
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1039/C3MD00245D
90667262 108979 0 None - 0 Guinea pig 6.7 pEC50 = 6.7 Binding
Agonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 minsAgonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 mins
ChEMBL 324 7 2 2 2.6 CC(CC(=O)/N=C(\N)NCCCc1ccccn1)c1ccccc1 10.1039/C3MD00245D
CHEMBL3220665 108979 0 None - 0 Guinea pig 6.7 pEC50 = 6.7 Binding
Agonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 minsAgonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 mins
ChEMBL 324 7 2 2 2.6 CC(CC(=O)/N=C(\N)NCCCc1ccccn1)c1ccccc1 10.1039/C3MD00245D
90667235 108973 0 None - 1 Guinea pig 6.7 pEC50 = 6.7 Binding
Agonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 minsAgonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 mins
ChEMBL 376 8 3 3 2.4 N/C(=N\C(=O)CC(c1ccccc1)c1ccccc1)NCCCc1ncn[nH]1 10.1039/C3MD00245D
CHEMBL3220636 108973 0 None - 1 Guinea pig 6.7 pEC50 = 6.7 Binding
Agonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 minsAgonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 mins
ChEMBL 376 8 3 3 2.4 N/C(=N\C(=O)CC(c1ccccc1)c1ccccc1)NCCCc1ncn[nH]1 10.1039/C3MD00245D
25149708 187842 0 None - 0 Guinea pig 7.7 pEC50 = 7.7 Binding
Activity at guinea pig recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at guinea pig recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay
ChEMBL 319 7 4 4 2.2 CC(CC(=O)NC(=N)NCCCc1c[nH]cn1)c1cccs1 10.1021/jm800841w
CHEMBL502339 187842 0 None - 0 Guinea pig 7.7 pEC50 = 7.7 Binding
Activity at guinea pig recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at guinea pig recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay
ChEMBL 319 7 4 4 2.2 CC(CC(=O)NC(=N)NCCCc1c[nH]cn1)c1cccs1 10.1021/jm800841w
90667232 108970 0 None - 1 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1cn[nH]c1)c1ccccc1 10.1039/C3MD00245D
CHEMBL3220633 108970 0 None - 1 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1cn[nH]c1)c1ccccc1 10.1039/C3MD00245D
10103168 25884 5 None - 2 Human 5.6 pEC50 = 5.6 Binding
Inhibition of human Histamine H2 receptor using [3H]tiotidineInhibition of human Histamine H2 receptor using [3H]tiotidine
ChEMBL 123 1 2 2 0.2 N[C@@H]1C[C@H]1c1c[nH]cn1 10.1021/jm020415q
CHEMBL13559 25884 5 None - 2 Human 5.6 pEC50 = 5.6 Binding
Inhibition of human Histamine H2 receptor using [3H]tiotidineInhibition of human Histamine H2 receptor using [3H]tiotidine
ChEMBL 123 1 2 2 0.2 N[C@@H]1C[C@H]1c1c[nH]cn1 10.1021/jm020415q
182527 110066 7 None - 0 Human 5.6 pEC50 = 5.6 Binding
Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 167 4 4 2 -0.2 N=C(N)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL325327 110066 7 None - 0 Human 5.6 pEC50 = 5.6 Binding
Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 167 4 4 2 -0.2 N=C(N)NCCCc1c[nH]cn1 10.1021/jm9000693
42626110 179179 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 310 5 4 2 1.6 N/C(=N\C(=O)c1cc2ccccc2[nH]1)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL474448 179179 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 310 5 4 2 1.6 N/C(=N\C(=O)c1cc2ccccc2[nH]1)NCCCc1c[nH]cn1 10.1021/jm9000693
42625224 180172 0 None - 1 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 395 9 5 3 1.5 N/C(=N\C(=O)CCCNC(=O)c1cc2ccccc2[nH]1)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL475620 180172 0 None - 1 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 395 9 5 3 1.5 N/C(=N\C(=O)CCCNC(=O)c1cc2ccccc2[nH]1)NCCCc1c[nH]cn1 10.1021/jm9000693
42625223 179335 0 None - 1 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 395 8 4 3 1.4 CN(CCC(=O)/N=C(\N)NCCCc1c[nH]cn1)C(=O)c1cc2ccccc2[nH]1 10.1021/jm9000693
CHEMBL474617 179335 0 None - 1 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 395 8 4 3 1.4 CN(CCC(=O)/N=C(\N)NCCCc1c[nH]cn1)C(=O)c1cc2ccccc2[nH]1 10.1021/jm9000693
42626109 179178 0 None - 1 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 324 6 4 2 1.5 N/C(=N\C(=O)Cc1c[nH]c2ccccc12)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL474447 179178 0 None - 1 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 324 6 4 2 1.5 N/C(=N\C(=O)Cc1c[nH]c2ccccc12)NCCCc1c[nH]cn1 10.1021/jm9000693
90667233 108971 0 None - 1 Guinea pig 6.4 pEC50 = 6.4 Binding
Agonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 minsAgonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 mins
ChEMBL 375 8 3 2 3.0 N/C(=N\C(=O)CC(c1ccccc1)c1ccccc1)NCCCc1cn[nH]c1 10.1039/C3MD00245D
CHEMBL3220634 108971 0 None - 1 Guinea pig 6.4 pEC50 = 6.4 Binding
Agonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 minsAgonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 mins
ChEMBL 375 8 3 2 3.0 N/C(=N\C(=O)CC(c1ccccc1)c1ccccc1)NCCCc1cn[nH]c1 10.1039/C3MD00245D
42625303 180174 0 None - 2 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 223 5 3 2 0.2 CCC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL475621 180174 0 None - 2 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 223 5 3 2 0.2 CCC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
90667235 108973 0 None - 1 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
ChEMBL 376 8 3 3 2.4 N/C(=N\C(=O)CC(c1ccccc1)c1ccccc1)NCCCc1ncn[nH]1 10.1039/C3MD00245D
CHEMBL3220636 108973 0 None - 1 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
ChEMBL 376 8 3 3 2.4 N/C(=N\C(=O)CC(c1ccccc1)c1ccccc1)NCCCc1ncn[nH]1 10.1039/C3MD00245D
1204 1893 114 None -173 25 Human 6.3 pEC50 = 6.3 Binding
Inhibition of human Histamine H2 receptor using [3H]tiotidineInhibition of human Histamine H2 receptor using [3H]tiotidine
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm020415q
1247 1893 114 None -173 25 Human 6.3 pEC50 = 6.3 Binding
Inhibition of human Histamine H2 receptor using [3H]tiotidineInhibition of human Histamine H2 receptor using [3H]tiotidine
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm020415q
1375 1893 114 None -173 25 Human 6.3 pEC50 = 6.3 Binding
Inhibition of human Histamine H2 receptor using [3H]tiotidineInhibition of human Histamine H2 receptor using [3H]tiotidine
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm020415q
774 1893 114 None -173 25 Human 6.3 pEC50 = 6.3 Binding
Inhibition of human Histamine H2 receptor using [3H]tiotidineInhibition of human Histamine H2 receptor using [3H]tiotidine
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm020415q
CHEMBL90 1893 114 None -173 25 Human 6.3 pEC50 = 6.3 Binding
Inhibition of human Histamine H2 receptor using [3H]tiotidineInhibition of human Histamine H2 receptor using [3H]tiotidine
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm020415q
DB05381 1893 114 None -173 25 Human 6.3 pEC50 = 6.3 Binding
Inhibition of human Histamine H2 receptor using [3H]tiotidineInhibition of human Histamine H2 receptor using [3H]tiotidine
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm020415q
90667232 108970 0 None - 1 Guinea pig 6.3 pEC50 = 6.3 Binding
Agonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 minsAgonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 mins
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1cn[nH]c1)c1ccccc1 10.1039/C3MD00245D
CHEMBL3220633 108970 0 None - 1 Guinea pig 6.3 pEC50 = 6.3 Binding
Agonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 minsAgonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 mins
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1cn[nH]c1)c1ccccc1 10.1039/C3MD00245D
25149521 178464 0 None - 1 Guinea pig 8.2 pEC50 = 8.2 Binding
Activity at guinea pig recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at guinea pig recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay
ChEMBL 375 8 4 3 3.2 N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1ccccc1 10.1021/jm800841w
CHEMBL471413 178464 0 None - 1 Guinea pig 8.2 pEC50 = 8.2 Binding
Activity at guinea pig recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at guinea pig recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay
ChEMBL 375 8 4 3 3.2 N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1ccccc1 10.1021/jm800841w
25149335 183633 0 None - 1 Human 7.2 pEC50 = 7.2 Binding
Activity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1021/jm800841w
CHEMBL483406 183633 0 None - 1 Human 7.2 pEC50 = 7.2 Binding
Activity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1021/jm800841w
25149335 183633 0 None - 1 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1021/jm9000693
CHEMBL483406 183633 0 None - 1 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1021/jm9000693
25149335 183633 0 None - 1 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1039/C3MD00245D
CHEMBL483406 183633 0 None - 1 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1039/C3MD00245D
10374457 28667 2 None - 2 Human 6.2 pEC50 = 6.2 Binding
Inhibition of human Histamine H2 receptor using [3H]tiotidineInhibition of human Histamine H2 receptor using [3H]tiotidine
ChEMBL 123 1 2 2 0.2 N[C@H]1C[C@@H]1c1c[nH]cn1 10.1021/jm020415q
CHEMBL13795 28667 2 None - 2 Human 6.2 pEC50 = 6.2 Binding
Inhibition of human Histamine H2 receptor using [3H]tiotidineInhibition of human Histamine H2 receptor using [3H]tiotidine
ChEMBL 123 1 2 2 0.2 N[C@H]1C[C@@H]1c1c[nH]cn1 10.1021/jm020415q
42625384 169195 0 None - 2 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 209 4 3 2 -0.2 CC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL443896 169195 0 None - 2 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 209 4 3 2 -0.2 CC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
90667234 108972 0 None - 2 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
ChEMBL 314 7 3 3 1.4 CC(CC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1039/C3MD00245D
CHEMBL3220635 108972 0 None - 2 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
ChEMBL 314 7 3 3 1.4 CC(CC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1039/C3MD00245D
25149521 178464 0 None - 1 Human 7.1 pEC50 = 7.1 Binding
Activity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay
ChEMBL 375 8 4 3 3.2 N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1ccccc1 10.1021/jm800841w
CHEMBL471413 178464 0 None - 1 Human 7.1 pEC50 = 7.1 Binding
Activity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay
ChEMBL 375 8 4 3 3.2 N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1ccccc1 10.1021/jm800841w
42625221 188987 0 None - 2 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 338 7 4 2 1.9 N/C(=N\C(=O)CCc1c[nH]c2ccccc12)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL514641 188987 0 None - 2 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 338 7 4 2 1.9 N/C(=N\C(=O)CCc1c[nH]c2ccccc12)NCCCc1c[nH]cn1 10.1021/jm9000693
42626111 189092 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 381 8 5 3 1.1 N/C(=N\C(=O)CCNC(=O)c1cc2ccccc2[nH]1)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL515428 189092 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 381 8 5 3 1.1 N/C(=N\C(=O)CCNC(=O)c1cc2ccccc2[nH]1)NCCCc1c[nH]cn1 10.1021/jm9000693
90667262 108979 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
ChEMBL 324 7 2 2 2.6 CC(CC(=O)/N=C(\N)NCCCc1ccccn1)c1ccccc1 10.1039/C3MD00245D
CHEMBL3220665 108979 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
ChEMBL 324 7 2 2 2.6 CC(CC(=O)/N=C(\N)NCCCc1ccccn1)c1ccccc1 10.1039/C3MD00245D
11829635 162676 4 None - 1 Human 7.0 pEC50 = 7.0 Binding
Inhibition of human Histamine H2 receptor using [3H]tiotidineInhibition of human Histamine H2 receptor using [3H]tiotidine
ChEMBL 151 3 2 2 0.9 NCC[C@H]1C[C@H]1c1c[nH]cn1 10.1021/jm020415q
CHEMBL418470 162676 4 None - 1 Human 7.0 pEC50 = 7.0 Binding
Inhibition of human Histamine H2 receptor using [3H]tiotidineInhibition of human Histamine H2 receptor using [3H]tiotidine
ChEMBL 151 3 2 2 0.9 NCC[C@H]1C[C@H]1c1c[nH]cn1 10.1021/jm020415q
42625222 179180 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 367 7 5 3 0.7 N/C(=N\C(=O)CNC(=O)c1cc2ccccc2[nH]1)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL474449 179180 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 367 7 5 3 0.7 N/C(=N\C(=O)CNC(=O)c1cc2ccccc2[nH]1)NCCCc1c[nH]cn1 10.1021/jm9000693
11539632 70202 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibitory concentration against histamine H2 receptorInhibitory concentration against histamine H2 receptor
ChEMBL 447 8 1 5 4.8 Cc1cc(OCCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL194837 70202 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibitory concentration against histamine H2 receptorInhibitory concentration against histamine H2 receptor
ChEMBL 447 8 1 5 4.8 Cc1cc(OCCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
132609385 157538 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]-aminopotentidine receptor from histamine H2 receptor (unknown origin)Displacement of [125I]-aminopotentidine receptor from histamine H2 receptor (unknown origin)
ChEMBL 324 5 0 3 3.8 COc1ccc(CN2CCCN(Cc3ccccc3)[C@@H](C)C2)cc1 10.1016/j.bmc.2017.07.027
CHEMBL4086541 157538 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]-aminopotentidine receptor from histamine H2 receptor (unknown origin)Displacement of [125I]-aminopotentidine receptor from histamine H2 receptor (unknown origin)
ChEMBL 324 5 0 3 3.8 COc1ccc(CN2CCCN(Cc3ccccc3)[C@@H](C)C2)cc1 10.1016/j.bmc.2017.07.027
1231 922 112 None -2 8 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]APT from human recombinant H2 receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [125I]APT from human recombinant H2 receptor expressed in CHO cells measured after 120 mins by scintillation counting method
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/j.bmc.2016.11.014
2756 922 112 None -2 8 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]APT from human recombinant H2 receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [125I]APT from human recombinant H2 receptor expressed in CHO cells measured after 120 mins by scintillation counting method
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/j.bmc.2016.11.014
645 922 112 None -2 8 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]APT from human recombinant H2 receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [125I]APT from human recombinant H2 receptor expressed in CHO cells measured after 120 mins by scintillation counting method
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/j.bmc.2016.11.014
CHEMBL30 922 112 None -2 8 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]APT from human recombinant H2 receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [125I]APT from human recombinant H2 receptor expressed in CHO cells measured after 120 mins by scintillation counting method
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/j.bmc.2016.11.014
DB00501 922 112 None -2 8 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]APT from human recombinant H2 receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [125I]APT from human recombinant H2 receptor expressed in CHO cells measured after 120 mins by scintillation counting method
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/j.bmc.2016.11.014
1231 922 112 None -2 8 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cellsDisplacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/j.bmc.2016.03.006
2756 922 112 None -2 8 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cellsDisplacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/j.bmc.2016.03.006
645 922 112 None -2 8 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cellsDisplacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/j.bmc.2016.03.006
CHEMBL30 922 112 None -2 8 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cellsDisplacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/j.bmc.2016.03.006
DB00501 922 112 None -2 8 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cellsDisplacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/j.bmc.2016.03.006
17747460 60985 8 None - 4 Human 5.0 pIC50 = 5 Binding
Binding affinity to human histamine H2 receptorBinding affinity to human histamine H2 receptor
ChEMBL 640 14 0 6 7.8 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1 10.1021/jm1013874
CHEMBL1767164 60985 8 None - 4 Human 5.0 pIC50 = 5 Binding
Binding affinity to human histamine H2 receptorBinding affinity to human histamine H2 receptor
ChEMBL 640 14 0 6 7.8 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1 10.1021/jm1013874
10205121 66344 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 464 6 1 4 6.5 O=C(O)c1cccc(CN2CCC(c3cn(Cc4ccc(Cl)s4)c4ccccc34)CC2)c1 10.1021/jm0498203
CHEMBL185489 66344 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 464 6 1 4 6.5 O=C(O)c1cccc(CN2CCC(c3cn(Cc4ccc(Cl)s4)c4ccccc34)CC2)c1 10.1021/jm0498203
10138404 136346 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 444 8 1 5 5.2 O=C(O)c1ccccc1OCCN1CCC(c2cn(Cc3ccco3)c3ccccc23)CC1 10.1021/jm0498203
CHEMBL374218 136346 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 444 8 1 5 5.2 O=C(O)c1ccccc1OCCN1CCC(c2cn(Cc3ccco3)c3ccccc23)CC1 10.1021/jm0498203
9932752 141439 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 436 8 1 4 5.1 O=C(O)c1ccccc1OCCN1CCC(c2cn(CC3CC3)c3cc(F)ccc23)CC1 10.1021/jm0498203
CHEMBL387391 141439 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 436 8 1 4 5.1 O=C(O)c1ccccc1OCCN1CCC(c2cn(CC3CC3)c3cc(F)ccc23)CC1 10.1021/jm0498203
44326821 206164 0 None - 0 Rat 4.0 pIC50 = 4 Binding
Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro
ChEMBL 559 12 5 6 2.2 CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)C 10.1021/jm00381a002
CHEMBL96738 206164 0 None - 0 Rat 4.0 pIC50 = 4 Binding
Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro
ChEMBL 559 12 5 6 2.2 CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)C 10.1021/jm00381a002
CHEMBL95063 214130 0 None - 0 Rat 4.0 pIC50 = 4 Binding
Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro
ChEMBL None None None CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/jm00381a002
135 2486 38 None -39 58 Human 6.0 pIC50 = 6 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
1796 2486 38 None -39 58 Human 6.0 pIC50 = 6 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
4184 2486 38 None -39 58 Human 6.0 pIC50 = 6 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
CHEMBL6437 2486 38 None -39 58 Human 6.0 pIC50 = 6 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
DB06148 2486 38 None -39 58 Human 6.0 pIC50 = 6 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
1231 922 112 None -2 8 Guinea pig 6.0 pIC50 = 6.0 Binding
Inhibition of guinea pig histamine H2 receptorInhibition of guinea pig histamine H2 receptor
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/j.bmc.2010.07.034
2756 922 112 None -2 8 Guinea pig 6.0 pIC50 = 6.0 Binding
Inhibition of guinea pig histamine H2 receptorInhibition of guinea pig histamine H2 receptor
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/j.bmc.2010.07.034
645 922 112 None -2 8 Guinea pig 6.0 pIC50 = 6.0 Binding
Inhibition of guinea pig histamine H2 receptorInhibition of guinea pig histamine H2 receptor
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/j.bmc.2010.07.034
CHEMBL30 922 112 None -2 8 Guinea pig 6.0 pIC50 = 6.0 Binding
Inhibition of guinea pig histamine H2 receptorInhibition of guinea pig histamine H2 receptor
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/j.bmc.2010.07.034
DB00501 922 112 None -2 8 Guinea pig 6.0 pIC50 = 6.0 Binding
Inhibition of guinea pig histamine H2 receptorInhibition of guinea pig histamine H2 receptor
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/j.bmc.2010.07.034
11785584 136428 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 512 8 1 5 6.5 O=C(O)c1ccccc1OCCN1CCC(c2cn(Cc3ccc(Cl)s3)c3cc(F)ccc23)CC1 10.1021/jm0498203
CHEMBL374459 136428 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 512 8 1 5 6.5 O=C(O)c1ccccc1OCCN1CCC(c2cn(Cc3ccc(Cl)s3)c3cc(F)ccc23)CC1 10.1021/jm0498203
10885636 110514 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of histamine H2 receptorInhibition of histamine H2 receptor
ChEMBL 503 9 0 4 5.7 N#Cc1ccc(CCOC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
CHEMBL326263 110514 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of histamine H2 receptorInhibition of histamine H2 receptor
ChEMBL 503 9 0 4 5.7 N#Cc1ccc(CCOC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
1588 2284 24 None -323 44 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
28864 2284 24 None -323 44 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
43 2284 24 None -323 44 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
CHEMBL157138 2284 24 None -323 44 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
DB00589 2284 24 None -323 44 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
176 394 63 None -6 31 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 394 63 None -6 31 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 394 63 None -6 31 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 394 63 None -6 31 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 394 63 None -6 31 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
657255 197396 29 None -3 15 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 nan
CHEMBL588119 197396 29 None -3 15 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 nan
124087 1357 106 None -29 15 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
7157 1357 106 None -29 15 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
814 1357 106 None -29 15 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
CHEMBL1172 1357 106 None -29 15 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
DB00967 1357 106 None -29 15 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
11057 175565 19 None -2 20 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
3468 175565 19 None -2 20 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
CHEMBL459265 175565 19 None -2 20 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
CHEMBL64894 175565 19 None -2 20 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
2286 3122 48 None -26 30 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
4927 3122 48 None -26 30 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
7282 3122 48 None -26 30 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
CHEMBL643 3122 48 None -26 30 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
DB01069 3122 48 None -26 30 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
1353 1872 85 None -131 86 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
3559 1872 85 None -131 86 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
86 1872 85 None -131 86 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
CHEMBL54 1872 85 None -131 86 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
DB00502 1872 85 None -131 86 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
11362693 141068 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 440 9 1 5 4.4 COCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccc(F)cc21 10.1021/jm0498203
CHEMBL385133 141068 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 440 9 1 5 4.4 COCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccc(F)cc21 10.1021/jm0498203
1201549 590 22 None -74 20 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
333 590 22 None -74 20 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
7601 590 22 None -74 20 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
CHEMBL1201203 590 22 None -74 20 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
CHEMBL438151 590 22 None -74 20 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
DB00245 590 22 None -74 20 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
1212 1624 45 None -323 66 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
204 1624 45 None -323 66 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
3372 1624 45 None -323 66 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
CHEMBL726 1624 45 None -323 66 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
DB00623 1624 45 None -323 66 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
9889247 84323 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 436 10 1 5 4.6 CCOCCn1cc(C2CCN(CCOc3cccc(C(=O)O)c3)CC2)c2ccccc21 10.1021/jm0498203
CHEMBL223024 84323 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 436 10 1 5 4.6 CCOCCn1cc(C2CCN(CCOc3cccc(C(=O)O)c3)CC2)c2ccccc21 10.1021/jm0498203
11071079 110091 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of histamine H2 receptorInhibition of histamine H2 receptor
ChEMBL 496 9 0 3 6.0 O=C(OCCc1ccc(F)cc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
CHEMBL325516 110091 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of histamine H2 receptorInhibition of histamine H2 receptor
ChEMBL 496 9 0 3 6.0 O=C(OCCc1ccc(F)cc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
10202996 84205 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 430 6 1 4 5.8 O=C(O)c1cccc(CN2CCC(c3cn(Cc4cccs4)c4ccccc34)CC2)c1 10.1021/jm0498203
CHEMBL222372 84205 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 430 6 1 4 5.8 O=C(O)c1cccc(CN2CCC(c3cn(Cc4cccs4)c4ccccc34)CC2)c1 10.1021/jm0498203
11113605 10392 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of histamine H2 receptorInhibition of histamine H2 receptor
ChEMBL 480 9 0 2 5.8 O=C(CCc1ccc(F)cc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
CHEMBL116735 10392 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of histamine H2 receptorInhibition of histamine H2 receptor
ChEMBL 480 9 0 2 5.8 O=C(CCc1ccc(F)cc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
11329753 84126 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 514 10 1 5 5.4 CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2cccc(Br)c21 10.1021/jm0498203
CHEMBL222083 84126 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 514 10 1 5 5.4 CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2cccc(Br)c21 10.1021/jm0498203
1231 922 112 None -2 8 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to human histamine H2 receptor by radioligand displacement assayBinding affinity to human histamine H2 receptor by radioligand displacement assay
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/j.ejmech.2013.01.044
2756 922 112 None -2 8 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to human histamine H2 receptor by radioligand displacement assayBinding affinity to human histamine H2 receptor by radioligand displacement assay
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/j.ejmech.2013.01.044
645 922 112 None -2 8 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to human histamine H2 receptor by radioligand displacement assayBinding affinity to human histamine H2 receptor by radioligand displacement assay
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/j.ejmech.2013.01.044
CHEMBL30 922 112 None -2 8 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to human histamine H2 receptor by radioligand displacement assayBinding affinity to human histamine H2 receptor by radioligand displacement assay
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/j.ejmech.2013.01.044
DB00501 922 112 None -2 8 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to human histamine H2 receptor by radioligand displacement assayBinding affinity to human histamine H2 receptor by radioligand displacement assay
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/j.ejmech.2013.01.044
104903 56035 14 None -5 6 Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 624 6 0 8 5.5 C[C@@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)C3=CC[C@]2(C)[C@H]1C(=O)CN1CCN(c2cc(N3CCCC3)nc(N3CCCC3)n2)CC1 nan
CHEMBL1630578 56035 14 None -5 6 Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 624 6 0 8 5.5 C[C@@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)C3=CC[C@]2(C)[C@H]1C(=O)CN1CCN(c2cc(N3CCCC3)nc(N3CCCC3)n2)CC1 nan
72548703 161007 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]APT from human recombinant histamine H2 receptor after 120 mins by scintillation counting analysisDisplacement of [125I]APT from human recombinant histamine H2 receptor after 120 mins by scintillation counting analysis
ChEMBL 583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 10.1016/j.bmcl.2018.03.093
CHEMBL4128926 161007 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]APT from human recombinant histamine H2 receptor after 120 mins by scintillation counting analysisDisplacement of [125I]APT from human recombinant histamine H2 receptor after 120 mins by scintillation counting analysis
ChEMBL 583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 10.1016/j.bmcl.2018.03.093
2389 3267 114 None -346 68 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
5073 3267 114 None -346 68 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
96 3267 114 None -346 68 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
CHEMBL85 3267 114 None -346 68 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
DB00734 3267 114 None -346 68 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
10139591 84203 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 462 7 1 5 5.5 COc1ccc(CN2CCC(c3cn(Cc4ccoc4)c4cc(F)ccc34)CC2)cc1C(=O)O 10.1021/jm0498203
CHEMBL222356 84203 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 462 7 1 5 5.5 COc1ccc(CN2CCC(c3cn(Cc4ccoc4)c4cc(F)ccc34)CC2)cc1C(=O)O 10.1021/jm0498203
11329754 141438 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 514 10 1 5 5.4 CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2cc(Br)ccc21 10.1021/jm0498203
CHEMBL387390 141438 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 514 10 1 5 5.4 CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2cc(Br)ccc21 10.1021/jm0498203
CHEMBL96946 214135 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/jm00381a002
57469 18663 120 None -1 3 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 240 2 1 4 2.8 CC(C)Cn1cnc2c(N)nc3ccccc3c21 nan
CHEMBL1282 18663 120 None -1 3 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 240 2 1 4 2.8 CC(C)Cn1cnc2c(N)nc3ccccc3c21 nan
3198 203792 73 None -19 34 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1201049 203792 73 None -19 34 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL808 203792 73 None -19 34 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
3042 1381 31 None -53 15 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
355 1381 31 None -53 15 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
868 1381 31 None -53 15 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
CHEMBL1123 1381 31 None -53 15 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
DB00804 1381 31 None -53 15 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
2247 502 77 None -56 42 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
249 502 77 None -56 42 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2603 502 77 None -56 42 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL296419 502 77 None -56 42 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
DB00637 502 77 None -56 42 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
9822631 122431 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 406 8 1 4 4.8 CCOCCn1cc(C2CCN(Cc3cccc(C(=O)O)c3)CC2)c2ccccc21 10.1021/jm0498203
CHEMBL360791 122431 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 406 8 1 4 4.8 CCOCCn1cc(C2CCN(Cc3cccc(C(=O)O)c3)CC2)c2ccccc21 10.1021/jm0498203
1231 922 112 None -2 8 Human 6.8 pIC50 = 6.8 Binding
Displacement of radiolabeled cimetidine from human histamine H2 receptorDisplacement of radiolabeled cimetidine from human histamine H2 receptor
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/jm8007618
2756 922 112 None -2 8 Human 6.8 pIC50 = 6.8 Binding
Displacement of radiolabeled cimetidine from human histamine H2 receptorDisplacement of radiolabeled cimetidine from human histamine H2 receptor
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/jm8007618
645 922 112 None -2 8 Human 6.8 pIC50 = 6.8 Binding
Displacement of radiolabeled cimetidine from human histamine H2 receptorDisplacement of radiolabeled cimetidine from human histamine H2 receptor
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/jm8007618
CHEMBL30 922 112 None -2 8 Human 6.8 pIC50 = 6.8 Binding
Displacement of radiolabeled cimetidine from human histamine H2 receptorDisplacement of radiolabeled cimetidine from human histamine H2 receptor
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/jm8007618
DB00501 922 112 None -2 8 Human 6.8 pIC50 = 6.8 Binding
Displacement of radiolabeled cimetidine from human histamine H2 receptorDisplacement of radiolabeled cimetidine from human histamine H2 receptor
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/jm8007618
10141470 123027 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 494 8 1 5 6.4 O=C(O)c1ccccc1OCCN1CCC(c2cn(Cc3ccc(Cl)s3)c3ccccc23)CC1 10.1021/jm0498203
CHEMBL361805 123027 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 494 8 1 5 6.4 O=C(O)c1ccccc1OCCN1CCC(c2cn(Cc3ccc(Cl)s3)c3ccccc23)CC1 10.1021/jm0498203
3158 55959 21 None -12589 20 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
CHEMBL1628227 55959 21 None -12589 20 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
11476077 135871 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 436 10 1 5 4.5 CCOCCn1cc(C2CCN(Cc3cccc(OCC(=O)O)c3)CC2)c2ccccc21 10.1021/jm0498203
CHEMBL373534 135871 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 436 10 1 5 4.5 CCOCCn1cc(C2CCN(Cc3cccc(OCC(=O)O)c3)CC2)c2ccccc21 10.1021/jm0498203
5291 205694 115 None -1 2 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 493 7 2 7 4.6 Cc1ccc(NC(=O)c2ccc(CN3CCN(C)CC3)cc2)cc1Nc1nccc(-c2cccnc2)n1 nan
CHEMBL941 205694 115 None -1 2 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 493 7 2 7 4.6 Cc1ccc(NC(=O)c2ccc(CN3CCN(C)CC3)cc2)cc1Nc1nccc(-c2cccnc2)n1 nan
277 1269 55 None -43 46 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
2913 1269 55 None -43 46 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
765 1269 55 None -43 46 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
CHEMBL516 1269 55 None -43 46 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
DB00434 1269 55 None -43 46 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
11730467 10910 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of histamine H2 receptorInhibition of histamine H2 receptor
ChEMBL 476 10 0 2 6.0 O=C(CCCc1ccccc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
CHEMBL117537 10910 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of histamine H2 receptorInhibition of histamine H2 receptor
ChEMBL 476 10 0 2 6.0 O=C(CCCc1ccccc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
CHEMBL328512 209541 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/jm00381a002
CHEMBL96681 214131 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CCC(=O)O)C(N)=O 10.1021/jm00381a002
2801 161313 56 None -12 29 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 nan
CHEMBL1200710 161313 56 None -12 29 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 nan
CHEMBL415 161313 56 None -12 29 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 nan
11430513 84194 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 436 10 1 5 4.5 CCOCCn1cc(C2CCN(Cc3ccccc3OCC(=O)O)CC2)c2ccccc21 10.1021/jm0498203
CHEMBL222217 84194 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 436 10 1 5 4.5 CCOCCn1cc(C2CCN(Cc3ccccc3OCC(=O)O)CC2)c2ccccc21 10.1021/jm0498203
10140544 141095 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 478 9 1 6 4.4 O=C(O)c1ccccc1OCCN1CCC(c2cn(CCC3COCCO3)c3ccccc23)CC1 10.1021/jm0498203
CHEMBL385311 141095 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 478 9 1 6 4.4 O=C(O)c1ccccc1OCCN1CCC(c2cn(CCC3COCCO3)c3ccccc23)CC1 10.1021/jm0498203
11189839 83903 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 438 9 1 4 5.5 CCCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccc(F)cc21 10.1021/jm0498203
CHEMBL221664 83903 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 438 9 1 4 5.5 CCCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccc(F)cc21 10.1021/jm0498203
3823 49936 38 None -66 11 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
76973198 49936 38 None -66 11 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
CHEMBL157101 49936 38 None -66 11 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
1235 3751 32 None -3 5 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]Aminopotentidine from human recombinant histamine H2 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Aminopotentidine from human recombinant histamine H2 receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 312 6 4 6 -0.1 N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N 10.1016/j.bmcl.2013.01.025
3959 3751 32 None -3 5 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]Aminopotentidine from human recombinant histamine H2 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Aminopotentidine from human recombinant histamine H2 receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 312 6 4 6 -0.1 N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N 10.1016/j.bmcl.2013.01.025
50287 3751 32 None -3 5 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]Aminopotentidine from human recombinant histamine H2 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Aminopotentidine from human recombinant histamine H2 receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 312 6 4 6 -0.1 N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N 10.1016/j.bmcl.2013.01.025
CHEMBL269646 3751 32 None -3 5 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]Aminopotentidine from human recombinant histamine H2 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Aminopotentidine from human recombinant histamine H2 receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 312 6 4 6 -0.1 N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N 10.1016/j.bmcl.2013.01.025
11166846 83871 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 450 10 1 5 4.9 CCOCCn1cc(C2CCN(CCOc3ccc(C)cc3C(=O)O)CC2)c2ccccc21 10.1021/jm0498203
CHEMBL221462 83871 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 450 10 1 5 4.9 CCOCCn1cc(C2CCN(CCOc3ccc(C)cc3C(=O)O)CC2)c2ccccc21 10.1021/jm0498203
4543 169972 36 None -22 30 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 nan
CHEMBL1201156 169972 36 None -22 30 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 nan
CHEMBL445 169972 36 None -22 30 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 nan
CHEMBL44345 212164 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/jm00381a002
2060890 201350 26 None - 0 Rat 3.6 pIC50 = 3.6 Binding
Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro
ChEMBL 342 5 3 2 3.2 O=C(N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)c1ccc(Cl)cc1 10.1021/jm00381a002
CHEMBL63544 201350 26 None - 0 Rat 3.6 pIC50 = 3.6 Binding
Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro
ChEMBL 342 5 3 2 3.2 O=C(N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)c1ccc(Cl)cc1 10.1021/jm00381a002
2281 3114 76 None - 0 Rat 2.6 pIC50 = 2.6 Binding
Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro
ChEMBL 334 10 2 3 2.3 CCCN(C(=O)C(NC(=O)c1ccccc1)CCC(=O)O)CCC 10.1021/jm00381a002
4922 3114 76 None - 0 Rat 2.6 pIC50 = 2.6 Binding
Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro
ChEMBL 334 10 2 3 2.3 CCCN(C(=O)C(NC(=O)c1ccccc1)CCC(=O)O)CCC 10.1021/jm00381a002
893 3114 76 None - 0 Rat 2.6 pIC50 = 2.6 Binding
Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro
ChEMBL 334 10 2 3 2.3 CCCN(C(=O)C(NC(=O)c1ccccc1)CCC(=O)O)CCC 10.1021/jm00381a002
CHEMBL316561 3114 76 None - 0 Rat 2.6 pIC50 = 2.6 Binding
Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro
ChEMBL 334 10 2 3 2.3 CCCN(C(=O)C(NC(=O)c1ccccc1)CCC(=O)O)CCC 10.1021/jm00381a002
DB13431 3114 76 None - 0 Rat 2.6 pIC50 = 2.6 Binding
Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro
ChEMBL 334 10 2 3 2.3 CCCN(C(=O)C(NC(=O)c1ccccc1)CCC(=O)O)CCC 10.1021/jm00381a002
2520 202301 65 None -20 12 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC nan
CHEMBL1280 202301 65 None -20 12 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC nan
CHEMBL6966 202301 65 None -20 12 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC nan
11293983 83861 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 454 10 1 5 4.8 CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccc(F)cc21 10.1021/jm0498203
CHEMBL221413 83861 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 454 10 1 5 4.8 CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccc(F)cc21 10.1021/jm0498203
2726 904 64 None -85 73 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
621 904 64 None -85 73 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
83 904 64 None -85 73 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL71 904 64 None -85 73 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
DB00477 904 64 None -85 73 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
118139356 179133 20 None - 0 Human 4.6 pIC50 = 4.6 Binding
Antagonist activity at human H2 receptorAntagonist activity at human H2 receptor
ChEMBL 435 7 2 7 3.2 Cc1cc(-c2ccnc(Nc3cnn(C)c3)n2)ccc1CNC(=O)N1CC(OC(C)C)C1 10.1021/acs.jmedchem.0c00702
CHEMBL4744041 179133 20 None - 0 Human 4.6 pIC50 = 4.6 Binding
Antagonist activity at human H2 receptorAntagonist activity at human H2 receptor
ChEMBL 435 7 2 7 3.2 Cc1cc(-c2ccnc(Nc3cnn(C)c3)n2)ccc1CNC(=O)N1CC(OC(C)C)C1 10.1021/acs.jmedchem.0c00702
1231 922 112 None -2 8 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human histamine H2 receptor by radioligand displacement assayBinding affinity to human histamine H2 receptor by radioligand displacement assay
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/j.bmc.2013.03.016
2756 922 112 None -2 8 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human histamine H2 receptor by radioligand displacement assayBinding affinity to human histamine H2 receptor by radioligand displacement assay
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/j.bmc.2013.03.016
645 922 112 None -2 8 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human histamine H2 receptor by radioligand displacement assayBinding affinity to human histamine H2 receptor by radioligand displacement assay
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/j.bmc.2013.03.016
CHEMBL30 922 112 None -2 8 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human histamine H2 receptor by radioligand displacement assayBinding affinity to human histamine H2 receptor by radioligand displacement assay
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/j.bmc.2013.03.016
DB00501 922 112 None -2 8 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human histamine H2 receptor by radioligand displacement assayBinding affinity to human histamine H2 receptor by radioligand displacement assay
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/j.bmc.2013.03.016
18609376 202646 61 None - 1 Human 4.6 pIC50 = 4.6 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 386 2 0 4 4.7 CC(=O)O[C@]1(C(C)=O)CC[C@H]2[C@@H]3C[C@H](C)C4=CC(=O)CC[C@]4(C)[C@H]3CC[C@@]21C nan
6279 202646 61 None - 1 Human 4.6 pIC50 = 4.6 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 386 2 0 4 4.7 CC(=O)O[C@]1(C(C)=O)CC[C@H]2[C@@H]3C[C@H](C)C4=CC(=O)CC[C@]4(C)[C@H]3CC[C@@]21C nan
CHEMBL717 202646 61 None - 1 Human 4.6 pIC50 = 4.6 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 386 2 0 4 4.7 CC(=O)O[C@]1(C(C)=O)CC[C@H]2[C@@H]3C[C@H](C)C4=CC(=O)CC[C@]4(C)[C@H]3CC[C@@]21C nan
2284 3121 27 None -53 29 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
4926 3121 27 None -53 29 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
7281 3121 27 None -53 29 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
CHEMBL564 3121 27 None -53 29 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
DB00420 3121 27 None -53 29 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
11443495 83918 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 504 10 1 5 5.7 CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccc(C(F)(F)F)cc21 10.1021/jm0498203
CHEMBL221718 83918 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 504 10 1 5 5.7 CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccc(C(F)(F)F)cc21 10.1021/jm0498203
10298838 168218 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 469 9 1 5 5.2 O=C(O)c1ccccc1OCCN1CCC(c2cn(CCc3ccccn3)c3ccccc23)CC1 10.1021/jm0498203
CHEMBL437519 168218 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 469 9 1 5 5.2 O=C(O)c1ccccc1OCCN1CCC(c2cn(CCc3ccccn3)c3ccccc23)CC1 10.1021/jm0498203
3191 102372 93 None -24 25 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
CHEMBL305660 102372 93 None -24 25 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
10162727 84181 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 478 7 1 5 6.0 COc1ccc(CN2CCC(c3cn(Cc4cccs4)c4cc(F)ccc34)CC2)cc1C(=O)O 10.1021/jm0498203
CHEMBL222139 84181 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 478 7 1 5 6.0 COc1ccc(CN2CCC(c3cn(Cc4cccs4)c4cc(F)ccc34)CC2)cc1C(=O)O 10.1021/jm0498203
CHEMBL2370238 208056 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N1CCCC[C@H]1C(=O)O 10.1021/jm00381a002
CHEMBL262692 208790 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/jm00381a002
CHEMBL289310 209116 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/jm00381a002
CHEMBL318221 209456 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)O 10.1021/jm00381a002
CHEMBL91765 214117 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro
ChEMBL None None None CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/jm00381a002
11211919 84315 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 406 8 1 4 4.8 CCOCCn1cc(C2CCN(Cc3ccccc3C(=O)O)CC2)c2ccccc21 10.1021/jm0498203
CHEMBL222984 84315 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 406 8 1 4 4.8 CCOCCn1cc(C2CCN(Cc3ccccc3C(=O)O)CC2)c2ccccc21 10.1021/jm0498203
10279311 83919 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 512 7 1 5 6.6 COc1ccc(CN2CCC(c3cn(Cc4ccc(Cl)s4)c4cc(F)ccc34)CC2)cc1C(=O)O 10.1021/jm0498203
CHEMBL221730 83919 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 512 7 1 5 6.6 COc1ccc(CN2CCC(c3cn(Cc4ccc(Cl)s4)c4cc(F)ccc34)CC2)cc1C(=O)O 10.1021/jm0498203
1599 2299 47 None -154 16 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 nan
3955 2299 47 None -154 16 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 nan
7215 2299 47 None -154 16 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 nan
CHEMBL841 2299 47 None -154 16 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 nan
DB00836 2299 47 None -154 16 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 nan
11247939 136568 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 450 10 1 5 4.9 CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2cccc(C)c21 10.1021/jm0498203
CHEMBL374754 136568 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 450 10 1 5 4.9 CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2cccc(C)c21 10.1021/jm0498203
10226501 137335 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 460 7 1 5 5.8 COc1ccc(CN2CCC(c3cn(Cc4cccs4)c4ccccc34)CC2)cc1C(=O)O 10.1021/jm0498203
CHEMBL376202 137335 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 460 7 1 5 5.8 COc1ccc(CN2CCC(c3cn(Cc4cccs4)c4ccccc34)CC2)cc1C(=O)O 10.1021/jm0498203
11282005 65720 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 436 10 1 5 4.6 CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccccc21 10.1021/jm0498203
CHEMBL183706 65720 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 436 10 1 5 4.6 CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccccc21 10.1021/jm0498203
CHEMBL330142 209570 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@H](CC(=O)O)C(N)=O 10.1021/jm00381a002
237 203147 43 None -3 13 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
CHEMBL546257 203147 43 None -3 13 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
CHEMBL554190 203147 43 None -3 13 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
CHEMBL7568 203147 43 None -3 13 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
135398737 942 89 None -64 92 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
38 942 89 None -64 92 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
722 942 89 None -64 92 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
CHEMBL42 942 89 None -64 92 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
DB00363 942 89 None -64 92 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
11005810 10352 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of histamine H2 receptorInhibition of histamine H2 receptor
ChEMBL 517 10 1 4 6.2 N#Cc1ccc(CCOC(=O)NC2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
CHEMBL116463 10352 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of histamine H2 receptorInhibition of histamine H2 receptor
ChEMBL 517 10 1 4 6.2 N#Cc1ccc(CCOC(=O)NC2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
26987 934 29 None -177 21 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
6063 934 29 None -177 21 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
671 934 29 None -177 21 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
CHEMBL1626 934 29 None -177 21 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
DB00283 934 29 None -177 21 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
11212029 84182 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 410 7 1 4 4.5 COCCn1cc(C2CCN(Cc3cccc(C(=O)O)c3)CC2)c2ccc(F)cc21 10.1021/jm0498203
CHEMBL222142 84182 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 410 7 1 4 4.5 COCCn1cc(C2CCN(Cc3cccc(C(=O)O)c3)CC2)c2ccc(F)cc21 10.1021/jm0498203
11259138 84574 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 436 10 1 5 4.5 CCOCCn1cc(C2CCN(Cc3ccc(OCC(=O)O)cc3)CC2)c2ccccc21 10.1021/jm0498203
CHEMBL223882 84574 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 436 10 1 5 4.5 CCOCCn1cc(C2CCN(Cc3ccc(OCC(=O)O)cc3)CC2)c2ccccc21 10.1021/jm0498203
4011 81982 43 None -27 24 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
CHEMBL21731 81982 43 None -27 24 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
CHEMBL94917 214128 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OCc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/jm00381a002
1530 2142 44 None -151 21 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
3827 2142 44 None -151 21 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
7206 2142 44 None -151 21 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
CHEMBL534 2142 44 None -151 21 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
DB00920 2142 44 None -151 21 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
1129 1584 89 None 1 2 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N nan
3325 1584 89 None 1 2 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N nan
5353622 1584 89 None 1 2 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N nan
5702160 1584 89 None 1 2 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N nan
7074 1584 89 None 1 2 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N nan
CHEMBL902 1584 89 None 1 2 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N nan
DB00927 1584 89 None 1 2 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N nan
10161929 136650 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 464 9 1 6 4.4 O=C(O)c1ccccc1OCCN1CCC(c2cn(CCC3OCCO3)c3ccccc23)CC1 10.1021/jm0498203
CHEMBL374869 136650 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 464 9 1 6 4.4 O=C(O)c1ccccc1OCCN1CCC(c2cn(CCC3OCCO3)c3ccccc23)CC1 10.1021/jm0498203
1231 922 112 None -2 8 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/acs.jmedchem.6b01422
2756 922 112 None -2 8 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/acs.jmedchem.6b01422
645 922 112 None -2 8 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/acs.jmedchem.6b01422
CHEMBL30 922 112 None -2 8 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/acs.jmedchem.6b01422
DB00501 922 112 None -2 8 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/acs.jmedchem.6b01422
11238716 83862 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 592 10 1 5 6.2 CCOCCn1cc(C2CCN(CCOc3c(Br)cc(Br)cc3C(=O)O)CC2)c2ccccc21 10.1021/jm0498203
CHEMBL221414 83862 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 592 10 1 5 6.2 CCOCCn1cc(C2CCN(CCOc3c(Br)cc(Br)cc3C(=O)O)CC2)c2ccccc21 10.1021/jm0498203
10204866 84298 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 460 8 1 5 5.7 O=C(O)c1ccccc1OCCN1CCC(c2cn(Cc3cccs3)c3ccccc23)CC1 10.1021/jm0498203
CHEMBL222881 84298 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 460 8 1 5 5.7 O=C(O)c1ccccc1OCCN1CCC(c2cn(Cc3cccs3)c3ccccc23)CC1 10.1021/jm0498203
11396873 136448 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 454 10 1 5 4.8 CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2cc(F)ccc21 10.1021/jm0498203
CHEMBL374585 136448 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 454 10 1 5 4.8 CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2cc(F)ccc21 10.1021/jm0498203
44326564 206126 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro
ChEMBL 531 12 6 6 1.6 CC(C)CC(NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/jm00381a002
CHEMBL96530 206126 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro
ChEMBL 531 12 6 6 1.6 CC(C)CC(NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/jm00381a002
CHEMBL1790763 207152 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/jm00381a002
2812 4696 96 None -33 34 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
CHEMBL104 4696 96 None -33 34 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
10478188 122414 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 436 9 1 5 4.8 CCOCCn1cc(C2CCN(Cc3ccc(OC)c(C(=O)O)c3)CC2)c2ccccc21 10.1021/jm0498203
CHEMBL360712 122414 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 436 9 1 5 4.8 CCOCCn1cc(C2CCN(Cc3ccc(OC)c(C(=O)O)c3)CC2)c2ccccc21 10.1021/jm0498203
1231 922 112 None -2 8 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C nan
2756 922 112 None -2 8 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C nan
645 922 112 None -2 8 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C nan
CHEMBL30 922 112 None -2 8 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C nan
DB00501 922 112 None -2 8 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C nan
11363750 84193 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 484 8 1 4 5.5 CCOCCn1cc(C2CCN(Cc3cc(C(=O)O)ccc3Br)CC2)c2ccccc21 10.1021/jm0498203
CHEMBL222214 84193 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 484 8 1 4 5.5 CCOCCn1cc(C2CCN(Cc3cc(C(=O)O)ccc3Br)CC2)c2ccccc21 10.1021/jm0498203
11247290 136167 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 424 8 1 4 4.9 CCOCCn1cc(C2CCN(Cc3ccc(F)c(C(=O)O)c3)CC2)c2ccccc21 10.1021/jm0498203
CHEMBL374059 136167 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 424 8 1 4 4.9 CCOCCn1cc(C2CCN(Cc3ccc(F)c(C(=O)O)c3)CC2)c2ccccc21 10.1021/jm0498203
10273238 84316 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 414 6 1 4 5.4 O=C(O)c1cccc(CN2CCC(c3cn(Cc4ccco4)c4ccccc34)CC2)c1 10.1021/jm0498203
CHEMBL222985 84316 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 414 6 1 4 5.4 O=C(O)c1cccc(CN2CCC(c3cn(Cc4ccco4)c4ccccc34)CC2)c1 10.1021/jm0498203
11351801 83917 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 466 11 1 6 4.6 CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2cc(OC)ccc21 10.1021/jm0498203
CHEMBL221716 83917 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 466 11 1 6 4.6 CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2cc(OC)ccc21 10.1021/jm0498203
4189 205185 91 None -36 34 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1559 205185 91 None -36 34 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL91 205185 91 None -36 34 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
9889248 84292 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 436 10 1 5 4.6 CCOCCn1cc(C2CCN(CCOc3ccc(C(=O)O)cc3)CC2)c2ccccc21 10.1021/jm0498203
CHEMBL222853 84292 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 436 10 1 5 4.6 CCOCCn1cc(C2CCN(CCOc3ccc(C(=O)O)cc3)CC2)c2ccccc21 10.1021/jm0498203
4601 205010 29 None -7 17 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
CHEMBL1201023 205010 29 None -7 17 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
CHEMBL900 205010 29 None -7 17 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
CHEMBL91752 214116 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/jm00381a002
CHEMBL94448 214123 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)O 10.1021/jm00381a002
CHEMBL94902 214126 1 None - 0 Rat 4.2 pIC50 = 4.2 Binding
Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)O 10.1021/jm00381a002
180 397 50 None -1412 39 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
200 397 50 None -1412 39 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
2160 397 50 None -1412 39 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
CHEMBL629 397 50 None -1412 39 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
DB00321 397 50 None -1412 39 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
10907460 9720 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of histamine H2 receptorInhibition of histamine H2 receptor
ChEMBL 521 11 1 3 5.8 CCOc1ccc(CCNC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
CHEMBL113956 9720 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of histamine H2 receptorInhibition of histamine H2 receptor
ChEMBL 521 11 1 3 5.8 CCOc1ccc(CCNC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
11340290 64018 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 466 11 1 6 4.6 CCOCCn1cc(C2CCN(CCOc3cc(OC)ccc3C(=O)O)CC2)c2ccccc21 10.1021/jm0498203
CHEMBL181278 64018 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 466 11 1 6 4.6 CCOCCn1cc(C2CCN(CCOc3cc(OC)ccc3C(=O)O)CC2)c2ccccc21 10.1021/jm0498203
1231 922 112 None -2 8 Human 6.1 pIC50 = 6.1 Binding
Inhibition of histamine H2 receptorInhibition of histamine H2 receptor
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/jm701575k
2756 922 112 None -2 8 Human 6.1 pIC50 = 6.1 Binding
Inhibition of histamine H2 receptorInhibition of histamine H2 receptor
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/jm701575k
645 922 112 None -2 8 Human 6.1 pIC50 = 6.1 Binding
Inhibition of histamine H2 receptorInhibition of histamine H2 receptor
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/jm701575k
CHEMBL30 922 112 None -2 8 Human 6.1 pIC50 = 6.1 Binding
Inhibition of histamine H2 receptorInhibition of histamine H2 receptor
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/jm701575k
DB00501 922 112 None -2 8 Human 6.1 pIC50 = 6.1 Binding
Inhibition of histamine H2 receptorInhibition of histamine H2 receptor
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/jm701575k
1210 903 45 None -281 21 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
1213 903 45 None -281 21 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
2725 903 45 None -281 21 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
33036 903 45 None -281 21 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
4411 903 45 None -281 21 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
616 903 45 None -281 21 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
6976 903 45 None -281 21 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
716121 903 45 None -281 21 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
90475904 903 45 None -281 21 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL1201353 903 45 None -281 21 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL1554789 903 45 None -281 21 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL505 903 45 None -281 21 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
DB01114 903 45 None -281 21 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
DB13679 903 45 None -281 21 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
11328514 137320 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 454 10 1 5 4.8 CCOCCn1cc(C2CCN(CCOc3cccc(F)c3C(=O)O)CC2)c2ccccc21 10.1021/jm0498203
CHEMBL376025 137320 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 454 10 1 5 4.8 CCOCCn1cc(C2CCN(CCOc3cccc(F)c3C(=O)O)CC2)c2ccccc21 10.1021/jm0498203
9804849 67102 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against Histamine H2 receptorInhibitory concentration against Histamine H2 receptor
ChEMBL 472 8 1 5 5.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL189118 67102 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against Histamine H2 receptorInhibitory concentration against Histamine H2 receptor
ChEMBL 472 8 1 5 5.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
10139592 84566 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 462 8 1 5 5.4 O=C(O)c1ccccc1OCCN1CCC(c2cn(Cc3ccco3)c3cc(F)ccc23)CC1 10.1021/jm0498203
CHEMBL223837 84566 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 462 8 1 5 5.4 O=C(O)c1ccccc1OCCN1CCC(c2cn(Cc3ccco3)c3cc(F)ccc23)CC1 10.1021/jm0498203
11385692 136512 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 462 8 1 5 5.4 O=C(O)c1ccccc1OCCN1CCC(c2cn(Cc3ccoc3)c3cc(F)ccc23)CC1 10.1021/jm0498203
CHEMBL374675 136512 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 462 8 1 5 5.4 O=C(O)c1ccccc1OCCN1CCC(c2cn(Cc3ccoc3)c3cc(F)ccc23)CC1 10.1021/jm0498203
9802248 165679 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 420 9 1 4 5.4 CCCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccccc21 10.1021/jm0498203
CHEMBL426786 165679 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 420 9 1 4 5.4 CCCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccccc21 10.1021/jm0498203
1016 3678 75 None -41 35 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2561 3678 75 None -41 35 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2733526 3678 75 None -41 35 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
5384 3678 75 None -41 35 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL83 3678 75 None -41 35 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
DB00675 3678 75 None -41 35 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
100 3733 52 None -46 56 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
2637 3733 52 None -46 56 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
5452 3733 52 None -46 56 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
CHEMBL479 3733 52 None -46 56 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
DB00679 3733 52 None -46 56 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
11202401 136570 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 478 11 1 6 4.8 CCOCCn1cc(C2CCN(CCOc3ccc(C(C)=O)cc3C(=O)O)CC2)c2ccccc21 10.1021/jm0498203
CHEMBL374755 136570 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes
ChEMBL 478 11 1 6 4.8 CCOCCn1cc(C2CCN(CCOc3ccc(C(C)=O)cc3C(=O)O)CC2)c2ccccc21 10.1021/jm0498203
133 2450 48 None -141 43 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
1723 2450 48 None -141 43 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
28693 2450 48 None -141 43 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
CHEMBL19215 2450 48 None -141 43 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
DB13520 2450 48 None -141 43 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
1129 1584 89 None -1 2 Guinea pig 7.0 pKd = 7 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N 10.1021/jm00091a012
3325 1584 89 None -1 2 Guinea pig 7.0 pKd = 7 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N 10.1021/jm00091a012
5353622 1584 89 None -1 2 Guinea pig 7.0 pKd = 7 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N 10.1021/jm00091a012
5702160 1584 89 None -1 2 Guinea pig 7.0 pKd = 7 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N 10.1021/jm00091a012
7074 1584 89 None -1 2 Guinea pig 7.0 pKd = 7 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N 10.1021/jm00091a012
CHEMBL902 1584 89 None -1 2 Guinea pig 7.0 pKd = 7 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N 10.1021/jm00091a012
DB00927 1584 89 None -1 2 Guinea pig 7.0 pKd = 7 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N 10.1021/jm00091a012
CHEMBL5087637 213769 0 None - 1 Human 6.0 pKd = 6 Binding
Binding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysisBinding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysis
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C 10.1016/j.bmcl.2021.128388
CHEMBL5095891 213769 0 None - 1 Human 6.0 pKd = 6 Binding
Binding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysisBinding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysis
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C 10.1016/j.bmcl.2021.128388
10949464 97724 0 None -12882 4 Guinea pig 5.0 pKd = 5 Binding
Activity at Histamine H2 receptor using functional H2 receptor assay on guinea pig atriumActivity at Histamine H2 receptor using functional H2 receptor assay on guinea pig atrium
ChEMBL 403 10 1 4 5.5 c1ccc2c(NCCCc3ccc(OCCCN4CCCCC4)cc3)ccnc2c1 10.1021/jm0110845
CHEMBL274041 97724 0 None -12882 4 Guinea pig 5.0 pKd = 5 Binding
Activity at Histamine H2 receptor using functional H2 receptor assay on guinea pig atriumActivity at Histamine H2 receptor using functional H2 receptor assay on guinea pig atrium
ChEMBL 403 10 1 4 5.5 c1ccc2c(NCCCc3ccc(OCCCN4CCCCC4)cc3)ccnc2c1 10.1021/jm0110845
10936212 11092 1 None -165 4 Guinea pig 5.0 pKd = 5.0 Binding
Potency at histamine H2 receptor subtype, was tested on guinea pig right atriumPotency at histamine H2 receptor subtype, was tested on guinea pig right atrium
ChEMBL 323 6 0 3 4.5 CC(=O)c1ccc(OCc2ccc(CN3CCCCC3)cc2)cc1 10.1021/jm021084k
CHEMBL1178750 11092 1 None -165 4 Guinea pig 5.0 pKd = 5.0 Binding
Potency at histamine H2 receptor subtype, was tested on guinea pig right atriumPotency at histamine H2 receptor subtype, was tested on guinea pig right atrium
ChEMBL 323 6 0 3 4.5 CC(=O)c1ccc(OCc2ccc(CN3CCCCC3)cc2)cc1 10.1021/jm021084k
CHEMBL39603 11092 1 None -165 4 Guinea pig 5.0 pKd = 5.0 Binding
Potency at histamine H2 receptor subtype, was tested on guinea pig right atriumPotency at histamine H2 receptor subtype, was tested on guinea pig right atrium
ChEMBL 323 6 0 3 4.5 CC(=O)c1ccc(OCc2ccc(CN3CCCCC3)cc2)cc1 10.1021/jm021084k
CHEMBL5093461 213767 0 None - 1 Human 7.0 pKd = 7.0 Binding
Binding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysisBinding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysis
ChEMBL None None None CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2nnc(N)s2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1016/j.bmcl.2021.128388
CHEMBL5095884 213767 0 None - 1 Human 7.0 pKd = 7.0 Binding
Binding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysisBinding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysis
ChEMBL None None None CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2nnc(N)s2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1016/j.bmcl.2021.128388
126688 400 28 None -2 4 Rat 4.9 pKd = 4.9 Binding
Affinity to the Histamine H2 receptor was determined expressed in CHO cell using [125I]iodoaminopotentidine as radioligandAffinity to the Histamine H2 receptor was determined expressed in CHO cell using [125I]iodoaminopotentidine as radioligand
ChEMBL 157 2 2 4 0.5 NCCc1sc(nc1C)N 10.1016/S0960-894X(01)80533-3
4025 400 28 None -2 4 Rat 4.9 pKd = 4.9 Binding
Affinity to the Histamine H2 receptor was determined expressed in CHO cell using [125I]iodoaminopotentidine as radioligandAffinity to the Histamine H2 receptor was determined expressed in CHO cell using [125I]iodoaminopotentidine as radioligand
ChEMBL 157 2 2 4 0.5 NCCc1sc(nc1C)N 10.1016/S0960-894X(01)80533-3
CHEMBL293762 400 28 None -2 4 Rat 4.9 pKd = 4.9 Binding
Affinity to the Histamine H2 receptor was determined expressed in CHO cell using [125I]iodoaminopotentidine as radioligandAffinity to the Histamine H2 receptor was determined expressed in CHO cell using [125I]iodoaminopotentidine as radioligand
ChEMBL 157 2 2 4 0.5 NCCc1sc(nc1C)N 10.1016/S0960-894X(01)80533-3
1204 1893 114 None -173 25 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
1247 1893 114 None -173 25 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
1375 1893 114 None -173 25 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
774 1893 114 None -173 25 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
CHEMBL90 1893 114 None -173 25 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
DB05381 1893 114 None -173 25 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
119570 3098 90 None -281 40 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/acs.jmedchem.1c00692
2233 3098 90 None -281 40 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/acs.jmedchem.1c00692
953 3098 90 None -281 40 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/acs.jmedchem.1c00692
CHEMBL301265 3098 90 None -281 40 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/acs.jmedchem.1c00692
DB00413 3098 90 None -281 40 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/acs.jmedchem.1c00692
168268716 192150 0 None 1 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 372 3 4 4 3.5 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NC2CCCCC2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5170276 192150 0 None 1 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 372 3 4 4 3.5 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NC2CCCCC2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5221176 192150 0 None 1 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 372 3 4 4 3.5 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NC2CCCCC2)cc1 10.1021/acs.jmedchem.1c00692
168268680 192154 0 None 1 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 662 11 8 8 4.8 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5172675 192154 0 None 1 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 662 11 8 8 4.8 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5221210 192154 0 None 1 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 662 11 8 8 4.8 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1 10.1021/acs.jmedchem.1c00692
168268827 192167 0 None 3 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 450 8 4 4 4.8 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5179906 192167 0 None 3 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 450 8 4 4 4.8 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5221314 192167 0 None 3 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 450 8 4 4 4.8 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)c1 10.1021/acs.jmedchem.1c00692
168268853 192173 0 None -2 6 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 389 8 4 5 1.9 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5180504 192173 0 None -2 6 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 389 8 4 5 1.9 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5221353 192173 0 None -2 6 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 389 8 4 5 1.9 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
168273471 192189 0 None 12 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 596 17 8 10 0.7 N/C(=N\C(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5173079 192189 0 None 12 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 596 17 8 10 0.7 N/C(=N\C(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221433 192189 0 None 12 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 596 17 8 10 0.7 N/C(=N\C(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
168273549 192191 0 None 1 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 436 6 4 4 4.3 Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5174342 192191 0 None 1 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 436 6 4 4 4.3 Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5221438 192191 0 None 1 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 436 6 4 4 4.3 Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1 10.1021/acs.jmedchem.1c00692
168273640 192193 0 None -6 6 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 568 15 8 10 -0.1 N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5176229 192193 0 None -6 6 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 568 15 8 10 -0.1 N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221444 192193 0 None -6 6 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 568 15 8 10 -0.1 N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
168273745 192196 0 None -13 6 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 332 6 4 4 1.5 N/C(=N\C(=O)NCc1ccccc1)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5178472 192196 0 None -13 6 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 332 6 4 4 1.5 N/C(=N\C(=O)NCc1ccccc1)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221451 192196 0 None -13 6 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 332 6 4 4 1.5 N/C(=N\C(=O)NCc1ccccc1)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
168274129 192197 0 None -6 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 370 12 5 6 1.0 NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5176780 192197 0 None -6 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 370 12 5 6 1.0 NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221468 192197 0 None -6 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 370 12 5 6 1.0 NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
168275750 192214 0 None -87 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 332 6 3 4 1.6 Cc1nnc(CCCN/C(N)=N/C(=O)NCc2ccccc2)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5175558 192214 0 None -87 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 332 6 3 4 1.6 Cc1nnc(CCCN/C(N)=N/C(=O)NCc2ccccc2)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221581 192214 0 None -87 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 332 6 3 4 1.6 Cc1nnc(CCCN/C(N)=N/C(=O)NCc2ccccc2)s1 10.1021/acs.jmedchem.1c00692
168276867 192223 0 None -1 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 662 11 8 8 4.8 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5174278 192223 0 None -1 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 662 11 8 8 4.8 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5221653 192223 0 None -1 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 662 11 8 8 4.8 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)c1 10.1021/acs.jmedchem.1c00692
168277996 192234 0 None -20 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 380 4 4 4 3.3 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCc2ccccc2)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5173373 192234 0 None -20 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 380 4 4 4 3.3 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCc2ccccc2)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5221736 192234 0 None -20 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 380 4 4 4 3.3 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCc2ccccc2)c1 10.1021/acs.jmedchem.1c00692
168278471 192236 0 None -18 6 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 312 8 4 4 1.5 CCCCCNC(=O)/N=C(\N)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5183205 192236 0 None -18 6 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 312 8 4 4 1.5 CCCCCNC(=O)/N=C(\N)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221757 192236 0 None -18 6 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 312 8 4 4 1.5 CCCCCNC(=O)/N=C(\N)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
168278543 192239 0 None 2 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 358 4 4 4 1.6 N/C(=N\C(=O)NCc1ccccc1)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
CHEMBL5184846 192239 0 None 2 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 358 4 4 4 1.6 N/C(=N\C(=O)NCc1ccccc1)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
CHEMBL5221764 192239 0 None 2 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 358 4 4 4 1.6 N/C(=N\C(=O)NCc1ccccc1)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
168280339 192253 0 None -52 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 372 8 3 5 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCn1cc(CN(C)C)nn1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5188592 192253 0 None -52 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 372 8 3 5 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCn1cc(CN(C)C)nn1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5221885 192253 0 None -52 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 372 8 3 5 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCn1cc(CN(C)C)nn1)c1ccccc1 10.1021/acs.jmedchem.1c00692
168281536 192269 0 None -9 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 369 12 4 5 1.7 Cc1nnc(CCCN/C(N)=N/C(=O)NCCCCCCCCN)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5189006 192269 0 None -9 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 369 12 4 5 1.7 Cc1nnc(CCCN/C(N)=N/C(=O)NCCCCCCCCN)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221966 192269 0 None -9 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 369 12 4 5 1.7 Cc1nnc(CCCN/C(N)=N/C(=O)NCCCCCCCCN)s1 10.1021/acs.jmedchem.1c00692
168281746 192270 0 None -676 6 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 365 6 4 5 1.6 CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5184911 192270 0 None -676 6 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 365 6 4 5 1.6 CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5221974 192270 0 None -676 6 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 365 6 4 5 1.6 CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1 10.1021/acs.jmedchem.1c00692
168283097 192281 0 None -22 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 311 9 4 5 0.8 CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)o1 10.1021/acs.jmedchem.1c00692
CHEMBL5186770 192281 0 None -22 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 311 9 4 5 0.8 CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)o1 10.1021/acs.jmedchem.1c00692
CHEMBL5222043 192281 0 None -22 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 311 9 4 5 0.8 CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)o1 10.1021/acs.jmedchem.1c00692
168283321 192283 0 None 2 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 364 7 4 4 2.3 Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1 10.1021/acs.jmedchem.1c00692
CHEMBL5183015 192283 0 None 2 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 364 7 4 4 2.3 Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1 10.1021/acs.jmedchem.1c00692
CHEMBL5222057 192283 0 None 2 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 364 7 4 4 2.3 Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1 10.1021/acs.jmedchem.1c00692
168283536 192288 0 None -53 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 312 8 3 4 1.6 CCCCCNC(=O)/N=C(/N)NCCCc1nnc(C)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5187758 192288 0 None -53 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 312 8 3 4 1.6 CCCCCNC(=O)/N=C(/N)NCCCc1nnc(C)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222074 192288 0 None -53 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 312 8 3 4 1.6 CCCCCNC(=O)/N=C(/N)NCCCc1nnc(C)s1 10.1021/acs.jmedchem.1c00692
168284289 192294 0 None 1 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 428 8 4 4 3.1 CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
CHEMBL5194860 192294 0 None 1 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 428 8 4 4 3.1 CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
CHEMBL5222123 192294 0 None 1 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 428 8 4 4 3.1 CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
168284480 192298 0 None -22 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 330 6 4 4 1.3 Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCc1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5197548 192298 0 None -22 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 330 6 4 4 1.3 Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCc1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222137 192298 0 None -22 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 330 6 4 4 1.3 Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCc1ccccc1 10.1021/acs.jmedchem.1c00692
168286141 192312 0 None 2 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 450 8 4 4 4.8 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5192993 192312 0 None 2 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 450 8 4 4 4.8 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222231 192312 0 None 2 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 450 8 4 4 4.8 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)cc1 10.1021/acs.jmedchem.1c00692
168286426 192314 0 None -5 6 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 403 10 4 5 2.3 CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5198795 192314 0 None -5 6 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 403 10 4 5 2.3 CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222241 192314 0 None -5 6 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 403 10 4 5 2.3 CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
168290235 192356 0 None -1737 20 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5201074 192356 0 None -1737 20 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222491 192356 0 None -1737 20 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
168290815 192361 0 None -537 6 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 327 9 4 5 1.2 CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5200771 192361 0 None -537 6 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 327 9 4 5 1.2 CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222529 192361 0 None -537 6 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 327 9 4 5 1.2 CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
168291233 192367 0 None -5 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 373 8 4 5 1.4 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)o2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5200106 192367 0 None -5 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 373 8 4 5 1.4 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)o2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222556 192367 0 None -5 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 373 8 4 5 1.4 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)o2)cc1 10.1021/acs.jmedchem.1c00692
168292954 192385 0 None -11 6 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 388 8 4 4 2.5 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5202592 192385 0 None -11 6 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 388 8 4 4 2.5 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222660 192385 0 None -11 6 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 388 8 4 4 2.5 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
168294161 192394 0 None 3 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 360 6 4 4 3.3 CCCCCNC(=O)/N=C(\N)Nc1cccc(-c2sc(N)nc2C)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5204739 192394 0 None 3 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 360 6 4 4 3.3 CCCCCNC(=O)/N=C(\N)Nc1cccc(-c2sc(N)nc2C)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5222742 192394 0 None 3 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 360 6 4 4 3.3 CCCCCNC(=O)/N=C(\N)Nc1cccc(-c2sc(N)nc2C)c1 10.1021/acs.jmedchem.1c00692
168294445 192398 0 None -1 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 414 6 4 4 2.6 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCC2CCc3nc(N)sc3C2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5208113 192398 0 None -1 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 414 6 4 4 2.6 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCC2CCc3nc(N)sc3C2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222768 192398 0 None -1 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 414 6 4 4 2.6 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCC2CCc3nc(N)sc3C2)cc1 10.1021/acs.jmedchem.1c00692
168294166 192402 0 None 1 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 360 6 4 4 3.3 CCCCCNC(=O)/N=C(\N)Nc1ccc(-c2sc(N)nc2C)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5209081 192402 0 None 1 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 360 6 4 4 3.3 CCCCCNC(=O)/N=C(\N)Nc1ccc(-c2sc(N)nc2C)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222775 192402 0 None 1 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 360 6 4 4 3.3 CCCCCNC(=O)/N=C(\N)Nc1ccc(-c2sc(N)nc2C)cc1 10.1021/acs.jmedchem.1c00692
168294449 192406 0 None -6 6 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 367 7 4 5 1.9 CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1 10.1021/acs.jmedchem.1c00692
CHEMBL5204599 192406 0 None -6 6 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 367 7 4 5 1.9 CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1 10.1021/acs.jmedchem.1c00692
CHEMBL5222793 192406 0 None -6 6 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 367 7 4 5 1.9 CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1 10.1021/acs.jmedchem.1c00692
168294767 192407 0 None -117 20 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5207281 192407 0 None -117 20 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222802 192407 0 None -117 20 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
168294770 192408 0 None 2 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 436 6 4 4 4.3 Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5208327 192408 0 None 2 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 436 6 4 4 4.3 Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222806 192408 0 None 2 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 436 6 4 4 4.3 Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)cc1 10.1021/acs.jmedchem.1c00692
168294776 192414 0 None -7 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 366 7 3 4 2.6 Cc1nnc(CCCN/C(N)=N/C(=O)NCC(C)C2CCCCC2)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5209479 192414 0 None -7 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 366 7 3 4 2.6 Cc1nnc(CCCN/C(N)=N/C(=O)NCC(C)C2CCCCC2)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222831 192414 0 None -7 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 366 7 3 4 2.6 Cc1nnc(CCCN/C(N)=N/C(=O)NCC(C)C2CCCCC2)s1 10.1021/acs.jmedchem.1c00692
168295528 192419 0 None -147 20 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5206565 192419 0 None -147 20 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222872 192419 0 None -147 20 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
168294178 192423 0 None 1 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 414 5 4 4 4.4 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)C2CCCCC2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5205197 192423 0 None 1 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 414 5 4 4 4.4 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)C2CCCCC2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222887 192423 0 None 1 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 414 5 4 4 4.4 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)C2CCCCC2)cc1 10.1021/acs.jmedchem.1c00692
168295541 192428 0 None -851 6 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 347 6 4 5 1.4 C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5208845 192428 0 None -851 6 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 347 6 4 5 1.4 C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222926 192428 0 None -851 6 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 347 6 4 5 1.4 C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1 10.1021/acs.jmedchem.1c00692
168295543 192429 0 None 1 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 380 4 4 4 3.3 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCc2ccccc2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5209021 192429 0 None 1 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 380 4 4 4 3.3 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCc2ccccc2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222929 192429 0 None 1 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 380 4 4 4 3.3 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCc2ccccc2)cc1 10.1021/acs.jmedchem.1c00692
168295803 192433 0 None 3 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 338 6 4 4 1.6 CCCCCNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
CHEMBL5207206 192433 0 None 3 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 338 6 4 4 1.6 CCCCCNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
CHEMBL5222937 192433 0 None 3 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 338 6 4 4 1.6 CCCCCNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
168294182 192436 0 None -3 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 314 6 4 2 1.7 C[C@@H](NC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5208722 192436 0 None -3 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 314 6 4 2 1.7 C[C@@H](NC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222960 192436 0 None -3 4 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 314 6 4 2 1.7 C[C@@H](NC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1021/acs.jmedchem.1c00692
156021166 177752 0 None - 1 Human 7.9 pKd = 7.9 Binding
Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry
ChEMBL 908 25 3 8 10.3 C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acsmedchemlett.0c00033
CHEMBL4647775 177752 0 None - 1 Human 7.9 pKd = 7.9 Binding
Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry
ChEMBL 908 25 3 8 10.3 C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acsmedchemlett.0c00033
CHEMBL4651205 177752 0 None - 1 Human 7.9 pKd = 7.9 Binding
Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry
ChEMBL 908 25 3 8 10.3 C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acsmedchemlett.0c00033
156015793 177674 0 None - 1 Human 6.9 pKd = 6.9 Binding
Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis
ChEMBL 880 23 3 8 9.5 C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acsmedchemlett.0c00033
CHEMBL4645867 177674 0 None - 1 Human 6.9 pKd = 6.9 Binding
Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis
ChEMBL 880 23 3 8 9.5 C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acsmedchemlett.0c00033
CHEMBL4650701 177674 0 None - 1 Human 6.9 pKd = 6.9 Binding
Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis
ChEMBL 880 23 3 8 9.5 C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acsmedchemlett.0c00033
14514732 203681 1 None - 1 Guinea pig 6.9 pKd = 6.9 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 367 8 2 3 4.3 O=C(NCCCOc1cccc(CN2CCCCC2)c1)Nc1ccccc1 10.1021/jm00091a012
CHEMBL80046 203681 1 None - 1 Guinea pig 6.9 pKd = 6.9 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 367 8 2 3 4.3 O=C(NCCCOc1cccc(CN2CCCCC2)c1)Nc1ccccc1 10.1021/jm00091a012
11003651 98140 0 None -24547 3 Guinea pig 4.9 pKd = 4.9 Binding
Activity at Histamine H2 receptor using functional H2 receptor assay on guinea pig atriumActivity at Histamine H2 receptor using functional H2 receptor assay on guinea pig atrium
ChEMBL 389 9 1 4 5.1 c1ccc2c(NCCc3ccc(OCCCN4CCCCC4)cc3)ccnc2c1 10.1021/jm0110845
CHEMBL276938 98140 0 None -24547 3 Guinea pig 4.9 pKd = 4.9 Binding
Activity at Histamine H2 receptor using functional H2 receptor assay on guinea pig atriumActivity at Histamine H2 receptor using functional H2 receptor assay on guinea pig atrium
ChEMBL 389 9 1 4 5.1 c1ccc2c(NCCc3ccc(OCCCN4CCCCC4)cc3)ccnc2c1 10.1021/jm0110845
90667228 108968 0 None - 1 Guinea pig 4.9 pKd = 4.9 Binding
Antagonist activity at guinea pig histamine H2 receptor assessed as inhibition of histamine-induced response after 30 minsAntagonist activity at guinea pig histamine H2 receptor assessed as inhibition of histamine-induced response after 30 mins
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1ncc[nH]1)c1ccccc1 10.1039/C3MD00245D
CHEMBL3220629 108968 0 None - 1 Guinea pig 4.9 pKd = 4.9 Binding
Antagonist activity at guinea pig histamine H2 receptor assessed as inhibition of histamine-induced response after 30 minsAntagonist activity at guinea pig histamine H2 receptor assessed as inhibition of histamine-induced response after 30 mins
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1ncc[nH]1)c1ccccc1 10.1039/C3MD00245D
156011186 177658 0 None - 1 Human 7.8 pKd = 7.8 Binding
Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry
ChEMBL 704 20 2 7 7.5 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O 10.1021/acsmedchemlett.0c00033
CHEMBL4637893 177658 0 None - 1 Human 7.8 pKd = 7.8 Binding
Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry
ChEMBL 704 20 2 7 7.5 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O 10.1021/acsmedchemlett.0c00033
CHEMBL4650588 177658 0 None - 1 Human 7.8 pKd = 7.8 Binding
Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry
ChEMBL 704 20 2 7 7.5 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O 10.1021/acsmedchemlett.0c00033
11046028 151994 0 None -257 4 Guinea pig 4.9 pKd = 4.9 Binding
Potency at histamine H2 receptor subtype, was tested on guinea pig right atriumPotency at histamine H2 receptor subtype, was tested on guinea pig right atrium
ChEMBL 338 6 1 4 4.5 C/C(=N\O)c1ccc(OCc2ccc(CN3CCCCC3)cc2)cc1 10.1021/jm021084k
CHEMBL39716 151994 0 None -257 4 Guinea pig 4.9 pKd = 4.9 Binding
Potency at histamine H2 receptor subtype, was tested on guinea pig right atriumPotency at histamine H2 receptor subtype, was tested on guinea pig right atrium
ChEMBL 338 6 1 4 4.5 C/C(=N\O)c1ccc(OCc2ccc(CN3CCCCC3)cc2)cc1 10.1021/jm021084k
156021166 177752 0 None - 1 Human 7.8 pKd = 7.8 Binding
Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis
ChEMBL 908 25 3 8 10.3 C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acsmedchemlett.0c00033
CHEMBL4647775 177752 0 None - 1 Human 7.8 pKd = 7.8 Binding
Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis
ChEMBL 908 25 3 8 10.3 C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acsmedchemlett.0c00033
CHEMBL4651205 177752 0 None - 1 Human 7.8 pKd = 7.8 Binding
Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis
ChEMBL 908 25 3 8 10.3 C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acsmedchemlett.0c00033
44267951 15271 0 None - 1 Guinea pig 7.8 pKd = 7.8 Binding
Evaluated for activity against Histamine H2 receptor in guinea pig atrium and represented pA2Evaluated for activity against Histamine H2 receptor in guinea pig atrium and represented pA2
ChEMBL 266 7 3 4 0.7 CSCC/N=C(\NC#N)NCCCc1c[nH]cn1 10.1021/jm00163a001
CHEMBL12158 15271 0 None - 1 Guinea pig 7.8 pKd = 7.8 Binding
Evaluated for activity against Histamine H2 receptor in guinea pig atrium and represented pA2Evaluated for activity against Histamine H2 receptor in guinea pig atrium and represented pA2
ChEMBL 266 7 3 4 0.7 CSCC/N=C(\NC#N)NCCCc1c[nH]cn1 10.1021/jm00163a001
14883414 103620 0 None - 1 Guinea pig 6.8 pKd = 6.8 Binding
Compound was evaluated in vitro inhibitory activity against histamine H2 receptor in isolated Guinea pig right atria.Compound was evaluated in vitro inhibitory activity against histamine H2 receptor in isolated Guinea pig right atria.
ChEMBL 382 8 3 4 3.8 Nc1cccc(NC(=O)NCCCOc2cccc(CN3CCCCC3)c2)c1 10.1021/jm00091a012
CHEMBL309401 103620 0 None - 1 Guinea pig 6.8 pKd = 6.8 Binding
Compound was evaluated in vitro inhibitory activity against histamine H2 receptor in isolated Guinea pig right atria.Compound was evaluated in vitro inhibitory activity against histamine H2 receptor in isolated Guinea pig right atria.
ChEMBL 382 8 3 4 3.8 Nc1cccc(NC(=O)NCCCOc2cccc(CN3CCCCC3)c2)c1 10.1021/jm00091a012
14514753 203876 1 None - 1 Guinea pig 6.8 pKd = 6.8 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 305 7 2 3 2.4 CNC(=O)NCCCOc1cccc(CN2CCCCC2)c1 10.1021/jm00091a012
CHEMBL81506 203876 1 None - 1 Guinea pig 6.8 pKd = 6.8 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 305 7 2 3 2.4 CNC(=O)NCCCOc1cccc(CN2CCCCC2)c1 10.1021/jm00091a012
14514749 203825 0 None - 1 Guinea pig 6.8 pKd = 6.8 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 427 10 2 5 4.3 COc1ccc(OC)c(NC(=O)NCCCOc2cccc(CN3CCCCC3)c2)c1 10.1021/jm00091a012
CHEMBL81039 203825 0 None - 1 Guinea pig 6.8 pKd = 6.8 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 427 10 2 5 4.3 COc1ccc(OC)c(NC(=O)NCCCOc2cccc(CN3CCCCC3)c2)c1 10.1021/jm00091a012
156015041 177648 0 None - 1 Human 7.8 pKd = 7.8 Binding
Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis
ChEMBL 1029 30 3 11 10.0 CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acsmedchemlett.0c00033
CHEMBL4637356 177648 0 None - 1 Human 7.8 pKd = 7.8 Binding
Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis
ChEMBL 1029 30 3 11 10.0 CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acsmedchemlett.0c00033
CHEMBL4650547 177648 0 None - 1 Human 7.8 pKd = 7.8 Binding
Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis
ChEMBL 1029 30 3 11 10.0 CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acsmedchemlett.0c00033
156015643 177710 0 None - 1 Human 6.8 pKd = 6.8 Binding
Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis
ChEMBL 1001 28 3 11 9.2 CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acsmedchemlett.0c00033
CHEMBL4645213 177710 0 None - 1 Human 6.8 pKd = 6.8 Binding
Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis
ChEMBL 1001 28 3 11 9.2 CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acsmedchemlett.0c00033
CHEMBL4650968 177710 0 None - 1 Human 6.8 pKd = 6.8 Binding
Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis
ChEMBL 1001 28 3 11 9.2 CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acsmedchemlett.0c00033
14514757 203663 1 None - 1 Guinea pig 6.8 pKd = 6.8 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 347 9 2 3 3.4 CC(C)CNC(=O)NCCCOc1cccc(CN2CCCCC2)c1 10.1021/jm00091a012
CHEMBL79974 203663 1 None - 1 Guinea pig 6.8 pKd = 6.8 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 347 9 2 3 3.4 CC(C)CNC(=O)NCCCOc1cccc(CN2CCCCC2)c1 10.1021/jm00091a012
14514734 105215 0 None - 1 Guinea pig 5.8 pKd = 5.8 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 435 8 2 3 5.3 O=C(NCCCOc1cccc(CN2CCCCC2)c1)Nc1ccc(C(F)(F)F)cc1 10.1021/jm00091a012
CHEMBL312601 105215 0 None - 1 Guinea pig 5.8 pKd = 5.8 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 435 8 2 3 5.3 O=C(NCCCOc1cccc(CN2CCCCC2)c1)Nc1ccc(C(F)(F)F)cc1 10.1021/jm00091a012
14514743 203920 0 None - 1 Guinea pig 6.8 pKd = 6.8 Binding
Compound was evaluated in vitro inhibitory activity against histamine H2 receptor in isolated Guinea pig right atria.Compound was evaluated in vitro inhibitory activity against histamine H2 receptor in isolated Guinea pig right atria.
ChEMBL 412 9 2 5 4.2 O=C(NCCCOc1cccc(CN2CCCCC2)c1)Nc1ccc([N+](=O)[O-])cc1 10.1021/jm00091a012
CHEMBL81859 203920 0 None - 1 Guinea pig 6.8 pKd = 6.8 Binding
Compound was evaluated in vitro inhibitory activity against histamine H2 receptor in isolated Guinea pig right atria.Compound was evaluated in vitro inhibitory activity against histamine H2 receptor in isolated Guinea pig right atria.
ChEMBL 412 9 2 5 4.2 O=C(NCCCOc1cccc(CN2CCCCC2)c1)Nc1ccc([N+](=O)[O-])cc1 10.1021/jm00091a012
156015722 177688 0 None - 1 Human 7.7 pKd = 7.7 Binding
Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry
ChEMBL 718 21 2 7 7.9 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O 10.1021/acsmedchemlett.0c00033
CHEMBL4644467 177688 0 None - 1 Human 7.7 pKd = 7.7 Binding
Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry
ChEMBL 718 21 2 7 7.9 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O 10.1021/acsmedchemlett.0c00033
CHEMBL4650837 177688 0 None - 1 Human 7.7 pKd = 7.7 Binding
Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry
ChEMBL 718 21 2 7 7.9 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O 10.1021/acsmedchemlett.0c00033
90667428 108986 0 None - 1 Guinea pig 4.7 pKd = 4.7 Binding
Antagonist activity at guinea pig histamine H2 receptor assessed as inhibition of histamine-induced response after 30 minsAntagonist activity at guinea pig histamine H2 receptor assessed as inhibition of histamine-induced response after 30 mins
ChEMBL 324 7 2 2 2.6 CC(CC(=O)/N=C(\N)NCCCc1ccncc1)c1ccccc1 10.1039/C3MD00245D
CHEMBL3220886 108986 0 None - 1 Guinea pig 4.7 pKd = 4.7 Binding
Antagonist activity at guinea pig histamine H2 receptor assessed as inhibition of histamine-induced response after 30 minsAntagonist activity at guinea pig histamine H2 receptor assessed as inhibition of histamine-induced response after 30 mins
ChEMBL 324 7 2 2 2.6 CC(CC(=O)/N=C(\N)NCCCc1ccncc1)c1ccccc1 10.1039/C3MD00245D
14514740 203683 0 None - 1 Guinea pig 6.7 pKd = 6.7 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 397 9 2 4 4.3 COc1cccc(NC(=O)NCCCOc2cccc(CN3CCCCC3)c2)c1 10.1021/jm00091a012
CHEMBL80084 203683 0 None - 1 Guinea pig 6.7 pKd = 6.7 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 397 9 2 4 4.3 COc1cccc(NC(=O)NCCCOc2cccc(CN3CCCCC3)c2)c1 10.1021/jm00091a012
10916261 35051 0 None -245470 4 Guinea pig 4.7 pKd = 4.7 Binding
Activity at Histamine H2 receptor using functional H2 receptor assay on guinea pig atriumActivity at Histamine H2 receptor using functional H2 receptor assay on guinea pig atrium
ChEMBL 395 7 1 4 5.9 Clc1ccc2c(Nc3ccc(OCCCN4CCCCC4)cc3)ccnc2c1 10.1021/jm0110845
CHEMBL14364 35051 0 None -245470 4 Guinea pig 4.7 pKd = 4.7 Binding
Activity at Histamine H2 receptor using functional H2 receptor assay on guinea pig atriumActivity at Histamine H2 receptor using functional H2 receptor assay on guinea pig atrium
ChEMBL 395 7 1 4 5.9 Clc1ccc2c(Nc3ccc(OCCCN4CCCCC4)cc3)ccnc2c1 10.1021/jm0110845
11080253 36337 0 None -12882 4 Guinea pig 4.7 pKd = 4.7 Binding
Activity at Histamine H2 receptor using functional H2 receptor assay on guinea pig atriumActivity at Histamine H2 receptor using functional H2 receptor assay on guinea pig atrium
ChEMBL 417 11 1 4 5.9 c1ccc2c(NCCCCc3ccc(OCCCN4CCCCC4)cc3)ccnc2c1 10.1021/jm0110845
CHEMBL14484 36337 0 None -12882 4 Guinea pig 4.7 pKd = 4.7 Binding
Activity at Histamine H2 receptor using functional H2 receptor assay on guinea pig atriumActivity at Histamine H2 receptor using functional H2 receptor assay on guinea pig atrium
ChEMBL 417 11 1 4 5.9 c1ccc2c(NCCCCc3ccc(OCCCN4CCCCC4)cc3)ccnc2c1 10.1021/jm0110845
11826604 39453 0 None -15135 4 Guinea pig 4.7 pKd = 4.7 Binding
Activity at Histamine H2 receptor using functional H2 receptor assay on guinea pig atriumActivity at Histamine H2 receptor using functional H2 receptor assay on guinea pig atrium
ChEMBL 457 10 1 4 6.4 c1ccc2c(NCCCc3ccc(OCCCN4CCCCC4)cc3)c3c(nc2c1)CCCC3 10.1021/jm0110845
CHEMBL14754 39453 0 None -15135 4 Guinea pig 4.7 pKd = 4.7 Binding
Activity at Histamine H2 receptor using functional H2 receptor assay on guinea pig atriumActivity at Histamine H2 receptor using functional H2 receptor assay on guinea pig atrium
ChEMBL 457 10 1 4 6.4 c1ccc2c(NCCCc3ccc(OCCCN4CCCCC4)cc3)c3c(nc2c1)CCCC3 10.1021/jm0110845
11048988 40693 0 None -9999 4 Guinea pig 4.7 pKd = 4.7 Binding
Activity at Histamine H2 receptor using functional H2 receptor assay on guinea pig atriumActivity at Histamine H2 receptor using functional H2 receptor assay on guinea pig atrium
ChEMBL 471 11 1 4 6.8 c1ccc2c(NCCCCc3ccc(OCCCN4CCCCC4)cc3)c3c(nc2c1)CCCC3 10.1021/jm0110845
CHEMBL14868 40693 0 None -9999 4 Guinea pig 4.7 pKd = 4.7 Binding
Activity at Histamine H2 receptor using functional H2 receptor assay on guinea pig atriumActivity at Histamine H2 receptor using functional H2 receptor assay on guinea pig atrium
ChEMBL 471 11 1 4 6.8 c1ccc2c(NCCCCc3ccc(OCCCN4CCCCC4)cc3)c3c(nc2c1)CCCC3 10.1021/jm0110845
14514754 203884 0 None - 1 Guinea pig 5.7 pKd = 5.7 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 347 7 2 3 3.5 CC(C)(C)NC(=O)NCCCOc1cccc(CN2CCCCC2)c1 10.1021/jm00091a012
CHEMBL81597 203884 0 None - 1 Guinea pig 5.7 pKd = 5.7 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 347 7 2 3 3.5 CC(C)(C)NC(=O)NCCCOc1cccc(CN2CCCCC2)c1 10.1021/jm00091a012
14514739 105482 0 None - 1 Guinea pig 5.7 pKd = 5.7 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 427 10 2 5 4.3 COc1ccc(NC(=O)NCCCOc2cccc(CN3CCCCC3)c2)c(OC)c1 10.1021/jm00091a012
CHEMBL313060 105482 0 None - 1 Guinea pig 5.7 pKd = 5.7 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 427 10 2 5 4.3 COc1ccc(NC(=O)NCCCOc2cccc(CN3CCCCC3)c2)c(OC)c1 10.1021/jm00091a012
CHEMBL5088914 213776 0 None - 1 Human 6.6 pKd = 6.6 Binding
Binding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysisBinding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysis
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C 10.1016/j.bmcl.2021.128388
CHEMBL5095949 213776 0 None - 1 Human 6.6 pKd = 6.6 Binding
Binding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysisBinding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysis
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C 10.1016/j.bmcl.2021.128388
44403829 71093 0 None - 1 Human 6.6 pKd = 6.6 Binding
Negative logarithm of the drug concentration against H2 histamine receptorNegative logarithm of the drug concentration against H2 histamine receptor
ChEMBL 743 15 4 7 5.3 CN1C(=O)[C@H](NC(=O)Nc2ccc(CC(=O)NCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm058225d
CHEMBL196143 71093 0 None - 1 Human 6.6 pKd = 6.6 Binding
Negative logarithm of the drug concentration against H2 histamine receptorNegative logarithm of the drug concentration against H2 histamine receptor
ChEMBL 743 15 4 7 5.3 CN1C(=O)[C@H](NC(=O)Nc2ccc(CC(=O)NCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm058225d
5105 176243 49 None -1 2 Human 6.6 pKd = 6.6 Binding
Negative logarithm of the drug concentration against H2 histamine receptorNegative logarithm of the drug concentration against H2 histamine receptor
ChEMBL 348 9 1 5 2.1 CC(=O)OCC(=O)NCCCOc1cccc(CN2CCCCC2)c1 10.1021/jm058225d
CHEMBL46102 176243 49 None -1 2 Human 6.6 pKd = 6.6 Binding
Negative logarithm of the drug concentration against H2 histamine receptorNegative logarithm of the drug concentration against H2 histamine receptor
ChEMBL 348 9 1 5 2.1 CC(=O)OCC(=O)NCCCOc1cccc(CN2CCCCC2)c1 10.1021/jm058225d
1231 922 112 None -2 8 Guinea pig 6.6 pKd = 6.6 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/jm00091a012
2756 922 112 None -2 8 Guinea pig 6.6 pKd = 6.6 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/jm00091a012
645 922 112 None -2 8 Guinea pig 6.6 pKd = 6.6 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/jm00091a012
CHEMBL30 922 112 None -2 8 Guinea pig 6.6 pKd = 6.6 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/jm00091a012
DB00501 922 112 None -2 8 Guinea pig 6.6 pKd = 6.6 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/jm00091a012
14514742 104938 0 None - 1 Guinea pig 6.6 pKd = 6.6 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 412 9 2 5 4.2 O=C(NCCCOc1cccc(CN2CCCCC2)c1)Nc1cccc([N+](=O)[O-])c1 10.1021/jm00091a012
CHEMBL311978 104938 0 None - 1 Guinea pig 6.6 pKd = 6.6 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 412 9 2 5 4.2 O=C(NCCCOc1cccc(CN2CCCCC2)c1)Nc1cccc([N+](=O)[O-])c1 10.1021/jm00091a012
156015152 177721 0 None - 1 Human 7.6 pKd = 7.6 Binding
Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry
ChEMBL 676 18 2 7 6.7 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O 10.1021/acsmedchemlett.0c00033
CHEMBL4641916 177721 0 None - 1 Human 7.6 pKd = 7.6 Binding
Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry
ChEMBL 676 18 2 7 6.7 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O 10.1021/acsmedchemlett.0c00033
CHEMBL4651017 177721 0 None - 1 Human 7.6 pKd = 7.6 Binding
Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry
ChEMBL 676 18 2 7 6.7 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O 10.1021/acsmedchemlett.0c00033
156015793 177674 0 None - 1 Human 6.5 pKd = 6.5 Binding
Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry
ChEMBL 880 23 3 8 9.5 C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acsmedchemlett.0c00033
CHEMBL4645867 177674 0 None - 1 Human 6.5 pKd = 6.5 Binding
Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry
ChEMBL 880 23 3 8 9.5 C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acsmedchemlett.0c00033
CHEMBL4650701 177674 0 None - 1 Human 6.5 pKd = 6.5 Binding
Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry
ChEMBL 880 23 3 8 9.5 C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acsmedchemlett.0c00033
14883413 203912 0 None - 1 Guinea pig 6.5 pKd = 6.5 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 411 8 2 5 4.0 O=C(NCCCOc1cccc(CN2CCCCC2)c1)Nc1ccc2c(c1)OCO2 10.1021/jm00091a012
CHEMBL81758 203912 0 None - 1 Guinea pig 6.5 pKd = 6.5 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 411 8 2 5 4.0 O=C(NCCCOc1cccc(CN2CCCCC2)c1)Nc1ccc2c(c1)OCO2 10.1021/jm00091a012
156015633 177670 0 None - 1 Human 7.5 pKd = 7.5 Binding
Binding affinity to human H2R expressing Sf9 cells incubated for 60 mins by microbeta scintillation counter methodBinding affinity to human H2R expressing Sf9 cells incubated for 60 mins by microbeta scintillation counter method
ChEMBL 498 17 3 7 3.6 CCC(=O)NCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O 10.1021/acsmedchemlett.0c00033
156020426 177670 0 None - 1 Human 7.5 pKd = 7.5 Binding
Binding affinity to human H2R expressing Sf9 cells incubated for 60 mins by microbeta scintillation counter methodBinding affinity to human H2R expressing Sf9 cells incubated for 60 mins by microbeta scintillation counter method
ChEMBL 498 17 3 7 3.6 CCC(=O)NCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O 10.1021/acsmedchemlett.0c00033
CHEMBL4648685 177670 0 None - 1 Human 7.5 pKd = 7.5 Binding
Binding affinity to human H2R expressing Sf9 cells incubated for 60 mins by microbeta scintillation counter methodBinding affinity to human H2R expressing Sf9 cells incubated for 60 mins by microbeta scintillation counter method
ChEMBL 498 17 3 7 3.6 CCC(=O)NCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O 10.1021/acsmedchemlett.0c00033
CHEMBL4650687 177670 0 None - 1 Human 7.5 pKd = 7.5 Binding
Binding affinity to human H2R expressing Sf9 cells incubated for 60 mins by microbeta scintillation counter methodBinding affinity to human H2R expressing Sf9 cells incubated for 60 mins by microbeta scintillation counter method
ChEMBL 498 17 3 7 3.6 CCC(=O)NCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O 10.1021/acsmedchemlett.0c00033
14514737 103681 0 None - 1 Guinea pig 6.5 pKd = 6.5 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 401 8 2 3 4.9 O=C(NCCCOc1cccc(CN2CCCCC2)c1)Nc1cccc(Cl)c1 10.1021/jm00091a012
CHEMBL309659 103681 0 None - 1 Guinea pig 6.5 pKd = 6.5 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 401 8 2 3 4.9 O=C(NCCCOc1cccc(CN2CCCCC2)c1)Nc1cccc(Cl)c1 10.1021/jm00091a012
11004759 42903 1 None -97723 4 Guinea pig 4.5 pKd = 4.5 Binding
Activity at Histamine H2 receptor using functional H2 receptor assay on guinea pig atriumActivity at Histamine H2 receptor using functional H2 receptor assay on guinea pig atrium
ChEMBL 443 9 1 4 6.0 c1ccc2c(NCCc3ccc(OCCCN4CCCCC4)cc3)c3c(nc2c1)CCCC3 10.1021/jm0110845
CHEMBL15056 42903 1 None -97723 4 Guinea pig 4.5 pKd = 4.5 Binding
Activity at Histamine H2 receptor using functional H2 receptor assay on guinea pig atriumActivity at Histamine H2 receptor using functional H2 receptor assay on guinea pig atrium
ChEMBL 443 9 1 4 6.0 c1ccc2c(NCCc3ccc(OCCCN4CCCCC4)cc3)c3c(nc2c1)CCCC3 10.1021/jm0110845
44352410 19370 0 None -7 3 Guinea pig 4.5 pKd = 4.5 Binding
Receptor profile was evaluated at Histamine H2 receptor of guinea pig atriumReceptor profile was evaluated at Histamine H2 receptor of guinea pig atrium
ChEMBL 270 5 1 3 3.0 CC(NC(=O)OCCCN1CCCCC1)C(C)(C)C 10.1021/jm020910m
CHEMBL130005 19370 0 None -7 3 Guinea pig 4.5 pKd = 4.5 Binding
Receptor profile was evaluated at Histamine H2 receptor of guinea pig atriumReceptor profile was evaluated at Histamine H2 receptor of guinea pig atrium
ChEMBL 270 5 1 3 3.0 CC(NC(=O)OCCCN1CCCCC1)C(C)(C)C 10.1021/jm020910m
CHEMBL5094663 213720 0 None - 1 Human 7.5 pKd = 7.5 Binding
Binding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysisBinding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysis
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](C)c3ccccc3C2(C)C)c2ccccc2C1(C)C 10.1016/j.bmcl.2021.128388
14514748 203685 1 None - 1 Guinea pig 6.5 pKd = 6.5 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 381 9 2 3 3.9 O=C(NCCCOc1cccc(CN2CCCCC2)c1)NCc1ccccc1 10.1021/jm00091a012
CHEMBL80105 203685 1 None - 1 Guinea pig 6.5 pKd = 6.5 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 381 9 2 3 3.9 O=C(NCCCOc1cccc(CN2CCCCC2)c1)NCc1ccccc1 10.1021/jm00091a012
11725577 11064 0 None -30 4 Guinea pig 5.4 pKd = 5.4 Binding
Potency at histamine H2 receptor subtype, was tested on guinea pig right atriumPotency at histamine H2 receptor subtype, was tested on guinea pig right atrium
ChEMBL 352 7 0 4 4.6 CO/N=C(\C)c1ccc(OCc2ccc(CN3CCCCC3)cc2)cc1 10.1021/jm021084k
CHEMBL1178642 11064 0 None -30 4 Guinea pig 5.4 pKd = 5.4 Binding
Potency at histamine H2 receptor subtype, was tested on guinea pig right atriumPotency at histamine H2 receptor subtype, was tested on guinea pig right atrium
ChEMBL 352 7 0 4 4.6 CO/N=C(\C)c1ccc(OCc2ccc(CN3CCCCC3)cc2)cc1 10.1021/jm021084k
CHEMBL35869 11064 0 None -30 4 Guinea pig 5.4 pKd = 5.4 Binding
Potency at histamine H2 receptor subtype, was tested on guinea pig right atriumPotency at histamine H2 receptor subtype, was tested on guinea pig right atrium
ChEMBL 352 7 0 4 4.6 CO/N=C(\C)c1ccc(OCc2ccc(CN3CCCCC3)cc2)cc1 10.1021/jm021084k
10067161 43854 1 None -239883 4 Guinea pig 4.4 pKd = 4.4 Binding
Activity at Histamine H2 receptor using functional H2 receptor assay on guinea pig atriumActivity at Histamine H2 receptor using functional H2 receptor assay on guinea pig atrium
ChEMBL 361 7 1 4 5.2 c1ccc2c(Nc3ccc(OCCCN4CCCCC4)cc3)ccnc2c1 10.1021/jm0110845
CHEMBL15153 43854 1 None -239883 4 Guinea pig 4.4 pKd = 4.4 Binding
Activity at Histamine H2 receptor using functional H2 receptor assay on guinea pig atriumActivity at Histamine H2 receptor using functional H2 receptor assay on guinea pig atrium
ChEMBL 361 7 1 4 5.2 c1ccc2c(Nc3ccc(OCCCN4CCCCC4)cc3)ccnc2c1 10.1021/jm0110845
129319 104399 21 None - 1 Guinea pig 7.4 pKd = 7.4 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 319 8 2 3 2.8 CCNC(=O)NCCCOc1cccc(CN2CCCCC2)c1 10.1021/jm00091a012
CHEMBL311206 104399 21 None - 1 Guinea pig 7.4 pKd = 7.4 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 319 8 2 3 2.8 CCNC(=O)NCCCOc1cccc(CN2CCCCC2)c1 10.1021/jm00091a012
14514752 203879 1 None - 1 Guinea pig 7.4 pKd = 7.4 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 373 8 2 3 4.1 O=C(NCCCOc1cccc(CN2CCCCC2)c1)NC1CCCCC1 10.1021/jm00091a012
CHEMBL81545 203879 1 None - 1 Guinea pig 7.4 pKd = 7.4 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 373 8 2 3 4.1 O=C(NCCCOc1cccc(CN2CCCCC2)c1)NC1CCCCC1 10.1021/jm00091a012
14514755 204013 1 None - 1 Guinea pig 7.4 pKd = 7.4 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 333 8 2 3 3.1 CC(C)NC(=O)NCCCOc1cccc(CN2CCCCC2)c1 10.1021/jm00091a012
CHEMBL82654 204013 1 None - 1 Guinea pig 7.4 pKd = 7.4 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 333 8 2 3 3.1 CC(C)NC(=O)NCCCOc1cccc(CN2CCCCC2)c1 10.1021/jm00091a012
14514746 203606 0 None - 1 Guinea pig 5.4 pKd = 5.4 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 413 9 2 4 4.8 COc1ccc(N/C(S)=N/CCCOc2cccc(CN3CCCCC3)c2)cc1 10.1021/jm00091a012
CHEMBL79507 203606 0 None - 1 Guinea pig 5.4 pKd = 5.4 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 413 9 2 4 4.8 COc1ccc(N/C(S)=N/CCCOc2cccc(CN3CCCCC3)c2)cc1 10.1021/jm00091a012
156014823 177742 0 None - 1 Human 6.4 pKd = 6.4 Binding
Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis
ChEMBL 1109 31 4 13 9.2 CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3cc(S(=O)(=O)O)ccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acsmedchemlett.0c00033
CHEMBL4641747 177742 0 None - 1 Human 6.4 pKd = 6.4 Binding
Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis
ChEMBL 1109 31 4 13 9.2 CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3cc(S(=O)(=O)O)ccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acsmedchemlett.0c00033
CHEMBL4651132 177742 0 None - 1 Human 6.4 pKd = 6.4 Binding
Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis
ChEMBL 1109 31 4 13 9.2 CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3cc(S(=O)(=O)O)ccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acsmedchemlett.0c00033
156015041 177648 0 None - 1 Human 7.3 pKd = 7.3 Binding
Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry
ChEMBL 1029 30 3 11 10.0 CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acsmedchemlett.0c00033
CHEMBL4637356 177648 0 None - 1 Human 7.3 pKd = 7.3 Binding
Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry
ChEMBL 1029 30 3 11 10.0 CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acsmedchemlett.0c00033
CHEMBL4650547 177648 0 None - 1 Human 7.3 pKd = 7.3 Binding
Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry
ChEMBL 1029 30 3 11 10.0 CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acsmedchemlett.0c00033
14514758 167449 1 None - 1 Guinea pig 7.3 pKd = 7.3 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 331 8 2 3 2.9 O=C(NCCCOc1cccc(CN2CCCCC2)c1)NC1CC1 10.1021/jm00091a012
CHEMBL432167 167449 1 None - 1 Guinea pig 7.3 pKd = 7.3 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 331 8 2 3 2.9 O=C(NCCCOc1cccc(CN2CCCCC2)c1)NC1CC1 10.1021/jm00091a012
90667234 108972 0 None 3 2 Guinea pig 6.3 pKd = 6.3 Binding
Antagonist activity at guinea pig histamine H2 receptor assessed as inhibition of histamine-induced response after 30 minsAntagonist activity at guinea pig histamine H2 receptor assessed as inhibition of histamine-induced response after 30 mins
ChEMBL 314 7 3 3 1.4 CC(CC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1039/C3MD00245D
CHEMBL3220635 108972 0 None 3 2 Guinea pig 6.3 pKd = 6.3 Binding
Antagonist activity at guinea pig histamine H2 receptor assessed as inhibition of histamine-induced response after 30 minsAntagonist activity at guinea pig histamine H2 receptor assessed as inhibition of histamine-induced response after 30 mins
ChEMBL 314 7 3 3 1.4 CC(CC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1039/C3MD00245D
14514745 203987 0 None - 1 Guinea pig 6.3 pKd = 6.3 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 411 10 2 4 4.7 CCOc1ccc(NC(=O)NCCCOc2cccc(CN3CCCCC3)c2)cc1 10.1021/jm00091a012
CHEMBL82430 203987 0 None - 1 Guinea pig 6.3 pKd = 6.3 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 411 10 2 4 4.7 CCOc1ccc(NC(=O)NCCCOc2cccc(CN3CCCCC3)c2)cc1 10.1021/jm00091a012
10873565 37588 0 None -10000 4 Guinea pig 5.3 pKd = 5.3 Binding
Activity at Histamine H2 receptor using functional H2 receptor assay on guinea pig atriumActivity at Histamine H2 receptor using functional H2 receptor assay on guinea pig atrium
ChEMBL 423 9 1 4 5.8 Clc1ccc2c(NCCc3ccc(OCCCN4CCCCC4)cc3)ccnc2c1 10.1021/jm0110845
CHEMBL14587 37588 0 None -10000 4 Guinea pig 5.3 pKd = 5.3 Binding
Activity at Histamine H2 receptor using functional H2 receptor assay on guinea pig atriumActivity at Histamine H2 receptor using functional H2 receptor assay on guinea pig atrium
ChEMBL 423 9 1 4 5.8 Clc1ccc2c(NCCc3ccc(OCCCN4CCCCC4)cc3)ccnc2c1 10.1021/jm0110845
CHEMBL5075713 213743 0 None - 1 Human 7.3 pKd = 7.3 Binding
Binding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysisBinding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysis
ChEMBL None None None CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2c[nH]cn2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1016/j.bmcl.2021.128388
CHEMBL5095559 213743 0 None - 1 Human 7.3 pKd = 7.3 Binding
Binding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysisBinding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysis
ChEMBL None None None CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2c[nH]cn2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1016/j.bmcl.2021.128388
156015643 177710 0 None - 1 Human 6.3 pKd = 6.3 Binding
Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry
ChEMBL 1001 28 3 11 9.2 CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acsmedchemlett.0c00033
CHEMBL4645213 177710 0 None - 1 Human 6.3 pKd = 6.3 Binding
Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry
ChEMBL 1001 28 3 11 9.2 CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acsmedchemlett.0c00033
CHEMBL4650968 177710 0 None - 1 Human 6.3 pKd = 6.3 Binding
Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry
ChEMBL 1001 28 3 11 9.2 CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acsmedchemlett.0c00033
5039 62838 13 None 2 2 Human 7.2 pKd = 7.2 Binding
Binding affinity to histamine H2 receptor (unknown origin)Binding affinity to histamine H2 receptor (unknown origin)
ChEMBL 314 10 2 7 1.5 CNC(=C[N+](=O)[O-])NCCSCc1ccc(CN(C)C)o1 10.1007/s00044-004-0012-z
CHEMBL1790041 62838 13 None 2 2 Human 7.2 pKd = 7.2 Binding
Binding affinity to histamine H2 receptor (unknown origin)Binding affinity to histamine H2 receptor (unknown origin)
ChEMBL 314 10 2 7 1.5 CNC(=C[N+](=O)[O-])NCCSCc1ccc(CN(C)C)o1 10.1007/s00044-004-0012-z
14514733 104415 0 None - 1 Guinea pig 6.2 pKd = 6.2 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 381 8 2 3 4.6 Cc1ccc(NC(=O)NCCCOc2cccc(CN3CCCCC3)c2)cc1 10.1021/jm00091a012
CHEMBL311272 104415 0 None - 1 Guinea pig 6.2 pKd = 6.2 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 381 8 2 3 4.6 Cc1ccc(NC(=O)NCCCOc2cccc(CN3CCCCC3)c2)cc1 10.1021/jm00091a012
14514731 105141 0 None - 1 Guinea pig 6.2 pKd = 6.2 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 397 9 2 4 4.3 COc1ccc(NC(=O)NCCCOc2cccc(CN3CCCCC3)c2)cc1 10.1021/jm00091a012
CHEMBL312419 105141 0 None - 1 Guinea pig 6.2 pKd = 6.2 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 397 9 2 4 4.3 COc1ccc(NC(=O)NCCCOc2cccc(CN3CCCCC3)c2)cc1 10.1021/jm00091a012
14514736 203877 0 None - 1 Guinea pig 6.2 pKd = 6.2 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 401 8 2 3 4.9 O=C(NCCCOc1cccc(CN2CCCCC2)c1)Nc1ccc(Cl)cc1 10.1021/jm00091a012
CHEMBL81520 203877 0 None - 1 Guinea pig 6.2 pKd = 6.2 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 401 8 2 3 4.9 O=C(NCCCOc1cccc(CN2CCCCC2)c1)Nc1ccc(Cl)cc1 10.1021/jm00091a012
156015722 177688 0 None - 1 Human 7.2 pKd = 7.2 Binding
Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by imaging flow cytometry analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by imaging flow cytometry analysis
ChEMBL 718 21 2 7 7.9 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O 10.1021/acsmedchemlett.0c00033
CHEMBL4644467 177688 0 None - 1 Human 7.2 pKd = 7.2 Binding
Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by imaging flow cytometry analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by imaging flow cytometry analysis
ChEMBL 718 21 2 7 7.9 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O 10.1021/acsmedchemlett.0c00033
CHEMBL4650837 177688 0 None - 1 Human 7.2 pKd = 7.2 Binding
Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by imaging flow cytometry analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by imaging flow cytometry analysis
ChEMBL 718 21 2 7 7.9 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O 10.1021/acsmedchemlett.0c00033
5039 62838 13 None -2 2 Guinea pig 7.2 pKd = 7.2 Binding
Compound was evaluated in vitro inhibitory activity against histamine H2 receptor in isolated Guinea pig right atria.Compound was evaluated in vitro inhibitory activity against histamine H2 receptor in isolated Guinea pig right atria.
ChEMBL 314 10 2 7 1.5 CNC(=C[N+](=O)[O-])NCCSCc1ccc(CN(C)C)o1 10.1021/jm00091a012
CHEMBL1790041 62838 13 None -2 2 Guinea pig 7.2 pKd = 7.2 Binding
Compound was evaluated in vitro inhibitory activity against histamine H2 receptor in isolated Guinea pig right atria.Compound was evaluated in vitro inhibitory activity against histamine H2 receptor in isolated Guinea pig right atria.
ChEMBL 314 10 2 7 1.5 CNC(=C[N+](=O)[O-])NCCSCc1ccc(CN(C)C)o1 10.1021/jm00091a012
CHEMBL5083588 213748 0 None - 1 Human 7.2 pKd = 7.2 Binding
Binding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysisBinding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysis
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C 10.1016/j.bmcl.2021.128388
CHEMBL5095633 213748 0 None - 1 Human 7.2 pKd = 7.2 Binding
Binding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysisBinding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysis
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C 10.1016/j.bmcl.2021.128388
156015152 177721 0 None - 1 Human 7.1 pKd = 7.1 Binding
Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis
ChEMBL 676 18 2 7 6.7 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O 10.1021/acsmedchemlett.0c00033
CHEMBL4641916 177721 0 None - 1 Human 7.1 pKd = 7.1 Binding
Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis
ChEMBL 676 18 2 7 6.7 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O 10.1021/acsmedchemlett.0c00033
CHEMBL4651017 177721 0 None - 1 Human 7.1 pKd = 7.1 Binding
Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis
ChEMBL 676 18 2 7 6.7 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O 10.1021/acsmedchemlett.0c00033
14514738 106640 0 None - 1 Guinea pig 6.1 pKd = 6.1 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 397 9 2 4 4.3 COc1ccccc1NC(=O)NCCCOc1cccc(CN2CCCCC2)c1 10.1021/jm00091a012
CHEMBL316154 106640 0 None - 1 Guinea pig 6.1 pKd = 6.1 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 397 9 2 4 4.3 COc1ccccc1NC(=O)NCCCOc1cccc(CN2CCCCC2)c1 10.1021/jm00091a012
9866657 11898 0 None -426 4 Guinea pig 5.1 pKd = 5.1 Binding
Potency at histamine H2 receptor subtype, was tested on guinea pig right atriumPotency at histamine H2 receptor subtype, was tested on guinea pig right atrium
ChEMBL 309 6 0 3 4.1 CC(=O)c1ccc(OCc2ccc(CN3CCCC3)cc2)cc1 10.1021/jm021084k
CHEMBL1183328 11898 0 None -426 4 Guinea pig 5.1 pKd = 5.1 Binding
Potency at histamine H2 receptor subtype, was tested on guinea pig right atriumPotency at histamine H2 receptor subtype, was tested on guinea pig right atrium
ChEMBL 309 6 0 3 4.1 CC(=O)c1ccc(OCc2ccc(CN3CCCC3)cc2)cc1 10.1021/jm021084k
CHEMBL290613 11898 0 None -426 4 Guinea pig 5.1 pKd = 5.1 Binding
Potency at histamine H2 receptor subtype, was tested on guinea pig right atriumPotency at histamine H2 receptor subtype, was tested on guinea pig right atrium
ChEMBL 309 6 0 3 4.1 CC(=O)c1ccc(OCc2ccc(CN3CCCC3)cc2)cc1 10.1021/jm021084k
3032915 15306 20 None -25 7 Human 5.1 pKd = 5.1 Binding
Binding affinity to histamine H2 receptor (unknown origin)Binding affinity to histamine H2 receptor (unknown origin)
ChEMBL 212 5 3 2 1.2 C/N=C(\S)NCCCCc1c[nH]cn1 10.1007/s00044-004-0012-z
CHEMBL12160 15306 20 None -25 7 Human 5.1 pKd = 5.1 Binding
Binding affinity to histamine H2 receptor (unknown origin)Binding affinity to histamine H2 receptor (unknown origin)
ChEMBL 212 5 3 2 1.2 C/N=C(\S)NCCCCc1c[nH]cn1 10.1007/s00044-004-0012-z
CHEMBL5078202 213750 0 None - 1 Human 7.1 pKd = 7.1 Binding
Binding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysisBinding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysis
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1 10.1016/j.bmcl.2021.128388
CHEMBL5095695 213750 0 None - 1 Human 7.1 pKd = 7.1 Binding
Binding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysisBinding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysis
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1 10.1016/j.bmcl.2021.128388
14514750 203482 1 None - 1 Guinea pig 7.1 pKd = 7.1 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 347 10 2 3 3.5 CCCCNC(=O)NCCCOc1cccc(CN2CCCCC2)c1 10.1021/jm00091a012
CHEMBL78519 203482 1 None - 1 Guinea pig 7.1 pKd = 7.1 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 347 10 2 3 3.5 CCCCNC(=O)NCCCOc1cccc(CN2CCCCC2)c1 10.1021/jm00091a012
14514735 203682 0 None - 1 Guinea pig 6.1 pKd = 6.1 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 435 8 2 3 5.3 O=C(NCCCOc1cccc(CN2CCCCC2)c1)Nc1cccc(C(F)(F)F)c1 10.1021/jm00091a012
CHEMBL80069 203682 0 None - 1 Guinea pig 6.1 pKd = 6.1 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 435 8 2 3 5.3 O=C(NCCCOc1cccc(CN2CCCCC2)c1)Nc1cccc(C(F)(F)F)c1 10.1021/jm00091a012
14994252 203462 0 None - 1 Guinea pig 7.1 pKd = 7.1 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 337 9 2 3 2.7 O=C(NCCF)NCCCOc1cccc(CN2CCCCC2)c1 10.1021/jm00091a012
CHEMBL78339 203462 0 None - 1 Guinea pig 7.1 pKd = 7.1 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 337 9 2 3 2.7 O=C(NCCF)NCCCOc1cccc(CN2CCCCC2)c1 10.1021/jm00091a012
156015152 177721 0 None - 1 Human 7.1 pKd = 7.1 Binding
Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by imaging flow cytometry analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by imaging flow cytometry analysis
ChEMBL 676 18 2 7 6.7 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O 10.1021/acsmedchemlett.0c00033
CHEMBL4641916 177721 0 None - 1 Human 7.1 pKd = 7.1 Binding
Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by imaging flow cytometry analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by imaging flow cytometry analysis
ChEMBL 676 18 2 7 6.7 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O 10.1021/acsmedchemlett.0c00033
CHEMBL4651017 177721 0 None - 1 Human 7.1 pKd = 7.1 Binding
Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by imaging flow cytometry analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by imaging flow cytometry analysis
ChEMBL 676 18 2 7 6.7 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O 10.1021/acsmedchemlett.0c00033
156015722 177688 0 None - 1 Human 7.1 pKd = 7.1 Binding
Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis
ChEMBL 718 21 2 7 7.9 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O 10.1021/acsmedchemlett.0c00033
CHEMBL4644467 177688 0 None - 1 Human 7.1 pKd = 7.1 Binding
Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis
ChEMBL 718 21 2 7 7.9 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O 10.1021/acsmedchemlett.0c00033
CHEMBL4650837 177688 0 None - 1 Human 7.1 pKd = 7.1 Binding
Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis
ChEMBL 718 21 2 7 7.9 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O 10.1021/acsmedchemlett.0c00033
14514756 203908 0 None - 1 Guinea pig 7.0 pKd = 7.0 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 347 9 2 3 3.5 CCC(C)NC(=O)NCCCOc1cccc(CN2CCCCC2)c1 10.1021/jm00091a012
CHEMBL81750 203908 0 None - 1 Guinea pig 7.0 pKd = 7.0 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 347 9 2 3 3.5 CCC(C)NC(=O)NCCCOc1cccc(CN2CCCCC2)c1 10.1021/jm00091a012
14514747 204007 0 None - 1 Guinea pig 7.0 pKd = 7.0 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 333 9 2 3 3.2 CCCNC(=O)NCCCOc1cccc(CN2CCCCC2)c1 10.1021/jm00091a012
CHEMBL82599 204007 0 None - 1 Guinea pig 7.0 pKd = 7.0 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
ChEMBL 333 9 2 3 3.2 CCCNC(=O)NCCCOc1cccc(CN2CCCCC2)c1 10.1021/jm00091a012
9990475 56168 0 None -3 3 Rat 5.0 pKd = 5.0 Binding
Affinity to the Histamine H2 receptor was determined expressed in CHO cell using [125I]iodoaminopotentidine as radioligandAffinity to the Histamine H2 receptor was determined expressed in CHO cell using [125I]iodoaminopotentidine as radioligand
ChEMBL 205 2 2 3 -0.5 Cc1nc(N)[se]c1CCN 10.1016/S0960-894X(01)80533-3
CHEMBL1632408 56168 0 None -3 3 Rat 5.0 pKd = 5.0 Binding
Affinity to the Histamine H2 receptor was determined expressed in CHO cell using [125I]iodoaminopotentidine as radioligandAffinity to the Histamine H2 receptor was determined expressed in CHO cell using [125I]iodoaminopotentidine as radioligand
ChEMBL 205 2 2 3 -0.5 Cc1nc(N)[se]c1CCN 10.1016/S0960-894X(01)80533-3
CHEMBL2448450 56168 0 None -3 3 Rat 5.0 pKd = 5.0 Binding
Affinity to the Histamine H2 receptor was determined expressed in CHO cell using [125I]iodoaminopotentidine as radioligandAffinity to the Histamine H2 receptor was determined expressed in CHO cell using [125I]iodoaminopotentidine as radioligand
ChEMBL 205 2 2 3 -0.5 Cc1nc(N)[se]c1CCN 10.1016/S0960-894X(01)80533-3
1232 2017 6 None -6 2 Guinea pig 9.2 pKi = 9.2 Binding
Inhibition of [125I]APT binding to histamine H2 receptor in guinea pig cerebral membranes.Inhibition of [125I]APT binding to histamine H2 receptor in guinea pig cerebral membranes.
ChEMBL 603 11 4 6 3.1 N#CNC(=NCCCOc1cccc(c1)CN1CCCCC1)NCCNC(=O)c1ccc(c(c1)I)N 10.1021/jm00090a013
181461 2017 6 None -6 2 Guinea pig 9.2 pKi = 9.2 Binding
Inhibition of [125I]APT binding to histamine H2 receptor in guinea pig cerebral membranes.Inhibition of [125I]APT binding to histamine H2 receptor in guinea pig cerebral membranes.
ChEMBL 603 11 4 6 3.1 N#CNC(=NCCCOc1cccc(c1)CN1CCCCC1)NCCNC(=O)c1ccc(c(c1)I)N 10.1021/jm00090a013
CHEMBL72193 2017 6 None -6 2 Guinea pig 9.2 pKi = 9.2 Binding
Inhibition of [125I]APT binding to histamine H2 receptor in guinea pig cerebral membranes.Inhibition of [125I]APT binding to histamine H2 receptor in guinea pig cerebral membranes.
ChEMBL 603 11 4 6 3.1 N#CNC(=NCCCOc1cccc(c1)CN1CCCCC1)NCCNC(=O)c1ccc(c(c1)I)N 10.1021/jm00090a013
9805944 55919 31 None -2 9 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]tiotidine from human histamine H2 receptorDisplacement of [3H]tiotidine from human histamine H2 receptor
ChEMBL 462 7 2 3 4.7 CNC(=O)C(CCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm800510m
CHEMBL1627 55919 31 None -2 9 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]tiotidine from human histamine H2 receptorDisplacement of [3H]tiotidine from human histamine H2 receptor
ChEMBL 462 7 2 3 4.7 CNC(=O)C(CCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm800510m
164622259 185138 0 None 2290 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 336 6 4 5 1.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCc1ccco1 10.1016/j.ejmech.2021.113190
CHEMBL4865965 185138 0 None 2290 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 336 6 4 5 1.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCc1ccco1 10.1016/j.ejmech.2021.113190
164610648 184245 0 None 87 4 Human 7.0 pKi = 7 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 374 7 4 4 2.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4852212 184245 0 None 87 4 Human 7.0 pKi = 7 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 374 7 4 4 2.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
10852027 98222 0 None -77 3 Guinea pig 6.0 pKi = 6 Binding
Binding affinity against H2 receptor of Guinea pig atriumBinding affinity against H2 receptor of Guinea pig atrium
ChEMBL 304 7 2 5 2.2 O=C(NCc1cccc([N+](=O)[O-])c1)OCCCc1c[nH]cn1 10.1021/jm9507688
CHEMBL277537 98222 0 None -77 3 Guinea pig 6.0 pKi = 6 Binding
Binding affinity against H2 receptor of Guinea pig atriumBinding affinity against H2 receptor of Guinea pig atrium
ChEMBL 304 7 2 5 2.2 O=C(NCc1cccc([N+](=O)[O-])c1)OCCCc1c[nH]cn1 10.1021/jm9507688
44334025 4464 0 None -269 3 Human 6.0 pKi = 6 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 462 10 1 5 3.8 O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccccc3Cl)C2)cc1)C1CC1 10.1016/s0960-894x(02)00685-6
CHEMBL102384 4464 0 None -269 3 Human 6.0 pKi = 6 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 462 10 1 5 3.8 O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccccc3Cl)C2)cc1)C1CC1 10.1016/s0960-894x(02)00685-6
44334781 5319 0 None -346 3 Human 6.0 pKi = 6 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 458 11 1 6 3.1 COc1ccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)cc1 10.1016/s0960-894x(02)00685-6
CHEMBL107162 5319 0 None -346 3 Human 6.0 pKi = 6 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 458 11 1 6 3.1 COc1ccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)cc1 10.1016/s0960-894x(02)00685-6
33630 178369 94 None -13 28 Human 6.0 pKi = 6 Binding
Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assay
ChEMBL 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL47050 178369 94 None -13 28 Human 6.0 pKi = 6 Binding
Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assay
ChEMBL 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
4023 196 19 None -3467 4 Human 5.0 pKi = 5 Binding
Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor
ChEMBL 349 7 0 4 3.6 N#Cc1ccc(cc1)c1ccc(cc1)OCCCN1CC[C@H](C1)N(C)C 10.1016/s0960-894x(02)00648-0
9884746 196 19 None -3467 4 Human 5.0 pKi = 5 Binding
Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor
ChEMBL 349 7 0 4 3.6 N#Cc1ccc(cc1)c1ccc(cc1)OCCCN1CC[C@H](C1)N(C)C 10.1016/s0960-894x(02)00648-0
CHEMBL319000 196 19 None -3467 4 Human 5.0 pKi = 5 Binding
Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor
ChEMBL 349 7 0 4 3.6 N#Cc1ccc(cc1)c1ccc(cc1)OCCCN1CC[C@H](C1)N(C)C 10.1016/s0960-894x(02)00648-0
44335456 4470 0 None -316 4 Human 5.0 pKi = 5 Binding
Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor
ChEMBL 336 6 1 4 3.5 N#Cc1ccc(-c2ccc(OCCCN3CCC(O)CC3)cc2)cc1 10.1016/s0960-894x(02)00648-0
CHEMBL102416 4470 0 None -316 4 Human 5.0 pKi = 5 Binding
Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor
ChEMBL 336 6 1 4 3.5 N#Cc1ccc(-c2ccc(OCCCN3CCC(O)CC3)cc2)cc1 10.1016/s0960-894x(02)00648-0
10268636 5196 0 None -1174 4 Human 5.0 pKi = 5 Binding
Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor
ChEMBL 335 7 1 4 3.3 CN[C@@H]1CCN(CCCOc2ccc(-c3ccc(C#N)cc3)cc2)C1 10.1016/s0960-894x(02)00648-0
CHEMBL106545 5196 0 None -1174 4 Human 5.0 pKi = 5 Binding
Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor
ChEMBL 335 7 1 4 3.3 CN[C@@H]1CCN(CCCOc2ccc(-c3ccc(C#N)cc3)cc2)C1 10.1016/s0960-894x(02)00648-0
44304327 199188 0 None -2511 3 Human 5.0 pKi = 5 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 535 11 1 6 4.3 CC(C)(C)OC(=O)N[C@H](Cc1ccccc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL60143 199188 0 None -2511 3 Human 5.0 pKi = 5 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 535 11 1 6 4.3 CC(C)(C)OC(=O)N[C@H](Cc1ccccc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
44304295 201172 0 None -2290 3 Human 5.0 pKi = 5 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 357 8 1 5 1.5 O=C1C[C@@H](N2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)CC2)N1 10.1016/s0960-894x(02)00310-4
CHEMBL62596 201172 0 None -2290 3 Human 5.0 pKi = 5 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 357 8 1 5 1.5 O=C1C[C@@H](N2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)CC2)N1 10.1016/s0960-894x(02)00310-4
44304331 201422 0 None -2187 3 Human 5.0 pKi = 5 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 449 11 1 5 3.2 N[C@H](CCc1ccccc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL64059 201422 0 None -2187 3 Human 5.0 pKi = 5 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 449 11 1 5 3.2 N[C@H](CCc1ccccc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
44275807 98500 0 None -9120 10 Human 5.0 pKi = 5 Binding
Binding affinity towards human histaminergic (H2) receptorBinding affinity towards human histaminergic (H2) receptor
ChEMBL 422 7 0 4 4.5 C[C@H]1CC[C@H](C)N1CCCOc1ccc(-c2ccc(C(=O)N3CCOCC3)cc2)cc1 10.1016/s0960-894x(03)00118-5
CHEMBL27979 98500 0 None -9120 10 Human 5.0 pKi = 5 Binding
Binding affinity towards human histaminergic (H2) receptorBinding affinity towards human histaminergic (H2) receptor
ChEMBL 422 7 0 4 4.5 C[C@H]1CC[C@H](C)N1CCCOc1ccc(-c2ccc(C(=O)N3CCOCC3)cc2)cc1 10.1016/s0960-894x(03)00118-5
10422468 202448 0 None -501 3 Human 5.0 pKi = 5 Binding
Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors
ChEMBL 254 7 3 2 2.4 CC(C)/N=C(\S)NCCCCCc1c[nH]cn1 10.1021/jm00012a025
CHEMBL70603 202448 0 None -501 3 Human 5.0 pKi = 5 Binding
Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors
ChEMBL 254 7 3 2 2.4 CC(C)/N=C(\S)NCCCCCc1c[nH]cn1 10.1021/jm00012a025
10466840 202766 0 None -1000 4 Human 5.0 pKi = 5 Binding
Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors
ChEMBL 240 7 3 2 2.0 CC/N=C(\S)NCCCCCc1c[nH]cn1 10.1021/jm00012a025
CHEMBL72424 202766 0 None -1000 4 Human 5.0 pKi = 5 Binding
Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors
ChEMBL 240 7 3 2 2.0 CC/N=C(\S)NCCCCCc1c[nH]cn1 10.1021/jm00012a025
9990475 56168 0 None -3 3 Human 5.0 pKi = 5 Binding
Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells
ChEMBL 205 2 2 3 -0.5 Cc1nc(N)[se]c1CCN 10.1016/j.bmcl.2010.10.041
CHEMBL1632408 56168 0 None -3 3 Human 5.0 pKi = 5 Binding
Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells
ChEMBL 205 2 2 3 -0.5 Cc1nc(N)[se]c1CCN 10.1016/j.bmcl.2010.10.041
CHEMBL2448450 56168 0 None -3 3 Human 5.0 pKi = 5 Binding
Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells
ChEMBL 205 2 2 3 -0.5 Cc1nc(N)[se]c1CCN 10.1016/j.bmcl.2010.10.041
10466840 202766 0 None -1000 4 Human 5.0 pKi = 5 Binding
Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells
ChEMBL 240 7 3 2 2.0 CC/N=C(\S)NCCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL72424 202766 0 None -1000 4 Human 5.0 pKi = 5 Binding
Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells
ChEMBL 240 7 3 2 2.0 CC/N=C(\S)NCCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
10686633 56223 0 None -4073 3 Guinea pig 4.0 pKi = 4 Binding
Binding affinity against H2 receptor of Guinea pig atriumBinding affinity against H2 receptor of Guinea pig atrium
ChEMBL 313 5 2 3 3.6 O=C(Nc1ccccc1C(F)(F)F)OCCCc1c[nH]cn1 10.1021/jm9507688
CHEMBL16373 56223 0 None -4073 3 Guinea pig 4.0 pKi = 4 Binding
Binding affinity against H2 receptor of Guinea pig atriumBinding affinity against H2 receptor of Guinea pig atrium
ChEMBL 313 5 2 3 3.6 O=C(Nc1ccccc1C(F)(F)F)OCCCc1c[nH]cn1 10.1021/jm9507688
10490047 58752 0 None -7585 2 Guinea pig 4.0 pKi = 4 Binding
Binding affinity against H2 receptor of Guinea pig atriumBinding affinity against H2 receptor of Guinea pig atrium
ChEMBL 237 6 2 3 1.9 O=C(NCC1CCC1)OCCCc1c[nH]cn1 10.1021/jm9507688
CHEMBL16957 58752 0 None -7585 2 Guinea pig 4.0 pKi = 4 Binding
Binding affinity against H2 receptor of Guinea pig atriumBinding affinity against H2 receptor of Guinea pig atrium
ChEMBL 237 6 2 3 1.9 O=C(NCC1CCC1)OCCCc1c[nH]cn1 10.1021/jm9507688
10731042 98184 0 None -194 3 Guinea pig 4.0 pKi = 4 Binding
Binding affinity against H2 receptor of Guinea pig atriumBinding affinity against H2 receptor of Guinea pig atrium
ChEMBL 274 6 3 4 1.9 Nc1ccc(CNC(=O)OCCCc2c[nH]cn2)cc1 10.1021/jm9507688
CHEMBL277285 98184 0 None -194 3 Guinea pig 4.0 pKi = 4 Binding
Binding affinity against H2 receptor of Guinea pig atriumBinding affinity against H2 receptor of Guinea pig atrium
ChEMBL 274 6 3 4 1.9 Nc1ccc(CNC(=O)OCCCc2c[nH]cn2)cc1 10.1021/jm9507688
44334252 4465 0 None -323 3 Human 4.0 pKi = 4 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 449 10 3 7 1.7 CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)[C@@H](CO)NC(=O)OC(C)(C)C)C2)cc1 10.1016/s0960-894x(02)00685-6
CHEMBL102390 4465 0 None -323 3 Human 4.0 pKi = 4 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 449 10 3 7 1.7 CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)[C@@H](CO)NC(=O)OC(C)(C)C)C2)cc1 10.1016/s0960-894x(02)00685-6
44335350 4996 0 None -389 3 Human 4.0 pKi = 4 Binding
Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor
ChEMBL 398 8 0 5 3.9 CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc(OC)cc3)cc2)CC1 10.1016/s0960-894x(02)00648-0
CHEMBL105483 4996 0 None -389 3 Human 4.0 pKi = 4 Binding
Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor
ChEMBL 398 8 0 5 3.9 CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc(OC)cc3)cc2)CC1 10.1016/s0960-894x(02)00648-0
44304211 101714 0 None -19054 3 Human 4.0 pKi = 4 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 373 9 1 5 1.9 CC[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL302829 101714 0 None -19054 3 Human 4.0 pKi = 4 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 373 9 1 5 1.9 CC[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
10451094 200777 0 None -199526 3 Human 4.0 pKi = 4 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 359 9 1 5 1.5 NCCC(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL61120 200777 0 None -199526 3 Human 4.0 pKi = 4 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 359 9 1 5 1.5 NCCC(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
29298 201749 1 None -1047 4 Human 5.0 pKi = 5.0 Binding
Compound was tested for its binding affinity towards human H2 receptorCompound was tested for its binding affinity towards human H2 receptor
ChEMBL 297 5 1 3 3.9 CN(C)CCCNc1c2c(nc3ccccc13)CCCCC2 10.1016/s0960-894x(03)00356-1
CHEMBL65849 201749 1 None -1047 4 Human 5.0 pKi = 5.0 Binding
Compound was tested for its binding affinity towards human H2 receptorCompound was tested for its binding affinity towards human H2 receptor
ChEMBL 297 5 1 3 3.9 CN(C)CCCNc1c2c(nc3ccccc13)CCCCC2 10.1016/s0960-894x(03)00356-1
164614645 184539 0 None 57 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 402 8 4 4 3.0 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(c1ccccc1)C(C)C 10.1016/j.ejmech.2021.113190
CHEMBL4856572 184539 0 None 57 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 402 8 4 4 3.0 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(c1ccccc1)C(C)C 10.1016/j.ejmech.2021.113190
164622886 185350 0 None 93 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 374 7 4 4 2.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC[C@@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4869389 185350 0 None 93 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 374 7 4 4 2.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC[C@@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
1588 2284 24 None -323 44 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
28864 2284 24 None -323 44 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
43 2284 24 None -323 44 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
CHEMBL157138 2284 24 None -323 44 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
DB00589 2284 24 None -323 44 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
10069595 201429 0 None -3235 3 Human 5.0 pKi = 5.0 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 400 11 0 4 4.2 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)C3CCC3)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL64100 201429 0 None -3235 3 Human 5.0 pKi = 5.0 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 400 11 0 4 4.2 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)C3CCC3)CC2)cc1 10.1016/s0960-894x(02)00309-8
44304318 201561 0 None -1584 3 Human 5.0 pKi = 5.0 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 373 9 1 5 1.8 C[C@@H](CN)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL64608 201561 0 None -1584 3 Human 5.0 pKi = 5.0 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 373 9 1 5 1.8 C[C@@H](CN)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
112936251 136729 1 None -10 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]UR-DE257 from human histamine 2 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]UR-DE257 from human histamine 2 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 359 5 1 5 3.5 CN1CCN(c2cc(-c3ccccc3)nc(NCc3ccccc3)n2)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL3752085 136729 1 None -10 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]UR-DE257 from human histamine 2 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]UR-DE257 from human histamine 2 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 359 5 1 5 3.5 CN1CCN(c2cc(-c3ccccc3)nc(NCc3ccccc3)n2)CC1 10.1016/j.bmcl.2015.12.035
127052293 139695 1 None -218 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]tiotidine from human histamine H2 receptor expressed in sf9 cell membrane co-expressing Gsalphas incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]tiotidine from human histamine H2 receptor expressed in sf9 cell membrane co-expressing Gsalphas incubated for 60 mins by liquid scintillation counting method
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3805361 139695 1 None -218 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]tiotidine from human histamine H2 receptor expressed in sf9 cell membrane co-expressing Gsalphas incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]tiotidine from human histamine H2 receptor expressed in sf9 cell membrane co-expressing Gsalphas incubated for 60 mins by liquid scintillation counting method
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
176 394 63 None -6 31 Human 5.0 pKi = 5.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 394 63 None -6 31 Human 5.0 pKi = 5.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 394 63 None -6 31 Human 5.0 pKi = 5.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 394 63 None -6 31 Human 5.0 pKi = 5.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 394 63 None -6 31 Human 5.0 pKi = 5.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
164627189 185729 0 None 275 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 298 6 4 4 1.0 CCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1016/j.ejmech.2021.113190
CHEMBL4874758 185729 0 None 275 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 298 6 4 4 1.0 CCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1016/j.ejmech.2021.113190
168294776 192414 0 None -7 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 366 7 3 4 2.6 Cc1nnc(CCCN/C(N)=N/C(=O)NCC(C)C2CCCCC2)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5209479 192414 0 None -7 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 366 7 3 4 2.6 Cc1nnc(CCCN/C(N)=N/C(=O)NCC(C)C2CCCCC2)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222831 192414 0 None -7 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 366 7 3 4 2.6 Cc1nnc(CCCN/C(N)=N/C(=O)NCC(C)C2CCCCC2)s1 10.1021/acs.jmedchem.1c00692
168294445 192398 0 None -1 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 414 6 4 4 2.6 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCC2CCc3nc(N)sc3C2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5208113 192398 0 None -1 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 414 6 4 4 2.6 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCC2CCc3nc(N)sc3C2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222768 192398 0 None -1 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 414 6 4 4 2.6 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCC2CCc3nc(N)sc3C2)cc1 10.1021/acs.jmedchem.1c00692
44304320 162711 0 None -4265 3 Human 5.0 pKi = 5.0 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 373 9 1 5 1.9 CC[C@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL418666 162711 0 None -4265 3 Human 5.0 pKi = 5.0 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 373 9 1 5 1.9 CC[C@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
44304319 200938 0 None -1202 3 Human 5.0 pKi = 5.0 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 373 9 1 5 1.8 C[C@H](CN)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL61288 200938 0 None -1202 3 Human 5.0 pKi = 5.0 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 373 9 1 5 1.8 C[C@H](CN)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
44304494 201294 0 None -8709 3 Human 5.0 pKi = 5.0 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 489 12 1 6 4.3 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](C)NC(=O)OC(C)(C)C)CC2)cc1 10.1016/s0960-894x(02)00310-4
CHEMBL63125 201294 0 None -8709 3 Human 5.0 pKi = 5.0 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 489 12 1 6 4.3 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](C)NC(=O)OC(C)(C)C)CC2)cc1 10.1016/s0960-894x(02)00310-4
132060746 162508 0 None -6 5 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 405 4 0 4 4.4 O=C(OCc1ccccc1)N1Cc2ccc(N3CCN(C4CCCC4)CC3)cc2C1 10.1016/j.ejmech.2018.02.024
CHEMBL4176474 162508 0 None -6 5 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 405 4 0 4 4.4 O=C(OCc1ccccc1)N1Cc2ccc(N3CCN(C4CCCC4)CC3)cc2C1 10.1016/j.ejmech.2018.02.024
124087 1357 106 None -29 15 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
7157 1357 106 None -29 15 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
814 1357 106 None -29 15 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
CHEMBL1172 1357 106 None -29 15 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
DB00967 1357 106 None -29 15 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
168284289 192294 0 None 1 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 428 8 4 4 3.1 CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
CHEMBL5194860 192294 0 None 1 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 428 8 4 4 3.1 CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
CHEMBL5222123 192294 0 None 1 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 428 8 4 4 3.1 CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
44304211 101714 0 None -19054 3 Human 5.0 pKi = 5.0 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 373 9 1 5 1.9 CC[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL302829 101714 0 None -19054 3 Human 5.0 pKi = 5.0 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 373 9 1 5 1.9 CC[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
132060752 162364 0 None -3 4 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 437 7 0 6 3.4 CCOC(=O)CCN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)C3)CC1 10.1016/j.ejmech.2018.02.024
CHEMBL4174189 162364 0 None -3 4 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 437 7 0 6 3.4 CCOC(=O)CCN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)C3)CC1 10.1016/j.ejmech.2018.02.024
CHEMBL5085542 213189 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCC[n+]1c(C)cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc1C 10.1016/j.bmcl.2021.128388
164626370 185881 0 None 1 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 338 6 4 4 1.8 CCCCCCNC(=O)/N=C(\N)NC1CCc2nc(N)sc2C1 10.1016/j.ejmech.2021.113190
CHEMBL4876799 185881 0 None 1 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 338 6 4 4 1.8 CCCCCCNC(=O)/N=C(\N)NC1CCc2nc(N)sc2C1 10.1016/j.ejmech.2021.113190
44304382 201602 0 None -1174 3 Human 5.0 pKi = 5.0 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 403 11 1 4 4.0 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)NC(C)C)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL64773 201602 0 None -1174 3 Human 5.0 pKi = 5.0 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 403 11 1 4 4.0 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)NC(C)C)CC2)cc1 10.1016/s0960-894x(02)00309-8
11057 175565 19 None -2 20 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
3468 175565 19 None -2 20 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
CHEMBL459265 175565 19 None -2 20 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
CHEMBL64894 175565 19 None -2 20 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
164616851 184357 0 None -1 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 376 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)N[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4853772 184357 0 None -1 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 376 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)N[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
2286 3122 48 None -26 30 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
4927 3122 48 None -26 30 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
7282 3122 48 None -26 30 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
CHEMBL643 3122 48 None -26 30 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
DB01069 3122 48 None -26 30 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
1353 1872 85 None -131 86 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
3559 1872 85 None -131 86 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
86 1872 85 None -131 86 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
CHEMBL54 1872 85 None -131 86 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
DB00502 1872 85 None -131 86 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
164612760 184125 0 None 38 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 390 7 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NC[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4850490 184125 0 None 38 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 390 7 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NC[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
44582678 180982 0 None -630 11 Human 5.9 pKi = 5.9 Binding
Inhibition of human cloned histamine H2 receptor by competitive binding experimentInhibition of human cloned histamine H2 receptor by competitive binding experiment
ChEMBL 401 9 1 4 4.3 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(C)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL476839 180982 0 None -630 11 Human 5.9 pKi = 5.9 Binding
Inhibition of human cloned histamine H2 receptor by competitive binding experimentInhibition of human cloned histamine H2 receptor by competitive binding experiment
ChEMBL 401 9 1 4 4.3 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(C)cc2)CC1 10.1016/j.bmc.2009.03.021
73353884 91876 0 None 2 8 Human 5.9 pKi = 5.9 Binding
Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay
ChEMBL 295 3 1 3 2.7 c1cc2c(cc1CN[C@H]1C3C4CC5C6C4CC3C6C51)OCO2 10.1016/j.bmc.2013.07.045
CHEMBL2429890 91876 0 None 2 8 Human 5.9 pKi = 5.9 Binding
Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay
ChEMBL 295 3 1 3 2.7 c1cc2c(cc1CN[C@H]1C3C4CC5C6C4CC3C6C51)OCO2 10.1016/j.bmc.2013.07.045
44304245 201628 0 None -2884 3 Human 4.9 pKi = 4.9 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 425 11 0 5 4.0 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3cccn3C)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL64884 201628 0 None -2884 3 Human 4.9 pKi = 4.9 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 425 11 0 5 4.0 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3cccn3C)CC2)cc1 10.1016/s0960-894x(02)00309-8
44335559 109208 0 None -6918 4 Human 4.9 pKi = 4.9 Binding
Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor
ChEMBL 334 6 0 3 4.7 CC1CCCN(CCCOc2ccc(-c3ccc(C#N)cc3)cc2)C1 10.1016/s0960-894x(02)00648-0
CHEMBL322873 109208 0 None -6918 4 Human 4.9 pKi = 4.9 Binding
Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor
ChEMBL 334 6 0 3 4.7 CC1CCCN(CCCOc2ccc(-c3ccc(C#N)cc3)cc2)C1 10.1016/s0960-894x(02)00648-0
1201549 590 22 None -74 20 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
333 590 22 None -74 20 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
7601 590 22 None -74 20 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
CHEMBL1201203 590 22 None -74 20 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
CHEMBL438151 590 22 None -74 20 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
DB00245 590 22 None -74 20 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
3037827 102661 5 None - 1 Guinea pig 7.9 pKi = 7.9 Binding
Inhibition of [125I]APT binding to histamine H2 receptor in guinea pig cerebral membranes.Inhibition of [125I]APT binding to histamine H2 receptor in guinea pig cerebral membranes.
ChEMBL 629 12 3 6 4.4 N#CN/C(=N\CCNC(=O)c1ccc(N=[N+]=[N-])c(I)c1)NCCCOc1cccc(CN2CCCCC2)c1 10.1021/jm00090a013
CHEMBL307952 102661 5 None - 1 Guinea pig 7.9 pKi = 7.9 Binding
Inhibition of [125I]APT binding to histamine H2 receptor in guinea pig cerebral membranes.Inhibition of [125I]APT binding to histamine H2 receptor in guinea pig cerebral membranes.
ChEMBL 629 12 3 6 4.4 N#CN/C(=N\CCNC(=O)c1ccc(N=[N+]=[N-])c(I)c1)NCCCOc1cccc(CN2CCCCC2)c1 10.1021/jm00090a013
168295541 192428 0 None -851 6 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 347 6 4 5 1.4 C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5208845 192428 0 None -851 6 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 347 6 4 5 1.4 C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222926 192428 0 None -851 6 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 347 6 4 5 1.4 C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1 10.1021/acs.jmedchem.1c00692
44334430 4373 0 None -398 3 Human 5.9 pKi = 5.9 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 428 10 1 5 3.1 O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccccc3)C2)cc1)C1CC1 10.1016/s0960-894x(02)00685-6
CHEMBL101691 4373 0 None -398 3 Human 5.9 pKi = 5.9 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 428 10 1 5 3.1 O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccccc3)C2)cc1)C1CC1 10.1016/s0960-894x(02)00685-6
44304457 201513 0 None -3981 3 Human 4.9 pKi = 4.9 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 376 10 0 5 3.6 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OC)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL64408 201513 0 None -3981 3 Human 4.9 pKi = 4.9 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 376 10 0 5 3.6 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OC)CC2)cc1 10.1016/s0960-894x(02)00309-8
44304431 201243 0 None -512 3 Human 4.9 pKi = 4.9 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 566 14 1 7 4.9 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](Cc3ccncc3)NC(=O)OC(C)(C)C)CC2)cc1 10.1016/s0960-894x(02)00310-4
CHEMBL62903 201243 0 None -512 3 Human 4.9 pKi = 4.9 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 566 14 1 7 4.9 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](Cc3ccncc3)NC(=O)OC(C)(C)C)CC2)cc1 10.1016/s0960-894x(02)00310-4
1212 1624 45 None -323 66 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
204 1624 45 None -323 66 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
3372 1624 45 None -323 66 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
CHEMBL726 1624 45 None -323 66 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
DB00623 1624 45 None -323 66 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
9872676 77811 0 None -3090 17 Human 5.9 pKi = 5.9 Binding
Binding affinity to H2 receptorBinding affinity to H2 receptor
ChEMBL 565 11 2 10 4.8 COc1nc(NCCCN2CCOCC2)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1 10.1021/jm060012g
CHEMBL210514 77811 0 None -3090 17 Human 5.9 pKi = 5.9 Binding
Binding affinity to H2 receptorBinding affinity to H2 receptor
ChEMBL 565 11 2 10 4.8 COc1nc(NCCCN2CCOCC2)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1 10.1021/jm060012g
44304751 100541 0 None -338 3 Human 4.9 pKi = 4.9 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 422 11 0 4 4.7 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3ccccc3)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL294519 100541 0 None -338 3 Human 4.9 pKi = 4.9 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 422 11 0 4 4.7 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3ccccc3)CC2)cc1 10.1016/s0960-894x(02)00309-8
44304990 201364 0 None -331 3 Human 4.9 pKi = 4.9 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 483 12 0 6 4.1 CCCCCC(=O)c1ccc(OCCCN2CCN(S(=O)(=O)c3ccc(C#N)cc3)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL63632 201364 0 None -331 3 Human 4.9 pKi = 4.9 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 483 12 0 6 4.1 CCCCCC(=O)c1ccc(OCCCN2CCN(S(=O)(=O)c3ccc(C#N)cc3)CC2)cc1 10.1016/s0960-894x(02)00309-8
44335225 163592 0 None -812 4 Human 4.9 pKi = 4.9 Binding
Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor
ChEMBL 347 6 1 4 3.1 N#Cc1ccc(-c2ccc(OCCCN3CC4CNCC4C3)cc2)cc1 10.1016/s0960-894x(02)00648-0
CHEMBL421026 163592 0 None -812 4 Human 4.9 pKi = 4.9 Binding
Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor
ChEMBL 347 6 1 4 3.1 N#Cc1ccc(-c2ccc(OCCCN3CC4CNCC4C3)cc2)cc1 10.1016/s0960-894x(02)00648-0
44304303 201629 0 None -954 3 Human 4.9 pKi = 4.9 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 371 8 1 5 1.6 O=C(c1ccc(OCCCN2CCN(C(=O)[C@@H]3CCN3)CC2)cc1)C1CC1 10.1016/s0960-894x(02)00310-4
CHEMBL64896 201629 0 None -954 3 Human 4.9 pKi = 4.9 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 371 8 1 5 1.6 O=C(c1ccc(OCCCN2CCN(C(=O)[C@@H]3CCN3)CC2)cc1)C1CC1 10.1016/s0960-894x(02)00310-4
164621681 184988 0 None 64 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 444 7 4 5 3.2 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(OC(F)(F)F)cc1 10.1016/j.ejmech.2021.113190
CHEMBL4863523 184988 0 None 64 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 444 7 4 5 3.2 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(OC(F)(F)F)cc1 10.1016/j.ejmech.2021.113190
10565409 51895 0 None -616 3 Guinea pig 4.9 pKi = 4.9 Binding
Binding affinity against H2 receptor of Guinea pig atriumBinding affinity against H2 receptor of Guinea pig atrium
ChEMBL 290 6 2 5 2.5 O=C(Nc1ccc([N+](=O)[O-])cc1)OCCCc1c[nH]cn1 10.1021/jm9507688
CHEMBL15883 51895 0 None -616 3 Guinea pig 4.9 pKi = 4.9 Binding
Binding affinity against H2 receptor of Guinea pig atriumBinding affinity against H2 receptor of Guinea pig atrium
ChEMBL 290 6 2 5 2.5 O=C(Nc1ccc([N+](=O)[O-])cc1)OCCCc1c[nH]cn1 10.1021/jm9507688
10805119 54302 0 None -645 3 Guinea pig 4.9 pKi = 4.9 Binding
Binding affinity against H2 receptor of Guinea pig atriumBinding affinity against H2 receptor of Guinea pig atrium
ChEMBL 313 5 2 3 3.6 O=C(Nc1cccc(C(F)(F)F)c1)OCCCc1c[nH]cn1 10.1021/jm9507688
CHEMBL16108 54302 0 None -645 3 Guinea pig 4.9 pKi = 4.9 Binding
Binding affinity against H2 receptor of Guinea pig atriumBinding affinity against H2 receptor of Guinea pig atrium
ChEMBL 313 5 2 3 3.6 O=C(Nc1cccc(C(F)(F)F)c1)OCCCc1c[nH]cn1 10.1021/jm9507688
10520238 57245 0 None -1023 3 Guinea pig 4.9 pKi = 4.9 Binding
Binding affinity against H2 receptor of Guinea pig atriumBinding affinity against H2 receptor of Guinea pig atrium
ChEMBL 327 6 2 3 3.3 O=C(NCc1ccc(C(F)(F)F)cc1)OCCCc1c[nH]cn1 10.1021/jm9507688
CHEMBL16654 57245 0 None -1023 3 Guinea pig 4.9 pKi = 4.9 Binding
Binding affinity against H2 receptor of Guinea pig atriumBinding affinity against H2 receptor of Guinea pig atrium
ChEMBL 327 6 2 3 3.3 O=C(NCc1ccc(C(F)(F)F)cc1)OCCCc1c[nH]cn1 10.1021/jm9507688
10732219 98474 0 None -602 3 Guinea pig 4.9 pKi = 4.9 Binding
Binding affinity against H2 receptor of Guinea pig atriumBinding affinity against H2 receptor of Guinea pig atrium
ChEMBL 290 6 2 5 2.5 O=C(Nc1cccc([N+](=O)[O-])c1)OCCCc1c[nH]cn1 10.1021/jm9507688
CHEMBL279617 98474 0 None -602 3 Guinea pig 4.9 pKi = 4.9 Binding
Binding affinity against H2 receptor of Guinea pig atriumBinding affinity against H2 receptor of Guinea pig atrium
ChEMBL 290 6 2 5 2.5 O=C(Nc1cccc([N+](=O)[O-])c1)OCCCc1c[nH]cn1 10.1021/jm9507688
409544 201216 3 None -8912 3 Human 4.9 pKi = 4.9 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 390 11 0 5 4.0 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OCC)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL62803 201216 3 None -8912 3 Human 4.9 pKi = 4.9 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 390 11 0 5 4.0 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OCC)CC2)cc1 10.1016/s0960-894x(02)00309-8
44304035 201609 0 None -181 3 Human 4.9 pKi = 4.9 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 410 9 0 5 3.7 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)Cc3ccccc3)cc2)CC1 10.1016/s0960-894x(02)00309-8
CHEMBL64799 201609 0 None -181 3 Human 4.9 pKi = 4.9 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 410 9 0 5 3.7 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)Cc3ccccc3)cc2)CC1 10.1016/s0960-894x(02)00309-8
44304393 105464 0 None -128 3 Human 4.9 pKi = 4.9 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 517 13 1 6 4.9 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](NC(=O)OC(C)(C)C)C(C)C)CC2)cc1 10.1016/s0960-894x(02)00310-4
CHEMBL312958 105464 0 None -128 3 Human 4.9 pKi = 4.9 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 517 13 1 6 4.9 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](NC(=O)OC(C)(C)C)C(C)C)CC2)cc1 10.1016/s0960-894x(02)00310-4
10039772 103869 0 None -501 3 Human 4.9 pKi = 4.9 Binding
Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors
ChEMBL 288 7 3 2 3.1 S=C(NCCCCCc1c[nH]cn1)Nc1ccccc1 10.1021/jm00012a025
CHEMBL310087 103869 0 None -501 3 Human 4.9 pKi = 4.9 Binding
Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors
ChEMBL 288 7 3 2 3.1 S=C(NCCCCCc1c[nH]cn1)Nc1ccccc1 10.1021/jm00012a025
44304246 200955 0 None -1513 3 Human 4.9 pKi = 4.9 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 426 11 0 5 4.6 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3occc3C)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL61396 200955 0 None -1513 3 Human 4.9 pKi = 4.9 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 426 11 0 5 4.6 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3occc3C)CC2)cc1 10.1016/s0960-894x(02)00309-8
44335463 4374 0 None -229 4 Human 4.9 pKi = 4.9 Binding
Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor
ChEMBL 357 7 1 4 3.2 CCOC(=O)N1CCN(CCCOc2ccc(-c3cc[nH]c3)cc2)CC1 10.1016/s0960-894x(02)00648-0
CHEMBL101692 4374 0 None -229 4 Human 4.9 pKi = 4.9 Binding
Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor
ChEMBL 357 7 1 4 3.2 CCOC(=O)N1CCN(CCCOc2ccc(-c3cc[nH]c3)cc2)CC1 10.1016/s0960-894x(02)00648-0
44335483 5206 0 None -426 4 Human 4.9 pKi = 4.9 Binding
Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor
ChEMBL 336 6 1 4 3.5 N#Cc1ccc(-c2ccc(OCCCN3CCCC(O)C3)cc2)cc1 10.1016/s0960-894x(02)00648-0
CHEMBL106596 5206 0 None -426 4 Human 4.9 pKi = 4.9 Binding
Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor
ChEMBL 336 6 1 4 3.5 N#Cc1ccc(-c2ccc(OCCCN3CCCC(O)C3)cc2)cc1 10.1016/s0960-894x(02)00648-0
156017225 177760 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method
ChEMBL 442 15 3 7 3.1 NCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O 10.1021/acsmedchemlett.0c00033
CHEMBL4642548 177760 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method
ChEMBL 442 15 3 7 3.1 NCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O 10.1021/acsmedchemlett.0c00033
CHEMBL4651234 177760 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method
ChEMBL 442 15 3 7 3.1 NCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O 10.1021/acsmedchemlett.0c00033
156015555 177727 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method
ChEMBL 456 16 3 7 3.5 NCCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O 10.1021/acsmedchemlett.0c00033
CHEMBL4644794 177727 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method
ChEMBL 456 16 3 7 3.5 NCCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O 10.1021/acsmedchemlett.0c00033
CHEMBL4651059 177727 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method
ChEMBL 456 16 3 7 3.5 NCCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O 10.1021/acsmedchemlett.0c00033
156014823 177742 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method
ChEMBL 1109 31 4 13 9.2 CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3cc(S(=O)(=O)O)ccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acsmedchemlett.0c00033
CHEMBL4641747 177742 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method
ChEMBL 1109 31 4 13 9.2 CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3cc(S(=O)(=O)O)ccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acsmedchemlett.0c00033
CHEMBL4651132 177742 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method
ChEMBL 1109 31 4 13 9.2 CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3cc(S(=O)(=O)O)ccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acsmedchemlett.0c00033
44304412 199953 0 None -912 3 Human 4.9 pKi = 4.9 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 517 13 1 6 4.9 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](NC(=O)OC(C)(C)C)C(C)C)CC2)cc1 10.1016/s0960-894x(02)00310-4
CHEMBL60598 199953 0 None -912 3 Human 4.9 pKi = 4.9 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 517 13 1 6 4.9 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](NC(=O)OC(C)(C)C)C(C)C)CC2)cc1 10.1016/s0960-894x(02)00310-4
59868 93707 56 None -20892 3 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 211 3 2 4 1.6 CCCN[C@@H]1CCc2nc(N)sc2C1 10.1016/j.ejmech.2021.113190
CHEMBL249420 93707 56 None -20892 3 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 211 3 2 4 1.6 CCCN[C@@H]1CCc2nc(N)sc2C1 10.1016/j.ejmech.2021.113190
119570 3098 90 None -281 40 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/acs.jmedchem.1c00692
2233 3098 90 None -281 40 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/acs.jmedchem.1c00692
953 3098 90 None -281 40 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/acs.jmedchem.1c00692
CHEMBL301265 3098 90 None -281 40 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/acs.jmedchem.1c00692
DB00413 3098 90 None -281 40 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/acs.jmedchem.1c00692
104903 56035 14 None -5 6 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 624 6 0 8 5.5 C[C@@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)C3=CC[C@]2(C)[C@H]1C(=O)CN1CCN(c2cc(N3CCCC3)nc(N3CCCC3)n2)CC1 nan
CHEMBL1630578 56035 14 None -5 6 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 624 6 0 8 5.5 C[C@@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)C3=CC[C@]2(C)[C@H]1C(=O)CN1CCN(c2cc(N3CCCC3)nc(N3CCCC3)n2)CC1 nan
CHEMBL4535474 212225 34 None -1 6 Human 6.9 pKi = 6.9 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000320b HRH2Selectivity interaction (GPCR panel (PDSP screen)) EUB0000320b HRH2
ChEMBL None None None CNCc1ccccc1-c1csc([C@@H](C)Nc2nc(C)nc3cc(OC)c(OC)cc23)c1 nan
1231 922 112 None -2 8 Human 6.9 pKi = 6.9 Binding
Binding affinity to human histamine H2 receptor by radioligand displacement assayBinding affinity to human histamine H2 receptor by radioligand displacement assay
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/j.ejmech.2013.01.044
2756 922 112 None -2 8 Human 6.9 pKi = 6.9 Binding
Binding affinity to human histamine H2 receptor by radioligand displacement assayBinding affinity to human histamine H2 receptor by radioligand displacement assay
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/j.ejmech.2013.01.044
645 922 112 None -2 8 Human 6.9 pKi = 6.9 Binding
Binding affinity to human histamine H2 receptor by radioligand displacement assayBinding affinity to human histamine H2 receptor by radioligand displacement assay
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/j.ejmech.2013.01.044
CHEMBL30 922 112 None -2 8 Human 6.9 pKi = 6.9 Binding
Binding affinity to human histamine H2 receptor by radioligand displacement assayBinding affinity to human histamine H2 receptor by radioligand displacement assay
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/j.ejmech.2013.01.044
DB00501 922 112 None -2 8 Human 6.9 pKi = 6.9 Binding
Binding affinity to human histamine H2 receptor by radioligand displacement assayBinding affinity to human histamine H2 receptor by radioligand displacement assay
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/j.ejmech.2013.01.044
44568347 191045 0 None -67 15 Human 5.9 pKi = 5.9 Binding
Antagonist activity at histamine H2 receptor (unknown origin) by PDSP assayAntagonist activity at histamine H2 receptor (unknown origin) by PDSP assay
ChEMBL 356 6 0 4 5.2 CCN(CC)CCCOC(=O)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
CHEMBL519609 191045 0 None -67 15 Human 5.9 pKi = 5.9 Binding
Antagonist activity at histamine H2 receptor (unknown origin) by PDSP assayAntagonist activity at histamine H2 receptor (unknown origin) by PDSP assay
ChEMBL 356 6 0 4 5.2 CCN(CC)CCCOC(=O)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
44304560 102277 0 None -10715 3 Human 4.9 pKi = 4.9 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 371 8 1 5 1.6 O=C(c1ccc(OCCCN2CCN(C(=O)[C@H]3CCN3)CC2)cc1)C1CC1 10.1016/s0960-894x(02)00310-4
CHEMBL305144 102277 0 None -10715 3 Human 4.9 pKi = 4.9 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 371 8 1 5 1.6 O=C(c1ccc(OCCCN2CCN(C(=O)[C@H]3CCN3)CC2)cc1)C1CC1 10.1016/s0960-894x(02)00310-4
44304760 201203 0 None -229 3 Human 4.9 pKi = 4.9 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 431 13 1 5 3.7 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](N)CC(C)C)CC2)cc1 10.1016/s0960-894x(02)00310-4
CHEMBL62741 201203 0 None -229 3 Human 4.9 pKi = 4.9 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 431 13 1 5 3.7 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](N)CC(C)C)CC2)cc1 10.1016/s0960-894x(02)00310-4
71525678 89281 0 None -1479 6 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]histamine from human histamine H2 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H2 receptor expressed in HEK cells
ChEMBL 258 3 2 6 0.6 CCc1cnc2c(N3CC(NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
CHEMBL2376800 89281 0 None -1479 6 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]histamine from human histamine H2 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H2 receptor expressed in HEK cells
ChEMBL 258 3 2 6 0.6 CCc1cnc2c(N3CC(NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
164610824 184517 0 None 14 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 452 8 4 4 3.6 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NCC(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4856200 184517 0 None 14 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 452 8 4 4 3.6 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NCC(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2021.113190
18539962 101648 0 None -537 3 Human 4.8 pKi = 4.8 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 318 10 1 4 3.1 CCCCCC(=O)c1ccc(OCCCN2CCNCC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL302445 101648 0 None -537 3 Human 4.8 pKi = 4.8 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 318 10 1 4 3.1 CCCCCC(=O)c1ccc(OCCCN2CCNCC2)cc1 10.1016/s0960-894x(02)00309-8
2389 3267 114 None -346 68 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
5073 3267 114 None -346 68 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
96 3267 114 None -346 68 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
CHEMBL85 3267 114 None -346 68 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
DB00734 3267 114 None -346 68 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
164620704 185491 0 None 17 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 416 8 4 4 3.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)c1ccc(C(C)C)cc1 10.1016/j.ejmech.2021.113190
CHEMBL4871482 185491 0 None 17 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 416 8 4 4 3.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)c1ccc(C(C)C)cc1 10.1016/j.ejmech.2021.113190
44304287 201200 0 None -912 3 Human 4.8 pKi = 4.8 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 428 11 0 5 4.7 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3cccs3)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL62726 201200 0 None -912 3 Human 4.8 pKi = 4.8 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 428 11 0 5 4.7 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3cccs3)CC2)cc1 10.1016/s0960-894x(02)00309-8
44304310 201574 0 None -1995 3 Human 4.8 pKi = 4.8 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 415 10 0 4 4.1 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)N3CCCC3)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL64667 201574 0 None -1995 3 Human 4.8 pKi = 4.8 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 415 10 0 4 4.1 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)N3CCCC3)CC2)cc1 10.1016/s0960-894x(02)00309-8
44304349 201104 0 None -275 3 Human 4.8 pKi = 4.8 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 566 14 1 7 4.9 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](Cc3ccncc3)NC(=O)OC(C)(C)C)CC2)cc1 10.1016/s0960-894x(02)00310-4
CHEMBL62266 201104 0 None -275 3 Human 4.8 pKi = 4.8 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 566 14 1 7 4.9 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](Cc3ccncc3)NC(=O)OC(C)(C)C)CC2)cc1 10.1016/s0960-894x(02)00310-4
73347825 92094 0 None -1 3 Human 5.8 pKi = 5.8 Binding
Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay
ChEMBL 311 5 1 3 2.9 COc1ccc(CN[C@H]2C3C4CC5C6C4CC3C6C52)cc1OC 10.1016/j.bmc.2013.07.045
CHEMBL2432046 92094 0 None -1 3 Human 5.8 pKi = 5.8 Binding
Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay
ChEMBL 311 5 1 3 2.9 COc1ccc(CN[C@H]2C3C4CC5C6C4CC3C6C52)cc1OC 10.1016/j.bmc.2013.07.045
57469 18663 120 None -1 3 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 240 2 1 4 2.8 CC(C)Cn1cnc2c(N)nc3ccccc3c21 nan
CHEMBL1282 18663 120 None -1 3 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 240 2 1 4 2.8 CC(C)Cn1cnc2c(N)nc3ccccc3c21 nan
168286426 192314 0 None -5 6 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 403 10 4 5 2.3 CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5198795 192314 0 None -5 6 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 403 10 4 5 2.3 CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222241 192314 0 None -5 6 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 403 10 4 5 2.3 CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
135156 177219 7 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human H2R expressing Sf9 cells incubated for 60 mins by microbeta scintillation counter methodBinding affinity to human H2R expressing Sf9 cells incubated for 60 mins by microbeta scintillation counter method
ChEMBL 343 8 2 6 1.7 Nc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O 10.1021/acsmedchemlett.0c00033
CHEMBL4643501 177219 7 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human H2R expressing Sf9 cells incubated for 60 mins by microbeta scintillation counter methodBinding affinity to human H2R expressing Sf9 cells incubated for 60 mins by microbeta scintillation counter method
ChEMBL 343 8 2 6 1.7 Nc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O 10.1021/acsmedchemlett.0c00033
69355600 78260 0 None -3715 4 Human 4.8 pKi = 4.8 Binding
Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor
ChEMBL 336 6 1 4 3.5 C[C@@]1(O)CCN(CCCOc2ccc(-c3ccc(C#N)cc3)cc2)C1 10.1016/s0960-894x(02)00648-0
CHEMBL2112461 78260 0 None -3715 4 Human 4.8 pKi = 4.8 Binding
Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor
ChEMBL 336 6 1 4 3.5 C[C@@]1(O)CCN(CCCOc2ccc(-c3ccc(C#N)cc3)cc2)C1 10.1016/s0960-894x(02)00648-0
44304293 201264 0 None -52 3 Human 4.8 pKi = 4.8 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 491 10 1 6 4.0 N[C@H](Cc1cc2ccccc2s1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL63002 201264 0 None -52 3 Human 4.8 pKi = 4.8 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 491 10 1 6 4.0 N[C@H](Cc1cc2ccccc2s1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
168295803 192433 0 None 3 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 338 6 4 4 1.6 CCCCCNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
CHEMBL5207206 192433 0 None 3 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 338 6 4 4 1.6 CCCCCNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
CHEMBL5222937 192433 0 None 3 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 338 6 4 4 1.6 CCCCCNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
44304283 201474 0 None -117 3 Human 5.8 pKi = 5.8 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 452 8 0 5 4.8 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)c3ccc(C(C)(C)C)cc3)cc2)CC1 10.1016/s0960-894x(02)00309-8
CHEMBL64247 201474 0 None -117 3 Human 5.8 pKi = 5.8 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 452 8 0 5 4.8 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)c3ccc(C(C)(C)C)cc3)cc2)CC1 10.1016/s0960-894x(02)00309-8
44334396 4832 0 None -575 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 446 10 1 5 3.2 O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccccc3F)C2)cc1)C1CC1 10.1016/s0960-894x(02)00685-6
CHEMBL104618 4832 0 None -575 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 446 10 1 5 3.2 O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccccc3F)C2)cc1)C1CC1 10.1016/s0960-894x(02)00685-6
3198 203792 73 None -19 34 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1201049 203792 73 None -19 34 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL808 203792 73 None -19 34 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
164622190 185024 0 None 93 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 360 7 4 4 1.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCc1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4864067 185024 0 None 93 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 360 7 4 4 1.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCc1ccccc1 10.1016/j.ejmech.2021.113190
10017820 202485 0 None -79 3 Human 5.8 pKi = 5.8 Binding
Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors
ChEMBL 302 8 3 2 2.8 S=C(NCCCCCc1c[nH]cn1)NCc1ccccc1 10.1021/jm00012a025
CHEMBL70811 202485 0 None -79 3 Human 5.8 pKi = 5.8 Binding
Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors
ChEMBL 302 8 3 2 2.8 S=C(NCCCCCc1c[nH]cn1)NCc1ccccc1 10.1021/jm00012a025
9974306 202759 0 None -199 4 Human 5.8 pKi = 5.8 Binding
Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors
ChEMBL 336 8 3 2 3.4 S=C(NCCCCCc1c[nH]cn1)NCc1ccc(Cl)cc1 10.1021/jm00012a025
CHEMBL72372 202759 0 None -199 4 Human 5.8 pKi = 5.8 Binding
Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors
ChEMBL 336 8 3 2 3.4 S=C(NCCCCCc1c[nH]cn1)NCc1ccc(Cl)cc1 10.1021/jm00012a025
9974306 202759 0 None -199 4 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells
ChEMBL 336 8 3 2 3.4 S=C(NCCCCCc1c[nH]cn1)NCc1ccc(Cl)cc1 10.1016/j.bmcl.2010.10.041
CHEMBL72372 202759 0 None -199 4 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells
ChEMBL 336 8 3 2 3.4 S=C(NCCCCCc1c[nH]cn1)NCc1ccc(Cl)cc1 10.1016/j.bmcl.2010.10.041
44270793 51053 0 None -154 3 Guinea pig 4.8 pKi = 4.8 Binding
Binding affinity against H2 receptor of Guinea pig atriumBinding affinity against H2 receptor of Guinea pig atrium
ChEMBL 328 6 2 4 2.9 O=C(NN1CCC(c2ccccc2)CC1)OCCCc1c[nH]cn1 10.1021/jm9507688
CHEMBL15813 51053 0 None -154 3 Guinea pig 4.8 pKi = 4.8 Binding
Binding affinity against H2 receptor of Guinea pig atriumBinding affinity against H2 receptor of Guinea pig atrium
ChEMBL 328 6 2 4 2.9 O=C(NN1CCC(c2ccccc2)CC1)OCCCc1c[nH]cn1 10.1021/jm9507688
10662264 56185 0 None -1023 3 Guinea pig 4.8 pKi = 4.8 Binding
Binding affinity against H2 receptor of Guinea pig atriumBinding affinity against H2 receptor of Guinea pig atrium
ChEMBL 304 7 2 5 2.2 O=C(NCc1ccc([N+](=O)[O-])cc1)OCCCc1c[nH]cn1 10.1021/jm9507688
CHEMBL16338 56185 0 None -1023 3 Guinea pig 4.8 pKi = 4.8 Binding
Binding affinity against H2 receptor of Guinea pig atriumBinding affinity against H2 receptor of Guinea pig atrium
ChEMBL 304 7 2 5 2.2 O=C(NCc1ccc([N+](=O)[O-])cc1)OCCCc1c[nH]cn1 10.1021/jm9507688
10682710 57176 1 None -1513 3 Guinea pig 4.8 pKi = 4.8 Binding
Binding affinity against H2 receptor of Guinea pig atriumBinding affinity against H2 receptor of Guinea pig atrium
ChEMBL 259 6 2 3 2.3 O=C(NCc1ccccc1)OCCCc1c[nH]cn1 10.1021/jm9507688
CHEMBL16592 57176 1 None -1513 3 Guinea pig 4.8 pKi = 4.8 Binding
Binding affinity against H2 receptor of Guinea pig atriumBinding affinity against H2 receptor of Guinea pig atrium
ChEMBL 259 6 2 3 2.3 O=C(NCc1ccccc1)OCCCc1c[nH]cn1 10.1021/jm9507688
10711079 98274 0 None -831 3 Guinea pig 4.8 pKi = 4.8 Binding
Binding affinity against H2 receptor of Guinea pig atriumBinding affinity against H2 receptor of Guinea pig atrium
ChEMBL 323 5 2 3 3.4 O=C(Nc1ccc(Br)cc1)OCCCc1c[nH]cn1 10.1021/jm9507688
CHEMBL277989 98274 0 None -831 3 Guinea pig 4.8 pKi = 4.8 Binding
Binding affinity against H2 receptor of Guinea pig atriumBinding affinity against H2 receptor of Guinea pig atrium
ChEMBL 323 5 2 3 3.4 O=C(Nc1ccc(Br)cc1)OCCCc1c[nH]cn1 10.1021/jm9507688
44280956 116965 0 None - 1 Guinea pig 4.8 pKi = 4.8 Binding
Evaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atriumEvaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atrium
ChEMBL 273 5 3 5 2.1 CN/C(=C\[N+](=O)[O-])Nc1cccc(-c2[nH]cnc2C)c1 10.1021/jm00356a005
CHEMBL33996 116965 0 None - 1 Guinea pig 4.8 pKi = 4.8 Binding
Evaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atriumEvaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atrium
ChEMBL 273 5 3 5 2.1 CN/C(=C\[N+](=O)[O-])Nc1cccc(-c2[nH]cnc2C)c1 10.1021/jm00356a005
3042 1381 31 None -53 15 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
355 1381 31 None -53 15 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
868 1381 31 None -53 15 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
CHEMBL1123 1381 31 None -53 15 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
DB00804 1381 31 None -53 15 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
10343536 4878 0 None -1000 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 446 10 1 5 3.2 O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3cccc(F)c3)C2)cc1)C1CC1 10.1016/s0960-894x(02)00685-6
CHEMBL104809 4878 0 None -1000 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 446 10 1 5 3.2 O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3cccc(F)c3)C2)cc1)C1CC1 10.1016/s0960-894x(02)00685-6
71452695 78258 0 None -398 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 453 10 1 6 3.0 N#Cc1ccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)cc1 10.1016/s0960-894x(02)00685-6
CHEMBL2112451 78258 0 None -398 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 453 10 1 6 3.0 N#Cc1ccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)cc1 10.1016/s0960-894x(02)00685-6
2247 502 77 None -56 42 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
249 502 77 None -56 42 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2603 502 77 None -56 42 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL296419 502 77 None -56 42 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
DB00637 502 77 None -56 42 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
44335185 106894 0 None -14 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor
ChEMBL 446 7 0 4 4.7 CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc(Br)cc3)cc2)CC1 10.1016/s0960-894x(02)00648-0
CHEMBL317900 106894 0 None -14 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor
ChEMBL 446 7 0 4 4.7 CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc(Br)cc3)cc2)CC1 10.1016/s0960-894x(02)00648-0
44304743 100130 0 None -97 3 Human 4.8 pKi = 4.8 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 431 13 1 5 3.7 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](N)CC(C)C)CC2)cc1 10.1016/s0960-894x(02)00310-4
CHEMBL291847 100130 0 None -97 3 Human 4.8 pKi = 4.8 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 431 13 1 5 3.7 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](N)CC(C)C)CC2)cc1 10.1016/s0960-894x(02)00310-4
164628701 185875 0 None 144 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 338 5 4 4 1.9 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC1CCCCC1 10.1016/j.ejmech.2021.113190
CHEMBL4876743 185875 0 None 144 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 338 5 4 4 1.9 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC1CCCCC1 10.1016/j.ejmech.2021.113190
9880208 4840 0 None -2041 4 Human 4.8 pKi = 4.8 Binding
Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor
ChEMBL 322 6 1 4 3.1 N#Cc1ccc(-c2ccc(OCCCN3CC[C@@H](O)C3)cc2)cc1 10.1016/s0960-894x(02)00648-0
CHEMBL104669 4840 0 None -2041 4 Human 4.8 pKi = 4.8 Binding
Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor
ChEMBL 322 6 1 4 3.1 N#Cc1ccc(-c2ccc(OCCCN3CC[C@@H](O)C3)cc2)cc1 10.1016/s0960-894x(02)00648-0
156015722 177688 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method
ChEMBL 718 21 2 7 7.9 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O 10.1021/acsmedchemlett.0c00033
CHEMBL4644467 177688 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method
ChEMBL 718 21 2 7 7.9 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O 10.1021/acsmedchemlett.0c00033
CHEMBL4650837 177688 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method
ChEMBL 718 21 2 7 7.9 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O 10.1021/acsmedchemlett.0c00033
156015152 177721 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method
ChEMBL 676 18 2 7 6.7 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O 10.1021/acsmedchemlett.0c00033
CHEMBL4641916 177721 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method
ChEMBL 676 18 2 7 6.7 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O 10.1021/acsmedchemlett.0c00033
CHEMBL4651017 177721 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method
ChEMBL 676 18 2 7 6.7 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O 10.1021/acsmedchemlett.0c00033
164609729 184505 0 None -2 6 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 360 6 4 4 2.3 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)N[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4856059 184505 0 None -2 6 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 360 6 4 4 2.3 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)N[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
1231 922 112 None -2 8 Human 6.8 pKi = 6.8 Binding
Displacement of radiolabeled cimetidine from human histamine H2 receptorDisplacement of radiolabeled cimetidine from human histamine H2 receptor
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/jm8007618
2756 922 112 None -2 8 Human 6.8 pKi = 6.8 Binding
Displacement of radiolabeled cimetidine from human histamine H2 receptorDisplacement of radiolabeled cimetidine from human histamine H2 receptor
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/jm8007618
645 922 112 None -2 8 Human 6.8 pKi = 6.8 Binding
Displacement of radiolabeled cimetidine from human histamine H2 receptorDisplacement of radiolabeled cimetidine from human histamine H2 receptor
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/jm8007618
CHEMBL30 922 112 None -2 8 Human 6.8 pKi = 6.8 Binding
Displacement of radiolabeled cimetidine from human histamine H2 receptorDisplacement of radiolabeled cimetidine from human histamine H2 receptor
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/jm8007618
DB00501 922 112 None -2 8 Human 6.8 pKi = 6.8 Binding
Displacement of radiolabeled cimetidine from human histamine H2 receptorDisplacement of radiolabeled cimetidine from human histamine H2 receptor
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/jm8007618
9906447 193894 1 None -2344 13 Human 5.8 pKi = 5.8 Binding
Binding affinity to human recombinant H2 receptorBinding affinity to human recombinant H2 receptor
ChEMBL 351 5 0 3 4.8 C[C@@H]1CCCN1CCc1cc2cc(C(=O)c3ccc(F)cc3)ccc2o1 10.1021/jm201690h
CHEMBL2031738 193894 1 None -2344 13 Human 5.8 pKi = 5.8 Binding
Binding affinity to human recombinant H2 receptorBinding affinity to human recombinant H2 receptor
ChEMBL 351 5 0 3 4.8 C[C@@H]1CCCN1CCc1cc2cc(C(=O)c3ccc(F)cc3)ccc2o1 10.1021/jm201690h
CHEMBL555146 193894 1 None -2344 13 Human 5.8 pKi = 5.8 Binding
Binding affinity to human recombinant H2 receptorBinding affinity to human recombinant H2 receptor
ChEMBL 351 5 0 3 4.8 C[C@@H]1CCCN1CCc1cc2cc(C(=O)c3ccc(F)cc3)ccc2o1 10.1021/jm201690h
10064805 101893 0 None -95 4 Human 5.8 pKi = 5.8 Binding
Compound was tested for its binding affinity towards human H2 receptorCompound was tested for its binding affinity towards human H2 receptor
ChEMBL 323 4 1 3 4.4 CN1CCCC1CCNc1c2c(nc3ccccc13)CCCCC2 10.1016/s0960-894x(03)00356-1
CHEMBL303824 101893 0 None -95 4 Human 5.8 pKi = 5.8 Binding
Compound was tested for its binding affinity towards human H2 receptorCompound was tested for its binding affinity towards human H2 receptor
ChEMBL 323 4 1 3 4.4 CN1CCCC1CCNc1c2c(nc3ccccc13)CCCCC2 10.1016/s0960-894x(03)00356-1
73349359 92097 0 None -2 8 Human 5.8 pKi = 5.8 Binding
Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay
ChEMBL 341 6 1 4 2.9 COc1cc(CN[C@H]2C3C4CC5C6C4CC3C6C52)cc(OC)c1OC 10.1016/j.bmc.2013.07.045
CHEMBL2432051 92097 0 None -2 8 Human 5.8 pKi = 5.8 Binding
Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay
ChEMBL 341 6 1 4 2.9 COc1cc(CN[C@H]2C3C4CC5C6C4CC3C6C52)cc(OC)c1OC 10.1016/j.bmc.2013.07.045
44304308 101999 0 None -691 3 Human 4.8 pKi = 4.8 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 432 8 0 5 3.7 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)c3cccc(F)c3F)cc2)CC1 10.1016/s0960-894x(02)00309-8
CHEMBL304027 101999 0 None -691 3 Human 4.8 pKi = 4.8 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 432 8 0 5 3.7 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)c3cccc(F)c3F)cc2)CC1 10.1016/s0960-894x(02)00309-8
44582676 189177 0 None -549 18 Human 5.8 pKi = 5.8 Binding
Inhibition of human cloned histamine H2 receptor by competitive binding experimentInhibition of human cloned histamine H2 receptor by competitive binding experiment
ChEMBL 403 9 0 4 4.3 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL516088 189177 0 None -549 18 Human 5.8 pKi = 5.8 Binding
Inhibition of human cloned histamine H2 receptor by competitive binding experimentInhibition of human cloned histamine H2 receptor by competitive binding experiment
ChEMBL 403 9 0 4 4.3 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
132060776 161840 0 None -6 16 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 419 4 0 4 4.4 O=C(OCc1ccccc1)N1CCc2ccc(N3CCN(C4CCCC4)CC3)cc2C1 10.1016/j.ejmech.2018.02.024
CHEMBL4165863 161840 0 None -6 16 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 419 4 0 4 4.4 O=C(OCc1ccccc1)N1CCc2ccc(N3CCN(C4CCCC4)CC3)cc2C1 10.1016/j.ejmech.2018.02.024
73346042 91388 3 None -17782 17 Human 5.8 pKi = 5.8 Binding
Binding affinity to histamine H2 receptor (unknown origin)Binding affinity to histamine H2 receptor (unknown origin)
ChEMBL 405 9 0 8 0.9 Cn1c(=O)cnn(CCCCN2CCN(c3ccccc3OCCF)CC2)c1=O 10.1016/j.bmc.2013.05.050
CHEMBL2413153 91388 3 None -17782 17 Human 5.8 pKi = 5.8 Binding
Binding affinity to histamine H2 receptor (unknown origin)Binding affinity to histamine H2 receptor (unknown origin)
ChEMBL 405 9 0 8 0.9 Cn1c(=O)cnn(CCCCN2CCN(c3ccccc3OCCF)CC2)c1=O 10.1016/j.bmc.2013.05.050
44304385 201479 0 None -3548 3 Human 4.8 pKi = 4.8 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 404 11 0 5 4.4 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OC(C)C)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL64259 201479 0 None -3548 3 Human 4.8 pKi = 4.8 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 404 11 0 5 4.4 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OC(C)C)CC2)cc1 10.1016/s0960-894x(02)00309-8
10455457 201703 0 None -3019 3 Human 4.8 pKi = 4.8 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 431 10 0 5 3.3 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)N3CCOCC3)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL65518 201703 0 None -3019 3 Human 4.8 pKi = 4.8 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 431 10 0 5 3.3 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)N3CCOCC3)CC2)cc1 10.1016/s0960-894x(02)00309-8
44304066 201068 0 None -407 3 Human 4.8 pKi = 4.8 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 449 11 1 5 3.0 CN[C@H](Cc1ccccc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL62050 201068 0 None -407 3 Human 4.8 pKi = 4.8 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 449 11 1 5 3.0 CN[C@H](Cc1ccccc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
71452383 83368 0 None 1 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to Histamine H2 receptorBinding affinity to Histamine H2 receptor
ChEMBL 339 5 1 4 2.0 COc1ccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1OC 10.1016/j.bmcl.2012.08.046
CHEMBL2205814 83368 0 None 1 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to Histamine H2 receptorBinding affinity to Histamine H2 receptor
ChEMBL 339 5 1 4 2.0 COc1ccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1OC 10.1016/j.bmcl.2012.08.046
1235 3751 32 None -3 5 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]Aminopotentidine from human recombinant histamine H2 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Aminopotentidine from human recombinant histamine H2 receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 312 6 4 6 -0.1 N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N 10.1016/j.bmcl.2013.01.025
3959 3751 32 None -3 5 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]Aminopotentidine from human recombinant histamine H2 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Aminopotentidine from human recombinant histamine H2 receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 312 6 4 6 -0.1 N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N 10.1016/j.bmcl.2013.01.025
50287 3751 32 None -3 5 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]Aminopotentidine from human recombinant histamine H2 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Aminopotentidine from human recombinant histamine H2 receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 312 6 4 6 -0.1 N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N 10.1016/j.bmcl.2013.01.025
CHEMBL269646 3751 32 None -3 5 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]Aminopotentidine from human recombinant histamine H2 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Aminopotentidine from human recombinant histamine H2 receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 312 6 4 6 -0.1 N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N 10.1016/j.bmcl.2013.01.025
4806 3933 85 None -5 13 Human 6.8 pKi = 6.8 Binding
Binding affinity to human histamine H2 receptorBinding affinity to human histamine H2 receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
7351 3933 85 None -5 13 Human 6.8 pKi = 6.8 Binding
Binding affinity to human histamine H2 receptorBinding affinity to human histamine H2 receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
9966051 3933 85 None -5 13 Human 6.8 pKi = 6.8 Binding
Binding affinity to human histamine H2 receptorBinding affinity to human histamine H2 receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
CHEMBL2104993 3933 85 None -5 13 Human 6.8 pKi = 6.8 Binding
Binding affinity to human histamine H2 receptorBinding affinity to human histamine H2 receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
DB09068 3933 85 None -5 13 Human 6.8 pKi = 6.8 Binding
Binding affinity to human histamine H2 receptorBinding affinity to human histamine H2 receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
10003483 4561 0 None -660 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 442 10 1 5 3.4 Cc1cccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)c1 10.1016/s0960-894x(02)00685-6
CHEMBL103027 4561 0 None -660 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 442 10 1 5 3.4 Cc1cccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)c1 10.1016/s0960-894x(02)00685-6
CHEMBL5076746 213739 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(N)(=O)=O)c3ccccc3C2(C)C)c2cc(S(=O)(=O)[O-])ccc2C1(C)C 10.1016/j.bmcl.2021.128388
CHEMBL5095519 213739 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(N)(=O)=O)c3ccccc3C2(C)C)c2cc(S(=O)(=O)[O-])ccc2C1(C)C 10.1016/j.bmcl.2021.128388
156015638 177687 0 None -1819 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human recombinant H2R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]UR-DE257 from Gsalphas-coupled human recombinant H2R expressed in baculovirus infected Sf9 insect cell membranes
ChEMBL 415 10 1 2 5.5 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4642520 177687 0 None -1819 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human recombinant H2R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]UR-DE257 from Gsalphas-coupled human recombinant H2R expressed in baculovirus infected Sf9 insect cell membranes
ChEMBL 415 10 1 2 5.5 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4650832 177687 0 None -1819 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human recombinant H2R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]UR-DE257 from Gsalphas-coupled human recombinant H2R expressed in baculovirus infected Sf9 insect cell membranes
ChEMBL 415 10 1 2 5.5 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
168281536 192269 0 None -9 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 369 12 4 5 1.7 Cc1nnc(CCCN/C(N)=N/C(=O)NCCCCCCCCN)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5189006 192269 0 None -9 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 369 12 4 5 1.7 Cc1nnc(CCCN/C(N)=N/C(=O)NCCCCCCCCN)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221966 192269 0 None -9 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 369 12 4 5 1.7 Cc1nnc(CCCN/C(N)=N/C(=O)NCCCCCCCCN)s1 10.1021/acs.jmedchem.1c00692
3158 55959 21 None -12589 20 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
CHEMBL1628227 55959 21 None -12589 20 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
44304399 201494 0 None -91 3 Human 5.7 pKi = 5.7 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 418 13 0 5 4.8 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OCCCC)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL64317 201494 0 None -91 3 Human 5.7 pKi = 5.7 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 418 13 0 5 4.8 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OCCCC)CC2)cc1 10.1016/s0960-894x(02)00309-8
44304376 201272 0 None -354 3 Human 4.7 pKi = 4.7 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 423 11 0 5 4.1 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3ccccn3)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL63036 201272 0 None -354 3 Human 4.7 pKi = 4.7 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 423 11 0 5 4.1 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3ccccn3)CC2)cc1 10.1016/s0960-894x(02)00309-8
44304244 201477 0 None -1174 3 Human 4.7 pKi = 4.7 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 372 12 0 4 4.2 CCCCCC(=O)c1ccc(OCCCN2CCN(CC3CC3)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL64253 201477 0 None -1174 3 Human 4.7 pKi = 4.7 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 372 12 0 4 4.2 CCCCCC(=O)c1ccc(OCCCN2CCN(CC3CC3)CC2)cc1 10.1016/s0960-894x(02)00309-8
44335384 4555 0 None -2630 4 Human 4.7 pKi = 4.7 Binding
Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor
ChEMBL 334 6 0 3 4.9 CC1CCCCN1CCCOc1ccc(-c2ccc(C#N)cc2)cc1 10.1016/s0960-894x(02)00648-0
CHEMBL102984 4555 0 None -2630 4 Human 4.7 pKi = 4.7 Binding
Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor
ChEMBL 334 6 0 3 4.9 CC1CCCCN1CCCOc1ccc(-c2ccc(C#N)cc2)cc1 10.1016/s0960-894x(02)00648-0
73355418 92100 0 None -1 3 Human 5.7 pKi = 5.7 Binding
Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay
ChEMBL 325 5 0 3 3.3 COc1ccc(CN(C)[C@H]2C3C4CC5C6C4CC3C6C52)cc1OC 10.1016/j.bmc.2013.07.045
CHEMBL2432056 92100 0 None -1 3 Human 5.7 pKi = 5.7 Binding
Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay
ChEMBL 325 5 0 3 3.3 COc1ccc(CN(C)[C@H]2C3C4CC5C6C4CC3C6C52)cc1OC 10.1016/j.bmc.2013.07.045
156011186 177658 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method
ChEMBL 704 20 2 7 7.5 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O 10.1021/acsmedchemlett.0c00033
CHEMBL4637893 177658 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method
ChEMBL 704 20 2 7 7.5 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O 10.1021/acsmedchemlett.0c00033
CHEMBL4650588 177658 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method
ChEMBL 704 20 2 7 7.5 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O 10.1021/acsmedchemlett.0c00033
168294449 192406 0 None -6 6 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 367 7 4 5 1.9 CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1 10.1021/acs.jmedchem.1c00692
CHEMBL5204599 192406 0 None -6 6 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 367 7 4 5 1.9 CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1 10.1021/acs.jmedchem.1c00692
CHEMBL5222793 192406 0 None -6 6 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 367 7 4 5 1.9 CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1 10.1021/acs.jmedchem.1c00692
168294161 192394 0 None 3 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 360 6 4 4 3.3 CCCCCNC(=O)/N=C(\N)Nc1cccc(-c2sc(N)nc2C)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5204739 192394 0 None 3 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 360 6 4 4 3.3 CCCCCNC(=O)/N=C(\N)Nc1cccc(-c2sc(N)nc2C)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5222742 192394 0 None 3 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 360 6 4 4 3.3 CCCCCNC(=O)/N=C(\N)Nc1cccc(-c2sc(N)nc2C)c1 10.1021/acs.jmedchem.1c00692
9923186 107043 0 None -977 4 Human 4.7 pKi = 4.7 Binding
Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor
ChEMBL 322 6 1 4 3.1 N#Cc1ccc(-c2ccc(OCCCN3CC[C@H](O)C3)cc2)cc1 10.1016/s0960-894x(02)00648-0
CHEMBL318801 107043 0 None -977 4 Human 4.7 pKi = 4.7 Binding
Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor
ChEMBL 322 6 1 4 3.1 N#Cc1ccc(-c2ccc(OCCCN3CC[C@H](O)C3)cc2)cc1 10.1016/s0960-894x(02)00648-0
12192007 167833 35 None -724 3 Human 4.7 pKi = 4.7 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 191 2 2 2 0.8 N[C@@H](C(=O)O)C1Cc2ccccc2C1 10.1016/s0960-894x(02)00310-4
CHEMBL434785 167833 35 None -724 3 Human 4.7 pKi = 4.7 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 191 2 2 2 0.8 N[C@@H](C(=O)O)C1Cc2ccccc2C1 10.1016/s0960-894x(02)00310-4
44304013 201196 0 None -363 3 Human 4.7 pKi = 4.7 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 401 8 1 5 2.6 CC(C)(C)[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL62716 201196 0 None -363 3 Human 4.7 pKi = 4.7 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 401 8 1 5 2.6 CC(C)(C)[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
72901200 119259 21 None -1318 4 Human 5.7 pKi = 5.7 Binding
Selectivity interaction (PRESTO-Tango GPCR-ome screening) EUB0000539a HRH2Selectivity interaction (PRESTO-Tango GPCR-ome screening) EUB0000539a HRH2
ChEMBL 322 7 2 4 3.8 Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1 nan
CHEMBL3480577 119259 21 None -1318 4 Human 5.7 pKi = 5.7 Binding
Selectivity interaction (PRESTO-Tango GPCR-ome screening) EUB0000539a HRH2Selectivity interaction (PRESTO-Tango GPCR-ome screening) EUB0000539a HRH2
ChEMBL 322 7 2 4 3.8 Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1 nan
5291 205694 115 None -1 2 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 493 7 2 7 4.6 Cc1ccc(NC(=O)c2ccc(CN3CCN(C)CC3)cc2)cc1Nc1nccc(-c2cccnc2)n1 nan
CHEMBL941 205694 115 None -1 2 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 493 7 2 7 4.6 Cc1ccc(NC(=O)c2ccc(CN3CCN(C)CC3)cc2)cc1Nc1nccc(-c2cccnc2)n1 nan
44304259 100135 0 None -660 3 Human 4.7 pKi = 4.7 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 462 11 0 5 5.4 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3sccc3Cl)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL291882 100135 0 None -660 3 Human 4.7 pKi = 4.7 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 462 11 0 5 5.4 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3sccc3Cl)CC2)cc1 10.1016/s0960-894x(02)00309-8
10341609 198576 0 None -4365 3 Human 4.7 pKi = 4.7 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 412 11 1 5 3.4 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3c[nH]cn3)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL59715 198576 0 None -4365 3 Human 4.7 pKi = 4.7 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 412 11 1 5 3.4 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3c[nH]cn3)CC2)cc1 10.1016/s0960-894x(02)00309-8
277 1269 55 None -43 46 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
2913 1269 55 None -43 46 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
765 1269 55 None -43 46 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
CHEMBL516 1269 55 None -43 46 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
DB00434 1269 55 None -43 46 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
20552188 116415 0 None - 1 Guinea pig 6.7 pKi = 6.7 Binding
Evaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atriumEvaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atrium
ChEMBL 333 6 4 7 1.4 CN/C(=C/[N+](=O)[O-])Nc1cccc(-c2csc(N=C(N)N)n2)c1 10.1021/jm00356a005
CHEMBL33850 116415 0 None - 1 Guinea pig 6.7 pKi = 6.7 Binding
Evaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atriumEvaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atrium
ChEMBL 333 6 4 7 1.4 CN/C(=C/[N+](=O)[O-])Nc1cccc(-c2csc(N=C(N)N)n2)c1 10.1021/jm00356a005
153287553 170528 0 None -316 6 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]-Iodoaminopotentidine from human recombinant histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-Iodoaminopotentidine from human recombinant histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 264 1 1 2 3.7 C[C@@]12CN(c3ccccc3)c3ccccc3[C@@H]1CCN2 10.1021/acsmedchemlett.9b00225
CHEMBL4457754 170528 0 None -316 6 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]-Iodoaminopotentidine from human recombinant histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-Iodoaminopotentidine from human recombinant histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 264 1 1 2 3.7 C[C@@]12CN(c3ccccc3)c3ccccc3[C@@H]1CCN2 10.1021/acsmedchemlett.9b00225
164619039 185556 0 None 17 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 366 4 4 4 3.0 N/C(=N\C(=O)NCc1ccccc1)Nc1cccc(-c2csc(N)n2)c1 10.1016/j.ejmech.2021.113190
CHEMBL4872277 185556 0 None 17 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 366 4 4 4 3.0 N/C(=N\C(=O)NCc1ccccc1)Nc1cccc(-c2csc(N)n2)c1 10.1016/j.ejmech.2021.113190
10263017 205719 2 None -31 3 Human 4.7 pKi = 4.7 Binding
Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.
ChEMBL 223 10 2 2 3.0 NCCCCCCCCCCc1c[nH]cn1 10.1021/jm00002a008
CHEMBL94249 205719 2 None -31 3 Human 4.7 pKi = 4.7 Binding
Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.
ChEMBL 223 10 2 2 3.0 NCCCCCCCCCCc1c[nH]cn1 10.1021/jm00002a008
44304247 201112 0 None -1905 3 Human 4.7 pKi = 4.7 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 412 11 0 5 4.3 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3ccco3)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL62312 201112 0 None -1905 3 Human 4.7 pKi = 4.7 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 412 11 0 5 4.3 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3ccco3)CC2)cc1 10.1016/s0960-894x(02)00309-8
5250783 168810 3 None -1995 3 Human 4.7 pKi = 4.7 Binding
Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors
ChEMBL 226 6 3 2 1.6 C/N=C(\S)NCCCCCc1c[nH]cn1 10.1021/jm00012a025
CHEMBL44220 168810 3 None -1995 3 Human 4.7 pKi = 4.7 Binding
Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors
ChEMBL 226 6 3 2 1.6 C/N=C(\S)NCCCCCc1c[nH]cn1 10.1021/jm00012a025
164626153 185786 0 None 4 6 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 378 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1cccc(F)c1 10.1016/j.ejmech.2021.113190
CHEMBL4875600 185786 0 None 4 6 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 378 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1cccc(F)c1 10.1016/j.ejmech.2021.113190
15179508 202979 0 None 851 2 Guinea pig 8.6 pKi = 8.6 Binding
Inhibition of [125I]APT binding to H2 receptors in guinea pig cerebral membranes.Inhibition of [125I]APT binding to H2 receptors in guinea pig cerebral membranes.
ChEMBL 588 11 3 5 3.5 N#CN/C(=N\CCNC(=O)c1cccc(I)c1)NCCCOc1cccc(CN2CCCCC2)c1 10.1021/jm00090a013
CHEMBL73994 202979 0 None 851 2 Guinea pig 8.6 pKi = 8.6 Binding
Inhibition of [125I]APT binding to H2 receptors in guinea pig cerebral membranes.Inhibition of [125I]APT binding to H2 receptors in guinea pig cerebral membranes.
ChEMBL 588 11 3 5 3.5 N#CN/C(=N\CCNC(=O)c1cccc(I)c1)NCCCOc1cccc(CN2CCCCC2)c1 10.1021/jm00090a013
2801 161313 56 None -12 29 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 nan
CHEMBL1200710 161313 56 None -12 29 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 nan
CHEMBL415 161313 56 None -12 29 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 nan
156015243 177653 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method
ChEMBL 1081 29 4 13 8.5 CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3cc(S(=O)(=O)O)ccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acsmedchemlett.0c00033
CHEMBL4648203 177653 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method
ChEMBL 1081 29 4 13 8.5 CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3cc(S(=O)(=O)O)ccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acsmedchemlett.0c00033
CHEMBL4650564 177653 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method
ChEMBL 1081 29 4 13 8.5 CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3cc(S(=O)(=O)O)ccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acsmedchemlett.0c00033
44304068 101864 0 None -125 3 Human 4.7 pKi = 4.7 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 441 10 1 5 3.5 N[C@H](CC1CCCCC1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL303737 101864 0 None -125 3 Human 4.7 pKi = 4.7 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 441 10 1 5 3.5 N[C@H](CC1CCCCC1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
44304030 199267 0 None -154 3 Human 4.7 pKi = 4.7 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 511 11 1 5 4.4 N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL60189 199267 0 None -154 3 Human 4.7 pKi = 4.7 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 511 11 1 5 4.4 N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
44304991 201363 0 None -1659 3 Human 4.7 pKi = 4.7 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 424 12 0 5 3.6 CCCCCC(=O)c1ccc(OCCCN2CCN(S(=O)(=O)C(C)C)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL63631 201363 0 None -1659 3 Human 4.7 pKi = 4.7 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 424 12 0 5 3.6 CCCCCC(=O)c1ccc(OCCCN2CCN(S(=O)(=O)C(C)C)CC2)cc1 10.1016/s0960-894x(02)00309-8
44304294 201265 0 None -97 3 Human 4.7 pKi = 4.7 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 485 10 1 5 3.9 N[C@H](Cc1cccc2ccccc12)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL63003 201265 0 None -97 3 Human 4.7 pKi = 4.7 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 485 10 1 5 3.9 N[C@H](Cc1cccc2ccccc12)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL4520788 212215 6 None 3 25 Human 7.7 pKi = 7.7 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000743a HRH2Selectivity interaction (GPCR panel (PDSP screen)) EUB0000743a HRH2
ChEMBL None None None CNCc1ccccc1-c1csc([C@H](C)Nc2nc(C)nc3cc(OC)c(OC)cc23)c1 nan
156021166 177752 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method
ChEMBL 908 25 3 8 10.3 C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acsmedchemlett.0c00033
CHEMBL4647775 177752 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method
ChEMBL 908 25 3 8 10.3 C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acsmedchemlett.0c00033
CHEMBL4651205 177752 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method
ChEMBL 908 25 3 8 10.3 C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acsmedchemlett.0c00033
CHEMBL5094663 213720 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](C)c3ccccc3C2(C)C)c2ccccc2C1(C)C 10.1016/j.bmcl.2021.128388
21830793 91389 5 None -14125 46 Human 5.7 pKi = 5.7 Binding
Binding affinity to histamine H2 receptor (unknown origin)Binding affinity to histamine H2 receptor (unknown origin)
ChEMBL 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 10.1016/j.bmc.2013.05.050
CHEMBL2413154 91389 5 None -14125 46 Human 5.7 pKi = 5.7 Binding
Binding affinity to histamine H2 receptor (unknown origin)Binding affinity to histamine H2 receptor (unknown origin)
ChEMBL 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 10.1016/j.bmc.2013.05.050
11948707 165603 0 None -5248 13 Human 5.7 pKi = 5.7 Binding
Binding affinity to histamine H2 receptor by radioligand binding assayBinding affinity to histamine H2 receptor by radioligand binding assay
ChEMBL 373 7 0 8 0.6 COc1cccc(N2CCN(CCCCn3ncc(=O)n(C)c3=O)CC2)c1 10.1016/j.bmcl.2006.01.052
CHEMBL426317 165603 0 None -5248 13 Human 5.7 pKi = 5.7 Binding
Binding affinity to histamine H2 receptor by radioligand binding assayBinding affinity to histamine H2 receptor by radioligand binding assay
ChEMBL 373 7 0 8 0.6 COc1cccc(N2CCN(CCCCn3ncc(=O)n(C)c3=O)CC2)c1 10.1016/j.bmcl.2006.01.052
168295543 192429 0 None 1 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 380 4 4 4 3.3 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCc2ccccc2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5209021 192429 0 None 1 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 380 4 4 4 3.3 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCc2ccccc2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222929 192429 0 None 1 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 380 4 4 4 3.3 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCc2ccccc2)cc1 10.1021/acs.jmedchem.1c00692
44304459 172021 0 None -575 3 Human 5.7 pKi = 5.7 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 418 13 0 5 4.8 CCCCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OCC)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL449040 172021 0 None -575 3 Human 5.7 pKi = 5.7 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 418 13 0 5 4.8 CCCCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OCC)CC2)cc1 10.1016/s0960-894x(02)00309-8
53320569 56544 0 None 3 2 Human 5.7 pKi = 5.7 Binding
Inhibition of H2 receptorInhibition of H2 receptor
ChEMBL 269 3 1 1 3.1 Fc1cccc(CN[C@H]2C3C4CC5C6C4CC3C6C52)c1 10.1016/j.bmcl.2010.11.075
CHEMBL1643899 56544 0 None 3 2 Human 5.7 pKi = 5.7 Binding
Inhibition of H2 receptorInhibition of H2 receptor
ChEMBL 269 3 1 1 3.1 Fc1cccc(CN[C@H]2C3C4CC5C6C4CC3C6C52)c1 10.1016/j.bmcl.2010.11.075
53320569 56544 0 None 3 2 Human 5.7 pKi = 5.7 Binding
Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay
ChEMBL 269 3 1 1 3.1 Fc1cccc(CN[C@H]2C3C4CC5C6C4CC3C6C52)c1 10.1016/j.bmc.2013.07.045
CHEMBL1643899 56544 0 None 3 2 Human 5.7 pKi = 5.7 Binding
Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay
ChEMBL 269 3 1 1 3.1 Fc1cccc(CN[C@H]2C3C4CC5C6C4CC3C6C52)c1 10.1016/j.bmc.2013.07.045
3823 49936 38 None -66 11 Human 4.7 pKi = 4.7 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
76973198 49936 38 None -66 11 Human 4.7 pKi = 4.7 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
CHEMBL157101 49936 38 None -66 11 Human 4.7 pKi = 4.7 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
168283536 192288 0 None -53 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 312 8 3 4 1.6 CCCCCNC(=O)/N=C(/N)NCCCc1nnc(C)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5187758 192288 0 None -53 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 312 8 3 4 1.6 CCCCCNC(=O)/N=C(/N)NCCCc1nnc(C)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222074 192288 0 None -53 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 312 8 3 4 1.6 CCCCCNC(=O)/N=C(/N)NCCCc1nnc(C)s1 10.1021/acs.jmedchem.1c00692
44304021 102309 0 None -562 3 Human 4.7 pKi = 4.7 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 374 8 0 5 3.4 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)C=C(C)C)cc2)CC1 10.1016/s0960-894x(02)00309-8
CHEMBL305313 102309 0 None -562 3 Human 4.7 pKi = 4.7 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 374 8 0 5 3.4 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)C=C(C)C)cc2)CC1 10.1016/s0960-894x(02)00309-8
168278471 192236 0 None -18 6 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 312 8 4 4 1.5 CCCCCNC(=O)/N=C(\N)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5183205 192236 0 None -18 6 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 312 8 4 4 1.5 CCCCCNC(=O)/N=C(\N)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221757 192236 0 None -18 6 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 312 8 4 4 1.5 CCCCCNC(=O)/N=C(\N)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
44334235 4548 0 None -199 3 Human 5.7 pKi = 5.7 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 442 10 1 5 3.4 Cc1ccccc1S(=O)(=O)N[C@H]1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)C1 10.1016/s0960-894x(02)00685-6
CHEMBL102929 4548 0 None -199 3 Human 5.7 pKi = 5.7 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 442 10 1 5 3.4 Cc1ccccc1S(=O)(=O)N[C@H]1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)C1 10.1016/s0960-894x(02)00685-6
44334503 4911 0 None -144 3 Human 4.7 pKi = 4.7 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 349 9 3 6 0.2 CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)[C@@H](N)CO)C2)cc1 10.1016/s0960-894x(02)00685-6
CHEMBL104994 4911 0 None -144 3 Human 4.7 pKi = 4.7 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 349 9 3 6 0.2 CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)[C@@H](N)CO)C2)cc1 10.1016/s0960-894x(02)00685-6
44304036 96321 0 None -407 3 Human 4.7 pKi = 4.7 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 360 8 0 5 3.0 C=C(C)C(=O)c1ccc(OCCCN2CCN(C(=O)OCC)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL264761 96321 0 None -407 3 Human 4.7 pKi = 4.7 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 360 8 0 5 3.0 C=C(C)C(=O)c1ccc(OCCCN2CCN(C(=O)OCC)CC2)cc1 10.1016/s0960-894x(02)00309-8
44304269 100065 0 None -3548 3 Human 4.7 pKi = 4.7 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 423 11 0 5 4.1 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3ccncc3)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL291394 100065 0 None -3548 3 Human 4.7 pKi = 4.7 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 423 11 0 5 4.1 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3ccncc3)CC2)cc1 10.1016/s0960-894x(02)00309-8
44304037 102207 0 None -6165 3 Human 4.7 pKi = 4.7 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 362 9 0 5 3.2 CCCC(=O)c1ccc(OCCCN2CCN(C(=O)OCC)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL304714 102207 0 None -6165 3 Human 4.7 pKi = 4.7 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 362 9 0 5 3.2 CCCC(=O)c1ccc(OCCCN2CCN(C(=O)OCC)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL5094083 213682 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay
ChEMBL None None None C=C(/N=C(\C)NCCCc1nnc(N)s1)NCCCCCCCCN 10.1016/j.bmcl.2021.128388
164611143 184123 0 None 75 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 414 6 4 4 2.9 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(c1ccccc1)C(F)(F)F 10.1016/j.ejmech.2021.113190
CHEMBL4850448 184123 0 None 75 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 414 6 4 4 2.9 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(c1ccccc1)C(F)(F)F 10.1016/j.ejmech.2021.113190
44304438 201469 0 None -2089 3 Human 4.6 pKi = 4.6 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 420 13 0 5 4.1 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)CSCC)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL64235 201469 0 None -2089 3 Human 4.6 pKi = 4.6 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 420 13 0 5 4.1 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)CSCC)CC2)cc1 10.1016/s0960-894x(02)00309-8
44304307 201533 0 None -3548 3 Human 4.6 pKi = 4.6 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 388 12 0 4 4.2 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)CCC)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL64479 201533 0 None -3548 3 Human 4.6 pKi = 4.6 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 388 12 0 4 4.2 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)CCC)CC2)cc1 10.1016/s0960-894x(02)00309-8
44335405 5019 0 None -194 4 Human 4.6 pKi = 4.6 Binding
Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor
ChEMBL 321 6 1 4 2.9 N#Cc1ccc(-c2ccc(OCCCN3CCNCC3)cc2)cc1 10.1016/s0960-894x(02)00648-0
CHEMBL105594 5019 0 None -194 4 Human 4.6 pKi = 4.6 Binding
Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor
ChEMBL 321 6 1 4 2.9 N#Cc1ccc(-c2ccc(OCCCN3CCNCC3)cc2)cc1 10.1016/s0960-894x(02)00648-0
44304415 200334 0 None -9549 3 Human 4.6 pKi = 4.6 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 505 13 2 7 3.2 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](CO)NC(=O)OC(C)(C)C)CC2)cc1 10.1016/s0960-894x(02)00310-4
CHEMBL60837 200334 0 None -9549 3 Human 4.6 pKi = 4.6 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 505 13 2 7 3.2 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](CO)NC(=O)OC(C)(C)C)CC2)cc1 10.1016/s0960-894x(02)00310-4
4543 169972 36 None -22 30 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 nan
CHEMBL1201156 169972 36 None -22 30 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 nan
CHEMBL445 169972 36 None -22 30 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 nan
44334214 4532 0 None -380 3 Human 5.6 pKi = 5.6 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 427 9 1 6 2.6 CC(=O)c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccc(C#N)cc3)C2)cc1 10.1016/s0960-894x(02)00685-6
CHEMBL102840 4532 0 None -380 3 Human 5.6 pKi = 5.6 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 427 9 1 6 2.6 CC(=O)c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccc(C#N)cc3)C2)cc1 10.1016/s0960-894x(02)00685-6
168268827 192167 0 None 3 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 450 8 4 4 4.8 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5179906 192167 0 None 3 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 450 8 4 4 4.8 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5221314 192167 0 None 3 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 450 8 4 4 4.8 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)c1 10.1021/acs.jmedchem.1c00692
168294770 192408 0 None 2 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 436 6 4 4 4.3 Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5208327 192408 0 None 2 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 436 6 4 4 4.3 Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222806 192408 0 None 2 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 436 6 4 4 4.3 Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)cc1 10.1021/acs.jmedchem.1c00692
44304325 199983 0 None -1096 3 Human 4.6 pKi = 4.6 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 389 11 1 4 3.6 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)NCC)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL60620 199983 0 None -1096 3 Human 4.6 pKi = 4.6 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 389 11 1 4 3.6 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)NCC)CC2)cc1 10.1016/s0960-894x(02)00309-8
44335368 4966 0 None -63 3 Human 4.6 pKi = 4.6 Binding
Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor
ChEMBL 393 7 0 5 3.8 CCOC(=O)N1CCN(CCCOc2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/s0960-894x(02)00648-0
CHEMBL105268 4966 0 None -63 3 Human 4.6 pKi = 4.6 Binding
Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor
ChEMBL 393 7 0 5 3.8 CCOC(=O)N1CCN(CCCOc2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/s0960-894x(02)00648-0
44335238 5005 0 None -11220 4 Human 4.6 pKi = 4.6 Binding
Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor
ChEMBL 348 6 0 3 5.3 CC1CCCC(C)N1CCCOc1ccc(-c2ccc(C#N)cc2)cc1 10.1016/s0960-894x(02)00648-0
CHEMBL105515 5005 0 None -11220 4 Human 4.6 pKi = 4.6 Binding
Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor
ChEMBL 348 6 0 3 5.3 CC1CCCC(C)N1CCCOc1ccc(-c2ccc(C#N)cc2)cc1 10.1016/s0960-894x(02)00648-0
44333987 108049 0 None -26 3 Human 4.6 pKi = 4.6 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 433 9 2 6 2.8 CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)[C@H](C)NC(=O)OC(C)(C)C)C2)cc1 10.1016/s0960-894x(02)00685-6
CHEMBL320174 108049 0 None -26 3 Human 4.6 pKi = 4.6 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 433 9 2 6 2.8 CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)[C@H](C)NC(=O)OC(C)(C)C)C2)cc1 10.1016/s0960-894x(02)00685-6
44582675 189099 0 None -3311 16 Human 5.6 pKi = 5.6 Binding
Inhibition of human cloned histamine H2 receptor by competitive binding experimentInhibition of human cloned histamine H2 receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1[C@H](O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL515472 189099 0 None -3311 16 Human 5.6 pKi = 5.6 Binding
Inhibition of human cloned histamine H2 receptor by competitive binding experimentInhibition of human cloned histamine H2 receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1[C@H](O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
168283321 192283 0 None 2 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 364 7 4 4 2.3 Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1 10.1021/acs.jmedchem.1c00692
CHEMBL5183015 192283 0 None 2 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 364 7 4 4 2.3 Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1 10.1021/acs.jmedchem.1c00692
CHEMBL5222057 192283 0 None 2 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 364 7 4 4 2.3 Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1 10.1021/acs.jmedchem.1c00692
44304437 100514 0 None -426 3 Human 4.6 pKi = 4.6 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 404 11 1 5 3.1 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)C(C)(C)O)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL294349 100514 0 None -426 3 Human 4.6 pKi = 4.6 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 404 11 1 5 3.1 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)C(C)(C)O)CC2)cc1 10.1016/s0960-894x(02)00309-8
44304049 101655 0 None -891 3 Human 4.6 pKi = 4.6 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 421 9 1 5 2.9 N[C@@H](C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1)c1ccccc1 10.1016/s0960-894x(02)00310-4
CHEMBL302468 101655 0 None -891 3 Human 4.6 pKi = 4.6 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 421 9 1 5 2.9 N[C@@H](C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1)c1ccccc1 10.1016/s0960-894x(02)00310-4
146025727 171109 0 None -93 27 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 411 3 0 5 6.4 FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4466483 171109 0 None -93 27 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 411 3 0 5 6.4 FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL5087637 213769 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C 10.1016/j.bmcl.2021.128388
CHEMBL5095891 213769 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C 10.1016/j.bmcl.2021.128388
44304304 169485 0 None -3981 3 Human 4.6 pKi = 4.6 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 423 9 0 6 3.5 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)/C=C/c3cccnc3)cc2)CC1 10.1016/s0960-894x(02)00309-8
CHEMBL444307 169485 0 None -3981 3 Human 4.6 pKi = 4.6 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 423 9 0 6 3.5 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)/C=C/c3cccnc3)cc2)CC1 10.1016/s0960-894x(02)00309-8
1248 1391 27 None -123 7 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells
ChEMBL 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1016/j.bmcl.2010.10.041
3077 1391 27 None -123 7 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells
ChEMBL 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1016/j.bmcl.2010.10.041
90045 1391 27 None -123 7 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells
ChEMBL 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1016/j.bmcl.2010.10.041
CHEMBL12344 1391 27 None -123 7 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells
ChEMBL 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1016/j.bmcl.2010.10.041
145988693 166602 0 None -10 17 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assay
ChEMBL 524 7 1 3 7.1 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCN(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL4291048 166602 0 None -10 17 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assay
ChEMBL 524 7 1 3 7.1 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCN(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
2520 202301 65 None -20 12 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC nan
CHEMBL1280 202301 65 None -20 12 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC nan
CHEMBL6966 202301 65 None -20 12 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC nan
2726 904 64 None -85 73 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
621 904 64 None -85 73 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
83 904 64 None -85 73 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL71 904 64 None -85 73 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
DB00477 904 64 None -85 73 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
168273745 192196 0 None -13 6 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 332 6 4 4 1.5 N/C(=N\C(=O)NCc1ccccc1)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5178472 192196 0 None -13 6 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 332 6 4 4 1.5 N/C(=N\C(=O)NCc1ccccc1)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221451 192196 0 None -13 6 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 332 6 4 4 1.5 N/C(=N\C(=O)NCc1ccccc1)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
155543832 172630 0 None -234 7 Human 5.6 pKi = 5.6 Binding
Inhibition of histamine H2 receptor (unknown origin)Inhibition of histamine H2 receptor (unknown origin)
ChEMBL 451 6 3 7 3.4 O[C@H]1[C@H](n2cnc3c(NC(C4CCC4)C4CCC4)nc(Cl)nc32)[C@H]2C[C@@]2(CCl)[C@H]1O 10.1021/acs.jmedchem.8b01662
CHEMBL4522864 172630 0 None -234 7 Human 5.6 pKi = 5.6 Binding
Inhibition of histamine H2 receptor (unknown origin)Inhibition of histamine H2 receptor (unknown origin)
ChEMBL 451 6 3 7 3.4 O[C@H]1[C@H](n2cnc3c(NC(C4CCC4)C4CCC4)nc(Cl)nc32)[C@H]2C[C@@]2(CCl)[C@H]1O 10.1021/acs.jmedchem.8b01662
1204 1893 114 None -173 25 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2021.128388
1247 1893 114 None -173 25 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2021.128388
1375 1893 114 None -173 25 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2021.128388
774 1893 114 None -173 25 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2021.128388
CHEMBL90 1893 114 None -173 25 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2021.128388
DB05381 1893 114 None -173 25 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2021.128388
CHEMBL5077939 213755 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)O)c3ccccc3C2(C)C)c2cc(S(=O)(=O)[O-])ccc2C1(C)C 10.1016/j.bmcl.2021.128388
CHEMBL5095769 213755 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)O)c3ccccc3C2(C)C)c2cc(S(=O)(=O)[O-])ccc2C1(C)C 10.1016/j.bmcl.2021.128388
CHEMBL5093461 213767 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay
ChEMBL None None None CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2nnc(N)s2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1016/j.bmcl.2021.128388
CHEMBL5095884 213767 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay
ChEMBL None None None CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2nnc(N)s2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1016/j.bmcl.2021.128388
1204 1893 114 None -173 25 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2021.113190
1247 1893 114 None -173 25 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2021.113190
1375 1893 114 None -173 25 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2021.113190
774 1893 114 None -173 25 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2021.113190
CHEMBL90 1893 114 None -173 25 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2021.113190
DB05381 1893 114 None -173 25 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2021.113190
1204 1893 114 None -173 25 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
1247 1893 114 None -173 25 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
1375 1893 114 None -173 25 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
774 1893 114 None -173 25 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
CHEMBL90 1893 114 None -173 25 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
DB05381 1893 114 None -173 25 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
156015793 177674 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method
ChEMBL 880 23 3 8 9.5 C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acsmedchemlett.0c00033
CHEMBL4645867 177674 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method
ChEMBL 880 23 3 8 9.5 C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acsmedchemlett.0c00033
CHEMBL4650701 177674 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method
ChEMBL 880 23 3 8 9.5 C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acsmedchemlett.0c00033
44304091 201253 0 None -338 3 Human 5.6 pKi = 5.6 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 432 14 0 5 5.2 CCCCCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OCC)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL62949 201253 0 None -338 3 Human 5.6 pKi = 5.6 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 432 14 0 5 5.2 CCCCCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OCC)CC2)cc1 10.1016/s0960-894x(02)00309-8
44304516 164793 0 None -630 3 Human 4.6 pKi = 4.6 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 357 8 1 5 1.5 O=C1C[C@H](N2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)CC2)N1 10.1016/s0960-894x(02)00310-4
CHEMBL423666 164793 0 None -630 3 Human 4.6 pKi = 4.6 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 357 8 1 5 1.5 O=C1C[C@H](N2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)CC2)N1 10.1016/s0960-894x(02)00310-4
18609376 202646 61 None - 1 Human 4.6 pKi = 4.6 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 386 2 0 4 4.7 CC(=O)O[C@]1(C(C)=O)CC[C@H]2[C@@H]3C[C@H](C)C4=CC(=O)CC[C@]4(C)[C@H]3CC[C@@]21C nan
6279 202646 61 None - 1 Human 4.6 pKi = 4.6 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 386 2 0 4 4.7 CC(=O)O[C@]1(C(C)=O)CC[C@H]2[C@@H]3C[C@H](C)C4=CC(=O)CC[C@]4(C)[C@H]3CC[C@@]21C nan
CHEMBL717 202646 61 None - 1 Human 4.6 pKi = 4.6 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 386 2 0 4 4.7 CC(=O)O[C@]1(C(C)=O)CC[C@H]2[C@@H]3C[C@H](C)C4=CC(=O)CC[C@]4(C)[C@H]3CC[C@@]21C nan
44304256 167445 0 None -1000 3 Human 4.6 pKi = 4.6 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 360 12 0 4 4.2 CCCCCC(=O)c1ccc(OCCCN2CCN(CCC)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL432144 167445 0 None -1000 3 Human 4.6 pKi = 4.6 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 360 12 0 4 4.2 CCCCCC(=O)c1ccc(OCCCN2CCN(CCC)CC2)cc1 10.1016/s0960-894x(02)00309-8
44304032 199792 0 None -616 3 Human 4.6 pKi = 4.6 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 413 11 0 6 3.7 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3cnco3)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL60509 199792 0 None -616 3 Human 4.6 pKi = 4.6 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 413 11 0 6 3.7 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3cnco3)CC2)cc1 10.1016/s0960-894x(02)00309-8
53324045 56761 0 None -7 16 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assay
ChEMBL 487 7 1 2 7.3 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL1644980 56761 0 None -7 16 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assay
ChEMBL 487 7 1 2 7.3 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2018.10.036
164614549 184350 0 None -2 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 340 9 4 4 2.2 CCCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1016/j.ejmech.2021.113190
CHEMBL4853668 184350 0 None -2 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 340 9 4 4 2.2 CCCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1016/j.ejmech.2021.113190
164619208 185070 0 None 446 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 378 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccccc1F 10.1016/j.ejmech.2021.113190
CHEMBL4864852 185070 0 None 446 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 378 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccccc1F 10.1016/j.ejmech.2021.113190
2284 3121 27 None -53 29 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
4926 3121 27 None -53 29 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
7281 3121 27 None -53 29 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
CHEMBL564 3121 27 None -53 29 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
DB00420 3121 27 None -53 29 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
71525681 89284 0 None -346 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]histamine from human histamine H2 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H2 receptor expressed in HEK cells
ChEMBL 298 3 2 6 1.7 CNC1CN(c2nc(N)nc3cc(C4CCCC4)cnc23)C1 10.1016/j.bmcl.2013.02.091
CHEMBL2376803 89284 0 None -346 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]histamine from human histamine H2 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H2 receptor expressed in HEK cells
ChEMBL 298 3 2 6 1.7 CNC1CN(c2nc(N)nc3cc(C4CCCC4)cnc23)C1 10.1016/j.bmcl.2013.02.091
132060743 161674 0 None -1 13 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 351 3 0 4 3.1 CN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)C3)CC1 10.1016/j.ejmech.2018.02.024
CHEMBL4163428 161674 0 None -1 13 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 351 3 0 4 3.1 CN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)C3)CC1 10.1016/j.ejmech.2018.02.024
3191 102372 93 None -24 25 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
CHEMBL305660 102372 93 None -24 25 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
44335387 108050 0 None -1023 4 Human 4.5 pKi = 4.5 Binding
Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor
ChEMBL 393 7 0 5 3.8 CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc(C#N)cc3)cc2)CC1 10.1016/s0960-894x(02)00648-0
CHEMBL320178 108050 0 None -1023 4 Human 4.5 pKi = 4.5 Binding
Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor
ChEMBL 393 7 0 5 3.8 CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc(C#N)cc3)cc2)CC1 10.1016/s0960-894x(02)00648-0
44334406 4779 0 None -75 3 Human 6.5 pKi = 6.5 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 462 10 1 5 3.8 O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccc(Cl)cc3)C2)cc1)C1CC1 10.1016/s0960-894x(02)00685-6
CHEMBL104344 4779 0 None -75 3 Human 6.5 pKi = 6.5 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 462 10 1 5 3.8 O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccc(Cl)cc3)C2)cc1)C1CC1 10.1016/s0960-894x(02)00685-6
44334368 108717 0 None -57 3 Human 6.5 pKi = 6.5 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 506 10 1 5 3.9 O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccc(Br)cc3)C2)cc1)C1CC1 10.1016/s0960-894x(02)00685-6
CHEMBL321709 108717 0 None -57 3 Human 6.5 pKi = 6.5 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 506 10 1 5 3.9 O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccc(Br)cc3)C2)cc1)C1CC1 10.1016/s0960-894x(02)00685-6
1204 1893 114 None -173 25 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acsmedchemlett.0c00033
1247 1893 114 None -173 25 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acsmedchemlett.0c00033
1375 1893 114 None -173 25 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acsmedchemlett.0c00033
774 1893 114 None -173 25 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acsmedchemlett.0c00033
CHEMBL90 1893 114 None -173 25 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acsmedchemlett.0c00033
DB05381 1893 114 None -173 25 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acsmedchemlett.0c00033
44304291 201155 0 None -6606 3 Human 4.5 pKi = 4.5 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 388 11 0 4 4.0 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)C(C)C)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL62527 201155 0 None -6606 3 Human 4.5 pKi = 4.5 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 388 11 0 4 4.0 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)C(C)C)CC2)cc1 10.1016/s0960-894x(02)00309-8
168294767 192407 0 None -117 20 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5207281 192407 0 None -117 20 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222802 192407 0 None -117 20 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
136092260 102481 6 None - 1 Guinea pig 8.4 pKi = 8.4 Binding
In vitro inhibition of Histamine H2 receptor by measuring its ability to block the histamine-stimulated adenylate cyclase of guinea pig hippocampal homogenateIn vitro inhibition of Histamine H2 receptor by measuring its ability to block the histamine-stimulated adenylate cyclase of guinea pig hippocampal homogenate
ChEMBL 363 8 2 7 2.7 Nc1n[s+]([O-])nc1NCCCOc1cccc(CN2CCCCC2)c1 10.1021/jm00345a002
5486883 102481 6 None - 1 Guinea pig 8.4 pKi = 8.4 Binding
In vitro inhibition of Histamine H2 receptor by measuring its ability to block the histamine-stimulated adenylate cyclase of guinea pig hippocampal homogenateIn vitro inhibition of Histamine H2 receptor by measuring its ability to block the histamine-stimulated adenylate cyclase of guinea pig hippocampal homogenate
ChEMBL 363 8 2 7 2.7 Nc1n[s+]([O-])nc1NCCCOc1cccc(CN2CCCCC2)c1 10.1021/jm00345a002
CHEMBL306465 102481 6 None - 1 Guinea pig 8.4 pKi = 8.4 Binding
In vitro inhibition of Histamine H2 receptor by measuring its ability to block the histamine-stimulated adenylate cyclase of guinea pig hippocampal homogenateIn vitro inhibition of Histamine H2 receptor by measuring its ability to block the histamine-stimulated adenylate cyclase of guinea pig hippocampal homogenate
ChEMBL 363 8 2 7 2.7 Nc1n[s+]([O-])nc1NCCCOc1cccc(CN2CCCCC2)c1 10.1021/jm00345a002
CHEMBL5078202 213750 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1 10.1016/j.bmcl.2021.128388
CHEMBL5095695 213750 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1 10.1016/j.bmcl.2021.128388
164627241 185837 0 None 95 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 438 6 4 4 3.1 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(Br)cc1 10.1016/j.ejmech.2021.113190
CHEMBL4876267 185837 0 None 95 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 438 6 4 4 3.1 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(Br)cc1 10.1016/j.ejmech.2021.113190
164618508 185340 0 None 165 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 374 6 4 4 2.7 Cc1ccc(C(C)NC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1 10.1016/j.ejmech.2021.113190
CHEMBL4869194 185340 0 None 165 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 374 6 4 4 2.7 Cc1ccc(C(C)NC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1 10.1016/j.ejmech.2021.113190
10324985 76413 7 None -223 17 Human 6.5 pKi = 6.5 Binding
Binding affinity to histamine H2 receptorBinding affinity to histamine H2 receptor
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
CHEMBL199824 76413 7 None -223 17 Human 6.5 pKi = 6.5 Binding
Binding affinity to histamine H2 receptorBinding affinity to histamine H2 receptor
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
CHEMBL2068762 76413 7 None -223 17 Human 6.5 pKi = 6.5 Binding
Binding affinity to histamine H2 receptorBinding affinity to histamine H2 receptor
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
156010170 177749 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method
ChEMBL 414 13 3 7 2.3 NCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O 10.1021/acsmedchemlett.0c00033
CHEMBL4632998 177749 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method
ChEMBL 414 13 3 7 2.3 NCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O 10.1021/acsmedchemlett.0c00033
CHEMBL4651192 177749 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method
ChEMBL 414 13 3 7 2.3 NCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O 10.1021/acsmedchemlett.0c00033
168277996 192234 0 None -20 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 380 4 4 4 3.3 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCc2ccccc2)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5173373 192234 0 None -20 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 380 4 4 4 3.3 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCc2ccccc2)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5221736 192234 0 None -20 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 380 4 4 4 3.3 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCc2ccccc2)c1 10.1021/acs.jmedchem.1c00692
168278543 192239 0 None 2 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 358 4 4 4 1.6 N/C(=N\C(=O)NCc1ccccc1)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
CHEMBL5184846 192239 0 None 2 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 358 4 4 4 1.6 N/C(=N\C(=O)NCc1ccccc1)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
CHEMBL5221764 192239 0 None 2 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 358 4 4 4 1.6 N/C(=N\C(=O)NCc1ccccc1)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
1231 922 112 None -2 8 Guinea pig 6.5 pKi = 6.5 Binding
Inhibition of [125I]APT binding to H2 receptors in guinea pig cerebral membranes.Inhibition of [125I]APT binding to H2 receptors in guinea pig cerebral membranes.
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/jm00090a013
2756 922 112 None -2 8 Guinea pig 6.5 pKi = 6.5 Binding
Inhibition of [125I]APT binding to H2 receptors in guinea pig cerebral membranes.Inhibition of [125I]APT binding to H2 receptors in guinea pig cerebral membranes.
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/jm00090a013
645 922 112 None -2 8 Guinea pig 6.5 pKi = 6.5 Binding
Inhibition of [125I]APT binding to H2 receptors in guinea pig cerebral membranes.Inhibition of [125I]APT binding to H2 receptors in guinea pig cerebral membranes.
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/jm00090a013
CHEMBL30 922 112 None -2 8 Guinea pig 6.5 pKi = 6.5 Binding
Inhibition of [125I]APT binding to H2 receptors in guinea pig cerebral membranes.Inhibition of [125I]APT binding to H2 receptors in guinea pig cerebral membranes.
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/jm00090a013
DB00501 922 112 None -2 8 Guinea pig 6.5 pKi = 6.5 Binding
Inhibition of [125I]APT binding to H2 receptors in guinea pig cerebral membranes.Inhibition of [125I]APT binding to H2 receptors in guinea pig cerebral membranes.
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/jm00090a013
1599 2299 47 None -154 16 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 nan
3955 2299 47 None -154 16 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 nan
7215 2299 47 None -154 16 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 nan
CHEMBL841 2299 47 None -154 16 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 nan
DB00836 2299 47 None -154 16 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 nan
73349361 92102 0 None -3 7 Human 5.5 pKi = 5.5 Binding
Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay
ChEMBL 279 4 0 1 3.3 CN(CCc1ccccc1)[C@H]1C2C3CC4C5C3CC2C5C41 10.1016/j.bmc.2013.07.045
CHEMBL2432058 92102 0 None -3 7 Human 5.5 pKi = 5.5 Binding
Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay
ChEMBL 279 4 0 1 3.3 CN(CCc1ccccc1)[C@H]1C2C3CC4C5C3CC2C5C41 10.1016/j.bmc.2013.07.045
168294178 192423 0 None 1 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 414 5 4 4 4.4 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)C2CCCCC2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5205197 192423 0 None 1 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 414 5 4 4 4.4 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)C2CCCCC2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222887 192423 0 None 1 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 414 5 4 4 4.4 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)C2CCCCC2)cc1 10.1021/acs.jmedchem.1c00692
164609493 183844 0 None -1 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 350 6 4 5 1.9 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccco1 10.1016/j.ejmech.2021.113190
CHEMBL4846380 183844 0 None -1 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 350 6 4 5 1.9 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccco1 10.1016/j.ejmech.2021.113190
164614907 183991 0 None 323 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 378 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(F)cc1 10.1016/j.ejmech.2021.113190
CHEMBL4848697 183991 0 None 323 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 378 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(F)cc1 10.1016/j.ejmech.2021.113190
1235 3751 32 None 1 5 Guinea pig 7.5 pKi = 7.5 Binding
Evaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atriumEvaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atrium
ChEMBL 312 6 4 6 -0.1 N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N 10.1021/jm00356a005
3959 3751 32 None 1 5 Guinea pig 7.5 pKi = 7.5 Binding
Evaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atriumEvaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atrium
ChEMBL 312 6 4 6 -0.1 N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N 10.1021/jm00356a005
50287 3751 32 None 1 5 Guinea pig 7.5 pKi = 7.5 Binding
Evaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atriumEvaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atrium
ChEMBL 312 6 4 6 -0.1 N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N 10.1021/jm00356a005
CHEMBL269646 3751 32 None 1 5 Guinea pig 7.5 pKi = 7.5 Binding
Evaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atriumEvaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atrium
ChEMBL 312 6 4 6 -0.1 N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N 10.1021/jm00356a005
44334521 107337 0 None -36 3 Human 4.5 pKi = 4.5 Binding
Binding affinity towards human Histamine H2 receptor (For compound 11)Binding affinity towards human Histamine H2 receptor (For compound 11)
ChEMBL 262 6 1 4 1.7 CC(=O)c1ccc(OCCCN2CC[C@H](N)C2)cc1 10.1016/s0960-894x(02)00685-6
CHEMBL319231 107337 0 None -36 3 Human 4.5 pKi = 4.5 Binding
Binding affinity towards human Histamine H2 receptor (For compound 11)Binding affinity towards human Histamine H2 receptor (For compound 11)
ChEMBL 262 6 1 4 1.7 CC(=O)c1ccc(OCCCN2CC[C@H](N)C2)cc1 10.1016/s0960-894x(02)00685-6
168286141 192312 0 None 2 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 450 8 4 4 4.8 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5192993 192312 0 None 2 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 450 8 4 4 4.8 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222231 192312 0 None 2 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 450 8 4 4 4.8 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)cc1 10.1021/acs.jmedchem.1c00692
44281115 99239 0 None - 1 Guinea pig 6.5 pKi = 6.5 Binding
Evaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atriumEvaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atrium
ChEMBL 348 4 5 8 2.0 N=C(N)Nc1nc(-c2cccc(Nc3n[s+]([O-])nc3N)c2)cs1 10.1021/jm00356a005
CHEMBL284743 99239 0 None - 1 Guinea pig 6.5 pKi = 6.5 Binding
Evaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atriumEvaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atrium
ChEMBL 348 4 5 8 2.0 N=C(N)Nc1nc(-c2cccc(Nc3n[s+]([O-])nc3N)c2)cs1 10.1021/jm00356a005
14022519 168781 0 None - 1 Guinea pig 6.5 pKi = 6.5 Binding
Evaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atriumEvaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atrium
ChEMBL 314 3 4 5 1.2 C/N=C(\NC#N)Nc1cccc(-c2csc(N=C(N)N)n2)c1 10.1021/jm00356a005
CHEMBL441965 168781 0 None - 1 Guinea pig 6.5 pKi = 6.5 Binding
Evaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atriumEvaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atrium
ChEMBL 314 3 4 5 1.2 C/N=C(\NC#N)Nc1cccc(-c2csc(N=C(N)N)n2)c1 10.1021/jm00356a005
50898777 56131 0 None -29512 8 Human 5.5 pKi = 5.5 Binding
Binding affinity to Histamine receptor H2Binding affinity to Histamine receptor H2
ChEMBL 441 9 1 6 3.6 COC(=O)CCCCCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1 10.1016/j.bmc.2010.10.011
CHEMBL1632158 56131 0 None -29512 8 Human 5.5 pKi = 5.5 Binding
Binding affinity to Histamine receptor H2Binding affinity to Histamine receptor H2
ChEMBL 441 9 1 6 3.6 COC(=O)CCCCCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1 10.1016/j.bmc.2010.10.011
11723317 102408 0 None -100 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors
ChEMBL 316 9 3 2 2.8 S=C(NCCCCCc1c[nH]cn1)NCCc1ccccc1 10.1021/jm00012a025
CHEMBL305929 102408 0 None -100 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors
ChEMBL 316 9 3 2 2.8 S=C(NCCCCCc1c[nH]cn1)NCCc1ccccc1 10.1021/jm00012a025
164610421 184668 0 None 7 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 332 5 4 4 2.1 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)Nc1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4858567 184668 0 None 7 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 332 5 4 4 2.1 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)Nc1ccccc1 10.1016/j.ejmech.2021.113190
71525679 89282 0 None -223 6 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]histamine from human histamine H2 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H2 receptor expressed in HEK cells
ChEMBL 272 3 2 6 1.0 CCc1cnc2c(N3CC[C@@H](NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
CHEMBL2376801 89282 0 None -223 6 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]histamine from human histamine H2 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H2 receptor expressed in HEK cells
ChEMBL 272 3 2 6 1.0 CCc1cnc2c(N3CC[C@@H](NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
10833949 56880 0 None -2570 3 Guinea pig 4.5 pKi = 4.5 Binding
Binding affinity against H2 receptor of Guinea pig atriumBinding affinity against H2 receptor of Guinea pig atrium
ChEMBL 385 6 2 3 2.9 O=C(NCc1ccc(I)cc1)OCCCc1c[nH]cn1 10.1021/jm9507688
CHEMBL16496 56880 0 None -2570 3 Guinea pig 4.5 pKi = 4.5 Binding
Binding affinity against H2 receptor of Guinea pig atriumBinding affinity against H2 receptor of Guinea pig atrium
ChEMBL 385 6 2 3 2.9 O=C(NCc1ccc(I)cc1)OCCCc1c[nH]cn1 10.1021/jm9507688
10420190 205023 0 None -31 3 Human 4.5 pKi = 4.5 Binding
Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.
ChEMBL 195 8 2 2 2.3 NCCCCCCCCc1c[nH]cn1 10.1021/jm00002a008
CHEMBL90063 205023 0 None -31 3 Human 4.5 pKi = 4.5 Binding
Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.
ChEMBL 195 8 2 2 2.3 NCCCCCCCCc1c[nH]cn1 10.1021/jm00002a008
44304558 100537 0 None -10000 3 Human 4.5 pKi = 4.5 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 374 11 0 4 3.8 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)CC)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL294502 100537 0 None -10000 3 Human 4.5 pKi = 4.5 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 374 11 0 4 3.8 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)CC)CC2)cc1 10.1016/s0960-894x(02)00309-8
44304288 101724 0 None -14791 3 Human 4.5 pKi = 4.5 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 386 11 0 4 3.8 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)C3CC3)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL302886 101724 0 None -14791 3 Human 4.5 pKi = 4.5 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 386 11 0 4 3.8 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)C3CC3)CC2)cc1 10.1016/s0960-894x(02)00309-8
44304451 101807 0 None -1862 3 Human 4.5 pKi = 4.5 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 417 12 1 5 3.3 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](N)C(C)C)CC2)cc1 10.1016/s0960-894x(02)00310-4
CHEMBL303369 101807 0 None -1862 3 Human 4.5 pKi = 4.5 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 417 12 1 5 3.3 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](N)C(C)C)CC2)cc1 10.1016/s0960-894x(02)00310-4
25128822 186888 0 None -5888 5 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]UR-DE257 from human histamine 2 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]UR-DE257 from human histamine 2 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 295 1 1 5 1.6 CN1CCN(c2nc(N)nc3c2CCc2ccccc2-3)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL494093 186888 0 None -5888 5 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]UR-DE257 from human histamine 2 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]UR-DE257 from human histamine 2 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 295 1 1 5 1.6 CN1CCN(c2nc(N)nc3c2CCc2ccccc2-3)CC1 10.1016/j.bmcl.2015.12.035
44281238 112456 0 None - 1 Guinea pig 4.5 pKi = 4.5 Binding
Evaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atriumEvaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atrium
ChEMBL 333 6 4 7 1.4 CN/C(=C\[N+](=O)[O-])Nc1ccc(-c2csc(N=C(N)N)n2)cc1 10.1021/jm00356a005
CHEMBL33108 112456 0 None - 1 Guinea pig 4.5 pKi = 4.5 Binding
Evaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atriumEvaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atrium
ChEMBL 333 6 4 7 1.4 CN/C(=C\[N+](=O)[O-])Nc1ccc(-c2csc(N=C(N)N)n2)cc1 10.1021/jm00356a005
44455426 154598 0 None -346 13 Human 5.5 pKi = 5.5 Binding
Inhibition of human cloned histamine H2 receptor by competitive binding experimentInhibition of human cloned histamine H2 receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL402143 154598 0 None -346 13 Human 5.5 pKi = 5.5 Binding
Inhibition of human cloned histamine H2 receptor by competitive binding experimentInhibition of human cloned histamine H2 receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
71456046 83647 0 None -2089 7 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysisDisplacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysis
ChEMBL 389 6 0 4 4.2 COc1ccccc1N1CCN(Cc2cc(CN(C)C)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207637 83647 0 None -2089 7 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysisDisplacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysis
ChEMBL 389 6 0 4 4.2 COc1ccccc1N1CCN(Cc2cc(CN(C)C)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
44307779 201856 0 None -275 4 Human 5.5 pKi = 5.5 Binding
Compound was tested for its binding affinity towards human H2 receptorCompound was tested for its binding affinity towards human H2 receptor
ChEMBL 332 2 0 2 4.7 C(#Cc1c2c(nc3ccccc13)CCCCC2)CCN1CCCCC1 10.1016/s0960-894x(03)00356-1
CHEMBL66660 201856 0 None -275 4 Human 5.5 pKi = 5.5 Binding
Compound was tested for its binding affinity towards human H2 receptorCompound was tested for its binding affinity towards human H2 receptor
ChEMBL 332 2 0 2 4.7 C(#Cc1c2c(nc3ccccc13)CCCCC2)CCN1CCCCC1 10.1016/s0960-894x(03)00356-1
156015643 177710 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method
ChEMBL 1001 28 3 11 9.2 CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acsmedchemlett.0c00033
CHEMBL4645213 177710 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method
ChEMBL 1001 28 3 11 9.2 CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acsmedchemlett.0c00033
CHEMBL4650968 177710 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method
ChEMBL 1001 28 3 11 9.2 CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acsmedchemlett.0c00033
CHEMBL5092102 213562 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay
ChEMBL None None None NCCCCCCCCNC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1016/j.bmcl.2021.128388
168274129 192197 0 None -6 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 370 12 5 6 1.0 NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5176780 192197 0 None -6 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 370 12 5 6 1.0 NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221468 192197 0 None -6 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 370 12 5 6 1.0 NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
44334212 4546 0 None -72 3 Human 6.5 pKi = 6.5 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 456 11 1 5 3.7 CCc1ccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)cc1 10.1016/s0960-894x(02)00685-6
CHEMBL102925 4546 0 None -72 3 Human 6.5 pKi = 6.5 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 456 11 1 5 3.7 CCc1ccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)cc1 10.1016/s0960-894x(02)00685-6
168273549 192191 0 None 1 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 436 6 4 4 4.3 Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5174342 192191 0 None 1 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 436 6 4 4 4.3 Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5221438 192191 0 None 1 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 436 6 4 4 4.3 Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1 10.1021/acs.jmedchem.1c00692
44335430 5210 0 None -144 3 Human 4.5 pKi = 4.5 Binding
Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor
ChEMBL 374 7 0 5 4.0 CCOC(=O)N1CCN(CCCOc2ccc(-c3cccs3)cc2)CC1 10.1016/s0960-894x(02)00648-0
CHEMBL106602 5210 0 None -144 3 Human 4.5 pKi = 4.5 Binding
Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor
ChEMBL 374 7 0 5 4.0 CCOC(=O)N1CCN(CCCOc2ccc(-c3cccs3)cc2)CC1 10.1016/s0960-894x(02)00648-0
44304064 102324 0 None -1096 3 Human 4.5 pKi = 4.5 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 451 10 2 6 2.5 N[C@H](Cc1ccc(O)cc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL305371 102324 0 None -1096 3 Human 4.5 pKi = 4.5 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 451 10 2 6 2.5 N[C@H](Cc1ccc(O)cc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
164611807 184391 0 None 162 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 376 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)N[C@@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4854278 184391 0 None 162 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 376 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)N[C@@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
122442272 137807 0 None -120 15 Human 5.5 pKi = 5.5 Binding
Binding affinity to histamine H2 receptor (unknown origin) by radioligand binding assayBinding affinity to histamine H2 receptor (unknown origin) by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769968 137807 0 None -120 15 Human 5.5 pKi = 5.5 Binding
Binding affinity to histamine H2 receptor (unknown origin) by radioligand binding assayBinding affinity to histamine H2 receptor (unknown origin) by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771384 137807 0 None -120 15 Human 5.5 pKi = 5.5 Binding
Binding affinity to histamine H2 receptor (unknown origin) by radioligand binding assayBinding affinity to histamine H2 receptor (unknown origin) by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
122442272 137807 0 None -120 15 Human 5.5 pKi = 5.5 Binding
Binding affinity to histamine H2 receptor (unknown origin) by radioligand binding assayBinding affinity to histamine H2 receptor (unknown origin) by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769968 137807 0 None -120 15 Human 5.5 pKi = 5.5 Binding
Binding affinity to histamine H2 receptor (unknown origin) by radioligand binding assayBinding affinity to histamine H2 receptor (unknown origin) by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771384 137807 0 None -120 15 Human 5.5 pKi = 5.5 Binding
Binding affinity to histamine H2 receptor (unknown origin) by radioligand binding assayBinding affinity to histamine H2 receptor (unknown origin) by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
44335336 4475 0 None -263 4 Human 4.5 pKi = 4.5 Binding
Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor
ChEMBL 335 6 1 4 3.4 N#Cc1ccc(-c2ccc(OCCCN3CCC(N)CC3)cc2)cc1 10.1016/s0960-894x(02)00648-0
CHEMBL102452 4475 0 None -263 4 Human 4.5 pKi = 4.5 Binding
Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor
ChEMBL 335 6 1 4 3.4 N#Cc1ccc(-c2ccc(OCCCN3CCC(N)CC3)cc2)cc1 10.1016/s0960-894x(02)00648-0
168268680 192154 0 None 1 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 662 11 8 8 4.8 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5172675 192154 0 None 1 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 662 11 8 8 4.8 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5221210 192154 0 None 1 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 662 11 8 8 4.8 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1 10.1021/acs.jmedchem.1c00692
44304445 201290 0 None -30 3 Human 5.5 pKi = 5.5 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 531 14 1 6 5.3 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](CC(C)C)NC(=O)OC(C)(C)C)CC2)cc1 10.1016/s0960-894x(02)00310-4
CHEMBL63112 201290 0 None -30 3 Human 5.5 pKi = 5.5 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 531 14 1 6 5.3 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](CC(C)C)NC(=O)OC(C)(C)C)CC2)cc1 10.1016/s0960-894x(02)00310-4
44304462 201184 0 None -4897 3 Human 4.5 pKi = 4.5 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 405 12 2 6 1.7 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](N)CO)CC2)cc1 10.1016/s0960-894x(02)00310-4
CHEMBL62660 201184 0 None -4897 3 Human 4.5 pKi = 4.5 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 405 12 2 6 1.7 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](N)CO)CC2)cc1 10.1016/s0960-894x(02)00310-4
44304741 201219 0 None -3388 3 Human 4.5 pKi = 4.5 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 466 13 1 6 3.3 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](N)Cc3ccncc3)CC2)cc1 10.1016/s0960-894x(02)00310-4
CHEMBL62808 201219 0 None -3388 3 Human 4.5 pKi = 4.5 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 466 13 1 6 3.3 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](N)Cc3ccncc3)CC2)cc1 10.1016/s0960-894x(02)00310-4
73355417 92093 0 None 1 3 Human 5.5 pKi = 5.5 Binding
Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay
ChEMBL 251 3 1 1 2.9 c1ccc(CN[C@H]2C3C4CC5C6C4CC3C6C52)cc1 10.1016/j.bmc.2013.07.045
CHEMBL2432045 92093 0 None 1 3 Human 5.5 pKi = 5.5 Binding
Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay
ChEMBL 251 3 1 1 2.9 c1ccc(CN[C@H]2C3C4CC5C6C4CC3C6C52)cc1 10.1016/j.bmc.2013.07.045
237 203147 43 None -3 13 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
CHEMBL546257 203147 43 None -3 13 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
CHEMBL554190 203147 43 None -3 13 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
CHEMBL7568 203147 43 None -3 13 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
164614841 184682 0 None 223 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 388 7 4 4 3.0 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(c1ccccc1)C(C)C 10.1016/j.ejmech.2021.113190
CHEMBL4858849 184682 0 None 223 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 388 7 4 4 3.0 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(c1ccccc1)C(C)C 10.1016/j.ejmech.2021.113190
44333988 4452 0 None -93 3 Human 5.5 pKi = 5.5 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 367 8 1 5 2.6 CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)c3cccnc3)C2)cc1 10.1016/s0960-894x(02)00685-6
CHEMBL102331 4452 0 None -93 3 Human 5.5 pKi = 5.5 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 367 8 1 5 2.6 CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)c3cccnc3)C2)cc1 10.1016/s0960-894x(02)00685-6
156013896 177655 0 None -1548 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human recombinant H2R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]UR-DE257 from Gsalphas-coupled human recombinant H2R expressed in baculovirus infected Sf9 insect cell membranes
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4635634 177655 0 None -1548 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human recombinant H2R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]UR-DE257 from Gsalphas-coupled human recombinant H2R expressed in baculovirus infected Sf9 insect cell membranes
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4650570 177655 0 None -1548 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human recombinant H2R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]UR-DE257 from Gsalphas-coupled human recombinant H2R expressed in baculovirus infected Sf9 insect cell membranes
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
135398737 942 89 None -64 92 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
38 942 89 None -64 92 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
722 942 89 None -64 92 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
CHEMBL42 942 89 None -64 92 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
DB00363 942 89 None -64 92 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
71455894 83374 0 None -3 12 Human 5.5 pKi = 5.5 Binding
Binding affinity to Histamine H2 receptorBinding affinity to Histamine H2 receptor
ChEMBL 325 4 1 4 2.0 COc1ccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1OC 10.1016/j.bmcl.2012.08.046
CHEMBL2205827 83374 0 None -3 12 Human 5.5 pKi = 5.5 Binding
Binding affinity to Histamine H2 receptorBinding affinity to Histamine H2 receptor
ChEMBL 325 4 1 4 2.0 COc1ccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1OC 10.1016/j.bmcl.2012.08.046
71455894 83374 0 None -3 12 Human 5.5 pKi = 5.5 Binding
Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay
ChEMBL 325 4 1 4 2.0 COc1ccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1OC 10.1016/j.bmc.2013.07.045
CHEMBL2205827 83374 0 None -3 12 Human 5.5 pKi = 5.5 Binding
Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay
ChEMBL 325 4 1 4 2.0 COc1ccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1OC 10.1016/j.bmc.2013.07.045
44335407 171268 0 None -15 3 Human 5.4 pKi = 5.4 Binding
Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor
ChEMBL 452 8 0 5 4.8 CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc(OC(F)(F)F)cc3)cc2)CC1 10.1016/s0960-894x(02)00648-0
CHEMBL446885 171268 0 None -15 3 Human 5.4 pKi = 5.4 Binding
Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor
ChEMBL 452 8 0 5 4.8 CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc(OC(F)(F)F)cc3)cc2)CC1 10.1016/s0960-894x(02)00648-0
26987 934 29 None -177 21 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
6063 934 29 None -177 21 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
671 934 29 None -177 21 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
CHEMBL1626 934 29 None -177 21 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
DB00283 934 29 None -177 21 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
155513890 169243 0 None -177 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells after 90 mins by scintillation counting methodDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells after 90 mins by scintillation counting method
ChEMBL 369 2 2 5 4.1 Clc1ccc(C#Cc2nc(N[C@H]3C[C@H]4CC[C@@H]3C4)c3nc[nH]c3n2)s1 10.1039/C8MD00317C
CHEMBL4439593 169243 0 None -177 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells after 90 mins by scintillation counting methodDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells after 90 mins by scintillation counting method
ChEMBL 369 2 2 5 4.1 Clc1ccc(C#Cc2nc(N[C@H]3C[C@H]4CC[C@@H]3C4)c3nc[nH]c3n2)s1 10.1039/C8MD00317C
126720252 164112 0 None -12 12 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-Iodoaminopotentidine from human histamine H2 receptor expressed in HEK293T cell membranes after 90 mins by scintillation counting methodDisplacement of [125I]-Iodoaminopotentidine from human histamine H2 receptor expressed in HEK293T cell membranes after 90 mins by scintillation counting method
ChEMBL 697 15 2 6 9.2 NCCCCCCn1cc(CCCCN2CCC(c3ccc(-c4cc(C(=O)O)cc5cc(-c6ccc(C(F)(F)F)cc6)ccc45)cc3)CC2)nn1 10.1021/acs.jmedchem.8b00168
CHEMBL4216870 164112 0 None -12 12 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-Iodoaminopotentidine from human histamine H2 receptor expressed in HEK293T cell membranes after 90 mins by scintillation counting methodDisplacement of [125I]-Iodoaminopotentidine from human histamine H2 receptor expressed in HEK293T cell membranes after 90 mins by scintillation counting method
ChEMBL 697 15 2 6 9.2 NCCCCCCn1cc(CCCCN2CCC(c3ccc(-c4cc(C(=O)O)cc5cc(-c6ccc(C(F)(F)F)cc6)ccc45)cc3)CC2)nn1 10.1021/acs.jmedchem.8b00168
164618283 183951 0 None 158 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 390 7 4 5 2.4 COc1ccc(C(C)NC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1 10.1016/j.ejmech.2021.113190
CHEMBL4848026 183951 0 None 158 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 390 7 4 5 2.4 COc1ccc(C(C)NC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1 10.1016/j.ejmech.2021.113190
44304282 201414 0 None -12 3 Human 5.4 pKi = 5.4 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 410 8 0 5 3.8 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)c3cccc(C)c3)cc2)CC1 10.1016/s0960-894x(02)00309-8
CHEMBL64021 201414 0 None -12 3 Human 5.4 pKi = 5.4 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 410 8 0 5 3.8 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)c3cccc(C)c3)cc2)CC1 10.1016/s0960-894x(02)00309-8
44304383 201603 0 None -371 3 Human 5.4 pKi = 5.4 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 418 12 0 5 4.6 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OCC(C)C)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL64775 201603 0 None -371 3 Human 5.4 pKi = 5.4 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 418 12 0 5 4.6 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OCC(C)C)CC2)cc1 10.1016/s0960-894x(02)00309-8
44304753 201496 0 None -4073 3 Human 4.4 pKi = 4.4 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 466 13 1 6 3.3 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](N)Cc3ccncc3)CC2)cc1 10.1016/s0960-894x(02)00310-4
CHEMBL64321 201496 0 None -4073 3 Human 4.4 pKi = 4.4 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 466 13 1 6 3.3 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](N)Cc3ccncc3)CC2)cc1 10.1016/s0960-894x(02)00310-4
9818650 201822 0 None -1513 4 Human 5.4 pKi = 5.4 Binding
Compound was tested for its binding affinity towards human H2 receptorCompound was tested for its binding affinity towards human H2 receptor
ChEMBL 323 5 1 3 4.4 c1ccc2c(NCCCN3CCCC3)c3c(nc2c1)CCCCC3 10.1016/s0960-894x(03)00356-1
CHEMBL66388 201822 0 None -1513 4 Human 5.4 pKi = 5.4 Binding
Compound was tested for its binding affinity towards human H2 receptorCompound was tested for its binding affinity towards human H2 receptor
ChEMBL 323 5 1 3 4.4 c1ccc2c(NCCCN3CCCC3)c3c(nc2c1)CCCCC3 10.1016/s0960-894x(03)00356-1
CHEMBL4777443 212276 0 None -181 14 Human 5.4 pKi = 5.4 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000741a HRH2Selectivity interaction (GPCR panel (PDSP screen)) EUB0000741a HRH2
ChEMBL None None None CC(C)(C)OC(=O)N1CCCC1CN[C@H]1CC[C@@](c2cc(F)ccc2F)(S(=O)(=O)c2ccc(Cl)cc2)CC1 nan
44334782 5338 0 None -91 3 Human 6.4 pKi = 6.4 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 442 10 1 5 3.4 Cc1ccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)cc1 10.1016/s0960-894x(02)00685-6
CHEMBL107293 5338 0 None -91 3 Human 6.4 pKi = 6.4 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 442 10 1 5 3.4 Cc1ccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)cc1 10.1016/s0960-894x(02)00685-6
168276867 192223 0 None -1 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 662 11 8 8 4.8 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5174278 192223 0 None -1 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 662 11 8 8 4.8 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5221653 192223 0 None -1 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 662 11 8 8 4.8 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)c1 10.1021/acs.jmedchem.1c00692
44335571 5185 0 None -1513 4 Human 4.4 pKi = 4.4 Binding
Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor
ChEMBL 322 6 0 4 3.3 N#Cc1ccc(-c2ccc(OCCCN3CCOCC3)cc2)cc1 10.1016/s0960-894x(02)00648-0
CHEMBL106483 5185 0 None -1513 4 Human 4.4 pKi = 4.4 Binding
Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor
ChEMBL 322 6 0 4 3.3 N#Cc1ccc(-c2ccc(OCCCN3CCOCC3)cc2)cc1 10.1016/s0960-894x(02)00648-0
44304450 201170 0 None -478 3 Human 4.4 pKi = 4.4 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 417 12 1 5 3.3 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](N)C(C)C)CC2)cc1 10.1016/s0960-894x(02)00310-4
CHEMBL62592 201170 0 None -478 3 Human 4.4 pKi = 4.4 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 417 12 1 5 3.3 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](N)C(C)C)CC2)cc1 10.1016/s0960-894x(02)00310-4
168283097 192281 0 None -22 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 311 9 4 5 0.8 CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)o1 10.1021/acs.jmedchem.1c00692
CHEMBL5186770 192281 0 None -22 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 311 9 4 5 0.8 CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)o1 10.1021/acs.jmedchem.1c00692
CHEMBL5222043 192281 0 None -22 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 311 9 4 5 0.8 CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)o1 10.1021/acs.jmedchem.1c00692
168284480 192298 0 None -22 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 330 6 4 4 1.3 Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCc1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5197548 192298 0 None -22 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 330 6 4 4 1.3 Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCc1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222137 192298 0 None -22 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 330 6 4 4 1.3 Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCc1ccccc1 10.1021/acs.jmedchem.1c00692
73346334 92095 0 None -4 7 Human 5.4 pKi = 5.4 Binding
Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay
ChEMBL 265 4 1 1 3.0 c1ccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)cc1 10.1016/j.bmc.2013.07.045
CHEMBL2432048 92095 0 None -4 7 Human 5.4 pKi = 5.4 Binding
Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay
ChEMBL 265 4 1 1 3.0 c1ccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)cc1 10.1016/j.bmc.2013.07.045
164608815 183862 0 None 1 6 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 380 7 4 4 2.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1 10.1016/j.ejmech.2021.113190
CHEMBL4846638 183862 0 None 1 6 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 380 7 4 4 2.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1 10.1016/j.ejmech.2021.113190
4011 81982 43 None -27 24 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
CHEMBL21731 81982 43 None -27 24 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
136002184 99211 0 None - 1 Guinea pig 6.4 pKi = 6.4 Binding
Evaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atriumEvaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atrium
ChEMBL 362 5 4 8 2.0 CNc1n[s+]([O-])nc1Nc1cccc(-c2csc(N=C(N)N)n2)c1 10.1021/jm00356a005
44281474 99211 0 None - 1 Guinea pig 6.4 pKi = 6.4 Binding
Evaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atriumEvaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atrium
ChEMBL 362 5 4 8 2.0 CNc1n[s+]([O-])nc1Nc1cccc(-c2csc(N=C(N)N)n2)c1 10.1021/jm00356a005
CHEMBL284556 99211 0 None - 1 Guinea pig 6.4 pKi = 6.4 Binding
Evaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atriumEvaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atrium
ChEMBL 362 5 4 8 2.0 CNc1n[s+]([O-])nc1Nc1cccc(-c2csc(N=C(N)N)n2)c1 10.1021/jm00356a005
10588560 96113 0 None -165 3 Guinea pig 5.4 pKi = 5.4 Binding
Binding affinity against H2 receptor of Guinea pig atriumBinding affinity against H2 receptor of Guinea pig atrium
ChEMBL 277 6 2 3 2.4 O=C(NCc1ccc(F)cc1)OCCCc1c[nH]cn1 10.1021/jm9507688
CHEMBL263070 96113 0 None -165 3 Guinea pig 5.4 pKi = 5.4 Binding
Binding affinity against H2 receptor of Guinea pig atriumBinding affinity against H2 receptor of Guinea pig atrium
ChEMBL 277 6 2 3 2.4 O=C(NCc1ccc(F)cc1)OCCCc1c[nH]cn1 10.1021/jm9507688
44335237 5037 0 None -144 3 Human 5.4 pKi = 5.4 Binding
Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor
ChEMBL 407 7 0 5 4.1 CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc(C#N)cc3C)cc2)CC1 10.1016/s0960-894x(02)00648-0
CHEMBL105669 5037 0 None -144 3 Human 5.4 pKi = 5.4 Binding
Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor
ChEMBL 407 7 0 5 4.1 CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc(C#N)cc3C)cc2)CC1 10.1016/s0960-894x(02)00648-0
3032915 15306 20 None -25 7 Human 5.4 pKi = 5.4 Binding
Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors
ChEMBL 212 5 3 2 1.2 C/N=C(\S)NCCCCc1c[nH]cn1 10.1021/jm00012a025
CHEMBL12160 15306 20 None -25 7 Human 5.4 pKi = 5.4 Binding
Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors
ChEMBL 212 5 3 2 1.2 C/N=C(\S)NCCCCc1c[nH]cn1 10.1021/jm00012a025
10085839 202787 0 None -125 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors
ChEMBL 294 7 3 2 2.9 S=C(NCCCCCc1c[nH]cn1)NC1CCCCC1 10.1021/jm00012a025
CHEMBL72571 202787 0 None -125 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors
ChEMBL 294 7 3 2 2.9 S=C(NCCCCCc1c[nH]cn1)NC1CCCCC1 10.1021/jm00012a025
3032915 15306 20 None -25 7 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells
ChEMBL 212 5 3 2 1.2 C/N=C(\S)NCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL12160 15306 20 None -25 7 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells
ChEMBL 212 5 3 2 1.2 C/N=C(\S)NCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
164619427 185477 0 None 7 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 380 5 4 4 3.1 N/C(=N\C(=O)NCCc1ccccc1)Nc1cccc(-c2csc(N)n2)c1 10.1016/j.ejmech.2021.113190
CHEMBL4871221 185477 0 None 7 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 380 5 4 4 3.1 N/C(=N\C(=O)NCCc1ccccc1)Nc1cccc(-c2csc(N)n2)c1 10.1016/j.ejmech.2021.113190
10358195 57143 0 None -2570 3 Guinea pig 4.4 pKi = 4.4 Binding
Binding affinity against H2 receptor of Guinea pig atriumBinding affinity against H2 receptor of Guinea pig atrium
ChEMBL 313 5 2 3 3.6 O=C(Nc1ccc(C(F)(F)F)cc1)OCCCc1c[nH]cn1 10.1021/jm9507688
CHEMBL16565 57143 0 None -2570 3 Guinea pig 4.4 pKi = 4.4 Binding
Binding affinity against H2 receptor of Guinea pig atriumBinding affinity against H2 receptor of Guinea pig atrium
ChEMBL 313 5 2 3 3.6 O=C(Nc1ccc(C(F)(F)F)cc1)OCCCc1c[nH]cn1 10.1021/jm9507688
10660952 97659 0 None -602 3 Guinea pig 4.4 pKi = 4.4 Binding
Binding affinity against H2 receptor of Guinea pig atriumBinding affinity against H2 receptor of Guinea pig atrium
ChEMBL 287 7 1 3 3.0 CCN(Cc1ccccc1)C(=O)OCCCc1c[nH]cn1 10.1021/jm9507688
CHEMBL273549 97659 0 None -602 3 Guinea pig 4.4 pKi = 4.4 Binding
Binding affinity against H2 receptor of Guinea pig atriumBinding affinity against H2 receptor of Guinea pig atrium
ChEMBL 287 7 1 3 3.0 CCN(Cc1ccccc1)C(=O)OCCCc1c[nH]cn1 10.1021/jm9507688
1204 1893 114 None -173 25 Human 4.4 pKi = 4.4 Binding
Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm00002a008
1247 1893 114 None -173 25 Human 4.4 pKi = 4.4 Binding
Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm00002a008
1375 1893 114 None -173 25 Human 4.4 pKi = 4.4 Binding
Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm00002a008
774 1893 114 None -173 25 Human 4.4 pKi = 4.4 Binding
Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm00002a008
CHEMBL90 1893 114 None -173 25 Human 4.4 pKi = 4.4 Binding
Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm00002a008
DB05381 1893 114 None -173 25 Human 4.4 pKi = 4.4 Binding
Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm00002a008
44304387 201230 0 None -7943 3 Human 4.4 pKi = 4.4 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 334 7 0 5 2.4 CCOC(=O)N1CCN(CCCOc2ccc(C(C)=O)cc2)CC1 10.1016/s0960-894x(02)00309-8
CHEMBL62840 201230 0 None -7943 3 Human 4.4 pKi = 4.4 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 334 7 0 5 2.4 CCOC(=O)N1CCN(CCCOc2ccc(C(C)=O)cc2)CC1 10.1016/s0960-894x(02)00309-8
44304312 162225 0 None -1348 3 Human 4.4 pKi = 4.4 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 453 10 1 5 2.9 N[C@H](Cc1ccc(F)cc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL417215 162225 0 None -1348 3 Human 4.4 pKi = 4.4 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 453 10 1 5 2.9 N[C@H](Cc1ccc(F)cc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
44281484 109850 0 None - 1 Guinea pig 4.4 pKi = 4.4 Binding
Evaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atriumEvaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atrium
ChEMBL 254 2 3 3 1.9 C/N=C(\NC#N)Nc1cccc(-c2[nH]cnc2C)c1 10.1021/jm00356a005
CHEMBL32409 109850 0 None - 1 Guinea pig 4.4 pKi = 4.4 Binding
Evaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atriumEvaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atrium
ChEMBL 254 2 3 3 1.9 C/N=C(\NC#N)Nc1cccc(-c2[nH]cnc2C)c1 10.1021/jm00356a005
164612037 184785 0 None -85 20 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1016/j.ejmech.2021.113190
CHEMBL4860528 184785 0 None -85 20 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1016/j.ejmech.2021.113190
46884734 7875 0 None -6 2 Human 8.4 pKi = 8.4 Binding
Inhibition of H2 receptorInhibition of H2 receptor
ChEMBL 341 6 0 4 3.7 COc1nccnc1[C@H](C)C1=C(CCN(C)C)Cc2cc(F)ccc21 10.1016/j.bmcl.2010.07.117
CHEMBL1090526 7875 0 None -6 2 Human 8.4 pKi = 8.4 Binding
Inhibition of H2 receptorInhibition of H2 receptor
ChEMBL 341 6 0 4 3.7 COc1nccnc1[C@H](C)C1=C(CCN(C)C)Cc2cc(F)ccc21 10.1016/j.bmcl.2010.07.117
168273471 192189 0 None 12 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 596 17 8 10 0.7 N/C(=N\C(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5173079 192189 0 None 12 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 596 17 8 10 0.7 N/C(=N\C(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221433 192189 0 None 12 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 596 17 8 10 0.7 N/C(=N\C(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
71452382 83366 0 None -12 10 Human 6.4 pKi = 6.4 Binding
Binding affinity to Histamine H2 receptorBinding affinity to Histamine H2 receptor
ChEMBL 309 4 1 3 2.0 COc1ccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1 10.1016/j.bmcl.2012.08.046
CHEMBL2205812 83366 0 None -12 10 Human 6.4 pKi = 6.4 Binding
Binding affinity to Histamine H2 receptorBinding affinity to Histamine H2 receptor
ChEMBL 309 4 1 3 2.0 COc1ccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1 10.1016/j.bmcl.2012.08.046
44334035 109543 0 None -79 3 Human 5.4 pKi = 5.4 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 476 10 1 7 4.1 O=C(N[C@H]1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)C1)c1csc(-c2cccnc2)n1 10.1016/s0960-894x(02)00685-6
CHEMBL323517 109543 0 None -79 3 Human 5.4 pKi = 5.4 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 476 10 1 7 4.1 O=C(N[C@H]1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)C1)c1csc(-c2cccnc2)n1 10.1016/s0960-894x(02)00685-6
44334281 4676 0 None -128 3 Human 4.4 pKi = 4.4 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 433 9 2 6 2.8 CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)[C@@H](C)NC(=O)OC(C)(C)C)C2)cc1 10.1016/s0960-894x(02)00685-6
CHEMBL103828 4676 0 None -128 3 Human 4.4 pKi = 4.4 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 433 9 2 6 2.8 CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)[C@@H](C)NC(=O)OC(C)(C)C)C2)cc1 10.1016/s0960-894x(02)00685-6
145980875 166143 0 None -3 11 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assay
ChEMBL 443 7 1 2 6.2 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCCc2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL4282702 166143 0 None -3 11 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assay
ChEMBL 443 7 1 2 6.2 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCCc2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
1530 2142 44 None -151 21 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
3827 2142 44 None -151 21 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
7206 2142 44 None -151 21 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
CHEMBL534 2142 44 None -151 21 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
DB00920 2142 44 None -151 21 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
CHEMBL5090859 213499 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCCC[n+]1c(C)cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc1C 10.1016/j.bmcl.2021.128388
44478385 5684 2 None -70 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]tiotidine from human histamine H2 receptor expressed in Sf9 cellsDisplacement of [3H]tiotidine from human histamine H2 receptor expressed in Sf9 cells
ChEMBL 342 9 3 4 2.5 N#C/N=C(/NCCCCc1c[nH]cn1)NCCSc1ccccc1 10.1021/jm900526h
CHEMBL1078642 5684 2 None -70 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]tiotidine from human histamine H2 receptor expressed in Sf9 cellsDisplacement of [3H]tiotidine from human histamine H2 receptor expressed in Sf9 cells
ChEMBL 342 9 3 4 2.5 N#C/N=C(/NCCCCc1c[nH]cn1)NCCSc1ccccc1 10.1021/jm900526h
44304012 201135 0 None -21379 3 Human 4.4 pKi = 4.4 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 389 11 1 5 2.7 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](C)N)CC2)cc1 10.1016/s0960-894x(02)00310-4
CHEMBL62421 201135 0 None -21379 3 Human 4.4 pKi = 4.4 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 389 11 1 5 2.7 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](C)N)CC2)cc1 10.1016/s0960-894x(02)00310-4
1129 1584 89 None 1 2 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N nan
3325 1584 89 None 1 2 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N nan
5353622 1584 89 None 1 2 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N nan
5702160 1584 89 None 1 2 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N nan
7074 1584 89 None 1 2 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N nan
CHEMBL902 1584 89 None 1 2 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N nan
DB00927 1584 89 None 1 2 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N nan
12016525 201217 0 None -2041 3 Human 4.4 pKi = 4.4 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 359 8 1 5 1.5 C[C@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL62804 201217 0 None -2041 3 Human 4.4 pKi = 4.4 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 359 8 1 5 1.5 C[C@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
71457844 83648 0 None -2187 7 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysisDisplacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysis
ChEMBL 429 6 0 4 5.1 COc1ccccc1N1CCN(Cc2cc(CN3CCCCC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207638 83648 0 None -2187 7 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysisDisplacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysis
ChEMBL 429 6 0 4 5.1 COc1ccccc1N1CCN(Cc2cc(CN3CCCCC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
50878551 90300 60 None -109 18 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]Tiotidine from human recombinant histamine H2 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]Tiotidine from human recombinant histamine H2 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2013.03.066
CHEMBL2391541 90300 60 None -109 18 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]Tiotidine from human recombinant histamine H2 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]Tiotidine from human recombinant histamine H2 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2013.03.066
164608941 183791 0 None 75 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 390 7 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NC[C@@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4845733 183791 0 None 75 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 390 7 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NC[C@@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
50878551 90300 60 None -109 18 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]Tiotidine from human recombinant histamine H2 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]Tiotidine from human recombinant histamine H2 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2013.03.066
CHEMBL2391541 90300 60 None -109 18 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]Tiotidine from human recombinant histamine H2 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]Tiotidine from human recombinant histamine H2 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2013.03.066
44304309 168639 0 None -630 3 Human 4.4 pKi = 4.4 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 414 8 0 5 3.6 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)c3ccc(F)cc3)cc2)CC1 10.1016/s0960-894x(02)00309-8
CHEMBL440864 168639 0 None -630 3 Human 4.4 pKi = 4.4 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 414 8 0 5 3.6 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)c3ccc(F)cc3)cc2)CC1 10.1016/s0960-894x(02)00309-8
164627020 185816 0 None 144 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 422 7 4 4 3.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4876025 185816 0 None 144 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 422 7 4 4 3.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2021.113190
53324553 56545 0 None -6 10 Human 5.4 pKi = 5.4 Binding
Inhibition of H2 receptorInhibition of H2 receptor
ChEMBL 283 4 1 1 3.1 Fc1cccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)c1 10.1016/j.bmcl.2010.11.075
CHEMBL1643900 56545 0 None -6 10 Human 5.4 pKi = 5.4 Binding
Inhibition of H2 receptorInhibition of H2 receptor
ChEMBL 283 4 1 1 3.1 Fc1cccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)c1 10.1016/j.bmcl.2010.11.075
53324553 56545 0 None -6 10 Human 5.4 pKi = 5.4 Binding
Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay
ChEMBL 283 4 1 1 3.1 Fc1cccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)c1 10.1016/j.bmc.2013.07.045
CHEMBL1643900 56545 0 None -6 10 Human 5.4 pKi = 5.4 Binding
Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay
ChEMBL 283 4 1 1 3.1 Fc1cccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)c1 10.1016/j.bmc.2013.07.045
53325861 56546 0 None -2 3 Human 5.4 pKi = 5.4 Binding
Inhibition of H2 receptorInhibition of H2 receptor
ChEMBL 297 4 0 1 3.4 CN(CCc1cccc(F)c1)[C@H]1C2C3CC4C5C3CC2C5C41 10.1016/j.bmcl.2010.11.075
CHEMBL1643902 56546 0 None -2 3 Human 5.4 pKi = 5.4 Binding
Inhibition of H2 receptorInhibition of H2 receptor
ChEMBL 297 4 0 1 3.4 CN(CCc1cccc(F)c1)[C@H]1C2C3CC4C5C3CC2C5C41 10.1016/j.bmcl.2010.11.075
53325861 56546 0 None -2 3 Human 5.4 pKi = 5.4 Binding
Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay
ChEMBL 297 4 0 1 3.4 CN(CCc1cccc(F)c1)[C@H]1C2C3CC4C5C3CC2C5C41 10.1016/j.bmc.2013.07.045
CHEMBL1643902 56546 0 None -2 3 Human 5.4 pKi = 5.4 Binding
Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay
ChEMBL 297 4 0 1 3.4 CN(CCc1cccc(F)c1)[C@H]1C2C3CC4C5C3CC2C5C41 10.1016/j.bmc.2013.07.045
44304449 198805 0 None -309 3 Human 5.4 pKi = 5.4 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 531 14 1 6 5.3 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](CC(C)C)NC(=O)OC(C)(C)C)CC2)cc1 10.1016/s0960-894x(02)00310-4
CHEMBL59870 198805 0 None -309 3 Human 5.4 pKi = 5.4 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 531 14 1 6 5.3 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](CC(C)C)NC(=O)OC(C)(C)C)CC2)cc1 10.1016/s0960-894x(02)00310-4
164626509 185743 0 None 3 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 358 3 4 4 3.2 N/C(=N\C(=O)NC1CCCCC1)Nc1cccc(-c2csc(N)n2)c1 10.1016/j.ejmech.2021.113190
CHEMBL4874969 185743 0 None 3 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 358 3 4 4 3.2 N/C(=N\C(=O)NC1CCCCC1)Nc1cccc(-c2csc(N)n2)c1 10.1016/j.ejmech.2021.113190
168280339 192253 0 None -52 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 372 8 3 5 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCn1cc(CN(C)C)nn1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5188592 192253 0 None -52 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 372 8 3 5 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCn1cc(CN(C)C)nn1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5221885 192253 0 None -52 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 372 8 3 5 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCn1cc(CN(C)C)nn1)c1ccccc1 10.1021/acs.jmedchem.1c00692
168294166 192402 0 None 1 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 360 6 4 4 3.3 CCCCCNC(=O)/N=C(\N)Nc1ccc(-c2sc(N)nc2C)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5209081 192402 0 None 1 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 360 6 4 4 3.3 CCCCCNC(=O)/N=C(\N)Nc1ccc(-c2sc(N)nc2C)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222775 192402 0 None 1 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 360 6 4 4 3.3 CCCCCNC(=O)/N=C(\N)Nc1ccc(-c2sc(N)nc2C)cc1 10.1021/acs.jmedchem.1c00692
44304014 100305 0 None -5370 3 Human 4.3 pKi = 4.3 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 431 10 1 6 2.3 CC(C)(C)OC[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL293033 100305 0 None -5370 3 Human 4.3 pKi = 4.3 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 431 10 1 6 2.3 CC(C)(C)OC[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
164622153 184976 0 None 95 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 394 6 4 4 3.0 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(Cl)cc1 10.1016/j.ejmech.2021.113190
CHEMBL4863347 184976 0 None 95 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 394 6 4 4 3.0 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(Cl)cc1 10.1016/j.ejmech.2021.113190
71459761 83652 0 None -75 7 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysisDisplacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysis
ChEMBL 540 7 0 5 6.1 COc1ccccc1N1CCN(Cc2cc(CN3CCN(c4ccc(Cl)cc4)CC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207642 83652 0 None -75 7 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysisDisplacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysis
ChEMBL 540 7 0 5 6.1 COc1ccccc1N1CCN(Cc2cc(CN3CCN(c4ccc(Cl)cc4)CC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
44334556 106770 0 None -77 3 Human 4.3 pKi = 4.3 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 449 10 3 7 1.7 CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)[C@H](CO)NC(=O)OC(C)(C)C)C2)cc1 10.1016/s0960-894x(02)00685-6
CHEMBL316968 106770 0 None -77 3 Human 4.3 pKi = 4.3 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 449 10 3 7 1.7 CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)[C@H](CO)NC(=O)OC(C)(C)C)C2)cc1 10.1016/s0960-894x(02)00685-6
44304377 201080 0 None -2570 3 Human 4.3 pKi = 4.3 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 424 11 0 6 3.5 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3cnccn3)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL62115 201080 0 None -2570 3 Human 4.3 pKi = 4.3 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 424 11 0 6 3.5 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3cnccn3)CC2)cc1 10.1016/s0960-894x(02)00309-8
44304313 199890 0 None -2041 3 Human 4.3 pKi = 4.3 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 441 10 1 6 2.8 N[C@H](Cc1ccsc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL60559 199890 0 None -2041 3 Human 4.3 pKi = 4.3 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 441 10 1 6 2.8 N[C@H](Cc1ccsc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
44304277 100467 0 None -645 3 Human 4.3 pKi = 4.3 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 401 10 1 5 2.4 CN[C@@H](C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1)C(C)C 10.1016/s0960-894x(02)00310-4
CHEMBL294087 100467 0 None -645 3 Human 4.3 pKi = 4.3 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 401 10 1 5 2.4 CN[C@@H](C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1)C(C)C 10.1016/s0960-894x(02)00310-4
1231 922 112 None -2 8 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/acs.jmedchem.6b01422
2756 922 112 None -2 8 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/acs.jmedchem.6b01422
645 922 112 None -2 8 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/acs.jmedchem.6b01422
CHEMBL30 922 112 None -2 8 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/acs.jmedchem.6b01422
DB00501 922 112 None -2 8 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/acs.jmedchem.6b01422
44467360 124002 0 None 3 2 Human 5.3 pKi = 5.3 Binding
Inhibition of human histamine H2 receptorInhibition of human histamine H2 receptor
ChEMBL 420 3 2 6 1.5 COc1nc(N2C[C@H]3C(=O)N(C)C(=N)N[C@@]3(c3ccc(F)cc3F)C2)nc(C)c1F 10.1021/acs.jmedchem.5b01995
CHEMBL3640290 124002 0 None 3 2 Human 5.3 pKi = 5.3 Binding
Inhibition of human histamine H2 receptorInhibition of human histamine H2 receptor
ChEMBL 420 3 2 6 1.5 COc1nc(N2C[C@H]3C(=O)N(C)C(=N)N[C@@]3(c3ccc(F)cc3F)C2)nc(C)c1F 10.1021/acs.jmedchem.5b01995
168295528 192419 0 None -147 20 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5206565 192419 0 None -147 20 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222872 192419 0 None -147 20 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
168290815 192361 0 None -537 6 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 327 9 4 5 1.2 CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5200771 192361 0 None -537 6 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 327 9 4 5 1.2 CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222529 192361 0 None -537 6 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 327 9 4 5 1.2 CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
168273640 192193 0 None -6 6 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 568 15 8 10 -0.1 N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5176229 192193 0 None -6 6 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 568 15 8 10 -0.1 N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221444 192193 0 None -6 6 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 568 15 8 10 -0.1 N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
15179520 102193 0 None - 1 Guinea pig 8.3 pKi = 8.3 Binding
Inhibition of [125I]APT binding to H2 receptors in guinea pig cerebral membranes.Inhibition of [125I]APT binding to H2 receptors in guinea pig cerebral membranes.
ChEMBL 602 12 3 5 3.9 N#CN/C(=N\CCNC(=O)c1cccc(I)c1)NCCCCOc1cccc(CN2CCCCC2)c1 10.1021/jm00090a013
CHEMBL304608 102193 0 None - 1 Guinea pig 8.3 pKi = 8.3 Binding
Inhibition of [125I]APT binding to H2 receptors in guinea pig cerebral membranes.Inhibition of [125I]APT binding to H2 receptors in guinea pig cerebral membranes.
ChEMBL 602 12 3 5 3.9 N#CN/C(=N\CCNC(=O)c1cccc(I)c1)NCCCCOc1cccc(CN2CCCCC2)c1 10.1021/jm00090a013
1235 3751 32 None 1 5 Guinea pig 8.3 pKi = 8.3 Binding
Inhibition of [125I]APT binding to H2 receptors in guinea pig cerebral membranes.Inhibition of [125I]APT binding to H2 receptors in guinea pig cerebral membranes.
ChEMBL 312 6 4 6 -0.1 N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N 10.1021/jm00090a013
3959 3751 32 None 1 5 Guinea pig 8.3 pKi = 8.3 Binding
Inhibition of [125I]APT binding to H2 receptors in guinea pig cerebral membranes.Inhibition of [125I]APT binding to H2 receptors in guinea pig cerebral membranes.
ChEMBL 312 6 4 6 -0.1 N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N 10.1021/jm00090a013
50287 3751 32 None 1 5 Guinea pig 8.3 pKi = 8.3 Binding
Inhibition of [125I]APT binding to H2 receptors in guinea pig cerebral membranes.Inhibition of [125I]APT binding to H2 receptors in guinea pig cerebral membranes.
ChEMBL 312 6 4 6 -0.1 N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N 10.1021/jm00090a013
CHEMBL269646 3751 32 None 1 5 Guinea pig 8.3 pKi = 8.3 Binding
Inhibition of [125I]APT binding to H2 receptors in guinea pig cerebral membranes.Inhibition of [125I]APT binding to H2 receptors in guinea pig cerebral membranes.
ChEMBL 312 6 4 6 -0.1 N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N 10.1021/jm00090a013
46780481 107032 18 None -21 54 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1016/j.bmcl.2013.12.024
9903970 107032 18 None -21 54 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1016/j.bmcl.2013.12.024
CHEMBL3187365 107032 18 None -21 54 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1016/j.bmcl.2013.12.024
CHEMBL3544974 107032 18 None -21 54 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1016/j.bmcl.2013.12.024
46780481 107032 18 None -21 54 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1016/j.bmcl.2013.12.024
9903970 107032 18 None -21 54 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1016/j.bmcl.2013.12.024
CHEMBL3187365 107032 18 None -21 54 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1016/j.bmcl.2013.12.024
CHEMBL3544974 107032 18 None -21 54 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1016/j.bmcl.2013.12.024
44334395 4877 0 None -144 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 446 10 1 5 3.2 O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccc(F)cc3)C2)cc1)C1CC1 10.1016/s0960-894x(02)00685-6
CHEMBL104808 4877 0 None -144 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 446 10 1 5 3.2 O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccc(F)cc3)C2)cc1)C1CC1 10.1016/s0960-894x(02)00685-6
1204 1893 114 None -173 25 Human 5.3 pKi = 5.3 Binding
Binding affinity to histamine H2 receptor (unknown origin)Binding affinity to histamine H2 receptor (unknown origin)
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
1247 1893 114 None -173 25 Human 5.3 pKi = 5.3 Binding
Binding affinity to histamine H2 receptor (unknown origin)Binding affinity to histamine H2 receptor (unknown origin)
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
1375 1893 114 None -173 25 Human 5.3 pKi = 5.3 Binding
Binding affinity to histamine H2 receptor (unknown origin)Binding affinity to histamine H2 receptor (unknown origin)
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
774 1893 114 None -173 25 Human 5.3 pKi = 5.3 Binding
Binding affinity to histamine H2 receptor (unknown origin)Binding affinity to histamine H2 receptor (unknown origin)
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
CHEMBL90 1893 114 None -173 25 Human 5.3 pKi = 5.3 Binding
Binding affinity to histamine H2 receptor (unknown origin)Binding affinity to histamine H2 receptor (unknown origin)
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
DB05381 1893 114 None -173 25 Human 5.3 pKi = 5.3 Binding
Binding affinity to histamine H2 receptor (unknown origin)Binding affinity to histamine H2 receptor (unknown origin)
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
44334265 109182 0 None -25 3 Human 5.3 pKi = 5.3 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 368 8 1 6 2.0 CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)c3cnccn3)C2)cc1 10.1016/s0960-894x(02)00685-6
CHEMBL322695 109182 0 None -25 3 Human 5.3 pKi = 5.3 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 368 8 1 6 2.0 CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)c3cnccn3)C2)cc1 10.1016/s0960-894x(02)00685-6
44334521 107337 0 None -36 3 Human 4.3 pKi = 4.3 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 262 6 1 4 1.7 CC(=O)c1ccc(OCCCN2CC[C@H](N)C2)cc1 10.1016/s0960-894x(02)00685-6
CHEMBL319231 107337 0 None -36 3 Human 4.3 pKi = 4.3 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 262 6 1 4 1.7 CC(=O)c1ccc(OCCCN2CC[C@H](N)C2)cc1 10.1016/s0960-894x(02)00685-6
1226 1980 16 None -7 7 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells
ChEMBL 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C 10.1016/j.bmcl.2010.10.041
41376 1980 16 None -7 7 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells
ChEMBL 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C 10.1016/j.bmcl.2010.10.041
CHEMBL12608 1980 16 None -7 7 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells
ChEMBL 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C 10.1016/j.bmcl.2010.10.041
1231 922 112 None -2 8 Guinea pig 6.3 pKi = 6.3 Binding
Evaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atriumEvaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atrium
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/jm00356a005
2756 922 112 None -2 8 Guinea pig 6.3 pKi = 6.3 Binding
Evaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atriumEvaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atrium
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/jm00356a005
645 922 112 None -2 8 Guinea pig 6.3 pKi = 6.3 Binding
Evaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atriumEvaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atrium
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/jm00356a005
CHEMBL30 922 112 None -2 8 Guinea pig 6.3 pKi = 6.3 Binding
Evaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atriumEvaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atrium
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/jm00356a005
DB00501 922 112 None -2 8 Guinea pig 6.3 pKi = 6.3 Binding
Evaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atriumEvaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atrium
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/jm00356a005
1231 922 112 None -2 8 Guinea pig 6.3 pKi = 6.3 Binding
In vitro inhibition of Histamine H2 receptor by measuring its ability to block the histamine-stimulated adenylate cyclase of guinea pig hippocampal homogenateIn vitro inhibition of Histamine H2 receptor by measuring its ability to block the histamine-stimulated adenylate cyclase of guinea pig hippocampal homogenate
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/jm00345a002
2756 922 112 None -2 8 Guinea pig 6.3 pKi = 6.3 Binding
In vitro inhibition of Histamine H2 receptor by measuring its ability to block the histamine-stimulated adenylate cyclase of guinea pig hippocampal homogenateIn vitro inhibition of Histamine H2 receptor by measuring its ability to block the histamine-stimulated adenylate cyclase of guinea pig hippocampal homogenate
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/jm00345a002
645 922 112 None -2 8 Guinea pig 6.3 pKi = 6.3 Binding
In vitro inhibition of Histamine H2 receptor by measuring its ability to block the histamine-stimulated adenylate cyclase of guinea pig hippocampal homogenateIn vitro inhibition of Histamine H2 receptor by measuring its ability to block the histamine-stimulated adenylate cyclase of guinea pig hippocampal homogenate
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/jm00345a002
CHEMBL30 922 112 None -2 8 Guinea pig 6.3 pKi = 6.3 Binding
In vitro inhibition of Histamine H2 receptor by measuring its ability to block the histamine-stimulated adenylate cyclase of guinea pig hippocampal homogenateIn vitro inhibition of Histamine H2 receptor by measuring its ability to block the histamine-stimulated adenylate cyclase of guinea pig hippocampal homogenate
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/jm00345a002
DB00501 922 112 None -2 8 Guinea pig 6.3 pKi = 6.3 Binding
In vitro inhibition of Histamine H2 receptor by measuring its ability to block the histamine-stimulated adenylate cyclase of guinea pig hippocampal homogenateIn vitro inhibition of Histamine H2 receptor by measuring its ability to block the histamine-stimulated adenylate cyclase of guinea pig hippocampal homogenate
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1021/jm00345a002
5039 62838 13 None -2 2 Guinea pig 6.3 pKi = 6.3 Binding
In vitro inhibition of Histamine H2 receptor by measuring its ability to block the histamine-stimulated adenylate cyclase of guinea pig hippocampal homogenateIn vitro inhibition of Histamine H2 receptor by measuring its ability to block the histamine-stimulated adenylate cyclase of guinea pig hippocampal homogenate
ChEMBL 314 10 2 7 1.5 CNC(=C[N+](=O)[O-])NCCSCc1ccc(CN(C)C)o1 10.1021/jm00345a002
CHEMBL1790041 62838 13 None -2 2 Guinea pig 6.3 pKi = 6.3 Binding
In vitro inhibition of Histamine H2 receptor by measuring its ability to block the histamine-stimulated adenylate cyclase of guinea pig hippocampal homogenateIn vitro inhibition of Histamine H2 receptor by measuring its ability to block the histamine-stimulated adenylate cyclase of guinea pig hippocampal homogenate
ChEMBL 314 10 2 7 1.5 CNC(=C[N+](=O)[O-])NCCSCc1ccc(CN(C)C)o1 10.1021/jm00345a002
10474353 58454 0 None -524 3 Guinea pig 5.3 pKi = 5.3 Binding
Binding affinity against H2 receptor of Guinea pig atriumBinding affinity against H2 receptor of Guinea pig atrium
ChEMBL 371 5 2 3 3.2 O=C(Nc1ccc(I)cc1)OCCCc1c[nH]cn1 10.1021/jm9507688
CHEMBL16874 58454 0 None -524 3 Guinea pig 5.3 pKi = 5.3 Binding
Binding affinity against H2 receptor of Guinea pig atriumBinding affinity against H2 receptor of Guinea pig atrium
ChEMBL 371 5 2 3 3.2 O=C(Nc1ccc(I)cc1)OCCCc1c[nH]cn1 10.1021/jm9507688
10015196 103132 0 None -251 3 Human 5.3 pKi = 5.3 Binding
Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors
ChEMBL 254 8 3 2 2.4 CCC/N=C(\S)NCCCCCc1c[nH]cn1 10.1021/jm00012a025
CHEMBL308717 103132 0 None -251 3 Human 5.3 pKi = 5.3 Binding
Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors
ChEMBL 254 8 3 2 2.4 CCC/N=C(\S)NCCCCCc1c[nH]cn1 10.1021/jm00012a025
10803416 54315 0 None -1621 3 Guinea pig 4.3 pKi = 4.3 Binding
Binding affinity against H2 receptor of Guinea pig atriumBinding affinity against H2 receptor of Guinea pig atrium
ChEMBL 290 6 2 5 2.5 O=C(Nc1ccccc1[N+](=O)[O-])OCCCc1c[nH]cn1 10.1021/jm9507688
CHEMBL16109 54315 0 None -1621 3 Guinea pig 4.3 pKi = 4.3 Binding
Binding affinity against H2 receptor of Guinea pig atriumBinding affinity against H2 receptor of Guinea pig atrium
ChEMBL 290 6 2 5 2.5 O=C(Nc1ccccc1[N+](=O)[O-])OCCCc1c[nH]cn1 10.1021/jm9507688
44304056 102238 0 None -5754 3 Human 4.3 pKi = 4.3 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 401 10 1 5 2.6 CC(C)N[C@H](C)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL304888 102238 0 None -5754 3 Human 4.3 pKi = 4.3 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 401 10 1 5 2.6 CC(C)N[C@H](C)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
44304316 201434 0 None -416 3 Human 4.3 pKi = 4.3 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 485 8 0 6 3.6 CC(C)(C)OC(=O)N1CCC[C@@H]1C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL64120 201434 0 None -416 3 Human 4.3 pKi = 4.3 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 485 8 0 6 3.6 CC(C)(C)OC(=O)N1CCC[C@@H]1C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
1204 1893 114 None -173 25 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1247 1893 114 None -173 25 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1375 1893 114 None -173 25 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
774 1893 114 None -173 25 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL90 1893 114 None -173 25 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
DB05381 1893 114 None -173 25 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
132060770 162077 0 None -8 10 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 451 7 0 6 3.5 CCOC(=O)CCN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)CC3)CC1 10.1016/j.ejmech.2018.02.024
CHEMBL4169689 162077 0 None -8 10 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 451 7 0 6 3.5 CCOC(=O)CCN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)CC3)CC1 10.1016/j.ejmech.2018.02.024
2812 4696 96 None -33 34 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
CHEMBL104 4696 96 None -33 34 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
164622330 185270 0 None -2 6 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 360 6 4 4 2.3 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)N[C@@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4867962 185270 0 None -2 6 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 360 6 4 4 2.3 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)N[C@@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
164627774 185973 0 None 1 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 344 3 4 4 1.4 N/C(=N\C(=O)NCc1ccccc1)NC1CCc2nc(N)sc2C1 10.1016/j.ejmech.2021.113190
CHEMBL4878215 185973 0 None 1 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 344 3 4 4 1.4 N/C(=N\C(=O)NCc1ccccc1)NC1CCc2nc(N)sc2C1 10.1016/j.ejmech.2021.113190
71452172 83091 0 None -1 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]tiotidine from human recombinant histamine H2 receptor after 1.5 hrs by microbeta scintillation counting analysisDisplacement of [3H]tiotidine from human recombinant histamine H2 receptor after 1.5 hrs by microbeta scintillation counting analysis
ChEMBL 274 6 1 5 2.4 c1ccc(OCc2cc(OC[C@@H]3CCCN3)no2)cc1 10.1021/ml3002715
CHEMBL2203551 83091 0 None -1 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]tiotidine from human recombinant histamine H2 receptor after 1.5 hrs by microbeta scintillation counting analysisDisplacement of [3H]tiotidine from human recombinant histamine H2 receptor after 1.5 hrs by microbeta scintillation counting analysis
ChEMBL 274 6 1 5 2.4 c1ccc(OCc2cc(OC[C@@H]3CCCN3)no2)cc1 10.1021/ml3002715
155552683 173584 0 None -40 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells after 90 mins by scintillation counting methodDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells after 90 mins by scintillation counting method
ChEMBL 379 4 2 5 4.1 Clc1ccc(C#Cc2nc(NCCc3ccccc3)c3nc[nH]c3n2)s1 10.1039/C8MD00317C
CHEMBL4546937 173584 0 None -40 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells after 90 mins by scintillation counting methodDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells after 90 mins by scintillation counting method
ChEMBL 379 4 2 5 4.1 Clc1ccc(C#Cc2nc(NCCc3ccccc3)c3nc[nH]c3n2)s1 10.1039/C8MD00317C
164622256 185124 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 318 4 4 4 2.2 CCCNC(=O)/N=C(\N)Nc1cccc(-c2csc(N)n2)c1 10.1016/j.ejmech.2021.113190
CHEMBL4865670 185124 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 318 4 4 4 2.2 CCCNC(=O)/N=C(\N)Nc1cccc(-c2csc(N)n2)c1 10.1016/j.ejmech.2021.113190
145992489 166413 0 None -1 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assay
ChEMBL 535 7 1 2 7.8 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC=C(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL4287623 166413 0 None -1 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assay
ChEMBL 535 7 1 2 7.8 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC=C(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
168290235 192356 0 None -1737 20 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5201074 192356 0 None -1737 20 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222491 192356 0 None -1737 20 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
5039 62838 13 None -2 2 Guinea pig 7.3 pKi = 7.3 Binding
Inhibition of [125I]APT binding to histamine H2 receptor in guinea pig cerebral membranes.Inhibition of [125I]APT binding to histamine H2 receptor in guinea pig cerebral membranes.
ChEMBL 314 10 2 7 1.5 CNC(=C[N+](=O)[O-])NCCSCc1ccc(CN(C)C)o1 10.1021/jm00090a013
CHEMBL1790041 62838 13 None -2 2 Guinea pig 7.3 pKi = 7.3 Binding
Inhibition of [125I]APT binding to histamine H2 receptor in guinea pig cerebral membranes.Inhibition of [125I]APT binding to histamine H2 receptor in guinea pig cerebral membranes.
ChEMBL 314 10 2 7 1.5 CNC(=C[N+](=O)[O-])NCCSCc1ccc(CN(C)C)o1 10.1021/jm00090a013
71454295 83651 0 None -660 7 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysisDisplacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysis
ChEMBL 536 8 0 6 5.5 COc1ccccc1N1CCN(Cc2cc(CN3CCN(c4ccccc4OC)CC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207641 83651 0 None -660 7 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysisDisplacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysis
ChEMBL 536 8 0 6 5.5 COc1ccccc1N1CCN(Cc2cc(CN3CCN(c4ccccc4OC)CC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
44304329 201527 0 None -1778 3 Human 4.3 pKi = 4.3 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 385 8 1 5 1.9 O=C(c1ccc(OCCCN2CCN(C(=O)[C@H]3CCCN3)CC2)cc1)C1CC1 10.1016/s0960-894x(02)00310-4
CHEMBL64461 201527 0 None -1778 3 Human 4.3 pKi = 4.3 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 385 8 1 5 1.9 O=C(c1ccc(OCCCN2CCN(C(=O)[C@H]3CCCN3)CC2)cc1)C1CC1 10.1016/s0960-894x(02)00310-4
24841480 183307 0 None -269 20 Human 6.3 pKi = 6.3 Binding
Antagonist activity at histamine H2 receptor (unknown origin) by PDSP assayAntagonist activity at histamine H2 receptor (unknown origin) by PDSP assay
ChEMBL 340 3 0 4 4.5 O=C(OCCN1CCCC1)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
CHEMBL481153 183307 0 None -269 20 Human 6.3 pKi = 6.3 Binding
Antagonist activity at histamine H2 receptor (unknown origin) by PDSP assayAntagonist activity at histamine H2 receptor (unknown origin) by PDSP assay
ChEMBL 340 3 0 4 4.5 O=C(OCCN1CCCC1)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
1231 922 112 None -2 8 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C nan
2756 922 112 None -2 8 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C nan
645 922 112 None -2 8 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C nan
CHEMBL30 922 112 None -2 8 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C nan
DB00501 922 112 None -2 8 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C nan
155558968 174236 0 None 1 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to human histamine 2 receptor expressed in HEK cells by radioligand binding assayBinding affinity to human histamine 2 receptor expressed in HEK cells by radioligand binding assay
ChEMBL 432 3 2 5 3.2 Cc1cccc(C)c1N1C(=O)[C@H](CC2CNc3ccccc32)NC2(CCN(C)CC2)C1=O 10.1016/j.ejmech.2018.12.048
CHEMBL4562437 174236 0 None 1 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to human histamine 2 receptor expressed in HEK cells by radioligand binding assayBinding affinity to human histamine 2 receptor expressed in HEK cells by radioligand binding assay
ChEMBL 432 3 2 5 3.2 Cc1cccc(C)c1N1C(=O)[C@H](CC2CNc3ccccc32)NC2(CCN(C)CC2)C1=O 10.1016/j.ejmech.2018.12.048
53325242 56760 0 None -2 17 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assay
ChEMBL 537 8 1 2 7.9 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL1644978 56760 0 None -2 17 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assay
ChEMBL 537 8 1 2 7.9 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
162644910 178821 0 None -50 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysis
ChEMBL 407 7 0 4 5.0 Clc1cccc(-c2ccc(OCCCN3CCN(c4ccncc4)CC3)cc2)c1 10.1016/j.ejmech.2020.113041
CHEMBL4740135 178821 0 None -50 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysis
ChEMBL 407 7 0 4 5.0 Clc1cccc(-c2ccc(OCCCN3CCN(c4ccncc4)CC3)cc2)c1 10.1016/j.ejmech.2020.113041
168268716 192150 0 None 1 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 372 3 4 4 3.5 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NC2CCCCC2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5170276 192150 0 None 1 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 372 3 4 4 3.5 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NC2CCCCC2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5221176 192150 0 None 1 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 372 3 4 4 3.5 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NC2CCCCC2)cc1 10.1021/acs.jmedchem.1c00692
71450707 83650 0 None -1445 7 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysisDisplacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysis
ChEMBL 444 6 0 5 3.9 COc1ccccc1N1CCN(Cc2cc(CN3CCN(C)CC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207640 83650 0 None -1445 7 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysisDisplacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysis
ChEMBL 444 6 0 5 3.9 COc1ccccc1N1CCN(Cc2cc(CN3CCN(C)CC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
155531772 176082 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of 20 nM [3H]UR-DE257 from human H2R expressed in Sf9 cell membranes co-expressing GsalphaS by competition binding assayDisplacement of 20 nM [3H]UR-DE257 from human H2R expressed in Sf9 cell membranes co-expressing GsalphaS by competition binding assay
ChEMBL 334 8 3 6 3.3 Cc1[nH]cnc1CSCCNc1ccnc(NCC(C)(C)C)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4466349 176082 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of 20 nM [3H]UR-DE257 from human H2R expressed in Sf9 cell membranes co-expressing GsalphaS by competition binding assayDisplacement of 20 nM [3H]UR-DE257 from human H2R expressed in Sf9 cell membranes co-expressing GsalphaS by competition binding assay
ChEMBL 334 8 3 6 3.3 Cc1[nH]cnc1CSCCNc1ccnc(NCC(C)(C)C)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4598197 176082 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of 20 nM [3H]UR-DE257 from human H2R expressed in Sf9 cell membranes co-expressing GsalphaS by competition binding assayDisplacement of 20 nM [3H]UR-DE257 from human H2R expressed in Sf9 cell membranes co-expressing GsalphaS by competition binding assay
ChEMBL 334 8 3 6 3.3 Cc1[nH]cnc1CSCCNc1ccnc(NCC(C)(C)C)n1 10.1021/acs.jmedchem.9b01342
CHEMBL5083588 213748 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C 10.1016/j.bmcl.2021.128388
CHEMBL5095633 213748 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C 10.1016/j.bmcl.2021.128388
44335351 4983 0 None -29 3 Human 5.3 pKi = 5.3 Binding
Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor
ChEMBL 402 7 0 4 4.6 CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc(Cl)cc3)cc2)CC1 10.1016/s0960-894x(02)00648-0
CHEMBL105385 4983 0 None -29 3 Human 5.3 pKi = 5.3 Binding
Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor
ChEMBL 402 7 0 4 4.6 CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc(Cl)cc3)cc2)CC1 10.1016/s0960-894x(02)00648-0
168275750 192214 0 None -87 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 332 6 3 4 1.6 Cc1nnc(CCCN/C(N)=N/C(=O)NCc2ccccc2)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5175558 192214 0 None -87 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 332 6 3 4 1.6 Cc1nnc(CCCN/C(N)=N/C(=O)NCc2ccccc2)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221581 192214 0 None -87 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 332 6 3 4 1.6 Cc1nnc(CCCN/C(N)=N/C(=O)NCc2ccccc2)s1 10.1021/acs.jmedchem.1c00692
44304475 201070 0 None -10471 3 Human 4.3 pKi = 4.3 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 348 8 0 5 2.8 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)CC)cc2)CC1 10.1016/s0960-894x(02)00309-8
CHEMBL62066 201070 0 None -10471 3 Human 4.3 pKi = 4.3 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 348 8 0 5 2.8 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)CC)cc2)CC1 10.1016/s0960-894x(02)00309-8
44335222 162892 0 None -20 3 Human 4.2 pKi = 4.2 Binding
Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor
ChEMBL 369 7 0 5 3.3 CCOC(=O)N1CCN(CCCOc2ccc(-c3ccncc3)cc2)CC1 10.1016/s0960-894x(02)00648-0
CHEMBL419912 162892 0 None -20 3 Human 4.2 pKi = 4.2 Binding
Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor
ChEMBL 369 7 0 5 3.3 CCOC(=O)N1CCN(CCCOc2ccc(-c3ccncc3)cc2)CC1 10.1016/s0960-894x(02)00648-0
44304357 198916 0 None -4786 3 Human 4.2 pKi = 4.2 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 415 9 1 5 3.0 CC(C)(C)C[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL59931 198916 0 None -4786 3 Human 4.2 pKi = 4.2 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 415 9 1 5 3.0 CC(C)(C)C[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
137645406 157348 0 None -75 13 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 491 8 0 7 5.4 COc1ccccc1N1CCC2(CCN(CCCSc3nnc(-c4ccccc4)n3C)CC2)CC1 10.1021/acs.jmedchem.9b00412
CHEMBL4084262 157348 0 None -75 13 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 491 8 0 7 5.4 COc1ccccc1N1CCC2(CCN(CCCSc3nnc(-c4ccccc4)n3C)CC2)CC1 10.1021/acs.jmedchem.9b00412
168294182 192436 0 None -3 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 314 6 4 2 1.7 C[C@@H](NC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5208722 192436 0 None -3 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 314 6 4 2 1.7 C[C@@H](NC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222960 192436 0 None -3 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 314 6 4 2 1.7 C[C@@H](NC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1021/acs.jmedchem.1c00692
135481708 201319 1 None - 1 Guinea pig 8.2 pKi = 8.2 Binding
In vitro inhibition of Histamine H2 receptor by measuring its ability to block the histamine-stimulated adenylate cyclase of guinea pig hippocampal homogenateIn vitro inhibition of Histamine H2 receptor by measuring its ability to block the histamine-stimulated adenylate cyclase of guinea pig hippocampal homogenate
ChEMBL 345 7 2 7 0.2 CN(C)Cc1ccc(CSCCNC2=NS(=O)(=O)N=C2N)o1 10.1021/jm00345a002
CHEMBL63299 201319 1 None - 1 Guinea pig 8.2 pKi = 8.2 Binding
In vitro inhibition of Histamine H2 receptor by measuring its ability to block the histamine-stimulated adenylate cyclase of guinea pig hippocampal homogenateIn vitro inhibition of Histamine H2 receptor by measuring its ability to block the histamine-stimulated adenylate cyclase of guinea pig hippocampal homogenate
ChEMBL 345 7 2 7 0.2 CN(C)Cc1ccc(CSCCNC2=NS(=O)(=O)N=C2N)o1 10.1021/jm00345a002
136023351 204980 16 None - 1 Guinea pig 8.2 pKi = 8.2 Binding
In vitro inhibition of Histamine H2 receptor by measuring its ability to block the histamine-stimulated adenylate cyclase of guinea pig hippocampal homogenateIn vitro inhibition of Histamine H2 receptor by measuring its ability to block the histamine-stimulated adenylate cyclase of guinea pig hippocampal homogenate
ChEMBL 329 8 2 8 1.8 CN(C)Cc1ccc(CSCCNc2n[s+]([O-])nc2N)o1 10.1021/jm00345a002
5384819 204980 16 None - 1 Guinea pig 8.2 pKi = 8.2 Binding
In vitro inhibition of Histamine H2 receptor by measuring its ability to block the histamine-stimulated adenylate cyclase of guinea pig hippocampal homogenateIn vitro inhibition of Histamine H2 receptor by measuring its ability to block the histamine-stimulated adenylate cyclase of guinea pig hippocampal homogenate
ChEMBL 329 8 2 8 1.8 CN(C)Cc1ccc(CSCCNc2n[s+]([O-])nc2N)o1 10.1021/jm00345a002
CHEMBL8982 204980 16 None - 1 Guinea pig 8.2 pKi = 8.2 Binding
In vitro inhibition of Histamine H2 receptor by measuring its ability to block the histamine-stimulated adenylate cyclase of guinea pig hippocampal homogenateIn vitro inhibition of Histamine H2 receptor by measuring its ability to block the histamine-stimulated adenylate cyclase of guinea pig hippocampal homogenate
ChEMBL 329 8 2 8 1.8 CN(C)Cc1ccc(CSCCNc2n[s+]([O-])nc2N)o1 10.1021/jm00345a002
168268853 192173 0 None -2 6 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 389 8 4 5 1.9 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5180504 192173 0 None -2 6 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 389 8 4 5 1.9 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5221353 192173 0 None -2 6 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 389 8 4 5 1.9 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
164609017 183833 0 None -1 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 416 10 4 4 3.2 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CCCc1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4846201 183833 0 None -1 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 416 10 4 4 3.2 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CCCc1ccccc1 10.1016/j.ejmech.2021.113190
164610289 184540 0 None 38 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 438 7 4 4 3.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NC(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4856602 184540 0 None 38 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 438 7 4 4 3.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NC(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2021.113190
44304378 162709 0 None -2951 3 Human 4.2 pKi = 4.2 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 423 11 0 5 4.1 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3cccnc3)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL418658 162709 0 None -2951 3 Human 4.2 pKi = 4.2 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 423 11 0 5 4.1 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3cccnc3)CC2)cc1 10.1016/s0960-894x(02)00309-8
44304348 100123 0 None -15135 3 Human 4.2 pKi = 4.2 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 387 10 1 5 2.3 CCC[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL291821 100123 0 None -15135 3 Human 4.2 pKi = 4.2 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 387 10 1 5 2.3 CCC[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
44334036 167218 0 None -154 3 Human 5.2 pKi = 5.2 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 391 8 1 5 3.0 CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)c3ccc(C#N)cc3)C2)cc1 10.1016/s0960-894x(02)00685-6
CHEMBL430502 167218 0 None -154 3 Human 5.2 pKi = 5.2 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 391 8 1 5 3.0 CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)c3ccc(C#N)cc3)C2)cc1 10.1016/s0960-894x(02)00685-6
71454294 83649 0 None -1348 7 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysisDisplacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysis
ChEMBL 431 6 0 5 4.0 COc1ccccc1N1CCN(Cc2cc(CN3CCOCC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207639 83649 0 None -1348 7 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysisDisplacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysis
ChEMBL 431 6 0 5 4.0 COc1ccccc1N1CCN(Cc2cc(CN3CCOCC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
71449142 79093 0 None -104 3 Human 5.2 pKi = 5.2 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 442 9 0 6 4.2 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)c3ccc(SC)cc3)cc2)CC1 10.1016/s0960-894x(02)00309-8
CHEMBL2113738 79093 0 None -104 3 Human 5.2 pKi = 5.2 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 442 9 0 6 4.2 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)c3ccc(SC)cc3)cc2)CC1 10.1016/s0960-894x(02)00309-8
44334037 4365 0 None -112 3 Human 5.2 pKi = 5.2 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 450 9 1 7 3.7 CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)c3csc(-c4cccnc4)n3)C2)cc1 10.1016/s0960-894x(02)00685-6
CHEMBL101634 4365 0 None -112 3 Human 5.2 pKi = 5.2 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 450 9 1 7 3.7 CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)c3csc(-c4cccnc4)n3)C2)cc1 10.1016/s0960-894x(02)00685-6
73355415 92087 0 None -32 13 Human 5.2 pKi = 5.2 Binding
Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay
ChEMBL 277 3 1 1 2.1 C1C2C3CC4C2C2C1C3[C@H](NCC13C5C6C7C5C1C7C63)C42 10.1016/j.bmc.2013.07.045
CHEMBL2432039 92087 0 None -32 13 Human 5.2 pKi = 5.2 Binding
Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay
ChEMBL 277 3 1 1 2.1 C1C2C3CC4C2C2C1C3[C@H](NCC13C5C6C7C5C1C7C63)C42 10.1016/j.bmc.2013.07.045
CHEMBL5092267 213571 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCC[n+]1c(C)cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc1C 10.1016/j.bmcl.2021.128388
164611474 184860 0 None 407 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 366 6 4 5 2.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1cccs1 10.1016/j.ejmech.2021.113190
CHEMBL4861704 184860 0 None 407 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 366 6 4 5 2.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1cccs1 10.1016/j.ejmech.2021.113190
164624107 185130 0 None -1 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 402 9 4 4 2.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CCc1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4865765 185130 0 None -1 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 402 9 4 4 2.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CCc1ccccc1 10.1016/j.ejmech.2021.113190
164620678 185427 0 None 177 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 374 7 4 4 2.7 CCC(NC(=O)/N=C(\N)NCCCc1sc(N)nc1C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4870510 185427 0 None 177 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 374 7 4 4 2.7 CCC(NC(=O)/N=C(\N)NCCCc1sc(N)nc1C)c1ccccc1 10.1016/j.ejmech.2021.113190
126688 400 28 None -1 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells
ChEMBL 157 2 2 4 0.5 NCCc1sc(nc1C)N 10.1016/j.bmcl.2010.10.041
4025 400 28 None -1 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells
ChEMBL 157 2 2 4 0.5 NCCc1sc(nc1C)N 10.1016/j.bmcl.2010.10.041
CHEMBL293762 400 28 None -1 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells
ChEMBL 157 2 2 4 0.5 NCCc1sc(nc1C)N 10.1016/j.bmcl.2010.10.041
10333098 53673 6 None -6025 2 Guinea pig 4.2 pKi = 4.2 Binding
Binding affinity against H2 receptor of Guinea pig atriumBinding affinity against H2 receptor of Guinea pig atrium
ChEMBL 265 6 2 3 2.6 O=C(NCC1CCCCC1)OCCCc1c[nH]cn1 10.1021/jm9507688
CHEMBL16056 53673 6 None -6025 2 Guinea pig 4.2 pKi = 4.2 Binding
Binding affinity against H2 receptor of Guinea pig atriumBinding affinity against H2 receptor of Guinea pig atrium
ChEMBL 265 6 2 3 2.6 O=C(NCC1CCCCC1)OCCCc1c[nH]cn1 10.1021/jm9507688
10611565 97855 0 None -2570 3 Guinea pig 4.2 pKi = 4.2 Binding
Binding affinity against H2 receptor of Guinea pig atriumBinding affinity against H2 receptor of Guinea pig atrium
ChEMBL 263 5 2 3 2.7 O=C(Nc1ccc(F)cc1)OCCCc1c[nH]cn1 10.1021/jm9507688
CHEMBL274989 97855 0 None -2570 3 Guinea pig 4.2 pKi = 4.2 Binding
Binding affinity against H2 receptor of Guinea pig atriumBinding affinity against H2 receptor of Guinea pig atrium
ChEMBL 263 5 2 3 2.7 O=C(Nc1ccc(F)cc1)OCCCc1c[nH]cn1 10.1021/jm9507688
155551348 173375 0 None 1 2 Human 5.2 pKi = 5.2 Binding
Inhibition of histamine H2 receptor (unknown origin)Inhibition of histamine H2 receptor (unknown origin)
ChEMBL 487 7 1 9 3.7 CCOC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@@H]1OC(C)(C)O[C@@H]12 10.1021/acs.jmedchem.8b01662
CHEMBL4541409 173375 0 None 1 2 Human 5.2 pKi = 5.2 Binding
Inhibition of histamine H2 receptor (unknown origin)Inhibition of histamine H2 receptor (unknown origin)
ChEMBL 487 7 1 9 3.7 CCOC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@@H]1OC(C)(C)O[C@@H]12 10.1021/acs.jmedchem.8b01662
168292954 192385 0 None -11 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 388 8 4 4 2.5 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5202592 192385 0 None -11 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 388 8 4 4 2.5 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222660 192385 0 None -11 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 388 8 4 4 2.5 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
162676676 182997 0 None -323 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysis
ChEMBL 389 8 0 5 4.5 c1ccc(Oc2ccc(OCCCN3CCN(c4ccncc4)CC3)cc2)cc1 10.1016/j.ejmech.2020.113041
CHEMBL4800672 182997 0 None -323 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysis
ChEMBL 389 8 0 5 4.5 c1ccc(Oc2ccc(OCCCN3CCN(c4ccncc4)CC3)cc2)cc1 10.1016/j.ejmech.2020.113041
CHEMBL5075713 213743 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay
ChEMBL None None None CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2c[nH]cn2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1016/j.bmcl.2021.128388
CHEMBL5095559 213743 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay
ChEMBL None None None CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2c[nH]cn2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1016/j.bmcl.2021.128388
4189 205185 91 None -36 34 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1559 205185 91 None -36 34 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL91 205185 91 None -36 34 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
130442572 171332 0 None -144 24 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 395 3 0 5 6.0 FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4469848 171332 0 None -144 24 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 395 3 0 5 6.0 FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
181743 177987 3 None -338 22 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]Tiotidine from human histamine H2 receptorDisplacement of [3H]Tiotidine from human histamine H2 receptor
ChEMBL 339 2 0 5 3.2 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2)OCO4 10.1016/j.bmcl.2009.11.053
CHEMBL467094 177987 3 None -338 22 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]Tiotidine from human histamine H2 receptorDisplacement of [3H]Tiotidine from human histamine H2 receptor
ChEMBL 339 2 0 5 3.2 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2)OCO4 10.1016/j.bmcl.2009.11.053
168291233 192367 0 None -5 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 373 8 4 5 1.4 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)o2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5200106 192367 0 None -5 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 373 8 4 5 1.4 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)o2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222556 192367 0 None -5 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 373 8 4 5 1.4 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)o2)cc1 10.1021/acs.jmedchem.1c00692
44304031 100192 0 None -933 3 Human 5.2 pKi = 5.2 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 452 10 0 6 4.1 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)/C=C/c3ccc(OC)cc3)cc2)CC1 10.1016/s0960-894x(02)00309-8
CHEMBL292275 100192 0 None -933 3 Human 5.2 pKi = 5.2 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 452 10 0 6 4.1 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)/C=C/c3ccc(OC)cc3)cc2)CC1 10.1016/s0960-894x(02)00309-8
18672441 94938 0 None -9332 4 Human 4.2 pKi = 4.2 Binding
Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor
ChEMBL 306 6 0 3 4.1 N#Cc1ccc(-c2ccc(OCCCN3CCCC3)cc2)cc1 10.1016/s0960-894x(02)00648-0
CHEMBL25688 94938 0 None -9332 4 Human 4.2 pKi = 4.2 Binding
Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor
ChEMBL 306 6 0 3 4.1 N#Cc1ccc(-c2ccc(OCCCN3CCCC3)cc2)cc1 10.1016/s0960-894x(02)00648-0
4601 205010 29 None -7 17 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
CHEMBL1201023 205010 29 None -7 17 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
CHEMBL900 205010 29 None -7 17 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
162664702 181618 0 None -50 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysis
ChEMBL 407 7 0 4 5.0 Clc1ccc(-c2ccc(OCCCN3CCN(c4ccncc4)CC3)cc2)cc1 10.1016/j.ejmech.2020.113041
CHEMBL4783066 181618 0 None -50 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysis
ChEMBL 407 7 0 4 5.0 Clc1ccc(-c2ccc(OCCCN3CCN(c4ccncc4)CC3)cc2)cc1 10.1016/j.ejmech.2020.113041
164611342 184495 0 None -1 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 346 6 4 4 1.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCc1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4856005 184495 0 None -1 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 346 6 4 4 1.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCc1ccccc1 10.1016/j.ejmech.2021.113190
164618690 185564 0 None 1 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 360 7 4 4 3.4 CCCCCCNC(=O)/N=C(\N)Nc1cccc(-c2csc(N)n2)c1 10.1016/j.ejmech.2021.113190
CHEMBL4872375 185564 0 None 1 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 360 7 4 4 3.4 CCCCCCNC(=O)/N=C(\N)Nc1cccc(-c2csc(N)n2)c1 10.1016/j.ejmech.2021.113190
127035835 136748 0 None -4 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]UR-DE257 from human histamine 2 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]UR-DE257 from human histamine 2 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 385 4 1 5 3.6 CN1CCN(c2nc(NCc3ccccc3)nc3c2CCc2ccccc2-3)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL3752270 136748 0 None -4 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]UR-DE257 from human histamine 2 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]UR-DE257 from human histamine 2 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 385 4 1 5 3.6 CN1CCN(c2nc(NCc3ccccc3)nc3c2CCc2ccccc2-3)CC1 10.1016/j.bmcl.2015.12.035
44304079 200930 0 None -9549 3 Human 4.2 pKi = 4.2 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 376 9 0 5 3.5 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)CC(C)C)cc2)CC1 10.1016/s0960-894x(02)00309-8
CHEMBL61231 200930 0 None -9549 3 Human 4.2 pKi = 4.2 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 376 9 0 5 3.5 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)CC(C)C)cc2)CC1 10.1016/s0960-894x(02)00309-8
44335428 4900 0 None -79 3 Human 4.2 pKi = 4.2 Binding
Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor
ChEMBL 358 7 1 5 2.6 CCOC(=O)N1CCN(CCCOc2ccc(-c3c[nH]cn3)cc2)CC1 10.1016/s0960-894x(02)00648-0
CHEMBL104947 4900 0 None -79 3 Human 4.2 pKi = 4.2 Binding
Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor
ChEMBL 358 7 1 5 2.6 CCOC(=O)N1CCN(CCCOc2ccc(-c3c[nH]cn3)cc2)CC1 10.1016/s0960-894x(02)00648-0
1231 922 112 None -2 8 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/j.bmcl.2013.12.024
2756 922 112 None -2 8 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/j.bmcl.2013.12.024
645 922 112 None -2 8 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/j.bmcl.2013.12.024
CHEMBL30 922 112 None -2 8 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/j.bmcl.2013.12.024
DB00501 922 112 None -2 8 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/j.bmcl.2013.12.024
1231 922 112 None -2 8 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/j.bmcl.2013.12.024
2756 922 112 None -2 8 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/j.bmcl.2013.12.024
645 922 112 None -2 8 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/j.bmcl.2013.12.024
CHEMBL30 922 112 None -2 8 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/j.bmcl.2013.12.024
DB00501 922 112 None -2 8 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)
ChEMBL 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 10.1016/j.bmcl.2013.12.024
164610892 184605 0 None 1 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 394 8 4 4 3.2 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CC1CCCCC1 10.1016/j.ejmech.2021.113190
CHEMBL4857560 184605 0 None 1 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 394 8 4 4 3.2 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CC1CCCCC1 10.1016/j.ejmech.2021.113190
44334407 108585 0 None -229 3 Human 6.2 pKi = 6.2 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 462 10 1 5 3.8 O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3cccc(Cl)c3)C2)cc1)C1CC1 10.1016/s0960-894x(02)00685-6
CHEMBL321320 108585 0 None -229 3 Human 6.2 pKi = 6.2 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 462 10 1 5 3.8 O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3cccc(Cl)c3)C2)cc1)C1CC1 10.1016/s0960-894x(02)00685-6
44304402 199517 0 None -426 3 Human 5.2 pKi = 5.2 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 415 12 0 6 4.5 CCCCCC(=O)c1ccc(OCCCN2CCN(Cc3nccs3)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL60360 199517 0 None -426 3 Human 5.2 pKi = 5.2 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 415 12 0 6 4.5 CCCCCC(=O)c1ccc(OCCCN2CCN(Cc3nccs3)CC2)cc1 10.1016/s0960-894x(02)00309-8
1258 194 8 None -35481 5 Human 4.2 pKi = 4.2 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 359 8 1 5 1.5 C[C@H](C(=O)N1CCN(CC1)CCCOc1ccc(cc1)C(=O)C1CC1)N 10.1016/s0960-894x(02)00310-4
9906860 194 8 None -35481 5 Human 4.2 pKi = 4.2 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 359 8 1 5 1.5 C[C@H](C(=O)N1CCN(CC1)CCCOc1ccc(cc1)C(=O)C1CC1)N 10.1016/s0960-894x(02)00310-4
CHEMBL302196 194 8 None -35481 5 Human 4.2 pKi = 4.2 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 359 8 1 5 1.5 C[C@H](C(=O)N1CCN(CC1)CCCOc1ccc(cc1)C(=O)C1CC1)N 10.1016/s0960-894x(02)00310-4
44334042 162925 0 None -64 3 Human 6.2 pKi = 6.2 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 453 10 1 6 3.0 N#Cc1ccccc1S(=O)(=O)N[C@H]1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)C1 10.1016/s0960-894x(02)00685-6
CHEMBL420108 162925 0 None -64 3 Human 6.2 pKi = 6.2 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 453 10 1 6 3.0 N#Cc1ccccc1S(=O)(=O)N[C@H]1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)C1 10.1016/s0960-894x(02)00685-6
44334234 109178 0 None -707 3 Human 5.2 pKi = 5.2 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 432 10 1 7 1.8 Cn1cnc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)c1 10.1016/s0960-894x(02)00685-6
CHEMBL322678 109178 0 None -707 3 Human 5.2 pKi = 5.2 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 432 10 1 7 1.8 Cn1cnc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)c1 10.1016/s0960-894x(02)00685-6
180 397 50 None -1412 39 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
200 397 50 None -1412 39 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
2160 397 50 None -1412 39 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
CHEMBL629 397 50 None -1412 39 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
DB00321 397 50 None -1412 39 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
164611757 184310 0 None 1 6 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 402 8 4 4 2.8 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1 10.1016/j.ejmech.2021.113190
CHEMBL4853107 184310 0 None 1 6 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 402 8 4 4 2.8 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1 10.1016/j.ejmech.2021.113190
44304003 201435 0 None -2511 3 Human 4.1 pKi = 4.1 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 384 9 1 6 1.4 N#CC[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL64124 201435 0 None -2511 3 Human 4.1 pKi = 4.1 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 384 9 1 6 1.4 N#CC[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
127052294 139759 0 None -33 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]tiotidine from human histamine H2 receptor expressed in sf9 cell membrane co-expressing Gsalphas incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]tiotidine from human histamine H2 receptor expressed in sf9 cell membrane co-expressing Gsalphas incubated for 60 mins by liquid scintillation counting method
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3806079 139759 0 None -33 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]tiotidine from human histamine H2 receptor expressed in sf9 cell membrane co-expressing Gsalphas incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]tiotidine from human histamine H2 receptor expressed in sf9 cell membrane co-expressing Gsalphas incubated for 60 mins by liquid scintillation counting method
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
71463063 83373 0 None -11 8 Human 5.1 pKi = 5.1 Binding
Binding affinity to Histamine H2 receptorBinding affinity to Histamine H2 receptor
ChEMBL 295 3 1 3 2.0 COc1ccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1 10.1016/j.bmcl.2012.08.046
CHEMBL2205825 83373 0 None -11 8 Human 5.1 pKi = 5.1 Binding
Binding affinity to Histamine H2 receptorBinding affinity to Histamine H2 receptor
ChEMBL 295 3 1 3 2.0 COc1ccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1 10.1016/j.bmcl.2012.08.046
44334369 4930 0 None -138 3 Human 6.1 pKi = 6.1 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 484 10 1 5 4.4 CC(C)(C)c1ccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)cc1 10.1016/s0960-894x(02)00685-6
CHEMBL105071 4930 0 None -138 3 Human 6.1 pKi = 6.1 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 484 10 1 5 4.4 CC(C)(C)c1ccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)cc1 10.1016/s0960-894x(02)00685-6
127049856 139702 0 None -25 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]tiotidine from human histamine H2 receptor expressed in sf9 cell membrane co-expressing Gsalphas incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]tiotidine from human histamine H2 receptor expressed in sf9 cell membrane co-expressing Gsalphas incubated for 60 mins by liquid scintillation counting method
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@H]1CC[C@@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3805431 139702 0 None -25 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]tiotidine from human histamine H2 receptor expressed in sf9 cell membrane co-expressing Gsalphas incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]tiotidine from human histamine H2 receptor expressed in sf9 cell membrane co-expressing Gsalphas incubated for 60 mins by liquid scintillation counting method
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@H]1CC[C@@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
9923147 4965 0 None -1202 4 Human 5.1 pKi = 5.1 Binding
Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor
ChEMBL 321 6 1 4 3.0 N#Cc1ccc(-c2ccc(OCCCN3CC[C@@H](N)C3)cc2)cc1 10.1016/s0960-894x(02)00648-0
CHEMBL105267 4965 0 None -1202 4 Human 5.1 pKi = 5.1 Binding
Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor
ChEMBL 321 6 1 4 3.0 N#Cc1ccc(-c2ccc(OCCCN3CC[C@@H](N)C3)cc2)cc1 10.1016/s0960-894x(02)00648-0
71463061 83367 0 None 1 9 Human 6.1 pKi = 6.1 Binding
Binding affinity to Histamine H2 receptorBinding affinity to Histamine H2 receptor
ChEMBL 339 5 1 4 2.0 COc1cccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)c1OC 10.1016/j.bmcl.2012.08.046
CHEMBL2205813 83367 0 None 1 9 Human 6.1 pKi = 6.1 Binding
Binding affinity to Histamine H2 receptorBinding affinity to Histamine H2 receptor
ChEMBL 339 5 1 4 2.0 COc1cccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)c1OC 10.1016/j.bmcl.2012.08.046
162662563 181454 0 None -123 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysis
ChEMBL 391 7 0 4 4.5 Fc1ccc(-c2ccc(OCCCN3CCN(c4ccncc4)CC3)cc2)cc1 10.1016/j.ejmech.2020.113041
CHEMBL4781093 181454 0 None -123 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysis
ChEMBL 391 7 0 4 4.5 Fc1ccc(-c2ccc(OCCCN3CCN(c4ccncc4)CC3)cc2)cc1 10.1016/j.ejmech.2020.113041
44435200 149131 0 None -4 4 Human 5.1 pKi = 5.1 Binding
Antagonist activity at histamine H2 receptor (unknown origin) by PDSP assayAntagonist activity at histamine H2 receptor (unknown origin) by PDSP assay
ChEMBL 345 4 0 2 5.8 O=C(CCCc1ccccc1)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
CHEMBL394755 149131 0 None -4 4 Human 5.1 pKi = 5.1 Binding
Antagonist activity at histamine H2 receptor (unknown origin) by PDSP assayAntagonist activity at histamine H2 receptor (unknown origin) by PDSP assay
ChEMBL 345 4 0 2 5.8 O=C(CCCc1ccccc1)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
44335389 5082 0 None -46 3 Human 5.1 pKi = 5.1 Binding
Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor
ChEMBL 413 8 0 6 3.8 CCOC(=O)N1CCN(CCCOc2ccc(-c3ccccc3[N+](=O)[O-])cc2)CC1 10.1016/s0960-894x(02)00648-0
CHEMBL105952 5082 0 None -46 3 Human 5.1 pKi = 5.1 Binding
Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor
ChEMBL 413 8 0 6 3.8 CCOC(=O)N1CCN(CCCOc2ccc(-c3ccccc3[N+](=O)[O-])cc2)CC1 10.1016/s0960-894x(02)00648-0
44304243 201500 0 None -562 3 Human 5.1 pKi = 5.1 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 374 13 0 4 4.6 CCCCCC(=O)c1ccc(OCCCN2CCN(CCCC)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL64334 201500 0 None -562 3 Human 5.1 pKi = 5.1 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 374 13 0 4 4.6 CCCCCC(=O)c1ccc(OCCCN2CCN(CCCC)CC2)cc1 10.1016/s0960-894x(02)00309-8
156015041 177648 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method
ChEMBL 1029 30 3 11 10.0 CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acsmedchemlett.0c00033
CHEMBL4637356 177648 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method
ChEMBL 1029 30 3 11 10.0 CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acsmedchemlett.0c00033
CHEMBL4650547 177648 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method
ChEMBL 1029 30 3 11 10.0 CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acsmedchemlett.0c00033
164617783 183997 0 None -1 6 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 388 8 4 4 2.8 CCC(CNC(=O)/N=C(\N)NCCCc1sc(N)nc1C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4848815 183997 0 None -1 6 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 388 8 4 4 2.8 CCC(CNC(=O)/N=C(\N)NCCCc1sc(N)nc1C)c1ccccc1 10.1016/j.ejmech.2021.113190
11393516 5087 0 None -933 4 Human 5.1 pKi = 5.1 Binding
Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor
ChEMBL 335 6 1 4 3.3 N#Cc1ccc(-c2ccc(OCCCN3CCCNCC3)cc2)cc1 10.1016/s0960-894x(02)00648-0
CHEMBL105967 5087 0 None -933 4 Human 5.1 pKi = 5.1 Binding
Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor
ChEMBL 335 6 1 4 3.3 N#Cc1ccc(-c2ccc(OCCCN3CCCNCC3)cc2)cc1 10.1016/s0960-894x(02)00648-0
75306277 108754 0 None -39 23 Human 7.1 pKi = 7.1 Binding
Binding affinity to H2 histamine receptor (unknown origin) by PDSP assayBinding affinity to H2 histamine receptor (unknown origin) by PDSP assay
ChEMBL 308 0 0 3 4.2 CN1CCC2C(C1)c1cccc3c1N2c1ccccc1CS3 10.1039/C2MD00311B
CHEMBL3217984 108754 0 None -39 23 Human 7.1 pKi = 7.1 Binding
Binding affinity to H2 histamine receptor (unknown origin) by PDSP assayBinding affinity to H2 histamine receptor (unknown origin) by PDSP assay
ChEMBL 308 0 0 3 4.2 CN1CCC2C(C1)c1cccc3c1N2c1ccccc1CS3 10.1039/C2MD00311B
44281132 99185 0 None - 1 Guinea pig 6.1 pKi = 6.1 Binding
Evaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atriumEvaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atrium
ChEMBL 288 3 3 6 2.2 Cc1[nH]cnc1-c1cccc(Nc2n[s+]([O-])nc2N)c1 10.1021/jm00356a005
CHEMBL284379 99185 0 None - 1 Guinea pig 6.1 pKi = 6.1 Binding
Evaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atriumEvaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atrium
ChEMBL 288 3 3 6 2.2 Cc1[nH]cnc1-c1cccc(Nc2n[s+]([O-])nc2N)c1 10.1021/jm00356a005
10517956 55947 0 None -66 3 Guinea pig 5.1 pKi = 5.1 Binding
Binding affinity against H2 receptor of Guinea pig atriumBinding affinity against H2 receptor of Guinea pig atrium
ChEMBL 295 5 2 3 3.7 O=C(Nc1ccc2ccccc2c1)OCCCc1c[nH]cn1 10.1021/jm9507688
CHEMBL16274 55947 0 None -66 3 Guinea pig 5.1 pKi = 5.1 Binding
Binding affinity against H2 receptor of Guinea pig atriumBinding affinity against H2 receptor of Guinea pig atrium
ChEMBL 295 5 2 3 3.7 O=C(Nc1ccc2ccccc2c1)OCCCc1c[nH]cn1 10.1021/jm9507688
44304088 200691 0 None -316 3 Human 5.1 pKi = 5.1 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 402 8 0 5 4.0 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)C3CCCCC3)cc2)CC1 10.1016/s0960-894x(02)00309-8
CHEMBL61070 200691 0 None -316 3 Human 5.1 pKi = 5.1 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 402 8 0 5 4.0 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)C3CCCCC3)cc2)CC1 10.1016/s0960-894x(02)00309-8
1269 121 33 None -269 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
37463 121 33 None -269 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL275443 121 33 None -269 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
10062176 55530 0 None -19498 3 Guinea pig 4.1 pKi = 4.1 Binding
Binding affinity against H2 receptor of Guinea pig atriumBinding affinity against H2 receptor of Guinea pig atrium
ChEMBL 279 5 2 3 3.2 O=C(Nc1ccc(Cl)cc1)OCCCc1c[nH]cn1 10.1021/jm9507688
CHEMBL16231 55530 0 None -19498 3 Guinea pig 4.1 pKi = 4.1 Binding
Binding affinity against H2 receptor of Guinea pig atriumBinding affinity against H2 receptor of Guinea pig atrium
ChEMBL 279 5 2 3 3.2 O=C(Nc1ccc(Cl)cc1)OCCCc1c[nH]cn1 10.1021/jm9507688
10541297 57230 0 None -3090 3 Guinea pig 4.1 pKi = 4.1 Binding
Binding affinity against H2 receptor of Guinea pig atriumBinding affinity against H2 receptor of Guinea pig atrium
ChEMBL 287 8 2 3 2.7 O=C(NCCCc1ccccc1)OCCCc1c[nH]cn1 10.1021/jm9507688
CHEMBL16639 57230 0 None -3090 3 Guinea pig 4.1 pKi = 4.1 Binding
Binding affinity against H2 receptor of Guinea pig atriumBinding affinity against H2 receptor of Guinea pig atrium
ChEMBL 287 8 2 3 2.7 O=C(NCCCc1ccccc1)OCCCc1c[nH]cn1 10.1021/jm9507688
10708894 98167 0 None -6025 3 Guinea pig 4.1 pKi = 4.1 Binding
Binding affinity against H2 receptor of Guinea pig atriumBinding affinity against H2 receptor of Guinea pig atrium
ChEMBL 293 6 2 3 2.9 O=C(NCc1ccc(Cl)cc1)OCCCc1c[nH]cn1 10.1021/jm9507688
CHEMBL277149 98167 0 None -6025 3 Guinea pig 4.1 pKi = 4.1 Binding
Binding affinity against H2 receptor of Guinea pig atriumBinding affinity against H2 receptor of Guinea pig atrium
ChEMBL 293 6 2 3 2.9 O=C(NCc1ccc(Cl)cc1)OCCCc1c[nH]cn1 10.1021/jm9507688
44304090 201252 0 None -16982 3 Human 4.1 pKi = 4.1 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 360 8 0 5 2.8 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00309-8
CHEMBL62948 201252 0 None -16982 3 Human 4.1 pKi = 4.1 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 360 8 0 5 2.8 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00309-8
44304067 199588 0 None -34673 3 Human 4.1 pKi = 4.1 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 359 9 1 5 1.4 CNCC(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL60401 199588 0 None -34673 3 Human 4.1 pKi = 4.1 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 359 9 1 5 1.4 CNCC(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
168281746 192270 0 None -676 6 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 365 6 4 5 1.6 CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5184911 192270 0 None -676 6 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 365 6 4 5 1.6 CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5221974 192270 0 None -676 6 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis
ChEMBL 365 6 4 5 1.6 CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1 10.1021/acs.jmedchem.1c00692
75201901 165861 14 None -588 24 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4277264 165861 14 None -588 24 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4448899 212178 40 None - 1 Human 5.1 pKi = 5.1 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000307b HRH2Selectivity interaction (GPCR panel (PDSP screen)) EUB0000307b HRH2
ChEMBL None None None Cc1c(NC(=O)c2cc(C(N)=O)nc3cc(F)ccc23)c(C(F)(F)F)nn1Cc1ccc(C#N)cc1 nan
21509921 103966 0 None -7 24 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104091 103966 0 None -7 24 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
21509921 103966 0 None -7 24 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104091 103966 0 None -7 24 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
44304270 199553 0 None -512 3 Human 5.1 pKi = 5.1 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 442 11 0 5 5.0 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3ccc(C)s3)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL60383 199553 0 None -512 3 Human 5.1 pKi = 5.1 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 442 11 0 5 5.0 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3ccc(C)s3)CC2)cc1 10.1016/s0960-894x(02)00309-8
130442480 174688 0 None -100 24 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
CHEMBL4572614 174688 0 None -100 24 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
1210 903 45 None -281 21 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
1213 903 45 None -281 21 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
2725 903 45 None -281 21 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
33036 903 45 None -281 21 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
4411 903 45 None -281 21 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
616 903 45 None -281 21 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
6976 903 45 None -281 21 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
716121 903 45 None -281 21 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
90475904 903 45 None -281 21 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL1201353 903 45 None -281 21 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL1554789 903 45 None -281 21 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL505 903 45 None -281 21 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
DB01114 903 45 None -281 21 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
DB13679 903 45 None -281 21 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
155539605 172266 0 None -3 6 Human 6.1 pKi = 6.1 Binding
Binding affinity to human histamine 2 receptor expressed in HEK cells by radioligand binding assayBinding affinity to human histamine 2 receptor expressed in HEK cells by radioligand binding assay
ChEMBL 313 1 0 4 2.1 CC1=NC2(CCN(C)CC2)C(=O)N(c2c(C)cccc2C)C1=O 10.1016/j.ejmech.2018.12.048
CHEMBL4514672 172266 0 None -3 6 Human 6.1 pKi = 6.1 Binding
Binding affinity to human histamine 2 receptor expressed in HEK cells by radioligand binding assayBinding affinity to human histamine 2 receptor expressed in HEK cells by radioligand binding assay
ChEMBL 313 1 0 4 2.1 CC1=NC2(CCN(C)CC2)C(=O)N(c2c(C)cccc2C)C1=O 10.1016/j.ejmech.2018.12.048
44582705 186403 0 None -181 14 Human 6.1 pKi = 6.1 Binding
Inhibition of human cloned histamine H2 receptor by competitive binding experimentInhibition of human cloned histamine H2 receptor by competitive binding experiment
ChEMBL 399 9 0 4 4.5 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(C)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL490632 186403 0 None -181 14 Human 6.1 pKi = 6.1 Binding
Inhibition of human cloned histamine H2 receptor by competitive binding experimentInhibition of human cloned histamine H2 receptor by competitive binding experiment
ChEMBL 399 9 0 4 4.5 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(C)cc2)CC1 10.1016/j.bmc.2009.03.021
145973771 164156 0 None 2 7 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]-Iodoaminopotentidine from human histamine H2 receptor expressed in HEK293T cell membranes after 90 mins by scintillation counting methodDisplacement of [125I]-Iodoaminopotentidine from human histamine H2 receptor expressed in HEK293T cell membranes after 90 mins by scintillation counting method
ChEMBL 797 16 2 7 10.8 CC(C)(C)OC(=O)NCCCCCCn1cc(CCCCN2CCC(c3ccc(-c4cc(C(=O)O)cc5cc(-c6ccc(C(F)(F)F)cc6)ccc45)cc3)CC2)nn1 10.1021/acs.jmedchem.8b00168
CHEMBL4217398 164156 0 None 2 7 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]-Iodoaminopotentidine from human histamine H2 receptor expressed in HEK293T cell membranes after 90 mins by scintillation counting methodDisplacement of [125I]-Iodoaminopotentidine from human histamine H2 receptor expressed in HEK293T cell membranes after 90 mins by scintillation counting method
ChEMBL 797 16 2 7 10.8 CC(C)(C)OC(=O)NCCCCCCn1cc(CCCCN2CCC(c3ccc(-c4cc(C(=O)O)cc5cc(-c6ccc(C(F)(F)F)cc6)ccc45)cc3)CC2)nn1 10.1021/acs.jmedchem.8b00168
44335412 106960 0 None -102 3 Human 5.1 pKi = 5.1 Binding
Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor
ChEMBL 413 8 0 6 3.8 CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc([N+](=O)[O-])cc3)cc2)CC1 10.1016/s0960-894x(02)00648-0
CHEMBL318320 106960 0 None -102 3 Human 5.1 pKi = 5.1 Binding
Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor
ChEMBL 413 8 0 6 3.8 CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc([N+](=O)[O-])cc3)cc2)CC1 10.1016/s0960-894x(02)00648-0
44304284 162716 0 None -208 3 Human 5.1 pKi = 5.1 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 426 9 0 6 3.5 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)c3ccc(OC)cc3)cc2)CC1 10.1016/s0960-894x(02)00309-8
CHEMBL418691 162716 0 None -208 3 Human 5.1 pKi = 5.1 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 426 9 0 6 3.5 CCOC(=O)N1CCN(CCCOc2ccc(C(=O)c3ccc(OC)cc3)cc2)CC1 10.1016/s0960-894x(02)00309-8
44304978 167315 0 None -3890 3 Human 4.1 pKi = 4.1 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 396 11 0 5 2.8 CCCCCC(=O)c1ccc(OCCCN2CCN(S(C)(=O)=O)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL431172 167315 0 None -3890 3 Human 4.1 pKi = 4.1 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 396 11 0 5 2.8 CCCCCC(=O)c1ccc(OCCCN2CCN(S(C)(=O)=O)CC2)cc1 10.1016/s0960-894x(02)00309-8
44304752 201512 0 None -39810 3 Human 4.1 pKi = 4.1 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 459 9 1 6 3.1 C[C@@H](NC(=O)OC(C)(C)C)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL64406 201512 0 None -39810 3 Human 4.1 pKi = 4.1 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 459 9 1 6 3.1 C[C@@H](NC(=O)OC(C)(C)C)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
11496610 4000 11 None -2 2 Human 6.1 pKi = 6.1 Binding
Inhibition of human histamine H2 receptorInhibition of human histamine H2 receptor
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1021/jm801572m
5582 4000 11 None -2 2 Human 6.1 pKi = 6.1 Binding
Inhibition of human histamine H2 receptorInhibition of human histamine H2 receptor
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1021/jm801572m
CHEMBL474991 4000 11 None -2 2 Human 6.1 pKi = 6.1 Binding
Inhibition of human histamine H2 receptorInhibition of human histamine H2 receptor
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1021/jm801572m
73355421 92106 0 None - 1 Human 5.1 pKi = 5.1 Binding
Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay
ChEMBL 309 3 0 3 3.0 CN(Cc1ccc2c(c1)OCO2)[C@H]1C2C3CC4C5C3CC2C5C41 10.1016/j.bmc.2013.07.045
CHEMBL2432062 92106 0 None - 1 Human 5.1 pKi = 5.1 Binding
Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay
ChEMBL 309 3 0 3 3.0 CN(Cc1ccc2c(c1)OCO2)[C@H]1C2C3CC4C5C3CC2C5C41 10.1016/j.bmc.2013.07.045
164620139 185196 0 None 56 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 436 8 4 4 3.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4866734 185196 0 None 56 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method
ChEMBL 436 8 4 4 3.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2021.113190
11846300 79841 3 None -1071 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]APT from human histamine H2 receptor transfected in COS7 cellsDisplacement of [3H]APT from human histamine H2 receptor transfected in COS7 cells
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1 10.1021/jm051008s
CHEMBL213912 79841 3 None -1071 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]APT from human histamine H2 receptor transfected in COS7 cellsDisplacement of [3H]APT from human histamine H2 receptor transfected in COS7 cells
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1 10.1021/jm051008s
137646281 157252 0 None -1995 17 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 423 8 0 7 3.8 COc1ccccc1N1CCN(CCCSc2nnc(-c3ccccc3)n2C)CC1 10.1021/acs.jmedchem.9b00412
CHEMBL4083252 157252 0 None -1995 17 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 423 8 0 7 3.8 COc1ccccc1N1CCN(CCCSc2nnc(-c3ccccc3)n2C)CC1 10.1021/acs.jmedchem.9b00412
657255 197396 29 None -3 15 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 nan
CHEMBL588119 197396 29 None -3 15 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 nan
44304439 102312 0 None -891 3 Human 5.1 pKi = 5.1 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 436 12 0 4 4.6 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)Cc3ccccc3)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL305338 102312 0 None -891 3 Human 5.1 pKi = 5.1 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 436 12 0 4 4.6 CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)Cc3ccccc3)CC2)cc1 10.1016/s0960-894x(02)00309-8
44304332 199649 0 None -19054 3 Human 4.1 pKi = 4.1 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 399 9 1 5 2.3 O=C(c1ccc(OCCCN2CCN(C(=O)C[C@H]3CCCN3)CC2)cc1)C1CC1 10.1016/s0960-894x(02)00310-4
CHEMBL60435 199649 0 None -19054 3 Human 4.1 pKi = 4.1 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 399 9 1 5 2.3 O=C(c1ccc(OCCCN2CCN(C(=O)C[C@H]3CCCN3)CC2)cc1)C1CC1 10.1016/s0960-894x(02)00310-4
44304719 201025 0 None -19498 3 Human 4.1 pKi = 4.1 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 425 10 2 6 1.5 N[C@H](Cc1c[nH]cn1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL61792 201025 0 None -19498 3 Human 4.1 pKi = 4.1 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 425 10 2 6 1.5 N[C@H](Cc1c[nH]cn1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
164435 202827 29 None 2754 2 Guinea pig 8.0 pKi = 8.0 Binding
Inhibition of [125I]APT binding to H2 receptors in guinea pig cerebral membranes.Inhibition of [125I]APT binding to H2 receptors in guinea pig cerebral membranes.
ChEMBL 477 11 4 6 2.5 N#CN/C(=N\CCNC(=O)c1ccc(N)cc1)NCCCOc1cccc(CN2CCCCC2)c1 10.1021/jm00090a013
CHEMBL72844 202827 29 None 2754 2 Guinea pig 8.0 pKi = 8.0 Binding
Inhibition of [125I]APT binding to H2 receptors in guinea pig cerebral membranes.Inhibition of [125I]APT binding to H2 receptors in guinea pig cerebral membranes.
ChEMBL 477 11 4 6 2.5 N#CN/C(=N\CCNC(=O)c1ccc(N)cc1)NCCCOc1cccc(CN2CCCCC2)c1 10.1021/jm00090a013
44334038 4381 0 None -316 3 Human 6.1 pKi = 6.1 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 453 10 1 6 3.0 N#Cc1cccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)c1 10.1016/s0960-894x(02)00685-6
CHEMBL101748 4381 0 None -316 3 Human 6.1 pKi = 6.1 Binding
Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor
ChEMBL 453 10 1 6 3.0 N#Cc1cccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)c1 10.1016/s0960-894x(02)00685-6
10472082 5057 0 None -13489 4 Human 5.0 pKi = 5.0 Binding
Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor
ChEMBL 334 6 0 3 4.9 C[C@@H]1CC[C@@H](C)N1CCCOc1ccc(-c2ccc(C#N)cc2)cc1 10.1016/s0960-894x(02)00648-0
CHEMBL105762 5057 0 None -13489 4 Human 5.0 pKi = 5.0 Binding
Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor
ChEMBL 334 6 0 3 4.9 C[C@@H]1CC[C@@H](C)N1CCCOc1ccc(-c2ccc(C#N)cc2)cc1 10.1016/s0960-894x(02)00648-0
44335558 109568 0 None -933 4 Human 5.0 pKi = 5.0 Binding
Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor
ChEMBL 334 6 0 3 4.7 CC1CCN(CCCOc2ccc(-c3ccc(C#N)cc3)cc2)CC1 10.1016/s0960-894x(02)00648-0
CHEMBL323562 109568 0 None -933 4 Human 5.0 pKi = 5.0 Binding
Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor
ChEMBL 334 6 0 3 4.7 CC1CCN(CCCOc2ccc(-c3ccc(C#N)cc3)cc2)CC1 10.1016/s0960-894x(02)00648-0
56963799 74531 0 None -2290 10 Human 6.0 pKi = 6.0 Binding
Binding affinity to human recombinant H2 receptorBinding affinity to human recombinant H2 receptor
ChEMBL 378 6 0 5 4.6 C[C@@H]1CCCN1CCc1cc2cc(C(=O)c3ccc([N+](=O)[O-])cc3)ccc2o1 10.1021/jm201690h
CHEMBL2031737 74531 0 None -2290 10 Human 6.0 pKi = 6.0 Binding
Binding affinity to human recombinant H2 receptorBinding affinity to human recombinant H2 receptor
ChEMBL 378 6 0 5 4.6 C[C@@H]1CCCN1CCc1cc2cc(C(=O)c3ccc([N+](=O)[O-])cc3)ccc2o1 10.1021/jm201690h
1016 3678 75 None -41 35 Human 5.0 pKi = 5.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2561 3678 75 None -41 35 Human 5.0 pKi = 5.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2733526 3678 75 None -41 35 Human 5.0 pKi = 5.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
5384 3678 75 None -41 35 Human 5.0 pKi = 5.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL83 3678 75 None -41 35 Human 5.0 pKi = 5.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
DB00675 3678 75 None -41 35 Human 5.0 pKi = 5.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
73213196 103968 1 None -8 13 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)
ChEMBL 288 0 0 2 3.9 CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104093 103968 1 None -8 13 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)
ChEMBL 288 0 0 2 3.9 CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1 10.1016/j.bmcl.2013.12.024
100 3733 52 None -46 56 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
2637 3733 52 None -46 56 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
5452 3733 52 None -46 56 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
CHEMBL479 3733 52 None -46 56 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
DB00679 3733 52 None -46 56 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
73213196 103968 1 None -8 13 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)
ChEMBL 288 0 0 2 3.9 CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104093 103968 1 None -8 13 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)
ChEMBL 288 0 0 2 3.9 CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1 10.1016/j.bmcl.2013.12.024
162657344 180340 0 None -1096 3 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysis
ChEMBL 388 8 1 5 4.4 c1ccc(Nc2ccc(OCCCN3CCN(c4ccncc4)CC3)cc2)cc1 10.1016/j.ejmech.2020.113041
CHEMBL4758080 180340 0 None -1096 3 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysis
ChEMBL 388 8 1 5 4.4 c1ccc(Nc2ccc(OCCCN3CCN(c4ccncc4)CC3)cc2)cc1 10.1016/j.ejmech.2020.113041
71459604 83365 0 None -1 14 Human 6.0 pKi = 6.0 Binding
Binding affinity to Histamine H2 receptorBinding affinity to Histamine H2 receptor
ChEMBL 309 4 1 3 2.0 COc1cccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)c1 10.1016/j.bmcl.2012.08.046
CHEMBL2205811 83365 0 None -1 14 Human 6.0 pKi = 6.0 Binding
Binding affinity to Histamine H2 receptorBinding affinity to Histamine H2 receptor
ChEMBL 309 4 1 3 2.0 COc1cccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)c1 10.1016/j.bmcl.2012.08.046
CHEMBL5088914 213776 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C 10.1016/j.bmcl.2021.128388
CHEMBL5095949 213776 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay
ChEMBL None None None Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C 10.1016/j.bmcl.2021.128388
44304223 198695 0 None -1023 3 Human 5.0 pKi = 5.0 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 374 12 0 4 4.5 CCCCCC(=O)c1ccc(OCCCN2CCN(CC(C)C)CC2)cc1 10.1016/s0960-894x(02)00309-8
CHEMBL59798 198695 0 None -1023 3 Human 5.0 pKi = 5.0 Binding
Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor
ChEMBL 374 12 0 4 4.5 CCCCCC(=O)c1ccc(OCCCN2CCN(CC(C)C)CC2)cc1 10.1016/s0960-894x(02)00309-8
133 2450 48 None -141 43 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
1723 2450 48 None -141 43 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
28693 2450 48 None -141 43 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
CHEMBL19215 2450 48 None -141 43 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
DB13520 2450 48 None -141 43 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
44335172 5013 0 None -467 3 Human 4.0 pKi = 4.0 Binding
Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor
ChEMBL 374 7 0 5 4.0 CCOC(=O)N1CCN(CCCOc2ccc(-c3ccsc3)cc2)CC1 10.1016/s0960-894x(02)00648-0
CHEMBL105567 5013 0 None -467 3 Human 4.0 pKi = 4.0 Binding
Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor
ChEMBL 374 7 0 5 4.0 CCOC(=O)N1CCN(CCCOc2ccc(-c3ccsc3)cc2)CC1 10.1016/s0960-894x(02)00648-0
44304311 198599 0 None -16982 3 Human 4.0 pKi = 4.0 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 442 10 1 7 2.2 N[C@H](Cc1nccs1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
CHEMBL59733 198599 0 None -16982 3 Human 4.0 pKi = 4.0 Binding
Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes
ChEMBL 442 10 1 7 2.2 N[C@H](Cc1nccs1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1 10.1016/s0960-894x(02)00310-4
71450548 83372 0 None -7 3 Human 5.0 pKi = 5.0 Binding
Binding affinity to Histamine H2 receptorBinding affinity to Histamine H2 receptor
ChEMBL 295 3 1 3 2.0 COc1cccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)c1 10.1016/j.bmcl.2012.08.046
CHEMBL2205824 83372 0 None -7 3 Human 5.0 pKi = 5.0 Binding
Binding affinity to Histamine H2 receptorBinding affinity to Histamine H2 receptor
ChEMBL 295 3 1 3 2.0 COc1cccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)c1 10.1016/j.bmcl.2012.08.046
127049855 139685 0 None -16 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]tiotidine from human histamine H2 receptor expressed in sf9 cell membrane co-expressing Gsalphas incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]tiotidine from human histamine H2 receptor expressed in sf9 cell membrane co-expressing Gsalphas incubated for 60 mins by liquid scintillation counting method
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@@H]1CC[C@@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3805220 139685 0 None -16 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]tiotidine from human histamine H2 receptor expressed in sf9 cell membrane co-expressing Gsalphas incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]tiotidine from human histamine H2 receptor expressed in sf9 cell membrane co-expressing Gsalphas incubated for 60 mins by liquid scintillation counting method
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@@H]1CC[C@@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
132060763 162299 0 None -3 8 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 405 5 0 4 4.1 C=C(C)CN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)CC3)CC1 10.1016/j.ejmech.2018.02.024
CHEMBL4173095 162299 0 None -3 8 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 405 5 0 4 4.1 C=C(C)CN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)CC3)CC1 10.1016/j.ejmech.2018.02.024
135 2486 38 None -39 58 Human 6.0 pKi = 6 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
1796 2486 38 None -39 58 Human 6.0 pKi = 6 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
4184 2486 38 None -39 58 Human 6.0 pKi = 6 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
CHEMBL6437 2486 38 None -39 58 Human 6.0 pKi = 6 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
DB06148 2486 38 None -39 58 Human 6.0 pKi = 6 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
2281 3114 76 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro
Drug Central 334 10 2 3 2.3 CCCN(C(=O)C(NC(=O)c1ccccc1)CCC(=O)O)CCC None
4922 3114 76 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro
Drug Central 334 10 2 3 2.3 CCCN(C(=O)C(NC(=O)c1ccccc1)CCC(=O)O)CCC None
893 3114 76 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro
Drug Central 334 10 2 3 2.3 CCCN(C(=O)C(NC(=O)c1ccccc1)CCC(=O)O)CCC None
CHEMBL316561 3114 76 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro
Drug Central 334 10 2 3 2.3 CCCN(C(=O)C(NC(=O)c1ccccc1)CCC(=O)O)CCC None
DB13431 3114 76 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro
Drug Central 334 10 2 3 2.3 CCCN(C(=O)C(NC(=O)c1ccccc1)CCC(=O)O)CCC None
1231 922 112 None -2 8 Human 8.2 pKd = 8.2 Binding
NoneNone
Drug Central 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C None
2756 922 112 None -2 8 Human 8.2 pKd = 8.2 Binding
NoneNone
Drug Central 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C None
645 922 112 None -2 8 Human 8.2 pKd = 8.2 Binding
NoneNone
Drug Central 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C None
CHEMBL30 922 112 None -2 8 Human 8.2 pKd = 8.2 Binding
NoneNone
Drug Central 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C None
DB00501 922 112 None -2 8 Human 8.2 pKd = 8.2 Binding
NoneNone
Drug Central 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C None
1231 922 112 None -2 8 Guinea pig 8.2 pKd = 8.2 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
Drug Central 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C None
2756 922 112 None -2 8 Guinea pig 8.2 pKd = 8.2 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
Drug Central 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C None
645 922 112 None -2 8 Guinea pig 8.2 pKd = 8.2 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
Drug Central 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C None
CHEMBL30 922 112 None -2 8 Guinea pig 8.2 pKd = 8.2 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
Drug Central 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C None
DB00501 922 112 None -2 8 Guinea pig 8.2 pKd = 8.2 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
Drug Central 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C None
1234 3227 0 None -2 7 Human 8.2 pKd = 8.2 Binding
NoneNone
Drug Central 314 10 2 7 1.5 CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C None
3001055 3227 0 None -2 7 Human 8.2 pKd = 8.2 Binding
NoneNone
Drug Central 314 10 2 7 1.5 CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C None
CHEMBL512 3227 0 None -2 7 Human 8.2 pKd = 8.2 Binding
NoneNone
Drug Central 314 10 2 7 1.5 CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C None
DB00863 3227 0 None -2 7 Human 8.2 pKd = 8.2 Binding
NoneNone
Drug Central 314 10 2 7 1.5 CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C None
3033637 215982 0 None - 1 Human 8.2 pKd = 8.2 Binding
NoneNone
Drug Central 331 10 2 8 1.3 CNC(NCCSCC1=CSC(CN(C)C)=N1)=C[N+]([O-])=O None
1129 1584 89 None -1 2 Guinea pig 8.2 pKd = 8.2 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
Drug Central 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N None
3325 1584 89 None -1 2 Guinea pig 8.2 pKd = 8.2 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
Drug Central 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N None
5353622 1584 89 None -1 2 Guinea pig 8.2 pKd = 8.2 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
Drug Central 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N None
5702160 1584 89 None -1 2 Guinea pig 8.2 pKd = 8.2 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
Drug Central 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N None
7074 1584 89 None -1 2 Guinea pig 8.2 pKd = 8.2 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
Drug Central 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N None
CHEMBL902 1584 89 None -1 2 Guinea pig 8.2 pKd = 8.2 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
Drug Central 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N None
DB00927 1584 89 None -1 2 Guinea pig 8.2 pKd = 8.2 Binding
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
Drug Central 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N None
1234 3227 0 None 1 7 Guinea pig 8.1 pKd = 8.1 Binding
Compound was evaluated in vitro inhibitory activity against histamine H2 receptor in isolated Guinea pig right atria.Compound was evaluated in vitro inhibitory activity against histamine H2 receptor in isolated Guinea pig right atria.
Drug Central 314 10 2 7 1.5 CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C None
3001055 3227 0 None 1 7 Guinea pig 8.1 pKd = 8.1 Binding
Compound was evaluated in vitro inhibitory activity against histamine H2 receptor in isolated Guinea pig right atria.Compound was evaluated in vitro inhibitory activity against histamine H2 receptor in isolated Guinea pig right atria.
Drug Central 314 10 2 7 1.5 CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C None
CHEMBL512 3227 0 None 1 7 Guinea pig 8.1 pKd = 8.1 Binding
Compound was evaluated in vitro inhibitory activity against histamine H2 receptor in isolated Guinea pig right atria.Compound was evaluated in vitro inhibitory activity against histamine H2 receptor in isolated Guinea pig right atria.
Drug Central 314 10 2 7 1.5 CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C None
DB00863 3227 0 None 1 7 Guinea pig 8.1 pKd = 8.1 Binding
Compound was evaluated in vitro inhibitory activity against histamine H2 receptor in isolated Guinea pig right atria.Compound was evaluated in vitro inhibitory activity against histamine H2 receptor in isolated Guinea pig right atria.
Drug Central 314 10 2 7 1.5 CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C None
5105 176243 49 None -1 2 Human 8.1 pKd = 8.1 Binding
NoneNone
Drug Central 348 9 1 5 2.1 CC(=O)OCC(=O)NCCCOc1cccc(CN2CCCCC2)c1 None
CHEMBL46102 176243 49 None -1 2 Human 8.1 pKd = 8.1 Binding
NoneNone
Drug Central 348 9 1 5 2.1 CC(=O)OCC(=O)NCCCOc1cccc(CN2CCCCC2)c1 None
1129 1584 89 None 1 2 Human 8.1 pKd = 8.1 Binding
NoneNone
Drug Central 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N None
3325 1584 89 None 1 2 Human 8.1 pKd = 8.1 Binding
NoneNone
Drug Central 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N None
5353622 1584 89 None 1 2 Human 8.1 pKd = 8.1 Binding
NoneNone
Drug Central 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N None
5702160 1584 89 None 1 2 Human 8.1 pKd = 8.1 Binding
NoneNone
Drug Central 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N None
7074 1584 89 None 1 2 Human 8.1 pKd = 8.1 Binding
NoneNone
Drug Central 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N None
CHEMBL902 1584 89 None 1 2 Human 8.1 pKd = 8.1 Binding
NoneNone
Drug Central 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N None
DB00927 1584 89 None 1 2 Human 8.1 pKd = 8.1 Binding
NoneNone
Drug Central 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N None
1235 3751 32 None -3 5 Human 8.2 pKd = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 6 4 6 -0.1 N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N 12869657
3959 3751 32 None -3 5 Human 8.2 pKd = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 6 4 6 -0.1 N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N 12869657
50287 3751 32 None -3 5 Human 8.2 pKd = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 6 4 6 -0.1 N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N 12869657
CHEMBL269646 3751 32 None -3 5 Human 8.2 pKd = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 6 4 6 -0.1 N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N 12869657
None 214377 0 3H-Histamine -6 3 Guinea pig 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 139 3 2 2 0.6 CC(CC1=CN=CN1)NC None
None 214378 0 3H-Histamine -6 3 Guinea pig 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 139 2 2 2 0.9 CC(C1=CN=CN1)C(C)N None
565544 109242 9 3H-Histamine -1 3 Guinea pig 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 125 2 2 2 0.5 CC(CN)c1cnc[nH]1 None
CHEMBL322988 109242 9 3H-Histamine -1 3 Guinea pig 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 125 2 2 2 0.5 CC(CN)c1cnc[nH]1 None
None 214362 0 3H-Histamine -8 7 Guinea pig 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 125 2 2 2 0.3 CC(CC1=CN=CN1)N None
1204 1893 114 3H-Histamine -794 25 Guinea pig 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1893 114 3H-Histamine -794 25 Guinea pig 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1893 114 3H-Histamine -794 25 Guinea pig 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1893 114 3H-Histamine -794 25 Guinea pig 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1893 114 3H-Histamine -794 25 Guinea pig 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1893 114 3H-Histamine -794 25 Guinea pig 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
202 1475 0 UNDEFINED -9 33 Guinea pig 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
60835 1475 0 UNDEFINED -9 33 Guinea pig 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
972 1475 0 UNDEFINED -9 33 Guinea pig 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
CHEMBL1175 1475 0 UNDEFINED -9 33 Guinea pig 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
DB00476 1475 0 UNDEFINED -9 33 Guinea pig 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
46222048 8881 0 UNDEFINED -4365 13 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 260 4 1 2 4.0 CC(C)(C)c1ccc(SCCc2c[nH]cn2)cc1 None
CHEMBL1098230 8881 0 UNDEFINED -4365 13 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 260 4 1 2 4.0 CC(C)(C)c1ccc(SCCc2c[nH]cn2)cc1 None
5656 201368 82 UNDEFINED -7 43 Guinea pig 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 None
CHEMBL637 201368 82 UNDEFINED -7 43 Guinea pig 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 None
54841 201428 51 UNDEFINED -1 30 Guinea pig 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 255 6 1 2 3.7 CNCC[C@@H](Oc1ccccc1C)c1ccccc1 None
CHEMBL641 201428 51 UNDEFINED -1 30 Guinea pig 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 255 6 1 2 3.7 CNCC[C@@H](Oc1ccccc1C)c1ccccc1 None
1269 121 33 3H-TIOTIDINE -338 4 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 None
37463 121 33 3H-TIOTIDINE -338 4 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 None
CHEMBL275443 121 33 3H-TIOTIDINE -338 4 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 None
179 396 107 3H-TIOTIDINE -4365 51 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2159 396 107 3H-TIOTIDINE -4365 51 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
963 396 107 3H-TIOTIDINE -4365 51 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
CHEMBL243712 396 107 3H-TIOTIDINE -4365 51 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
DB06288 396 107 3H-TIOTIDINE -4365 51 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
242 467 117 3H-TIOTIDINE -7244 52 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 467 117 3H-TIOTIDINE -7244 52 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 467 117 3H-TIOTIDINE -7244 52 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 467 117 3H-TIOTIDINE -7244 52 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 467 117 3H-TIOTIDINE -7244 52 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
1231 922 112 3H-Histamine -2 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C None
2756 922 112 3H-Histamine -2 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C None
645 922 112 3H-Histamine -2 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C None
CHEMBL30 922 112 3H-Histamine -2 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C None
DB00501 922 112 3H-Histamine -2 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C None
1248 1391 27 3H-TIOTIDINE -338 7 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 161 4 2 3 0.6 CN(CCCSC(=N)N)C None
3077 1391 27 3H-TIOTIDINE -338 7 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 161 4 2 3 0.6 CN(CCCSC(=N)N)C None
90045 1391 27 3H-TIOTIDINE -338 7 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 161 4 2 3 0.6 CN(CCCSC(=N)N)C None
CHEMBL12344 1391 27 3H-TIOTIDINE -338 7 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 161 4 2 3 0.6 CN(CCCSC(=N)N)C None
1204 1893 114 3H-TIOTIDINE -794 25 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1204 1893 114 3H-TIOTIDINE -173 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1893 114 3H-TIOTIDINE -794 25 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1893 114 3H-TIOTIDINE -173 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1893 114 3H-TIOTIDINE -794 25 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1893 114 3H-TIOTIDINE -173 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1893 114 3H-TIOTIDINE -794 25 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1893 114 3H-TIOTIDINE -173 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1893 114 3H-TIOTIDINE -794 25 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1893 114 3H-TIOTIDINE -173 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1893 114 3H-TIOTIDINE -794 25 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1893 114 3H-TIOTIDINE -173 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
134 2468 19 3H-TIOTIDINE -8511 68 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2468 19 3H-TIOTIDINE -8511 68 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2468 19 3H-TIOTIDINE -8511 68 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2468 19 3H-TIOTIDINE -8511 68 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2468 19 3H-TIOTIDINE -8511 68 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
15897 2807 0 3H-TIOTIDINE -354 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 2807 0 3H-TIOTIDINE -354 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 2807 0 3H-TIOTIDINE -354 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
2337 3193 72 3H-TIOTIDINE -1122 63 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3193 72 3H-TIOTIDINE -1122 63 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3193 72 3H-TIOTIDINE -1122 63 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3193 72 3H-TIOTIDINE -1122 63 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3193 72 3H-TIOTIDINE -1122 63 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
1234 3227 0 3H-Histamine -2 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 10 2 7 1.5 CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C None
3001055 3227 0 3H-Histamine -2 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 10 2 7 1.5 CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C None
CHEMBL512 3227 0 3H-Histamine -2 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 10 2 7 1.5 CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C None
DB00863 3227 0 3H-Histamine -2 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 10 2 7 1.5 CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C None
6917970 3622 54 3H-TIOTIDINE -2290 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O None
8370 3622 54 3H-TIOTIDINE -2290 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O None
CHEMBL487387 3622 54 3H-TIOTIDINE -2290 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O None
1267 3732 43 125I-aminopotentidine -4168 28 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
1267 3732 43 3H-TIOTIDINE -4168 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
3035905 3732 43 125I-aminopotentidine -4168 28 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
3035905 3732 43 3H-TIOTIDINE -4168 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
CHEMBL260374 3732 43 125I-aminopotentidine -4168 28 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
CHEMBL260374 3732 43 3H-TIOTIDINE -4168 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
1235 3751 32 3H-Histamine -3 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 312 6 4 6 -0.1 N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N None
3959 3751 32 3H-Histamine -3 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 312 6 4 6 -0.1 N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N None
50287 3751 32 3H-Histamine -3 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 312 6 4 6 -0.1 N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N None
CHEMBL269646 3751 32 3H-Histamine -3 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 312 6 4 6 -0.1 N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N None
2662 11264 124 3H-TIOTIDINE -41 31 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 381 3 1 4 3.5 Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1 None
CHEMBL118 11264 124 3H-TIOTIDINE -41 31 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 381 3 1 4 3.5 Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1 None
10297 26890 29 3H-TIOTIDINE -38 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
CHEMBL136560 26890 29 3H-TIOTIDINE -38 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
156391 46522 95 3H-TIOTIDINE -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 COc1ccc2cc([C@H](C)C(=O)O)ccc2c1 None
CHEMBL1200806 46522 95 3H-TIOTIDINE -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 COc1ccc2cc([C@H](C)C(=O)O)ccc2c1 None
CHEMBL154 46522 95 3H-TIOTIDINE -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 COc1ccc2cc([C@H](C)C(=O)O)ccc2c1 None
10624 69942 17 3H-TIOTIDINE -776 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
138543650 69942 17 3H-TIOTIDINE -776 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
CHEMBL194378 69942 17 3H-TIOTIDINE -776 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
2244 93785 96 3H-TIOTIDINE -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 180 2 1 3 1.3 CC(=O)Oc1ccccc1C(=O)O None
CHEMBL25 93785 96 3H-TIOTIDINE -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 180 2 1 3 1.3 CC(=O)Oc1ccccc1C(=O)O None
446220 132985 13 3H-TIOTIDINE -1778 46 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
CHEMBL370805 132985 13 3H-TIOTIDINE -1778 46 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
44208932 140163 6 UNDEFINED -120226 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 475 5 1 3 6.8 Cc1ccc(Cn2nc(C(=O)NC3C4(C)CCC(C4)C3(C)C)cc2-c2ccc(Cl)c(C)c2)cc1 None
CHEMBL381689 140163 6 UNDEFINED -120226 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 475 5 1 3 6.8 Cc1ccc(Cn2nc(C(=O)NC3C4(C)CCC(C4)C3(C)C)cc2-c2ccc(Cl)c(C)c2)cc1 None
1615 167217 22 3H-PYRILAMINE -26 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
1615 167217 22 3H-TIOTIDINE -26 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
CHEMBL43048 167217 22 3H-PYRILAMINE -26 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
CHEMBL43048 167217 22 3H-TIOTIDINE -26 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
12016890 190172 4 3H-TIOTIDINE -16982 12 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 318 4 1 3 2.6 NC(=O)c1ccc(F)c2c1CC(N(C1CCC1)C1CCC1)CO2 None
CHEMBL5183389 190172 4 3H-TIOTIDINE -16982 12 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 318 4 1 3 2.6 NC(=O)c1ccc(F)c2c1CC(N(C1CCC1)C1CCC1)CO2 None
54676228 192864 108 3H-TIOTIDINE -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 2 2 5 1.6 CN1C(C(=O)Nc2ccccn2)=C(O)c2ccccc2S1(=O)=O None
CHEMBL527 192864 108 3H-TIOTIDINE -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 2 2 5 1.6 CN1C(C(=O)Nc2ccccn2)=C(O)c2ccccc2S1(=O)=O None
4495 194850 87 3H-TIOTIDINE -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 308 5 1 5 2.8 CS(=O)(=O)Nc1ccc([N+](=O)[O-])cc1Oc1ccccc1 None
CHEMBL56367 194850 87 3H-TIOTIDINE -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 308 5 1 5 2.8 CS(=O)(=O)Nc1ccc([N+](=O)[O-])cc1Oc1ccccc1 None
54677470 198857 110 3H-TIOTIDINE -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 2 2 6 2.0 Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1 None
CHEMBL1256873 198857 110 3H-TIOTIDINE -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 2 2 6 2.0 Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1 None
CHEMBL599 198857 110 3H-TIOTIDINE -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 2 2 6 2.0 Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1 None
162265 200578 19 3H-TIOTIDINE -239 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
4786 200578 19 3H-TIOTIDINE -239 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
CHEMBL61006 200578 19 3H-TIOTIDINE -239 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
1973 201781 12 3H-APT -3 37 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
CHEMBL1394464 201781 12 3H-APT -3 37 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
CHEMBL66089 201781 12 3H-APT -3 37 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
4054 203780 64 3H-TIOTIDINE -1 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
CHEMBL1699 203780 64 3H-TIOTIDINE -1 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
CHEMBL807 203780 64 3H-TIOTIDINE -1 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
11954224 214164 0 3H-TIOTIDINE -141253 60 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
None 214207 0 I125- Tiotodine -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 329 2 0 4 3.6 CC1=NC=CN1CC2CCC3=C(C2=O)C4=CC=CC=C4N3C.Cl None
104911 214239 0 3H-TIOTIDINE -41686 38 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 530 7 0 5 5.1 COC1=CC=CC=C1N2CCN(CC2)CCN(C3=CC=CC=N3)C(=O)C4CCCCC4.Cl.Cl.Cl None
104911 214239 0 3H-TIOTIDINE -41686 38 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 530 7 0 5 5.1 COC1=CC=CC=C1N2CCN(CC2)CCN(C3=CC=CC=N3)C(=O)C4CCCCC4.Cl.Cl.Cl None
25137849 214415 0 3H-TIOTIDINE -4 41 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
71290 214415 0 3H-TIOTIDINE -4 41 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
3337 214431 0 3H-TIOTIDINE -1513 41 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
65801 214431 0 3H-TIOTIDINE -1513 41 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
66264 214431 0 3H-TIOTIDINE -1513 41 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
91452 214431 0 3H-TIOTIDINE -1513 41 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
3821 214539 0 3H-TIOTIDINE -1 18 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 237 2 1 2 2.9 CNC1(CCCCC1=O)C2=CC=CC=C2Cl None
None 214550 0 3H-TIOTIDINE -1 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 240 7 4 6 -0.8 C(C(C(=O)O)N)SSCC(C(=O)O)N None
None 214551 0 3H-TIOTIDINE -1 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 4 2 3 0.2 CSCCC(C(=O)O)N None
None 214552 0 3H-TIOTIDINE -1 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 135 3 3 3 -0.3 C(CS)C(C(=O)O)N None
None 214553 0 3H-TIOTIDINE -1 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 121 2 3 3 -0.7 C(C(C(=O)O)N)S None
None 214554 0 3H-TIOTIDINE -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 117 0 1 3 -0.0 C1CSC(=O)C1N None
None 214555 0 3H-TIOTIDINE -1 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 3 3 3 -1.4 C(C(C(=O)O)N)S(=O)O None
None 214556 0 3H-TIOTIDINE -1 39 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 3 3 4 -1.7 C(C(C(=O)O)N)S(=O)(=O)O None
None 214564 0 3H-TIOTIDINE -13 41 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 2 1 2 1.2 CC(C(=O)C1=CC=CC=C1)N None
1576 214565 0 3H-TIOTIDINE -16 41 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 163 3 1 2 1.5 CC(C(=O)C1=CC=CC=C1)NC None
135269 214629 0 3H-TIOTIDINE -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 222 5 1 3 2.5 CCCCC(=O)OC1=CC=CC=C1C(=O)O None
23681059 214630 0 3H-TIOTIDINE -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 CC(C1=CC2=C(C=C1)C=C(C=C2)OC)C(=O)O None
5018304 214631 0 3H-TIOTIDINE -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 317 4 1 3 0.0 C1=CC=C(C(=C1)CC(=O)[O-])NC2=C(C=CC=C2Cl)Cl.[Na+] None
3672 214632 0 3H-TIOTIDINE -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 206 4 1 1 3.1 CC(C)CC1=CC=C(C=C1)C(C)C(=O)O None
84003 214633 0 3H-TIOTIDINE -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 376 6 5 7 -0.0 C1CN2C(=CC=C2C(=O)C3=CC=CC=C3)C1C(=O)O.C(C(CO)(CO)N)O None
123619 214634 0 3H-TIOTIDINE -1412 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 358 3 0 4 4.2 CC1=NC=C(C=C1)C2=NC=C(C=C2C3=CC=C(C=C3)S(=O)(=O)C)Cl None
119828 214635 0 3H-TIOTIDINE -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 370 5 1 5 3.5 CCC(=O)NS(=O)(=O)C1=CC=C(C=C1)C2=C(ON=C2C3=CC=CC=C3)C None
5090 214636 0 3H-TIOTIDINE -1348 31 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 3 0 4 2.6 CS(=O)(=O)C1=CC=C(C=C1)C2=C(C(=O)OC2)C3=CC=CC=C3 None
119607 214637 0 3H-TIOTIDINE -97 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 3 1 4 3.0 CC1=C(C(=NO1)C2=CC=CC=C2)C3=CC=C(C=C3)S(=O)(=O)N None
None 214638 0 3H-TIOTIDINE -7 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 517 8 2 5 5.2 CC1=C(C2=C(N1C(=O)C3=CC=C(C=C3)Cl)C=CC(=C2)OC)CC(=O)NCCC4=CC=C(C=C4)NC(=O)C None
None 214693 0 Functional -660 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 322 5 2 3 4.1 CC(CC1=CNC2=C1C=C(C=C2)OCC3=CC=CS3)N.Cl None
None 214693 0 UNDEFINED -660 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 322 5 2 3 4.1 CC(CC1=CNC2=C1C=C(C=C2)OCC3=CC=CS3)N.Cl None
None 214737 0 3H-TIOTIDINE -4570 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 347 6 0 3 5.0 CC(=O)N(CC1=CC=CC=C1OC)C2=CC=CC=C2OC3=CC=CC=C3 None
None 214742 0 125I-aminopotentidine -10471285 17 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 372 2 1 3 4.4 CC(C)(C)C1=CC=C(C=C1)NC(=O)N2CCN(CC2)C3=C(C=CC=N3)Cl None
None 214743 0 125I-aminopotentidine -1 14 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 399 7 4 5 1.8 CN(C)CC(C1=CC=C(C=C1)O)C2(CCCCC2)O.C(CC(=O)O)C(=O)O.O None
None 215331 0 UNDEFINED -3467 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 463 4 1 4 3.7 C1C(C(=NN1C(=NS(=O)(=O)C2=CC=C(C=C2)C#N)N)C3=CC=C(C=C3)Cl)C4=CC=CC=C4 None
1353 1872 85 3H-TIOTIDINE -131 86 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1872 85 3H-TIOTIDINE -131 86 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1872 85 3H-TIOTIDINE -131 86 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1872 85 3H-TIOTIDINE -131 86 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1872 85 3H-TIOTIDINE -131 86 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1129 1584 89 3H-TIOTIDINE -1 2 Guinea pig 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N None
3325 1584 89 3H-TIOTIDINE -1 2 Guinea pig 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N None
5353622 1584 89 3H-TIOTIDINE -1 2 Guinea pig 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N None
5702160 1584 89 3H-TIOTIDINE -1 2 Guinea pig 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N None
7074 1584 89 3H-TIOTIDINE -1 2 Guinea pig 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N None
CHEMBL902 1584 89 3H-TIOTIDINE -1 2 Guinea pig 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N None
DB00927 1584 89 3H-TIOTIDINE -1 2 Guinea pig 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 337 7 4 6 -0.8 NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N None
2389 3267 114 3H-TIOTIDINE -346 68 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3267 114 3H-TIOTIDINE -346 68 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3267 114 3H-TIOTIDINE -346 68 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3267 114 3H-TIOTIDINE -346 68 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3267 114 3H-TIOTIDINE -346 68 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
115237 55281 113 3H-TIOTIDINE -123 55 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 55281 113 3H-TIOTIDINE -123 55 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
100 3733 52 3H-TIOTIDINE -46 56 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3733 52 3H-TIOTIDINE -46 56 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3733 52 3H-TIOTIDINE -46 56 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3733 52 3H-TIOTIDINE -46 56 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3733 52 3H-TIOTIDINE -46 56 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
1204 1893 114 3H-Histamine -173 25 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1893 114 3H-Histamine -173 25 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1893 114 3H-Histamine -173 25 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1893 114 3H-Histamine -173 25 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1893 114 3H-Histamine -173 25 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1893 114 3H-Histamine -173 25 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1235 3751 32 125I-iodoaminopotentidine -3 5 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 312 6 4 6 -0.1 N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N None
3959 3751 32 125I-iodoaminopotentidine -3 5 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 312 6 4 6 -0.1 N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N None
50287 3751 32 125I-iodoaminopotentidine -3 5 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 312 6 4 6 -0.1 N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N None
CHEMBL269646 3751 32 125I-iodoaminopotentidine -3 5 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 312 6 4 6 -0.1 N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N None
135398737 942 89 3H-TIOTIDINE -64 92 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 942 89 3H-TIOTIDINE -64 92 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 942 89 3H-TIOTIDINE -64 92 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 942 89 3H-TIOTIDINE -64 92 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 942 89 3H-TIOTIDINE -64 92 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1204 1893 114 3H-TIOTIDINE -316 25 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1893 114 3H-TIOTIDINE -316 25 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1893 114 3H-TIOTIDINE -316 25 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1893 114 3H-TIOTIDINE -316 25 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1893 114 3H-TIOTIDINE -316 25 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1893 114 3H-TIOTIDINE -316 25 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
2726 904 64 3H-TIOTIDINE -85 73 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 904 64 3H-TIOTIDINE -85 73 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 904 64 3H-TIOTIDINE -85 73 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 904 64 3H-TIOTIDINE -85 73 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 904 64 3H-TIOTIDINE -85 73 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
46780481 107032 18 3H-TIOTIDINE -21 54 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 107032 18 3H-TIOTIDINE -21 54 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 107032 18 3H-TIOTIDINE -21 54 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 107032 18 3H-TIOTIDINE -21 54 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
1613 2306 44 3H-TIOTIDINE -10 45 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2306 44 3H-TIOTIDINE -10 45 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2306 44 3H-TIOTIDINE -10 45 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2306 44 3H-TIOTIDINE -10 45 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2306 44 3H-TIOTIDINE -10 45 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
21830793 91389 5 3H-8-OH-DPAT -14125 46 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 None
CHEMBL2413154 91389 5 3H-8-OH-DPAT -14125 46 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 None
None 214492 0 125I-aminopotentidine -1905 21 Guinea pig 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 416 9 3 4 2.8 C1=CC(=CC=C1CCNC(N)SCCCC2=CN=CN2)I None
1226 1980 16 3H-Histamine -7 7 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C None
41376 1980 16 3H-Histamine -7 7 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C None
CHEMBL12608 1980 16 3H-Histamine -7 7 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C None
1248 1391 27 125I-iodoaminopotentidine -123 7 Human 4.6 pKi = 4.6 Binding
NoneNone
PDSP KiDatabase 161 4 2 3 0.6 CN(CCCSC(=N)N)C None
3077 1391 27 125I-iodoaminopotentidine -123 7 Human 4.6 pKi = 4.6 Binding
NoneNone
PDSP KiDatabase 161 4 2 3 0.6 CN(CCCSC(=N)N)C None
90045 1391 27 125I-iodoaminopotentidine -123 7 Human 4.6 pKi = 4.6 Binding
NoneNone
PDSP KiDatabase 161 4 2 3 0.6 CN(CCCSC(=N)N)C None
CHEMBL12344 1391 27 125I-iodoaminopotentidine -123 7 Human 4.6 pKi = 4.6 Binding
NoneNone
PDSP KiDatabase 161 4 2 3 0.6 CN(CCCSC(=N)N)C None
119570 3098 90 3H-TIOTIDINE -281 40 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2233 3098 90 3H-TIOTIDINE -281 40 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
953 3098 90 3H-TIOTIDINE -281 40 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
CHEMBL301265 3098 90 3H-TIOTIDINE -281 40 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
DB00413 3098 90 3H-TIOTIDINE -281 40 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
3032915 15306 20 3H-TIOTIDINE -51 7 Guinea pig 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 212 5 3 2 1.2 C/N=C(\S)NCCCCc1c[nH]cn1 None
CHEMBL12160 15306 20 3H-TIOTIDINE -51 7 Guinea pig 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 212 5 3 2 1.2 C/N=C(\S)NCCCCc1c[nH]cn1 None
1248 1391 27 3H-Histamine -123 7 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 161 4 2 3 0.6 CN(CCCSC(=N)N)C None
3077 1391 27 3H-Histamine -123 7 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 161 4 2 3 0.6 CN(CCCSC(=N)N)C None
90045 1391 27 3H-Histamine -123 7 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 161 4 2 3 0.6 CN(CCCSC(=N)N)C None
CHEMBL12344 1391 27 3H-Histamine -123 7 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 161 4 2 3 0.6 CN(CCCSC(=N)N)C None
213 3780 50 3H-TIOTIDINE -12 44 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
2717 3780 50 3H-TIOTIDINE -12 44 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
5533 3780 50 3H-TIOTIDINE -12 44 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
CHEMBL621 3780 50 3H-TIOTIDINE -12 44 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
DB00656 3780 50 3H-TIOTIDINE -12 44 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
1235 3751 32 3H-TIOTIDINE 1 5 Guinea pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 6 4 6 -0.1 N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N None
3959 3751 32 3H-TIOTIDINE 1 5 Guinea pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 6 4 6 -0.1 N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N None
50287 3751 32 3H-TIOTIDINE 1 5 Guinea pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 6 4 6 -0.1 N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N None
CHEMBL269646 3751 32 3H-TIOTIDINE 1 5 Guinea pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 6 4 6 -0.1 N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N None
135409468 1996 63 3H-TIOTIDINE -123 40 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
333 1996 63 3H-TIOTIDINE -123 40 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
CHEMBL845 1996 63 3H-TIOTIDINE -123 40 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
2865 4064 67 3H-TIOTIDINE -281 54 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4064 67 3H-TIOTIDINE -281 54 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4064 67 3H-TIOTIDINE -281 54 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4064 67 3H-TIOTIDINE -281 54 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4064 67 3H-TIOTIDINE -281 54 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
62865 1243 0 3H-Cimetidine -128 15 Guinea pig 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
746 1243 0 3H-Cimetidine -128 15 Guinea pig 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
84 1243 0 3H-Cimetidine -128 15 Guinea pig 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
CHEMBL2104153 1243 0 3H-Cimetidine -128 15 Guinea pig 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
DB09000 1243 0 3H-Cimetidine -128 15 Guinea pig 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
3032915 15306 20 3H-Histamine -25 7 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 212 5 3 2 1.2 C/N=C(\S)NCCCCc1c[nH]cn1 None
CHEMBL12160 15306 20 3H-Histamine -25 7 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 212 5 3 2 1.2 C/N=C(\S)NCCCCc1c[nH]cn1 None
1234 3227 0 3H-TIOTIDINE 1 7 Guinea pig 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 314 10 2 7 1.5 CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C None
3001055 3227 0 3H-TIOTIDINE 1 7 Guinea pig 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 314 10 2 7 1.5 CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C None
CHEMBL512 3227 0 3H-TIOTIDINE 1 7 Guinea pig 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 314 10 2 7 1.5 CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C None
DB00863 3227 0 3H-TIOTIDINE 1 7 Guinea pig 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 314 10 2 7 1.5 CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C None
3032915 15306 20 125I-iodoaminopotentidine -25 7 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 212 5 3 2 1.2 C/N=C(\S)NCCCCc1c[nH]cn1 None
CHEMBL12160 15306 20 125I-iodoaminopotentidine -25 7 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 212 5 3 2 1.2 C/N=C(\S)NCCCCc1c[nH]cn1 None
1204 1893 114 None -173 25 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1893 114 None -173 25 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1893 114 None -173 25 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1893 114 None -173 25 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1893 114 None -173 25 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1893 114 None -173 25 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
18609376 202646 61 None - 1 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 386 2 0 4 4.7 CC(=O)O[C@]1(C(C)=O)CC[C@H]2[C@@H]3C[C@H](C)C4=CC(=O)CC[C@]4(C)[C@H]3CC[C@@]21C None
6279 202646 61 None - 1 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 386 2 0 4 4.7 CC(=O)O[C@]1(C(C)=O)CC[C@H]2[C@@H]3C[C@H](C)C4=CC(=O)CC[C@]4(C)[C@H]3CC[C@@]21C None
CHEMBL717 202646 61 None - 1 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 386 2 0 4 4.7 CC(=O)O[C@]1(C(C)=O)CC[C@H]2[C@@H]3C[C@H](C)C4=CC(=O)CC[C@]4(C)[C@H]3CC[C@@]21C None
3823 49936 38 None -66 11 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 None
76973198 49936 38 None -66 11 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 None
CHEMBL157101 49936 38 None -66 11 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 None
104903 56035 14 None -5 6 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 624 6 0 8 5.5 C[C@@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)C3=CC[C@]2(C)[C@H]1C(=O)CN1CCN(c2cc(N3CCCC3)nc(N3CCCC3)n2)CC1 None
CHEMBL1630578 56035 14 None -5 6 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 624 6 0 8 5.5 C[C@@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)C3=CC[C@]2(C)[C@H]1C(=O)CN1CCN(c2cc(N3CCCC3)nc(N3CCCC3)n2)CC1 None
5048 3072 57 None -114 7 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 None
8924 3072 57 None -114 7 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 None
9948102 3072 57 None -114 7 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 None
CHEMBL462605 3072 57 None -114 7 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 None
DB11642 3072 57 None -114 7 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 None
176 394 63 None -6 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2157 394 63 None -6 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2566 394 63 None -6 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
CHEMBL633 394 63 None -6 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
DB01118 394 63 None -6 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
11954259 214191 0 3H-TIOTIDINE -1348 44 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CCC=C2C3=CC=CC=C3SC4=C2C=C(C=C4)S(=O)(=O)N(C)C None
135398745 2858 108 3H-TIOTIDINE -9 66 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2858 108 3H-TIOTIDINE -9 66 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2858 108 3H-TIOTIDINE -9 66 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2858 108 3H-TIOTIDINE -9 66 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
1231 922 112 3H-TIOTIDINE -2 8 Guinea pig 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C None
2756 922 112 3H-TIOTIDINE -2 8 Guinea pig 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C None
645 922 112 3H-TIOTIDINE -2 8 Guinea pig 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C None
CHEMBL30 922 112 3H-TIOTIDINE -2 8 Guinea pig 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C None
DB00501 922 112 3H-TIOTIDINE -2 8 Guinea pig 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C None
1016 3678 75 None -41 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
2561 3678 75 None -41 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
2733526 3678 75 None -41 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
5384 3678 75 None -41 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
CHEMBL83 3678 75 None -41 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
DB00675 3678 75 None -41 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
1210 903 45 None -281 21 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
1213 903 45 None -281 21 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
2725 903 45 None -281 21 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
33036 903 45 None -281 21 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
4411 903 45 None -281 21 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
616 903 45 None -281 21 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
6976 903 45 None -281 21 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
716121 903 45 None -281 21 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
90475904 903 45 None -281 21 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1201353 903 45 None -281 21 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1554789 903 45 None -281 21 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL505 903 45 None -281 21 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
DB01114 903 45 None -281 21 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
DB13679 903 45 None -281 21 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
4601 205010 29 None -7 17 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
CHEMBL1201023 205010 29 None -7 17 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
CHEMBL900 205010 29 None -7 17 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
4189 205185 91 None -36 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
CHEMBL1559 205185 91 None -36 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
CHEMBL91 205185 91 None -36 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
2812 4696 96 None -33 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
CHEMBL104 4696 96 None -33 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
1530 2142 44 None -151 21 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
3827 2142 44 None -151 21 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
7206 2142 44 None -151 21 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
CHEMBL534 2142 44 None -151 21 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
DB00920 2142 44 None -151 21 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
237 203147 43 None -3 13 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 None
CHEMBL546257 203147 43 None -3 13 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 None
CHEMBL554190 203147 43 None -3 13 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 None
CHEMBL7568 203147 43 None -3 13 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 None
2865 4064 67 None -281 54 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4064 67 None -281 54 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4064 67 None -281 54 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4064 67 None -281 54 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4064 67 None -281 54 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
213 3780 50 None -12 44 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
2717 3780 50 None -12 44 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
5533 3780 50 None -12 44 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
CHEMBL621 3780 50 None -12 44 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
DB00656 3780 50 None -12 44 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
1599 2299 47 None -154 16 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 None
3955 2299 47 None -154 16 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 None
7215 2299 47 None -154 16 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 None
CHEMBL841 2299 47 None -154 16 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 None
DB00836 2299 47 None -154 16 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 None
3191 102372 93 None -24 25 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 None
CHEMBL305660 102372 93 None -24 25 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 None
2284 3121 27 None -53 29 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
4926 3121 27 None -53 29 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
7281 3121 27 None -53 29 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
CHEMBL564 3121 27 None -53 29 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
DB00420 3121 27 None -53 29 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
2520 202301 65 None -20 12 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC None
CHEMBL1280 202301 65 None -20 12 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC None
CHEMBL6966 202301 65 None -20 12 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC None
4543 169972 36 None -22 30 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 None
CHEMBL1201156 169972 36 None -22 30 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 None
CHEMBL445 169972 36 None -22 30 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 None
2801 161313 56 None -12 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 None
CHEMBL1200710 161313 56 None -12 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 None
CHEMBL415 161313 56 None -12 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 None
5291 205694 115 None -1 2 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 493 7 2 7 4.6 Cc1ccc(NC(=O)c2ccc(CN3CCN(C)CC3)cc2)cc1Nc1nccc(-c2cccnc2)n1 None
CHEMBL941 205694 115 None -1 2 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 493 7 2 7 4.6 Cc1ccc(NC(=O)c2ccc(CN3CCN(C)CC3)cc2)cc1Nc1nccc(-c2cccnc2)n1 None
1225 1438 24 None -20 22 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
3958 1438 24 None -20 22 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
667477 1438 24 None -20 22 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
CHEMBL860 1438 24 None -20 22 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
DB01142 1438 24 None -20 22 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
2247 502 77 None -56 42 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
249 502 77 None -56 42 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
2603 502 77 None -56 42 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
CHEMBL296419 502 77 None -56 42 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
DB00637 502 77 None -56 42 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
3042 1381 31 None -53 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
355 1381 31 None -53 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
868 1381 31 None -53 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
CHEMBL1123 1381 31 None -53 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
DB00804 1381 31 None -53 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
3198 203792 73 None -19 34 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL1201049 203792 73 None -19 34 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL808 203792 73 None -19 34 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
57469 18663 120 None -1 3 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 240 2 1 4 2.8 CC(C)Cn1cnc2c(N)nc3ccccc3c21 None
CHEMBL1282 18663 120 None -1 3 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 240 2 1 4 2.8 CC(C)Cn1cnc2c(N)nc3ccccc3c21 None
1231 922 112 None 1 8 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C None
2756 922 112 None 1 8 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C None
645 922 112 None 1 8 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C None
CHEMBL30 922 112 None 1 8 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C None
DB00501 922 112 None 1 8 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C None
1201549 590 22 None -74 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
333 590 22 None -74 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
7601 590 22 None -74 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
CHEMBL1201203 590 22 None -74 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
CHEMBL438151 590 22 None -74 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
DB00245 590 22 None -74 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
2286 3122 48 None -26 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
4927 3122 48 None -26 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
7282 3122 48 None -26 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
CHEMBL643 3122 48 None -26 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
DB01069 3122 48 None -26 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
11057 175565 19 None -2 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 None
3468 175565 19 None -2 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 None
CHEMBL459265 175565 19 None -2 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 None
CHEMBL64894 175565 19 None -2 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 None
124087 1357 106 None -29 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
7157 1357 106 None -29 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
814 1357 106 None -29 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
CHEMBL1172 1357 106 None -29 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
DB00967 1357 106 None -29 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
1588 2284 24 None -323 44 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 2284 24 None -323 44 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 2284 24 None -323 44 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 2284 24 None -323 44 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 2284 24 None -323 44 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
103 4074 56 3H-TIOTIDINE -46 54 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4074 56 3H-TIOTIDINE -46 54 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4074 56 3H-TIOTIDINE -46 54 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4074 56 3H-TIOTIDINE -46 54 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4074 56 3H-TIOTIDINE -46 54 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
1226 1980 16 125I-iodoaminopotentidine -7 7 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C None
41376 1980 16 125I-iodoaminopotentidine -7 7 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C None
CHEMBL12608 1980 16 125I-iodoaminopotentidine -7 7 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C None
1204 1893 114 125I-iodoaminopotentidine -173 25 Human 4.3 pKi = 4.3 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1893 114 125I-iodoaminopotentidine -173 25 Human 4.3 pKi = 4.3 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1893 114 125I-iodoaminopotentidine -173 25 Human 4.3 pKi = 4.3 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1893 114 125I-iodoaminopotentidine -173 25 Human 4.3 pKi = 4.3 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1893 114 125I-iodoaminopotentidine -173 25 Human 4.3 pKi = 4.3 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1893 114 125I-iodoaminopotentidine -173 25 Human 4.3 pKi = 4.3 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1233 2469 0 3H-TIOTIDINE 3 4 Guinea pig 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 244 5 3 3 1.0 CNC(=S)NCCSCc1nc[nH]c1C None
1548992 2469 0 3H-TIOTIDINE 3 4 Guinea pig 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 244 5 3 3 1.0 CNC(=S)NCCSCc1nc[nH]c1C None
CHEMBL275446 2469 0 3H-TIOTIDINE 3 4 Guinea pig 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 244 5 3 3 1.0 CNC(=S)NCCSCc1nc[nH]c1C None
DB08805 2469 0 3H-TIOTIDINE 3 4 Guinea pig 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 244 5 3 3 1.0 CNC(=S)NCCSCc1nc[nH]c1C None
1212 1624 45 3H-TIOTIDINE -323 66 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1624 45 3H-TIOTIDINE -323 66 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1624 45 3H-TIOTIDINE -323 66 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1624 45 3H-TIOTIDINE -323 66 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1624 45 3H-TIOTIDINE -323 66 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
1223 938 32 3H-TIOTIDINE -32359 11 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N None
2790 938 32 3H-TIOTIDINE -32359 11 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N None
CHEMBL14690 938 32 3H-TIOTIDINE -32359 11 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N None
135 2486 38 None -39 58 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2486 38 None -39 58 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2486 38 None -39 58 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2486 38 None -39 58 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2486 38 None -39 58 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
33630 178369 94 None -13 28 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assay
Drug Central 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
CHEMBL47050 178369 94 None -13 28 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assay
Drug Central 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
1353 1872 85 None -131 86 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1872 85 None -131 86 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1872 85 None -131 86 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1872 85 None -131 86 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1872 85 None -131 86 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
133 2450 48 None -141 43 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2450 48 None -141 43 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2450 48 None -141 43 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2450 48 None -141 43 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2450 48 None -141 43 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1234 3227 0 None -1 7 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 314 10 2 7 1.5 CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C None
3001055 3227 0 None -1 7 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 314 10 2 7 1.5 CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C None
CHEMBL512 3227 0 None -1 7 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 314 10 2 7 1.5 CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C None
DB00863 3227 0 None -1 7 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 314 10 2 7 1.5 CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C None
1212 1624 45 None -323 66 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1624 45 None -323 66 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1624 45 None -323 66 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1624 45 None -323 66 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1624 45 None -323 66 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3389 215972 0 None -1 26 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 549 12 0 6 6.8 CCCCCCC(=O)OCCN1CCN(CCCN2C3=CC=CC=C3SC3=C2C=C(C=C3)C(F)(F)F)CC1 None
103 4074 56 None -46 54 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4074 56 None -46 54 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4074 56 None -46 54 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4074 56 None -46 54 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4074 56 None -46 54 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
212 3734 43 None -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
2639 3734 43 None -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
941651 3734 43 None -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
CHEMBL1201 3734 43 None -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
DB01623 3734 43 None -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
4011 81982 43 None -27 24 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 None
CHEMBL21731 81982 43 None -27 24 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 None
26987 934 29 None -177 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
6063 934 29 None -177 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
671 934 29 None -177 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
CHEMBL1626 934 29 None -177 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
DB00283 934 29 None -177 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
1613 2306 44 None -10 45 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2306 44 None -10 45 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2306 44 None -10 45 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2306 44 None -10 45 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2306 44 None -10 45 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
277 1269 55 None -43 46 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 1269 55 None -43 46 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 1269 55 None -43 46 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 1269 55 None -43 46 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 1269 55 None -43 46 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
4806 3933 85 None -5 13 Human 8.2 pKi = 8.2 Binding
Binding affinity to human histamine H2 receptorBinding affinity to human histamine H2 receptor
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
7351 3933 85 None -5 13 Human 8.2 pKi = 8.2 Binding
Binding affinity to human histamine H2 receptorBinding affinity to human histamine H2 receptor
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
9966051 3933 85 None -5 13 Human 8.2 pKi = 8.2 Binding
Binding affinity to human histamine H2 receptorBinding affinity to human histamine H2 receptor
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
CHEMBL2104993 3933 85 None -5 13 Human 8.2 pKi = 8.2 Binding
Binding affinity to human histamine H2 receptorBinding affinity to human histamine H2 receptor
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
DB09068 3933 85 None -5 13 Human 8.2 pKi = 8.2 Binding
Binding affinity to human histamine H2 receptorBinding affinity to human histamine H2 receptor
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
2726 904 64 None -85 73 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 904 64 None -85 73 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 904 64 None -85 73 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 904 64 None -85 73 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 904 64 None -85 73 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
135398737 942 89 None -64 92 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 942 89 None -64 92 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 942 89 None -64 92 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 942 89 None -64 92 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 942 89 None -64 92 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
100 3733 52 None -46 56 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3733 52 None -46 56 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3733 52 None -46 56 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3733 52 None -46 56 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3733 52 None -46 56 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2389 3267 114 None -346 68 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3267 114 None -346 68 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3267 114 None -346 68 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3267 114 None -346 68 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3267 114 None -346 68 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
115237 55281 113 None -123 55 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 55281 113 None -123 55 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
1226 1980 16 3H-TIOTIDINE -3 7 Guinea pig 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C None
41376 1980 16 3H-TIOTIDINE -3 7 Guinea pig 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C None
CHEMBL12608 1980 16 3H-TIOTIDINE -3 7 Guinea pig 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C None
1231 922 112 125I-iodoaminopotentidine -2 8 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C None
2756 922 112 125I-iodoaminopotentidine -2 8 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C None
645 922 112 125I-iodoaminopotentidine -2 8 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C None
CHEMBL30 922 112 125I-iodoaminopotentidine -2 8 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C None
DB00501 922 112 125I-iodoaminopotentidine -2 8 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C None
657255 197396 29 None -3 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 None
CHEMBL588119 197396 29 None -3 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug Central 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 None
135398745 2858 108 None -9 66 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2858 108 None -9 66 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2858 108 None -9 66 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2858 108 None -9 66 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
1234 3227 0 125I-iodoaminopotentidine -2 7 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 314 10 2 7 1.5 CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C None
3001055 3227 0 125I-iodoaminopotentidine -2 7 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 314 10 2 7 1.5 CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C None
CHEMBL512 3227 0 125I-iodoaminopotentidine -2 7 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 314 10 2 7 1.5 CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C None
DB00863 3227 0 125I-iodoaminopotentidine -2 7 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 314 10 2 7 1.5 CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C None
5048 3072 57 None -114 7 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 26084539
8924 3072 57 None -114 7 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 26084539
9948102 3072 57 None -114 7 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 26084539
CHEMBL462605 3072 57 None -114 7 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 26084539
DB11642 3072 57 None -114 7 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 26084539
1231 922 112 None 1 8 Rat 5.9 pKi = 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 9384502
2756 922 112 None 1 8 Rat 5.9 pKi = 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 9384502
645 922 112 None 1 8 Rat 5.9 pKi = 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 9384502
CHEMBL30 922 112 None 1 8 Rat 5.9 pKi = 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 9384502
DB00501 922 112 None 1 8 Rat 5.9 pKi = 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 9384502
1234 3227 0 None -1 7 Rat 6.2 pKi = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 10 2 7 1.5 CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C 9384502
3001055 3227 0 None -1 7 Rat 6.2 pKi = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 10 2 7 1.5 CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C 9384502
CHEMBL512 3227 0 None -1 7 Rat 6.2 pKi = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 10 2 7 1.5 CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C 9384502
DB00863 3227 0 None -1 7 Rat 6.2 pKi = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 10 2 7 1.5 CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C 9384502
1231 922 112 None -2 8 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 23466604
2756 922 112 None -2 8 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 23466604
645 922 112 None -2 8 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 23466604
CHEMBL30 922 112 None -2 8 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 23466604
DB00501 922 112 None -2 8 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C 23466604
1234 3227 0 None -2 7 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 10 2 7 1.5 CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C 7921611
3001055 3227 0 None -2 7 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 10 2 7 1.5 CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C 7921611
CHEMBL512 3227 0 None -2 7 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 10 2 7 1.5 CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C 7921611
DB00863 3227 0 None -2 7 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 10 2 7 1.5 CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C 7921611
1235 3751 32 None -1 5 Rat 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 6 4 6 -0.1 N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N 9384502
3959 3751 32 None -1 5 Rat 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 6 4 6 -0.1 N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N 9384502
50287 3751 32 None -1 5 Rat 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 6 4 6 -0.1 N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N 9384502
CHEMBL269646 3751 32 None -1 5 Rat 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 6 4 6 -0.1 N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N 9384502
1265 927 54 None -17782 8 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 270 7 1 3 3.0 O=C(c1ccc(cc1)OCCCc1[nH]cnc1)C1CC1 26084539
6422124 927 54 None -17782 8 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 270 7 1 3 3.0 O=C(c1ccc(cc1)OCCCc1[nH]cnc1)C1CC1 26084539
CHEMBL14638 927 54 None -17782 8 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 270 7 1 3 3.0 O=C(c1ccc(cc1)OCCCc1[nH]cnc1)C1CC1 26084539
441082 1136 40 None -2137 8 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 1 0 2 4.8 CN([C@H]1CC[C@]2(C(=CC[C@@H]3[C@@H]2CC[C@]24[C@H]3CC[C@@H]4[C@@H](N(C2)C)C)C1)C)C 26084539
8981 1136 40 None -2137 8 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 1 0 2 4.8 CN([C@H]1CC[C@]2(C(=CC[C@@H]3[C@@H]2CC[C@]24[C@H]3CC[C@@H]4[C@@H](N(C2)C)C)C1)C)C 26084539
CHEMBL191703 1136 40 None -2137 8 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 1 0 2 4.8 CN([C@H]1CC[C@]2(C(=CC[C@@H]3[C@@H]2CC[C@]24[C@H]3CC[C@@H]4[C@@H](N(C2)C)C)C1)C)C 26084539
11697697 2500 19 None -6309 6 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 431 6 0 5 4.6 Cc1nc2cccc(c2c(=O)n1c1ccc(cc1)OCCCN1CCCC1)C(F)(F)F 26084539
7346 2500 19 None -6309 6 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 431 6 0 5 4.6 Cc1nc2cccc(c2c(=O)n1c1ccc(cc1)OCCCN1CCCC1)C(F)(F)F 26084539
CHEMBL476323 2500 19 None -6309 6 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 431 6 0 5 4.6 Cc1nc2cccc(c2c(=O)n1c1ccc(cc1)OCCCN1CCCC1)C(F)(F)F 26084539
DB11910 2500 19 None -6309 6 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 431 6 0 5 4.6 Cc1nc2cccc(c2c(=O)n1c1ccc(cc1)OCCCN1CCCC1)C(F)(F)F 26084539
117072554 1984 0 None -1000 4 Human 5.3 pKi > 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 450 5 2 6 2.3 CN1CCN(CC1)C1=CC(=NC(N1)N)c1ccc2c(c1)CN(CC2)C(=O)CCC1CCCC1 26084539
8982 1984 0 None -1000 4 Human 5.3 pKi > 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 450 5 2 6 2.3 CN1CCN(CC1)C1=CC(=NC(N1)N)c1ccc2c(c1)CN(CC2)C(=O)CCC1CCCC1 26084539
24994634 2102 26 None -194 7 Human 6.0 pKi > 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 26084539
8984 2102 26 None -194 7 Human 6.0 pKi > 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 26084539
CHEMBL3236549 2102 26 None -194 7 Human 6.0 pKi > 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 26084539
45257132 3613 3 None -83 4 Human 6.0 pKi > 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 366 4 2 6 2.7 CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N 26084539
8983 3613 3 None -83 4 Human 6.0 pKi > 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 366 4 2 6 2.7 CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N 26084539
CHEMBL595180 3613 3 None -83 4 Human 6.0 pKi > 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 366 4 2 6 2.7 CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N 26084539
119570 3098 90 None -281 40 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2233 3098 90 None -281 40 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
953 3098 90 None -281 40 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
CHEMBL301265 3098 90 None -281 40 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
DB00413 3098 90 None -281 40 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
1204 1893 114 None -316 25 Rat 3.8 pKi None 3.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 9384502
1247 1893 114 None -316 25 Rat 3.8 pKi None 3.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 9384502
1375 1893 114 None -316 25 Rat 3.8 pKi None 3.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 9384502
774 1893 114 None -316 25 Rat 3.8 pKi None 3.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 9384502
CHEMBL90 1893 114 None -316 25 Rat 3.8 pKi None 3.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 9384502
DB05381 1893 114 None -316 25 Rat 3.8 pKi None 3.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 9384502
1218 227 47 None -3548 4 Human 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 330 4 0 3 5.0 N#Cc1ccc(cc1)c1ccc2c(c1)cc(o2)CCN1CCC[C@H]1C 15608078
9818903 227 47 None -3548 4 Human 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 330 4 0 3 5.0 N#Cc1ccc(cc1)c1ccc2c(c1)cc(o2)CCN1CCC[C@H]1C 15608078
CHEMBL351231 227 47 None -3548 4 Human 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 330 4 0 3 5.0 N#Cc1ccc(cc1)c1ccc2c(c1)cc(o2)CCN1CCC[C@H]1C 15608078
1223 938 32 None -32359 11 Human 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 12606603
2790 938 32 None -32359 11 Human 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 12606603
CHEMBL14690 938 32 None -32359 11 Human 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 12606603
1229 730 0 None -63 6 Rat 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 262 5 3 2 2.0 CNC(=S)NCCCCc1cccc2c1cn[nH]2 8692899
5311293 730 0 None -63 6 Rat 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 262 5 3 2 2.0 CNC(=S)NCCCCc1cccc2c1cn[nH]2 8692899
1233 2469 0 None -3 4 Rat 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 244 5 3 3 1.0 CNC(=S)NCCSCc1nc[nH]c1C 9384502
1548992 2469 0 None -3 4 Rat 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 244 5 3 3 1.0 CNC(=S)NCCSCc1nc[nH]c1C 9384502
CHEMBL275446 2469 0 None -3 4 Rat 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 244 5 3 3 1.0 CNC(=S)NCCSCc1nc[nH]c1C 9384502
DB08805 2469 0 None -3 4 Rat 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 244 5 3 3 1.0 CNC(=S)NCCSCc1nc[nH]c1C 9384502
1200 3888 1 None 4 3 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 335 8 4 5 0.7 O=C(NC(=NCCCc1cnc[nH]1)N)CSCc1nc[nH]c1C 16394198
25149519 3888 1 None 4 3 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 335 8 4 5 0.7 O=C(NC(=NCCCc1cnc[nH]1)N)CSCc1nc[nH]c1C 16394198
CHEMBL513056 3888 1 None 4 3 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 335 8 4 5 0.7 O=C(NC(=NCCCc1cnc[nH]1)N)CSCc1nc[nH]c1C 16394198
1199 2916 0 None 37 3 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 8 3 4 2.5 NC(=NCCCc1[nH]cnc1)NC(=O)CC(c1ccccn1)c1ccc(cc1)F 16394198
25149244 2916 0 None 37 3 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 8 3 4 2.5 NC(=NCCCc1[nH]cnc1)NC(=O)CC(c1ccccn1)c1ccc(cc1)F 16394198
CHEMBL472273 2916 0 None 37 3 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 8 3 4 2.5 NC(=NCCCc1[nH]cnc1)NC(=O)CC(c1ccccn1)c1ccc(cc1)F 16394198
1221 472 9 None -2 3 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 380 9 3 3 3.0 NC(=NCCCc1[nH]cnc1)NCCC(c1ccccn1)c1ccc(cc1)F 16394198
65895 472 9 None -2 3 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 380 9 3 3 3.0 NC(=NCCCc1[nH]cnc1)NCCC(c1ccccn1)c1ccc(cc1)F 16394198
CHEMBL293802 472 9 None -2 3 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 380 9 3 3 3.0 NC(=NCCCc1[nH]cnc1)NCCC(c1ccccn1)c1ccc(cc1)F 16394198
1226 1980 16 None -7 7 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C 16394198
41376 1980 16 None -7 7 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C 16394198
CHEMBL12608 1980 16 None -7 7 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C 16394198
1232 2017 6 None 6 2 Rat 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 603 11 4 6 3.1 N#CNC(=NCCCOc1cccc(c1)CN1CCCCC1)NCCNC(=O)c1ccc(c(c1)I)N 9384502
181461 2017 6 None 6 2 Rat 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 603 11 4 6 3.1 N#CNC(=NCCCOc1cccc(c1)CN1CCCCC1)NCCNC(=O)c1ccc(c(c1)I)N 9384502
CHEMBL72193 2017 6 None 6 2 Rat 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 603 11 4 6 3.1 N#CNC(=NCCCOc1cccc(c1)CN1CCCCC1)NCCNC(=O)c1ccc(c(c1)I)N 9384502