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Ligand source activities (1 row/activity)

Ligand Receptor Assay information Chemical information
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1251 1883 27 HRH3 H3 receptor Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmcl.2010.10.041
3035842 1883 27 HRH3 H3 receptor Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmcl.2010.10.041
CHEMBL18661 1883 27 HRH3 H3 receptor Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmcl.2010.10.041
1253 1927 5 HRH3 H3 receptor Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 342 6 1 2 3.2 Ic1ccc(cc1)COCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
132937 1927 5 HRH3 H3 receptor Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 342 6 1 2 3.2 Ic1ccc(cc1)COCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL19010 1927 5 HRH3 H3 receptor Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 342 6 1 2 3.2 Ic1ccc(cc1)COCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
11957573 1879 25 HRH3 H3 receptor Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.ejmech.2018.04.020
1250 1879 25 HRH3 H3 receptor Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.ejmech.2018.04.020
3692 1879 25 HRH3 H3 receptor Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.ejmech.2018.04.020
CHEMBL19439 1879 25 HRH3 H3 receptor Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.ejmech.2018.04.020
11957573 1879 25 HRH3 H3 receptor Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.ejmech.2018.04.020
1250 1879 25 HRH3 H3 receptor Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.ejmech.2018.04.020
3692 1879 25 HRH3 H3 receptor Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.ejmech.2018.04.020
CHEMBL19439 1879 25 HRH3 H3 receptor Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.ejmech.2018.04.020
145956362 161187 0 HRH3 H3 receptor Human 10.0 pEC50 = 10 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 500 7 1 5 5.0 COc1cc(N2C(=O)/C(=C\c3ccccc3)C2(C(=O)NC(C)(C)C)c2ccccc2)cc(OC)c1OC 10.1016/j.ejmech.2018.04.020
CHEMBL4159570 161187 0 HRH3 H3 receptor Human 10.0 pEC50 = 10 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 500 7 1 5 5.0 COc1cc(N2C(=O)/C(=C\c3ccccc3)C2(C(=O)NC(C)(C)C)c2ccccc2)cc(OC)c1OC 10.1016/j.ejmech.2018.04.020
145949589 161891 0 HRH3 H3 receptor Human 10.0 pEC50 = 10 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 520 6 1 3 5.9 COc1ccc(N2C(=O)/C(=C\c3ccccc3)C2(C(=O)NC2CCCCC2)c2cc(F)c(F)c(F)c2)cc1 10.1016/j.ejmech.2018.04.020
CHEMBL4170869 161891 0 HRH3 H3 receptor Human 10.0 pEC50 = 10 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 520 6 1 3 5.9 COc1ccc(N2C(=O)/C(=C\c3ccccc3)C2(C(=O)NC2CCCCC2)c2cc(F)c(F)c(F)c2)cc1 10.1016/j.ejmech.2018.04.020
155491015 175644 2 HRH3 H3 receptor Mouse 10.0 pEC50 = 10 Functional
Agonist activity at mouse H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by luciferase reporter gene assayAgonist activity at mouse H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by luciferase reporter gene assay
ChEMBL 207 4 2 5 0.2 CCCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4441731 175644 2 HRH3 H3 receptor Mouse 10.0 pEC50 = 10 Functional
Agonist activity at mouse H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by luciferase reporter gene assayAgonist activity at mouse H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by luciferase reporter gene assay
ChEMBL 207 4 2 5 0.2 CCCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4596734 175644 2 HRH3 H3 receptor Mouse 10.0 pEC50 = 10 Functional
Agonist activity at mouse H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by luciferase reporter gene assayAgonist activity at mouse H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by luciferase reporter gene assay
ChEMBL 207 4 2 5 0.2 CCCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
145956362 161187 0 HRH3 H3 receptor Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 500 7 1 5 5.0 COc1cc(N2C(=O)/C(=C\c3ccccc3)C2(C(=O)NC(C)(C)C)c2ccccc2)cc(OC)c1OC 10.1016/j.ejmech.2018.04.020
CHEMBL4159570 161187 0 HRH3 H3 receptor Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 500 7 1 5 5.0 COc1cc(N2C(=O)/C(=C\c3ccccc3)C2(C(=O)NC(C)(C)C)c2ccccc2)cc(OC)c1OC 10.1016/j.ejmech.2018.04.020
565544 109016 5 HRH3 H3 receptor Human 9.9 pEC50 = 9.9 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptor
ChEMBL 125 2 2 2 0.5 CC(CN)c1cnc[nH]1 10.1021/jm0300025
CHEMBL322988 109016 5 HRH3 H3 receptor Human 9.9 pEC50 = 9.9 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptor
ChEMBL 125 2 2 2 0.5 CC(CN)c1cnc[nH]1 10.1021/jm0300025
11957573 1879 25 HRH3 H3 receptor Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1250 1879 25 HRH3 H3 receptor Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
3692 1879 25 HRH3 H3 receptor Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL19439 1879 25 HRH3 H3 receptor Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1251 1883 27 HRH3 H3 receptor Human 9.9 pEC50 = 9.9 Functional
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm049475h
3035842 1883 27 HRH3 H3 receptor Human 9.9 pEC50 = 9.9 Functional
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm049475h
CHEMBL18661 1883 27 HRH3 H3 receptor Human 9.9 pEC50 = 9.9 Functional
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm049475h
145949589 161891 0 HRH3 H3 receptor Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 520 6 1 3 5.9 COc1ccc(N2C(=O)/C(=C\c3ccccc3)C2(C(=O)NC2CCCCC2)c2cc(F)c(F)c(F)c2)cc1 10.1016/j.ejmech.2018.04.020
CHEMBL4170869 161891 0 HRH3 H3 receptor Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 520 6 1 3 5.9 COc1ccc(N2C(=O)/C(=C\c3ccccc3)C2(C(=O)NC2CCCCC2)c2cc(F)c(F)c(F)c2)cc1 10.1016/j.ejmech.2018.04.020
1251 1883 27 HRH3 H3 receptor Human 9.9 pEC50 = 9.9 Binding
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm049932u
3035842 1883 27 HRH3 H3 receptor Human 9.9 pEC50 = 9.9 Binding
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm049932u
CHEMBL18661 1883 27 HRH3 H3 receptor Human 9.9 pEC50 = 9.9 Binding
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm049932u
1251 1883 27 HRH3 H3 receptor Human 9.9 pEC50 = 9.9 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm030905y
3035842 1883 27 HRH3 H3 receptor Human 9.9 pEC50 = 9.9 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm030905y
CHEMBL18661 1883 27 HRH3 H3 receptor Human 9.9 pEC50 = 9.9 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm030905y
4024 1884 11 HRH3 H3 receptor Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
9989505 1884 11 HRH3 H3 receptor Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL82298 1884 11 HRH3 H3 receptor Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
4024 1884 11 HRH3 H3 receptor Human 9.7 pEC50 = 9.7 Binding
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
ChEMBL 159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1 10.1021/jm049932u
9989505 1884 11 HRH3 H3 receptor Human 9.7 pEC50 = 9.7 Binding
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
ChEMBL 159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1 10.1021/jm049932u
CHEMBL82298 1884 11 HRH3 H3 receptor Human 9.7 pEC50 = 9.7 Binding
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
ChEMBL 159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1 10.1021/jm049932u
4024 1884 11 HRH3 H3 receptor Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human histamine H3 receptor assessed as beta galactosidase activityAgonist activity at human histamine H3 receptor assessed as beta galactosidase activity
ChEMBL 159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1 10.1021/jm7014149
9989505 1884 11 HRH3 H3 receptor Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human histamine H3 receptor assessed as beta galactosidase activityAgonist activity at human histamine H3 receptor assessed as beta galactosidase activity
ChEMBL 159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1 10.1021/jm7014149
CHEMBL82298 1884 11 HRH3 H3 receptor Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human histamine H3 receptor assessed as beta galactosidase activityAgonist activity at human histamine H3 receptor assessed as beta galactosidase activity
ChEMBL 159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1 10.1021/jm7014149
23628252 165285 0 HRH3 H3 receptor Human 9.7 pEC50 = 9.7 Functional
Inverse agonist activity at human histamine H3 receptor by GTP gammaS assayInverse agonist activity at human histamine H3 receptor by GTP gammaS assay
ChEMBL 419 9 1 6 4.7 CN(C)Cc1cc(OCCCN2CCCCC2)ccc1Nc1ncnc2ccccc12 10.1016/j.bmcl.2007.04.056
CHEMBL425994 165285 0 HRH3 H3 receptor Human 9.7 pEC50 = 9.7 Functional
Inverse agonist activity at human histamine H3 receptor by GTP gammaS assayInverse agonist activity at human histamine H3 receptor by GTP gammaS assay
ChEMBL 419 9 1 6 4.7 CN(C)Cc1cc(OCCCN2CCCCC2)ccc1Nc1ncnc2ccccc12 10.1016/j.bmcl.2007.04.056
49799506 10598 0 HRH3 H3 receptor Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 309 3 1 2 3.9 FC(F)(F)c1cccc(N2CCC(Cc3c[nH]cn3)CC2)c1 10.1016/j.bmc.2010.04.052
CHEMBL1172579 10598 0 HRH3 H3 receptor Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 309 3 1 2 3.9 FC(F)(F)c1cccc(N2CCC(Cc3c[nH]cn3)CC2)c1 10.1016/j.bmc.2010.04.052
10465285 9229 0 HRH3 H3 receptor Rat 9.7 pEC50 = 9.7 Binding
In vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortexIn vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortex
ChEMBL 196 7 1 2 2.4 CC(C)CCOCCCc1c[nH]cn1 10.1021/jm991068w
CHEMBL112084 9229 0 HRH3 H3 receptor Rat 9.7 pEC50 = 9.7 Binding
In vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortexIn vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortex
ChEMBL 196 7 1 2 2.4 CC(C)CCOCCCc1c[nH]cn1 10.1021/jm991068w
CHEMBL2145444 9229 0 HRH3 H3 receptor Rat 9.7 pEC50 = 9.7 Binding
In vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortexIn vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortex
ChEMBL 196 7 1 2 2.4 CC(C)CCOCCCc1c[nH]cn1 10.1021/jm991068w
10750963 12091 0 HRH3 H3 receptor Rat 9.6 pEC50 = 9.6 Binding
In vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortexIn vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortex
ChEMBL 210 8 1 2 2.8 CC(C)CCCOCCCc1c[nH]cn1 10.1021/jm991068w
CHEMBL1185581 12091 0 HRH3 H3 receptor Rat 9.6 pEC50 = 9.6 Binding
In vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortexIn vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortex
ChEMBL 210 8 1 2 2.8 CC(C)CCCOCCCc1c[nH]cn1 10.1021/jm991068w
CHEMBL2145442 12091 0 HRH3 H3 receptor Rat 9.6 pEC50 = 9.6 Binding
In vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortexIn vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortex
ChEMBL 210 8 1 2 2.8 CC(C)CCCOCCCc1c[nH]cn1 10.1021/jm991068w
145956355 161178 0 HRH3 H3 receptor Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 415 3 1 5 2.3 O=C1C=C[C@]23C(c4ccccc4)=CC(=O)N2[C@H](c2ccc([N+](=O)[O-])cc2)C(=O)N[C@@H]3C1 10.1016/j.ejmech.2018.04.020
CHEMBL4159472 161178 0 HRH3 H3 receptor Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 415 3 1 5 2.3 O=C1C=C[C@]23C(c4ccccc4)=CC(=O)N2[C@H](c2ccc([N+](=O)[O-])cc2)C(=O)N[C@@H]3C1 10.1016/j.ejmech.2018.04.020
145971293 162298 0 HRH3 H3 receptor Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 536 7 1 5 5.2 COc1cc(N2C(=O)/C(=C\c3ccccc3)C2(C(=O)NC(C)(C)C)c2cc(F)cc(F)c2)cc(OC)c1OC 10.1016/j.ejmech.2018.04.020
CHEMBL4177416 162298 0 HRH3 H3 receptor Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 536 7 1 5 5.2 COc1cc(N2C(=O)/C(=C\c3ccccc3)C2(C(=O)NC(C)(C)C)c2cc(F)cc(F)c2)cc(OC)c1OC 10.1016/j.ejmech.2018.04.020
145956355 161178 0 HRH3 H3 receptor Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 415 3 1 5 2.3 O=C1C=C[C@]23C(c4ccccc4)=CC(=O)N2[C@H](c2ccc([N+](=O)[O-])cc2)C(=O)N[C@@H]3C1 10.1016/j.ejmech.2018.04.020
CHEMBL4159472 161178 0 HRH3 H3 receptor Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 415 3 1 5 2.3 O=C1C=C[C@]23C(c4ccccc4)=CC(=O)N2[C@H](c2ccc([N+](=O)[O-])cc2)C(=O)N[C@@H]3C1 10.1016/j.ejmech.2018.04.020
145971293 162298 0 HRH3 H3 receptor Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 536 7 1 5 5.2 COc1cc(N2C(=O)/C(=C\c3ccccc3)C2(C(=O)NC(C)(C)C)c2cc(F)cc(F)c2)cc(OC)c1OC 10.1016/j.ejmech.2018.04.020
CHEMBL4177416 162298 0 HRH3 H3 receptor Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 536 7 1 5 5.2 COc1cc(N2C(=O)/C(=C\c3ccccc3)C2(C(=O)NC(C)(C)C)c2cc(F)cc(F)c2)cc(OC)c1OC 10.1016/j.ejmech.2018.04.020
155491015 175644 2 HRH3 H3 receptor Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 207 4 2 5 0.2 CCCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4441731 175644 2 HRH3 H3 receptor Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 207 4 2 5 0.2 CCCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4596734 175644 2 HRH3 H3 receptor Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 207 4 2 5 0.2 CCCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
11313837 2348 5 HRH3 H3 receptor Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human histamine H3 receptor assessed as beta galactosidase activityAgonist activity at human histamine H3 receptor assessed as beta galactosidase activity
ChEMBL 179 2 1 2 1.3 CN1CCC(CC1)Cc1[nH]cnc1 10.1021/jm7014149
1254 2348 5 HRH3 H3 receptor Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human histamine H3 receptor assessed as beta galactosidase activityAgonist activity at human histamine H3 receptor assessed as beta galactosidase activity
ChEMBL 179 2 1 2 1.3 CN1CCC(CC1)Cc1[nH]cnc1 10.1021/jm7014149
CHEMBL175782 2348 5 HRH3 H3 receptor Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human histamine H3 receptor assessed as beta galactosidase activityAgonist activity at human histamine H3 receptor assessed as beta galactosidase activity
ChEMBL 179 2 1 2 1.3 CN1CCC(CC1)Cc1[nH]cnc1 10.1021/jm7014149
1236 1936 17 HRH3 H3 receptor Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1016/j.bmcl.2010.10.041
1237 1936 17 HRH3 H3 receptor Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1016/j.bmcl.2010.10.041
156615 1936 17 HRH3 H3 receptor Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1016/j.bmcl.2010.10.041
CHEMBL268229 1936 17 HRH3 H3 receptor Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1016/j.bmcl.2010.10.041
11313837 2348 5 HRH3 H3 receptor Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 179 2 1 2 1.3 CN1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmcl.2010.10.041
1254 2348 5 HRH3 H3 receptor Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 179 2 1 2 1.3 CN1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmcl.2010.10.041
CHEMBL175782 2348 5 HRH3 H3 receptor Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 179 2 1 2 1.3 CN1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmcl.2010.10.041
11313837 2348 5 HRH3 H3 receptor Human 9.5 pEC50 = 9.5 Functional
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
ChEMBL 179 2 1 2 1.3 CN1CCC(CC1)Cc1[nH]cnc1 10.1021/jm049475h
1254 2348 5 HRH3 H3 receptor Human 9.5 pEC50 = 9.5 Functional
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
ChEMBL 179 2 1 2 1.3 CN1CCC(CC1)Cc1[nH]cnc1 10.1021/jm049475h
CHEMBL175782 2348 5 HRH3 H3 receptor Human 9.5 pEC50 = 9.5 Functional
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
ChEMBL 179 2 1 2 1.3 CN1CCC(CC1)Cc1[nH]cnc1 10.1021/jm049475h
44367568 45284 3 HRH3 H3 receptor Human 9.4 pEC50 = 9.4 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
ChEMBL 151 2 2 2 0.6 c1nc(C[C@@H]2CCNC2)c[nH]1 10.1021/jm030905y
CHEMBL153051 45284 3 HRH3 H3 receptor Human 9.4 pEC50 = 9.4 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
ChEMBL 151 2 2 2 0.6 c1nc(C[C@@H]2CCNC2)c[nH]1 10.1021/jm030905y
1239 1902 19 HRH3 H3 receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 3 2 2 0.2 CNCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1240 1902 19 HRH3 H3 receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 3 2 2 0.2 CNCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
912 1902 19 HRH3 H3 receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 3 2 2 0.2 CNCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL268490 1902 19 HRH3 H3 receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 3 2 2 0.2 CNCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
53321919 55964 0 HRH3 H3 receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 322 7 3 3 3.8 N=C(NCc1ccc(Cl)cc1)SCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL1632409 55964 0 HRH3 H3 receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 322 7 3 3 3.8 N=C(NCc1ccc(Cl)cc1)SCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
76328873 104778 0 HRH3 H3 receptor Human 9.4 pEC50 = 9.4 Functional
Inverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assay
ChEMBL 339 4 1 4 2.6 O=C1NN=C(c2ccc(OC3CCN(C4CCC4)CC3)cc2)[C@H]2C[C@@H]12 10.1016/j.bmcl.2014.01.061
CHEMBL3121095 104778 0 HRH3 H3 receptor Human 9.4 pEC50 = 9.4 Functional
Inverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assay
ChEMBL 339 4 1 4 2.6 O=C1NN=C(c2ccc(OC3CCN(C4CCC4)CC3)cc2)[C@H]2C[C@@H]12 10.1016/j.bmcl.2014.01.061
76321713 104779 0 HRH3 H3 receptor Human 9.3 pEC50 = 9.3 Functional
Inverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assay
ChEMBL 339 4 1 4 2.6 O=C1NN=C(c2ccc(OC3CCN(C4CCC4)CC3)cc2)[C@@H]2C[C@H]12 10.1016/j.bmcl.2014.01.061
CHEMBL3121096 104779 0 HRH3 H3 receptor Human 9.3 pEC50 = 9.3 Functional
Inverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assay
ChEMBL 339 4 1 4 2.6 O=C1NN=C(c2ccc(OC3CCN(C4CCC4)CC3)cc2)[C@@H]2C[C@H]12 10.1016/j.bmcl.2014.01.061
10176414 3814 9 HRH3 H3 receptor Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 184 4 3 3 1.0 NC(=N)SCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1246 3814 9 HRH3 H3 receptor Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 184 4 3 3 1.0 NC(=N)SCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL281576 3814 9 HRH3 H3 receptor Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 184 4 3 3 1.0 NC(=N)SCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
10130526 8887 0 HRH3 H3 receptor Rat 9.3 pEC50 = 9.3 Binding
In vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortexIn vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortex
ChEMBL 210 6 1 2 2.8 CC(C)(C)CCOCCCc1c[nH]cn1 10.1021/jm991068w
CHEMBL110098 8887 0 HRH3 H3 receptor Rat 9.3 pEC50 = 9.3 Binding
In vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortexIn vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortex
ChEMBL 210 6 1 2 2.8 CC(C)(C)CCOCCCc1c[nH]cn1 10.1021/jm991068w
CHEMBL2145443 8887 0 HRH3 H3 receptor Rat 9.3 pEC50 = 9.3 Binding
In vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortexIn vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortex
ChEMBL 210 6 1 2 2.8 CC(C)(C)CCOCCCc1c[nH]cn1 10.1021/jm991068w
11554040 88872 0 HRH3 H3 receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 442 7 0 7 4.6 CCOc1ccc(-n2ncc(-c3ccc4cc(CCN5CCC[C@H]5C)ccc4n3)c2C)nn1 10.1021/jm0705051
CHEMBL237394 88872 0 HRH3 H3 receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 442 7 0 7 4.6 CCOc1ccc(-n2ncc(-c3ccc4cc(CCN5CCC[C@H]5C)ccc4n3)c2C)nn1 10.1021/jm0705051
11554040 88872 0 HRH3 H3 receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 442 7 0 7 4.6 CCOc1ccc(-n2ncc(-c3ccc4cc(CCN5CCC[C@H]5C)ccc4n3)c2C)nn1 10.1021/jm0705051
CHEMBL237394 88872 0 HRH3 H3 receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 442 7 0 7 4.6 CCOc1ccc(-n2ncc(-c3ccc4cc(CCN5CCC[C@H]5C)ccc4n3)c2C)nn1 10.1021/jm0705051
118734876 117988 0 HRH3 H3 receptor Human 9.2 pEC50 = 9.2 Functional
Inverse agonist activity at human H3R expressed in CHO cells assessed as inhibition of RAMH-induced [35S]GTPgammaS binding relative to controlInverse agonist activity at human H3R expressed in CHO cells assessed as inhibition of RAMH-induced [35S]GTPgammaS binding relative to control
ChEMBL 327 6 1 4 2.4 C[C@@H]1CCCN1CCCOc1ccc(C2=NNC(=O)[C@H]3C[C@@H]23)cc1 10.1016/j.ejmech.2015.03.054
CHEMBL3417586 117988 0 HRH3 H3 receptor Human 9.2 pEC50 = 9.2 Functional
Inverse agonist activity at human H3R expressed in CHO cells assessed as inhibition of RAMH-induced [35S]GTPgammaS binding relative to controlInverse agonist activity at human H3R expressed in CHO cells assessed as inhibition of RAMH-induced [35S]GTPgammaS binding relative to control
ChEMBL 327 6 1 4 2.4 C[C@@H]1CCCN1CCCOc1ccc(C2=NNC(=O)[C@H]3C[C@@H]23)cc1 10.1016/j.ejmech.2015.03.054
155547602 175842 0 HRH3 H3 receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 193 3 2 5 -0.1 CCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4535316 175842 0 HRH3 H3 receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 193 3 2 5 -0.1 CCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4598409 175842 0 HRH3 H3 receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 193 3 2 5 -0.1 CCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
1249 1878 12 HRH3 H3 receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
13499360 1878 12 HRH3 H3 receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL90019 1878 12 HRH3 H3 receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL3220120 108707 0 HRH3 H3 receptor Human 9.2 pEC50 = 9.2 Functional
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation countingInverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation counting
ChEMBL 328 4 0 4 3.6 CC1(C)COC(c2ccc(O[C@H]3C[C@H](N4CCCCC4)C3)cc2)=N1 10.1039/C0MD00056F
1251 1883 27 HRH3 H3 receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm100643t
3035842 1883 27 HRH3 H3 receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm100643t
CHEMBL18661 1883 27 HRH3 H3 receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm100643t
1251 1883 27 HRH3 H3 receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmc.2010.04.052
3035842 1883 27 HRH3 H3 receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmc.2010.04.052
CHEMBL18661 1883 27 HRH3 H3 receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmc.2010.04.052
1236 1936 17 HRH3 H3 receptor Human 9.2 pEC50 = 9.2 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1021/jm030905y
1237 1936 17 HRH3 H3 receptor Human 9.2 pEC50 = 9.2 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1021/jm030905y
156615 1936 17 HRH3 H3 receptor Human 9.2 pEC50 = 9.2 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1021/jm030905y
CHEMBL268229 1936 17 HRH3 H3 receptor Human 9.2 pEC50 = 9.2 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1021/jm030905y
54764158 68505 0 HRH3 H3 receptor Human 9.2 pEC50 = 9.2 Functional
Inhibition of basal activity of human histamine H3 receptor expressed in CHO cells assessed as inhibition of RAHM-induced [35S]GTPgammaS binding after 4 hrs by beta liquid scintillation countingInhibition of basal activity of human histamine H3 receptor expressed in CHO cells assessed as inhibition of RAHM-induced [35S]GTPgammaS binding after 4 hrs by beta liquid scintillation counting
ChEMBL 326 6 0 4 3.3 C[C@@H]1CCCN1CCCOc1ccc(-c2ccc(=O)n(C)c2)cc1 10.1016/j.bmcl.2011.09.091
CHEMBL1923729 68505 0 HRH3 H3 receptor Human 9.2 pEC50 = 9.2 Functional
Inhibition of basal activity of human histamine H3 receptor expressed in CHO cells assessed as inhibition of RAHM-induced [35S]GTPgammaS binding after 4 hrs by beta liquid scintillation countingInhibition of basal activity of human histamine H3 receptor expressed in CHO cells assessed as inhibition of RAHM-induced [35S]GTPgammaS binding after 4 hrs by beta liquid scintillation counting
ChEMBL 326 6 0 4 3.3 C[C@@H]1CCCN1CCCOc1ccc(-c2ccc(=O)n(C)c2)cc1 10.1016/j.bmcl.2011.09.091
118734875 117987 0 HRH3 H3 receptor Human 9.2 pEC50 = 9.2 Functional
Inverse agonist activity at human H3R expressed in CHO cells assessed as inhibition of RAMH-induced [35S]GTPgammaS binding relative to controlInverse agonist activity at human H3R expressed in CHO cells assessed as inhibition of RAMH-induced [35S]GTPgammaS binding relative to control
ChEMBL 327 6 1 4 2.4 C[C@@H]1CCCN1CCCOc1ccc(C2=NNC(=O)[C@@H]3C[C@H]23)cc1 10.1016/j.ejmech.2015.03.054
CHEMBL3417585 117987 0 HRH3 H3 receptor Human 9.2 pEC50 = 9.2 Functional
Inverse agonist activity at human H3R expressed in CHO cells assessed as inhibition of RAMH-induced [35S]GTPgammaS binding relative to controlInverse agonist activity at human H3R expressed in CHO cells assessed as inhibition of RAMH-induced [35S]GTPgammaS binding relative to control
ChEMBL 327 6 1 4 2.4 C[C@@H]1CCCN1CCCOc1ccc(C2=NNC(=O)[C@@H]3C[C@H]23)cc1 10.1016/j.ejmech.2015.03.054
25265089 102978 0 HRH3 H3 receptor Human 9.2 pEC50 = 9.2 Functional
Inverse agonist activity at human histamine H3 receptor (445 amino acid residues) expressed in CHO cells by CRE-luciferase reporter gene assayInverse agonist activity at human histamine H3 receptor (445 amino acid residues) expressed in CHO cells by CRE-luciferase reporter gene assay
ChEMBL 382 4 1 5 3.9 Cc1cc(N2CC[C@H](N3CCC[C@@H]3C)C2)ccc1NC(=O)c1c(C)noc1C 10.1016/j.bmcl.2013.09.081
CHEMBL3087669 102978 0 HRH3 H3 receptor Human 9.2 pEC50 = 9.2 Functional
Inverse agonist activity at human histamine H3 receptor (445 amino acid residues) expressed in CHO cells by CRE-luciferase reporter gene assayInverse agonist activity at human histamine H3 receptor (445 amino acid residues) expressed in CHO cells by CRE-luciferase reporter gene assay
ChEMBL 382 4 1 5 3.9 Cc1cc(N2CC[C@H](N3CCC[C@@H]3C)C2)ccc1NC(=O)c1c(C)noc1C 10.1016/j.bmcl.2013.09.081
24994127 69080 0 HRH3 H3 receptor Human 9.2 pEC50 = 9.2 Functional
Inverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assay
ChEMBL 315 6 1 4 2.6 C[C@@H]1CCCN1CCCOc1ccc(C2=NNC(=O)CC2)cc1 10.1016/j.bmcl.2011.11.037
CHEMBL1935100 69080 0 HRH3 H3 receptor Human 9.2 pEC50 = 9.2 Functional
Inverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assay
ChEMBL 315 6 1 4 2.6 C[C@@H]1CCCN1CCCOc1ccc(C2=NNC(=O)CC2)cc1 10.1016/j.bmcl.2011.11.037
56835090 69094 0 HRH3 H3 receptor Human 9.1 pEC50 = 9.1 Functional
Inverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assay
ChEMBL 343 6 1 4 3.2 C[C@@H]1CCCN1CCCOc1ccc(C2=NNC(=O)C(C)(C)C2)cc1 10.1016/j.bmcl.2011.11.037
CHEMBL1935114 69094 0 HRH3 H3 receptor Human 9.1 pEC50 = 9.1 Functional
Inverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assay
ChEMBL 343 6 1 4 3.2 C[C@@H]1CCCN1CCCOc1ccc(C2=NNC(=O)C(C)(C)C2)cc1 10.1016/j.bmcl.2011.11.037
11554040 88872 0 HRH3 H3 receptor Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 442 7 0 7 4.6 CCOc1ccc(-n2ncc(-c3ccc4cc(CCN5CCC[C@H]5C)ccc4n3)c2C)nn1 10.1021/jm0705051
CHEMBL237394 88872 0 HRH3 H3 receptor Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 442 7 0 7 4.6 CCOc1ccc(-n2ncc(-c3ccc4cc(CCN5CCC[C@H]5C)ccc4n3)c2C)nn1 10.1021/jm0705051
11554040 88872 0 HRH3 H3 receptor Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 442 7 0 7 4.6 CCOc1ccc(-n2ncc(-c3ccc4cc(CCN5CCC[C@H]5C)ccc4n3)c2C)nn1 10.1021/jm0705051
CHEMBL237394 88872 0 HRH3 H3 receptor Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 442 7 0 7 4.6 CCOc1ccc(-n2ncc(-c3ccc4cc(CCN5CCC[C@H]5C)ccc4n3)c2C)nn1 10.1021/jm0705051
46222048 8715 0 HRH3 H3 receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 260 4 1 2 4.0 CC(C)(C)c1ccc(SCCc2c[nH]cn2)cc1 10.1021/jm100643t
CHEMBL1098230 8715 0 HRH3 H3 receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 260 4 1 2 4.0 CC(C)(C)c1ccc(SCCc2c[nH]cn2)cc1 10.1021/jm100643t
46222048 8715 0 HRH3 H3 receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 260 4 1 2 4.0 CC(C)(C)c1ccc(SCCc2c[nH]cn2)cc1 10.1021/jm901890s
CHEMBL1098230 8715 0 HRH3 H3 receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 260 4 1 2 4.0 CC(C)(C)c1ccc(SCCc2c[nH]cn2)cc1 10.1021/jm901890s
46222048 8715 0 HRH3 H3 receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 260 4 1 2 4.0 CC(C)(C)c1ccc(SCCc2c[nH]cn2)cc1 10.1016/j.bmc.2010.04.052
CHEMBL1098230 8715 0 HRH3 H3 receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 260 4 1 2 4.0 CC(C)(C)c1ccc(SCCc2c[nH]cn2)cc1 10.1016/j.bmc.2010.04.052
11647025 88803 0 HRH3 H3 receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 401 5 0 5 4.6 Cc1nc(N2CCCC2)ncc1-c1ccc2cc(CCN3CCC[C@H]3C)ccc2n1 10.1021/jm0705051
CHEMBL237191 88803 0 HRH3 H3 receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 401 5 0 5 4.6 Cc1nc(N2CCCC2)ncc1-c1ccc2cc(CCN3CCC[C@H]3C)ccc2n1 10.1021/jm0705051
11647025 88803 0 HRH3 H3 receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 401 5 0 5 4.6 Cc1nc(N2CCCC2)ncc1-c1ccc2cc(CCN3CCC[C@H]3C)ccc2n1 10.1021/jm0705051
CHEMBL237191 88803 0 HRH3 H3 receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 401 5 0 5 4.6 Cc1nc(N2CCCC2)ncc1-c1ccc2cc(CCN3CCC[C@H]3C)ccc2n1 10.1021/jm0705051
155558361 175399 0 HRH3 H3 receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 221 5 2 5 0.6 CCCCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4560428 175399 0 HRH3 H3 receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 221 5 2 5 0.6 CCCCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4594866 175399 0 HRH3 H3 receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 221 5 2 5 0.6 CCCCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
54753626 65343 0 HRH3 H3 receptor Human 9.1 pEC50 = 9.1 Functional
Inverse agonist activity at human histamine H3 receptor assessed as decrease of basal activity of [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as decrease of basal activity of [35S]GTPgammaS binding
ChEMBL 367 6 0 5 3.2 C[C@@H]1CCCN1CCCOc1ccc(-c2nn(C)c(=O)c3c2CCC3)cc1 10.1016/j.bmcl.2011.08.045
CHEMBL1835782 65343 0 HRH3 H3 receptor Human 9.1 pEC50 = 9.1 Functional
Inverse agonist activity at human histamine H3 receptor assessed as decrease of basal activity of [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as decrease of basal activity of [35S]GTPgammaS binding
ChEMBL 367 6 0 5 3.2 C[C@@H]1CCCN1CCCOc1ccc(-c2nn(C)c(=O)c3c2CCC3)cc1 10.1016/j.bmcl.2011.08.045
54753627 65344 0 HRH3 H3 receptor Human 9.1 pEC50 = 9.1 Functional
Inverse agonist activity at human histamine H3 receptor assessed as decrease of basal activity of [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as decrease of basal activity of [35S]GTPgammaS binding
ChEMBL 367 6 0 5 3.2 Cn1nc(-c2ccc(OCCCN3CCCCC3)cc2)c2c(c1=O)CCC2 10.1016/j.bmcl.2011.08.045
CHEMBL1835783 65344 0 HRH3 H3 receptor Human 9.1 pEC50 = 9.1 Functional
Inverse agonist activity at human histamine H3 receptor assessed as decrease of basal activity of [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as decrease of basal activity of [35S]GTPgammaS binding
ChEMBL 367 6 0 5 3.2 Cn1nc(-c2ccc(OCCCN3CCCCC3)cc2)c2c(c1=O)CCC2 10.1016/j.bmcl.2011.08.045
24993178 70166 0 HRH3 H3 receptor Human 9.1 pEC50 = 9.1 Functional
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 355 4 1 4 3.3 CC1(C)CC(c2ccc(OC3CCN(C4CCC4)CC3)cc2)=NNC1=O 10.1016/j.bmcl.2012.01.026
CHEMBL1950743 70166 0 HRH3 H3 receptor Human 9.1 pEC50 = 9.1 Functional
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 355 4 1 4 3.3 CC1(C)CC(c2ccc(OC3CCN(C4CCC4)CC3)cc2)=NNC1=O 10.1016/j.bmcl.2012.01.026
25265516 92345 0 HRH3 H3 receptor Human 9.1 pEC50 = 9.1 Functional
Antagonist activity at human histamine H3 receptor expressed in CHO cells co-expressing CRE-LucAntagonist activity at human histamine H3 receptor expressed in CHO cells co-expressing CRE-Luc
ChEMBL 371 4 1 4 3.4 Cc1cc(N2CC[C@H](N3CCC[C@@H]3C)C2)ccc1NC(=O)C1CCOCC1 10.1016/j.bmcl.2013.09.006
CHEMBL2441636 92345 0 HRH3 H3 receptor Human 9.1 pEC50 = 9.1 Functional
Antagonist activity at human histamine H3 receptor expressed in CHO cells co-expressing CRE-LucAntagonist activity at human histamine H3 receptor expressed in CHO cells co-expressing CRE-Luc
ChEMBL 371 4 1 4 3.4 Cc1cc(N2CC[C@H](N3CCC[C@@H]3C)C2)ccc1NC(=O)C1CCOCC1 10.1016/j.bmcl.2013.09.006
49856084 74602 0 HRH3 H3 receptor Human 9.1 pEC50 = 9.1 Functional
Inverse agonist activity at human histamine H3 receptor by [35S]-GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor by [35S]-GTPgammaS binding assay
ChEMBL 403 8 0 6 2.5 COC(=O)N1CCN(CC(=O)c2ccc(OCCCN3CCC[C@H]3C)cc2)CC1 10.1016/j.bmcl.2012.02.081
CHEMBL2036653 74602 0 HRH3 H3 receptor Human 9.1 pEC50 = 9.1 Functional
Inverse agonist activity at human histamine H3 receptor by [35S]-GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor by [35S]-GTPgammaS binding assay
ChEMBL 403 8 0 6 2.5 COC(=O)N1CCN(CC(=O)c2ccc(OCCCN3CCC[C@H]3C)cc2)CC1 10.1016/j.bmcl.2012.02.081
11957573 1879 25 HRH3 H3 receptor Rat 9.0 pEC50 = 9 Binding
In vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortexIn vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortex
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm991068w
1250 1879 25 HRH3 H3 receptor Rat 9.0 pEC50 = 9 Binding
In vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortexIn vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortex
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm991068w
3692 1879 25 HRH3 H3 receptor Rat 9.0 pEC50 = 9 Binding
In vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortexIn vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortex
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm991068w
CHEMBL19439 1879 25 HRH3 H3 receptor Rat 9.0 pEC50 = 9 Binding
In vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortexIn vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortex
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm991068w
23725172 63825 0 HRH3 H3 receptor Human 9.0 pEC50 = 9 Functional
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS binding
ChEMBL 327 6 0 5 2.7 C[C@@H]1CCCN1CCCOc1ccc(-c2ccc(=O)n(C)n2)cc1 10.1021/jm200401v
CHEMBL1813057 63825 0 HRH3 H3 receptor Human 9.0 pEC50 = 9 Functional
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS binding
ChEMBL 327 6 0 5 2.7 C[C@@H]1CCCN1CCCOc1ccc(-c2ccc(=O)n(C)n2)cc1 10.1021/jm200401v
49855513 74589 0 HRH3 H3 receptor Human 9.0 pEC50 = 9 Functional
Inverse agonist activity at human histamine H3 receptor by [35S]-GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor by [35S]-GTPgammaS binding assay
ChEMBL 449 9 0 5 3.6 C[C@@H]1CCCN1CCCOc1ccc(C(=O)CN2CCN(C(=O)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2012.02.081
CHEMBL2036635 74589 0 HRH3 H3 receptor Human 9.0 pEC50 = 9 Functional
Inverse agonist activity at human histamine H3 receptor by [35S]-GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor by [35S]-GTPgammaS binding assay
ChEMBL 449 9 0 5 3.6 C[C@@H]1CCCN1CCCOc1ccc(C(=O)CN2CCN(C(=O)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2012.02.081
11566918 185228 0 HRH3 H3 receptor Human 9.0 pEC50 = 9 Binding
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
ChEMBL 371 4 2 4 2.6 CC(C)N1CCC(Oc2ccc3[nH]c(C(=O)N4CCC(O)C4)cc3c2)CC1 10.1021/jm900409x
CHEMBL496616 185228 0 HRH3 H3 receptor Human 9.0 pEC50 = 9 Binding
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
ChEMBL 371 4 2 4 2.6 CC(C)N1CCC(Oc2ccc3[nH]c(C(=O)N4CCC(O)C4)cc3c2)CC1 10.1021/jm900409x
11957573 1879 25 HRH3 H3 receptor Rat 9.0 pEC50 = 9 Functional
The compound was evaluated for agonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uMThe compound was evaluated for agonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uM
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/S0960-894X(00)80219-X
1250 1879 25 HRH3 H3 receptor Rat 9.0 pEC50 = 9 Functional
The compound was evaluated for agonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uMThe compound was evaluated for agonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uM
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/S0960-894X(00)80219-X
3692 1879 25 HRH3 H3 receptor Rat 9.0 pEC50 = 9 Functional
The compound was evaluated for agonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uMThe compound was evaluated for agonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uM
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/S0960-894X(00)80219-X
CHEMBL19439 1879 25 HRH3 H3 receptor Rat 9.0 pEC50 = 9 Functional
The compound was evaluated for agonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uMThe compound was evaluated for agonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uM
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/S0960-894X(00)80219-X
145956781 161382 0 HRH3 H3 receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 552 7 1 5 5.7 COc1cc(N2C(=O)/C(=C\c3ccccc3)C2(C(=O)NC(C)(C)C)c2ccc(Cl)c(F)c2)cc(OC)c1OC 10.1016/j.ejmech.2018.04.020
CHEMBL4162793 161382 0 HRH3 H3 receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 552 7 1 5 5.7 COc1cc(N2C(=O)/C(=C\c3ccccc3)C2(C(=O)NC(C)(C)C)c2ccc(Cl)c(F)c2)cc(OC)c1OC 10.1016/j.ejmech.2018.04.020
4024 1884 11 HRH3 H3 receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1 10.1021/jm100643t
9989505 1884 11 HRH3 H3 receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1 10.1021/jm100643t
CHEMBL82298 1884 11 HRH3 H3 receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1 10.1021/jm100643t
46912441 10621 0 HRH3 H3 receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 309 3 1 2 3.9 FC(F)(F)c1ccc(N2CCC(Cc3c[nH]cn3)CC2)cc1 10.1016/j.bmc.2010.04.052
CHEMBL1172754 10621 0 HRH3 H3 receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 309 3 1 2 3.9 FC(F)(F)c1ccc(N2CCC(Cc3c[nH]cn3)CC2)cc1 10.1016/j.bmc.2010.04.052
49799253 10722 0 HRH3 H3 receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 259 3 1 2 3.0 Fc1ccc(N2CCC(Cc3c[nH]cn3)CC2)cc1 10.1016/j.bmc.2010.04.052
CHEMBL1173809 10722 0 HRH3 H3 receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 259 3 1 2 3.0 Fc1ccc(N2CCC(Cc3c[nH]cn3)CC2)cc1 10.1016/j.bmc.2010.04.052
24996644 69846 0 HRH3 H3 receptor Human 9.0 pEC50 = 9.0 Functional
Inverse agonist activity at human histamine H3 histamine receptor by [35S]GTPgammaS binding assayInverse agonist activity at human histamine H3 histamine receptor by [35S]GTPgammaS binding assay
ChEMBL 339 4 1 4 3.1 Cc1n[nH]c(=O)cc1-c1ccc(OC2CCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2011.11.118
CHEMBL1945845 69846 0 HRH3 H3 receptor Human 9.0 pEC50 = 9.0 Functional
Inverse agonist activity at human histamine H3 histamine receptor by [35S]GTPgammaS binding assayInverse agonist activity at human histamine H3 histamine receptor by [35S]GTPgammaS binding assay
ChEMBL 339 4 1 4 3.1 Cc1n[nH]c(=O)cc1-c1ccc(OC2CCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2011.11.118
53363442 63832 0 HRH3 H3 receptor Human 9.0 pEC50 = 9.0 Functional
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS binding
ChEMBL 313 6 1 4 2.7 C[C@@H]1CCCN1CCCOc1ccc(-c2cn[nH]c(=O)c2)cc1 10.1021/jm200401v
CHEMBL1813065 63832 0 HRH3 H3 receptor Human 9.0 pEC50 = 9.0 Functional
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS binding
ChEMBL 313 6 1 4 2.7 C[C@@H]1CCCN1CCCOc1ccc(-c2cn[nH]c(=O)c2)cc1 10.1021/jm200401v
25070031 64829 4 HRH3 H3 receptor Human 9.0 pEC50 = 9.0 Functional
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS binding
ChEMBL 313 6 1 4 2.7 C[C@@H]1CCCN1CCCOc1ccc(-c2ccc(=O)[nH]n2)cc1 10.1021/jm200401v
CHEMBL1829335 64829 4 HRH3 H3 receptor Human 9.0 pEC50 = 9.0 Functional
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS binding
ChEMBL 313 6 1 4 2.7 C[C@@H]1CCCN1CCCOc1ccc(-c2ccc(=O)[nH]n2)cc1 10.1021/jm200401v
24993500 70132 0 HRH3 H3 receptor Human 9.0 pEC50 = 9.0 Functional
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 325 4 1 4 2.8 O=c1ccc(-c2ccc(OC3CCN(C4CCC4)CC3)cc2)n[nH]1 10.1016/j.bmcl.2012.01.026
CHEMBL1950643 70132 0 HRH3 H3 receptor Human 9.0 pEC50 = 9.0 Functional
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 325 4 1 4 2.8 O=c1ccc(-c2ccc(OC3CCN(C4CCC4)CC3)cc2)n[nH]1 10.1016/j.bmcl.2012.01.026
11538251 146118 0 HRH3 H3 receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 385 4 0 5 4.6 Cc1cc2ncc(-c3ccc4cc(CCN5CCC[C@H]5C)ccc4n3)c(C)n2n1 10.1021/jm0705051
CHEMBL392573 146118 0 HRH3 H3 receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 385 4 0 5 4.6 Cc1cc2ncc(-c3ccc4cc(CCN5CCC[C@H]5C)ccc4n3)c(C)n2n1 10.1021/jm0705051
145956781 161382 0 HRH3 H3 receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 552 7 1 5 5.7 COc1cc(N2C(=O)/C(=C\c3ccccc3)C2(C(=O)NC(C)(C)C)c2ccc(Cl)c(F)c2)cc(OC)c1OC 10.1016/j.ejmech.2018.04.020
CHEMBL4162793 161382 0 HRH3 H3 receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 552 7 1 5 5.7 COc1cc(N2C(=O)/C(=C\c3ccccc3)C2(C(=O)NC(C)(C)C)c2ccc(Cl)c(F)c2)cc(OC)c1OC 10.1016/j.ejmech.2018.04.020
11538251 146118 0 HRH3 H3 receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 385 4 0 5 4.6 Cc1cc2ncc(-c3ccc4cc(CCN5CCC[C@H]5C)ccc4n3)c(C)n2n1 10.1021/jm0705051
CHEMBL392573 146118 0 HRH3 H3 receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 385 4 0 5 4.6 Cc1cc2ncc(-c3ccc4cc(CCN5CCC[C@H]5C)ccc4n3)c(C)n2n1 10.1021/jm0705051
CHEMBL4165989 161584 0 HRH3 H3 receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 458 5 1 4 5.4 COc1ccc(NC2(c3ccc(F)cc3)C(=O)N(C(C)(C)C)C(=O)/C2=C/c2ccccc2)cc1 10.1016/j.ejmech.2018.04.020
11708125 75927 2 HRH3 H3 receptor Human 8.9 pEC50 = 8.9 Functional
Activity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cellsActivity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cells
ChEMBL 167 5 1 2 1.3 CN(C)CCCCc1c[nH]cn1 10.1021/jm0504353
CHEMBL206000 75927 2 HRH3 H3 receptor Human 8.9 pEC50 = 8.9 Functional
Activity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cellsActivity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cells
ChEMBL 167 5 1 2 1.3 CN(C)CCCCc1c[nH]cn1 10.1021/jm0504353
89104074 175398 0 HRH3 H3 receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 179 2 2 5 -0.5 CNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4466700 175398 0 HRH3 H3 receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 179 2 2 5 -0.5 CNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4594865 175398 0 HRH3 H3 receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 179 2 2 5 -0.5 CNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4164467 161482 0 HRH3 H3 receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 548 6 1 5 6.0 COc1ccc(NC2(c3ccc(Br)cc3)C(=O)N(C(C)(C)C)C(=O)/C2=C/c2ccccc2)cc1OC 10.1016/j.ejmech.2018.04.020
1218 220 41 HRH3 H3 receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 330 4 0 3 5.0 N#Cc1ccc(cc1)c1ccc2c(c1)cc(o2)CCN1CCC[C@H]1C 10.1021/jm0705051
9818903 220 41 HRH3 H3 receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 330 4 0 3 5.0 N#Cc1ccc(cc1)c1ccc2c(c1)cc(o2)CCN1CCC[C@H]1C 10.1021/jm0705051
CHEMBL351231 220 41 HRH3 H3 receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 330 4 0 3 5.0 N#Cc1ccc(cc1)c1ccc2c(c1)cc(o2)CCN1CCC[C@H]1C 10.1021/jm0705051
1218 220 41 HRH3 H3 receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 330 4 0 3 5.0 N#Cc1ccc(cc1)c1ccc2c(c1)cc(o2)CCN1CCC[C@H]1C 10.1021/jm0705051
9818903 220 41 HRH3 H3 receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 330 4 0 3 5.0 N#Cc1ccc(cc1)c1ccc2c(c1)cc(o2)CCN1CCC[C@H]1C 10.1021/jm0705051
CHEMBL351231 220 41 HRH3 H3 receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 330 4 0 3 5.0 N#Cc1ccc(cc1)c1ccc2c(c1)cc(o2)CCN1CCC[C@H]1C 10.1021/jm0705051
CHEMBL4164467 161482 0 HRH3 H3 receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 548 6 1 5 6.0 COc1ccc(NC2(c3ccc(Br)cc3)C(=O)N(C(C)(C)C)C(=O)/C2=C/c2ccccc2)cc1OC 10.1016/j.ejmech.2018.04.020
CHEMBL4165989 161584 0 HRH3 H3 receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 458 5 1 4 5.4 COc1ccc(NC2(c3ccc(F)cc3)C(=O)N(C(C)(C)C)C(=O)/C2=C/c2ccccc2)cc1 10.1016/j.ejmech.2018.04.020
53483937 64845 0 HRH3 H3 receptor Human 8.9 pEC50 = 8.9 Functional
Antagonist activity at human histamine 3 receptor by [35S]GTPgammaS binding assayAntagonist activity at human histamine 3 receptor by [35S]GTPgammaS binding assay
ChEMBL 345 6 0 5 2.8 C[C@@H]1CCCN1CCCOc1ccc(-c2ccc(=O)n(C)n2)cc1F 10.1016/j.bmcl.2011.06.108
CHEMBL1829477 64845 0 HRH3 H3 receptor Human 8.9 pEC50 = 8.9 Functional
Antagonist activity at human histamine 3 receptor by [35S]GTPgammaS binding assayAntagonist activity at human histamine 3 receptor by [35S]GTPgammaS binding assay
ChEMBL 345 6 0 5 2.8 C[C@@H]1CCCN1CCCOc1ccc(-c2ccc(=O)n(C)n2)cc1F 10.1016/j.bmcl.2011.06.108
57396087 70169 0 HRH3 H3 receptor Human 8.9 pEC50 = 8.9 Functional
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 341 4 1 4 2.9 C[C@@H]1CC(=O)NN=C1c1ccc(OC2CCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2012.01.026
CHEMBL1950746 70169 0 HRH3 H3 receptor Human 8.9 pEC50 = 8.9 Functional
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 341 4 1 4 2.9 C[C@@H]1CC(=O)NN=C1c1ccc(OC2CCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2012.01.026
57397654 69091 0 HRH3 H3 receptor Human 8.9 pEC50 = 8.9 Functional
Inverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assay
ChEMBL 329 6 1 4 2.8 CC1CC(=O)NN=C1c1ccc(OCCCN2CCC[C@H]2C)cc1 10.1016/j.bmcl.2011.11.037
CHEMBL1935111 69091 0 HRH3 H3 receptor Human 8.9 pEC50 = 8.9 Functional
Inverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assay
ChEMBL 329 6 1 4 2.8 CC1CC(=O)NN=C1c1ccc(OCCCN2CCC[C@H]2C)cc1 10.1016/j.bmcl.2011.11.037
11819221 45303 2 HRH3 H3 receptor Human 8.9 pEC50 = 8.9 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
ChEMBL 151 2 2 2 0.6 c1nc(CC2CCNC2)c[nH]1 10.1021/jm030905y
CHEMBL153061 45303 2 HRH3 H3 receptor Human 8.9 pEC50 = 8.9 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
ChEMBL 151 2 2 2 0.6 c1nc(CC2CCNC2)c[nH]1 10.1021/jm030905y
57397654 69091 0 HRH3 H3 receptor Human 8.9 pEC50 = 8.9 Functional
Inverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assay
ChEMBL 329 6 1 4 2.8 CC1CC(=O)NN=C1c1ccc(OCCCN2CCC[C@H]2C)cc1 10.1016/j.bmcl.2011.11.037
CHEMBL1935111 69091 0 HRH3 H3 receptor Human 8.9 pEC50 = 8.9 Functional
Inverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assay
ChEMBL 329 6 1 4 2.8 CC1CC(=O)NN=C1c1ccc(OCCCN2CCC[C@H]2C)cc1 10.1016/j.bmcl.2011.11.037
11603648 147386 0 HRH3 H3 receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 397 5 0 5 4.8 Cc1c(-c2ccc3cc(CCN4CCC[C@H]4C)ccc3n2)cnn1-c1ccccn1 10.1021/jm0705051
CHEMBL393581 147386 0 HRH3 H3 receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 397 5 0 5 4.8 Cc1c(-c2ccc3cc(CCN4CCC[C@H]4C)ccc3n2)cnn1-c1ccccn1 10.1021/jm0705051
42625304 178236 0 HRH3 H3 receptor Human 8.9 pEC50 = 8.9 Binding
Agonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 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 178236 0 HRH3 H3 receptor Human 8.9 pEC50 = 8.9 Binding
Agonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 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
11603648 147386 0 HRH3 H3 receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 397 5 0 5 4.8 Cc1c(-c2ccc3cc(CCN4CCC[C@H]4C)ccc3n2)cnn1-c1ccccn1 10.1021/jm0705051
CHEMBL393581 147386 0 HRH3 H3 receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 397 5 0 5 4.8 Cc1c(-c2ccc3cc(CCN4CCC[C@H]4C)ccc3n2)cnn1-c1ccccn1 10.1021/jm0705051
5048 2942 48 HRH3 H3 receptor Guinea pig 8.8 pEC50 = 8.8 Functional
Antagonist activity at human histamine H3 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAntagonist activity at human histamine H3 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.1016/j.bmc.2009.03.014
8924 2942 48 HRH3 H3 receptor Guinea pig 8.8 pEC50 = 8.8 Functional
Antagonist activity at human histamine H3 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAntagonist activity at human histamine H3 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.1016/j.bmc.2009.03.014
9948102 2942 48 HRH3 H3 receptor Guinea pig 8.8 pEC50 = 8.8 Functional
Antagonist activity at human histamine H3 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAntagonist activity at human histamine H3 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.1016/j.bmc.2009.03.014
CHEMBL462605 2942 48 HRH3 H3 receptor Guinea pig 8.8 pEC50 = 8.8 Functional
Antagonist activity at human histamine H3 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAntagonist activity at human histamine H3 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.1016/j.bmc.2009.03.014
DB11642 2942 48 HRH3 H3 receptor Guinea pig 8.8 pEC50 = 8.8 Functional
Antagonist activity at human histamine H3 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAntagonist activity at human histamine H3 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.1016/j.bmc.2009.03.014
11710694 95890 0 HRH3 H3 receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 382 4 0 4 5.2 Cc1nc2ncccc2cc1-c1ccc2cc(CCN3CCC[C@H]3C)ccc2n1 10.1021/jm0705051
CHEMBL263101 95890 0 HRH3 H3 receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 382 4 0 4 5.2 Cc1nc2ncccc2cc1-c1ccc2cc(CCN3CCC[C@H]3C)ccc2n1 10.1021/jm0705051
42625386 177502 0 HRH3 H3 receptor Human 8.8 pEC50 = 8.8 Binding
Agonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 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 177502 0 HRH3 H3 receptor Human 8.8 pEC50 = 8.8 Binding
Agonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 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
42625303 179896 0 HRH3 H3 receptor Human 8.8 pEC50 = 8.8 Binding
Agonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 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 179896 0 HRH3 H3 receptor Human 8.8 pEC50 = 8.8 Binding
Agonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 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
11710694 95890 0 HRH3 H3 receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 382 4 0 4 5.2 Cc1nc2ncccc2cc1-c1ccc2cc(CCN3CCC[C@H]3C)ccc2n1 10.1021/jm0705051
CHEMBL263101 95890 0 HRH3 H3 receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 382 4 0 4 5.2 Cc1nc2ncccc2cc1-c1ccc2cc(CCN3CCC[C@H]3C)ccc2n1 10.1021/jm0705051
11689509 108711 0 HRH3 H3 receptor Human 8.8 pEC50 = 8.8 Functional
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation countingInverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation counting
ChEMBL 383 8 0 5 4.6 c1cc(-c2nc(CN3CCCCC3)co2)ccc1OCCCN1CCCCC1 10.1039/C0MD00056F
CHEMBL3220124 108711 0 HRH3 H3 receptor Human 8.8 pEC50 = 8.8 Functional
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation countingInverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation counting
ChEMBL 383 8 0 5 4.6 c1cc(-c2nc(CN3CCCCC3)co2)ccc1OCCCN1CCCCC1 10.1039/C0MD00056F
CHEMBL3220126 108713 0 HRH3 H3 receptor Human 8.8 pEC50 = 8.8 Functional
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation countingInverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation counting
ChEMBL 370 5 0 6 3.8 COC(=O)c1oc(-c2ccc(O[C@H]3C[C@H](N4CCCCC4)C3)cc2)nc1C 10.1039/C0MD00056F
46222045 8512 0 HRH3 H3 receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 243 4 2 2 3.4 CC(C)(C)c1ccc(NCCc2c[nH]cn2)cc1 10.1021/jm901890s
CHEMBL1096516 8512 0 HRH3 H3 receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 243 4 2 2 3.4 CC(C)(C)c1ccc(NCCc2c[nH]cn2)cc1 10.1021/jm901890s
49799184 10688 0 HRH3 H3 receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 291 3 1 2 4.0 c1ccc2cc(N3CCC(Cc4c[nH]cn4)CC3)ccc2c1 10.1016/j.bmc.2010.04.052
CHEMBL1173390 10688 0 HRH3 H3 receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 291 3 1 2 4.0 c1ccc2cc(N3CCC(Cc4c[nH]cn4)CC3)ccc2c1 10.1016/j.bmc.2010.04.052
57403054 70170 0 HRH3 H3 receptor Human 8.8 pEC50 = 8.8 Functional
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 341 4 1 4 2.9 C[C@H]1CC(=O)NN=C1c1ccc(OC2CCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2012.01.026
CHEMBL1950747 70170 0 HRH3 H3 receptor Human 8.8 pEC50 = 8.8 Functional
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 341 4 1 4 2.9 C[C@H]1CC(=O)NN=C1c1ccc(OC2CCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2012.01.026
25149708 185757 0 HRH3 H3 receptor Human 8.8 pEC50 = 8.8 Binding
Activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, G-beta-1-gamma-2 and RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, G-beta-1-gamma-2 and RGS4 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 185757 0 HRH3 H3 receptor Human 8.8 pEC50 = 8.8 Binding
Activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, G-beta-1-gamma-2 and RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, G-beta-1-gamma-2 and RGS4 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
CHEMBL4635634 177388 0 HRH3 H3 receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human H3R expressed in HEK293T-SP-FLAG-hH3R-CRE-CBR cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H3R expressed in HEK293T-SP-FLAG-hH3R-CRE-CBR cells incubated for 5 hrs by luciferase reporter gene assay
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 177388 0 HRH3 H3 receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human H3R expressed in HEK293T-SP-FLAG-hH3R-CRE-CBR cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H3R expressed in HEK293T-SP-FLAG-hH3R-CRE-CBR cells incubated for 5 hrs by luciferase reporter gene assay
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
49799537 10280 0 HRH3 H3 receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 270 4 2 3 2.9 CNc1ccc(N2CCC(Cc3c[nH]cn3)CC2)cc1 10.1016/j.bmc.2010.04.052
CHEMBL1169687 10280 0 HRH3 H3 receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 270 4 2 3 2.9 CNc1ccc(N2CCC(Cc3c[nH]cn3)CC2)cc1 10.1016/j.bmc.2010.04.052
59651957 74218 0 HRH3 H3 receptor Human 8.8 pEC50 = 8.8 Functional
Inverse agonist activity at human H3 receptor by [35S]GTPgamma binding assayInverse agonist activity at human H3 receptor by [35S]GTPgamma binding assay
ChEMBL 353 5 0 5 2.8 C[C@@H]1CCCN1CCCOc1ccc2c(c1)CCc1cc(=O)n(C)nc1-2 10.1016/j.bmcl.2012.04.001
CHEMBL2031470 74218 0 HRH3 H3 receptor Human 8.8 pEC50 = 8.8 Functional
Inverse agonist activity at human H3 receptor by [35S]GTPgamma binding assayInverse agonist activity at human H3 receptor by [35S]GTPgamma binding assay
ChEMBL 353 5 0 5 2.8 C[C@@H]1CCCN1CCCOc1ccc2c(c1)CCc1cc(=O)n(C)nc1-2 10.1016/j.bmcl.2012.04.001
1223 900 24 HRH3 H3 receptor Mouse 8.8 pEC50 = 8.8 Functional
Inverse agonist activity at mouse histamine H3 receptor overexpressed in HEK293 cells by [35S]GTPgammaS binding assayInverse agonist activity at mouse histamine H3 receptor overexpressed in HEK293 cells by [35S]GTPgammaS binding assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1016/j.bmcl.2009.06.025
2790 900 24 HRH3 H3 receptor Mouse 8.8 pEC50 = 8.8 Functional
Inverse agonist activity at mouse histamine H3 receptor overexpressed in HEK293 cells by [35S]GTPgammaS binding assayInverse agonist activity at mouse histamine H3 receptor overexpressed in HEK293 cells by [35S]GTPgammaS binding assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1016/j.bmcl.2009.06.025
CHEMBL14690 900 24 HRH3 H3 receptor Mouse 8.8 pEC50 = 8.8 Functional
Inverse agonist activity at mouse histamine H3 receptor overexpressed in HEK293 cells by [35S]GTPgammaS binding assayInverse agonist activity at mouse histamine H3 receptor overexpressed in HEK293 cells by [35S]GTPgammaS binding assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1016/j.bmcl.2009.06.025
56954322 81432 0 HRH3 H3 receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human H3R-Galphai2-Gbeta1gamma2-RGS4 expressed in Sf9 cells 0.1 nM to 1 mM by steady state GTPase activity assayAgonist activity at human H3R-Galphai2-Gbeta1gamma2-RGS4 expressed in Sf9 cells 0.1 nM to 1 mM 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 81432 0 HRH3 H3 receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human H3R-Galphai2-Gbeta1gamma2-RGS4 expressed in Sf9 cells 0.1 nM to 1 mM by steady state GTPase activity assayAgonist activity at human H3R-Galphai2-Gbeta1gamma2-RGS4 expressed in Sf9 cells 0.1 nM to 1 mM 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
49857998 74592 0 HRH3 H3 receptor Human 8.7 pEC50 = 8.7 Functional
Inverse agonist activity at human histamine H3 receptor by [35S]-GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor by [35S]-GTPgammaS binding assay
ChEMBL 380 8 0 4 3.9 C[C@@H]1CCCN1CCCOc1ccc(C(=O)CN2CCC(F)(F)CC2)cc1 10.1016/j.bmcl.2012.02.081
CHEMBL2036643 74592 0 HRH3 H3 receptor Human 8.7 pEC50 = 8.7 Functional
Inverse agonist activity at human histamine H3 receptor by [35S]-GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor by [35S]-GTPgammaS binding assay
ChEMBL 380 8 0 4 3.9 C[C@@H]1CCCN1CCCOc1ccc(C(=O)CN2CCC(F)(F)CC2)cc1 10.1016/j.bmcl.2012.02.081
46830167 8491 0 HRH3 H3 receptor Human 8.7 pEC50 = 8.7 Binding
Activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 and RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 and RGS4 by steady-state GTPase activity 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 8491 0 HRH3 H3 receptor Human 8.7 pEC50 = 8.7 Binding
Activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 and RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 and RGS4 by steady-state GTPase activity 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
11957573 1879 25 HRH3 H3 receptor Human 8.7 pEC50 = 8.7 Binding
Inhibition of human Histamine H3 receptor using [3H]N-alpha-methyl histamineInhibition of human Histamine H3 receptor using [3H]N-alpha-methyl histamine
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm020415q
1250 1879 25 HRH3 H3 receptor Human 8.7 pEC50 = 8.7 Binding
Inhibition of human Histamine H3 receptor using [3H]N-alpha-methyl histamineInhibition of human Histamine H3 receptor using [3H]N-alpha-methyl histamine
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm020415q
3692 1879 25 HRH3 H3 receptor Human 8.7 pEC50 = 8.7 Binding
Inhibition of human Histamine H3 receptor using [3H]N-alpha-methyl histamineInhibition of human Histamine H3 receptor using [3H]N-alpha-methyl histamine
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm020415q
CHEMBL19439 1879 25 HRH3 H3 receptor Human 8.7 pEC50 = 8.7 Binding
Inhibition of human Histamine H3 receptor using [3H]N-alpha-methyl histamineInhibition of human Histamine H3 receptor using [3H]N-alpha-methyl histamine
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm020415q
155540793 175432 0 HRH3 H3 receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 221 4 2 5 0.6 CCC(C)NC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4516714 175432 0 HRH3 H3 receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 221 4 2 5 0.6 CCC(C)NC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4595102 175432 0 HRH3 H3 receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 221 4 2 5 0.6 CCC(C)NC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
24825522 184965 0 HRH3 H3 receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 283 3 1 3 3.3 CC1CC(C)(C)N=C(c2cccc(Cc3c[nH]cn3)c2)O1 10.1021/jm7014149
CHEMBL494982 184965 0 HRH3 H3 receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 283 3 1 3 3.3 CC1CC(C)(C)N=C(c2cccc(Cc3c[nH]cn3)c2)O1 10.1021/jm7014149
16059780 168555 0 HRH3 H3 receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 334 4 0 4 4.0 Cc1nn(C)cc1-c1ccc2cc(CCN3CCC[C@H]3C)ccc2n1 10.1021/jm0705051
CHEMBL442242 168555 0 HRH3 H3 receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 334 4 0 4 4.0 Cc1nn(C)cc1-c1ccc2cc(CCN3CCC[C@H]3C)ccc2n1 10.1021/jm0705051
CHEMBL3220122 108709 0 HRH3 H3 receptor Human 8.7 pEC50 = 8.7 Functional
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation countingInverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation counting
ChEMBL 368 4 0 4 4.6 c1cc(C2=NC3(CCCCC3)CO2)ccc1O[C@H]1C[C@H](N2CCCCC2)C1 10.1039/C0MD00056F
11600849 139747 0 HRH3 H3 receptor Human 8.0 pEC50 = 8 Functional
Activity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cellsActivity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cells
ChEMBL 195 8 2 2 2.1 CCCNCCCCCc1c[nH]cn1 10.1021/jm0504353
CHEMBL381074 139747 0 HRH3 H3 receptor Human 8.0 pEC50 = 8 Functional
Activity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cellsActivity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cells
ChEMBL 195 8 2 2 2.1 CCCNCCCCCc1c[nH]cn1 10.1021/jm0504353
145951678 162123 0 HRH3 H3 receptor Human 8.0 pEC50 = 8 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 406 2 1 3 2.7 O=C1C=C[C@]23C(c4ccccc4)=CC(=O)N2[C@H](c2cc(F)cc(F)c2)C(=O)N[C@@H]3C1 10.1016/j.ejmech.2018.04.020
CHEMBL4174591 162123 0 HRH3 H3 receptor Human 8.0 pEC50 = 8 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 406 2 1 3 2.7 O=C1C=C[C@]23C(c4ccccc4)=CC(=O)N2[C@H](c2cc(F)cc(F)c2)C(=O)N[C@@H]3C1 10.1016/j.ejmech.2018.04.020
141272770 175538 0 HRH3 H3 receptor Human 8.0 pEC50 = 8 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 193 2 2 5 -0.2 CNC1CN(c2cc(C)nc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4468740 175538 0 HRH3 H3 receptor Human 8.0 pEC50 = 8 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 193 2 2 5 -0.2 CNC1CN(c2cc(C)nc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4595912 175538 0 HRH3 H3 receptor Human 8.0 pEC50 = 8 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 193 2 2 5 -0.2 CNC1CN(c2cc(C)nc(N)n2)C1 10.1021/acs.jmedchem.9b01462
1238 1952 8 HRH3 H3 receptor Human 8.0 pEC50 = 8 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 2 2 2 0.3 C[C@@H](Cc1cnc[nH]1)N 10.1016/j.bmcl.2010.10.041
6603865 1952 8 HRH3 H3 receptor Human 8.0 pEC50 = 8 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 2 2 2 0.3 C[C@@H](Cc1cnc[nH]1)N 10.1016/j.bmcl.2010.10.041
CHEMBL11919 1952 8 HRH3 H3 receptor Human 8.0 pEC50 = 8 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 2 2 2 0.3 C[C@@H](Cc1cnc[nH]1)N 10.1016/j.bmcl.2010.10.041
10154137 195441 3 HRH3 H3 receptor Human 8.0 pEC50 = 8 Binding
Inhibition of human Histamine H3 receptor using [3H]N-alpha-methyl histamineInhibition of human Histamine H3 receptor using [3H]N-alpha-methyl histamine
ChEMBL 151 3 2 2 0.9 NCC[C@@H]1C[C@@H]1c1c[nH]cn1 10.1021/jm020415q
CHEMBL60716 195441 3 HRH3 H3 receptor Human 8.0 pEC50 = 8 Binding
Inhibition of human Histamine H3 receptor using [3H]N-alpha-methyl histamineInhibition of human Histamine H3 receptor using [3H]N-alpha-methyl histamine
ChEMBL 151 3 2 2 0.9 NCC[C@@H]1C[C@@H]1c1c[nH]cn1 10.1021/jm020415q
145951678 162123 0 HRH3 H3 receptor Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 406 2 1 3 2.7 O=C1C=C[C@]23C(c4ccccc4)=CC(=O)N2[C@H](c2cc(F)cc(F)c2)C(=O)N[C@@H]3C1 10.1016/j.ejmech.2018.04.020
CHEMBL4174591 162123 0 HRH3 H3 receptor Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 406 2 1 3 2.7 O=C1C=C[C@]23C(c4ccccc4)=CC(=O)N2[C@H](c2cc(F)cc(F)c2)C(=O)N[C@@H]3C1 10.1016/j.ejmech.2018.04.020
25218397 74349 0 HRH3 H3 receptor Human 8.0 pEC50 = 8.0 Binding
Inverse agonist activity at human H3 receptor expressed in HEK293T cells assessed as inhibition of {35S]GTPgamma bindingInverse agonist activity at human H3 receptor expressed in HEK293T cells assessed as inhibition of {35S]GTPgamma binding
ChEMBL 391 5 0 3 3.2 CN(C)C(=O)c1ccc(-c2ccc3c(c2)CCN(CCN2CCCC2)C3=O)cc1 10.1021/jm300011d
CHEMBL2031874 74349 0 HRH3 H3 receptor Human 8.0 pEC50 = 8.0 Binding
Inverse agonist activity at human H3 receptor expressed in HEK293T cells assessed as inhibition of {35S]GTPgamma bindingInverse agonist activity at human H3 receptor expressed in HEK293T cells assessed as inhibition of {35S]GTPgamma binding
ChEMBL 391 5 0 3 3.2 CN(C)C(=O)c1ccc(-c2ccc3c(c2)CCN(CCN2CCCC2)C3=O)cc1 10.1021/jm300011d
42625223 179059 0 HRH3 H3 receptor Human 8.0 pEC50 = 8.0 Binding
Agonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 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 179059 0 HRH3 H3 receptor Human 8.0 pEC50 = 8.0 Binding
Agonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 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
155541911 172228 0 HRH3 H3 receptor Human 7.0 pEC50 = 7 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 235 3 1 5 0.9 CC(C)c1cc(N2CC(N(C)C)C2)nc(N)n1 10.1021/acs.jmedchem.9b01462
CHEMBL4519616 172228 0 HRH3 H3 receptor Human 7.0 pEC50 = 7 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 235 3 1 5 0.9 CC(C)c1cc(N2CC(N(C)C)C2)nc(N)n1 10.1021/acs.jmedchem.9b01462
10978141 4901 1 HRH3 H3 receptor Human 7.0 pEC50 = 7 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@H]2CC[C@H](c3c[nH]cn3)O2)cc1 10.1016/j.bmcl.2010.10.041
CHEMBL105803 4901 1 HRH3 H3 receptor Human 7.0 pEC50 = 7 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@H]2CC[C@H](c3c[nH]cn3)O2)cc1 10.1016/j.bmcl.2010.10.041
10678661 5110 1 HRH3 H3 receptor Human 7.0 pEC50 = 7 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 167 2 2 3 0.6 NC[C@@H]1CC[C@@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
CHEMBL106931 5110 1 HRH3 H3 receptor Human 7.0 pEC50 = 7 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 167 2 2 3 0.6 NC[C@@H]1CC[C@@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
1267 3569 38 HRH3 H3 receptor Human 7.0 pEC50 = 7 Functional
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation countingInverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation counting
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1039/C0MD00056F
3035905 3569 38 HRH3 H3 receptor Human 7.0 pEC50 = 7 Functional
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation countingInverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation counting
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1039/C0MD00056F
CHEMBL260374 3569 38 HRH3 H3 receptor Human 7.0 pEC50 = 7 Functional
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation countingInverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation counting
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1039/C0MD00056F
1278 2017 71 HRH3 H3 receptor Human 6.0 pEC50 = 6 Binding
Effective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cellsEffective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2004.08.035
1279 2017 71 HRH3 H3 receptor Human 6.0 pEC50 = 6 Binding
Effective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cellsEffective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2004.08.035
4908365 2017 71 HRH3 H3 receptor Human 6.0 pEC50 = 6 Binding
Effective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cellsEffective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2004.08.035
CHEMBL129198 2017 71 HRH3 H3 receptor Human 6.0 pEC50 = 6 Binding
Effective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cellsEffective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2004.08.035
44395364 66337 0 HRH3 H3 receptor Human 6.0 pEC50 = 6 Binding
Effective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cellsEffective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cells
ChEMBL 276 2 1 2 3.3 CN1CCC(C(=O)c2cc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2004.08.035
CHEMBL186456 66337 0 HRH3 H3 receptor Human 6.0 pEC50 = 6 Binding
Effective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cellsEffective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cells
ChEMBL 276 2 1 2 3.3 CN1CCC(C(=O)c2cc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2004.08.035
44395314 122910 0 HRH3 H3 receptor Human 6.0 pEC50 = 6 Binding
Effective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cellsEffective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cells
ChEMBL 278 2 2 2 3.2 CN1CCC(C(O)c2cc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2004.08.035
CHEMBL362163 122910 0 HRH3 H3 receptor Human 6.0 pEC50 = 6 Binding
Effective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cellsEffective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cells
ChEMBL 278 2 2 2 3.2 CN1CCC(C(O)c2cc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2004.08.035
10037650 4958 0 HRH3 H3 receptor Human 5.0 pEC50 = 5 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
CHEMBL106158 4958 0 HRH3 H3 receptor Human 5.0 pEC50 = 5 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
11043445 55965 1 HRH3 H3 receptor Human 5.0 pEC50 = 5 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@H]2CC[C@@H](c3c[nH]cn3)O2)cc1 10.1016/j.bmcl.2010.10.041
CHEMBL1632410 55965 1 HRH3 H3 receptor Human 5.0 pEC50 = 5 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@H]2CC[C@@H](c3c[nH]cn3)O2)cc1 10.1016/j.bmcl.2010.10.041
10945113 108902 1 HRH3 H3 receptor Human 5.0 pEC50 = 5 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@@H]2CC[C@@H](c3c[nH]cn3)O2)cc1 10.1016/j.bmcl.2010.10.041
CHEMBL322256 108902 1 HRH3 H3 receptor Human 5.0 pEC50 = 5 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@@H]2CC[C@@H](c3c[nH]cn3)O2)cc1 10.1016/j.bmcl.2010.10.041
10037650 4958 0 HRH3 H3 receptor Human 5.0 pEC50 = 5.0 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptor
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL106158 4958 0 HRH3 H3 receptor Human 5.0 pEC50 = 5.0 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptor
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
145953579 161626 0 HRH3 H3 receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 486 5 1 3 5.2 O=C1C=CC2(C=C1)C(c1ccccc1)=CC(=O)N2C(C(=O)NC1CCCCC1)c1ccc(Cl)cc1 10.1016/j.ejmech.2018.04.020
CHEMBL4166645 161626 0 HRH3 H3 receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 486 5 1 3 5.2 O=C1C=CC2(C=C1)C(c1ccccc1)=CC(=O)N2C(C(=O)NC1CCCCC1)c1ccc(Cl)cc1 10.1016/j.ejmech.2018.04.020
145952741 161677 0 HRH3 H3 receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 544 8 1 5 5.6 COc1cc(N2C(=O)/C(=C\c3ccccc3)C2(C(=O)NC2CCCCC2)c2ccc(F)cc2)cc(OC)c1OC 10.1016/j.ejmech.2018.04.020
CHEMBL4167482 161677 0 HRH3 H3 receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 544 8 1 5 5.6 COc1cc(N2C(=O)/C(=C\c3ccccc3)C2(C(=O)NC2CCCCC2)c2ccc(F)cc2)cc(OC)c1OC 10.1016/j.ejmech.2018.04.020
145953579 161626 0 HRH3 H3 receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 486 5 1 3 5.2 O=C1C=CC2(C=C1)C(c1ccccc1)=CC(=O)N2C(C(=O)NC1CCCCC1)c1ccc(Cl)cc1 10.1016/j.ejmech.2018.04.020
CHEMBL4166645 161626 0 HRH3 H3 receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 486 5 1 3 5.2 O=C1C=CC2(C=C1)C(c1ccccc1)=CC(=O)N2C(C(=O)NC1CCCCC1)c1ccc(Cl)cc1 10.1016/j.ejmech.2018.04.020
10678661 5110 1 HRH3 H3 receptor Human 7.0 pEC50 = 7.0 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptor
ChEMBL 167 2 2 3 0.6 NC[C@@H]1CC[C@@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL106931 5110 1 HRH3 H3 receptor Human 7.0 pEC50 = 7.0 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptor
ChEMBL 167 2 2 3 0.6 NC[C@@H]1CC[C@@H](c2c[nH]cn2)O1 10.1021/jm0300025
12769844 108751 0 HRH3 H3 receptor Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
ChEMBL 234 5 3 3 0.7 CN/C(=N/C#N)NCCCCc1nc[nH]c1C 10.1039/C3MD00245D
CHEMBL3220641 108751 0 HRH3 H3 receptor Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
ChEMBL 234 5 3 3 0.7 CN/C(=N/C#N)NCCCCc1nc[nH]c1C 10.1039/C3MD00245D
16739387 185800 0 HRH3 H3 receptor Human 8.0 pEC50 = 8.0 Binding
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
ChEMBL 563 6 0 6 5.1 CC(C)N1CCC(Oc2ccc3c(c2)cc(C(=O)N2CCC(F)(F)CC2)n3S(=O)(=O)c2ccc(F)cc2)CC1 10.1021/jm900409x
CHEMBL503070 185800 0 HRH3 H3 receptor Human 8.0 pEC50 = 8.0 Binding
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
ChEMBL 563 6 0 6 5.1 CC(C)N1CCC(Oc2ccc3c(c2)cc(C(=O)N2CCC(F)(F)CC2)n3S(=O)(=O)c2ccc(F)cc2)CC1 10.1021/jm900409x
1267 3569 38 HRH3 H3 receptor Mouse 8.0 pEC50 = 8.0 Functional
Inverse agonist activity at mouse histamine H3 receptor overexpressed in HEK293 cells by [35S]GTPgammaS binding assayInverse agonist activity at mouse histamine H3 receptor overexpressed in HEK293 cells by [35S]GTPgammaS binding assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmcl.2009.06.025
3035905 3569 38 HRH3 H3 receptor Mouse 8.0 pEC50 = 8.0 Functional
Inverse agonist activity at mouse histamine H3 receptor overexpressed in HEK293 cells by [35S]GTPgammaS binding assayInverse agonist activity at mouse histamine H3 receptor overexpressed in HEK293 cells by [35S]GTPgammaS binding assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmcl.2009.06.025
CHEMBL260374 3569 38 HRH3 H3 receptor Mouse 8.0 pEC50 = 8.0 Functional
Inverse agonist activity at mouse histamine H3 receptor overexpressed in HEK293 cells by [35S]GTPgammaS binding assayInverse agonist activity at mouse histamine H3 receptor overexpressed in HEK293 cells by [35S]GTPgammaS binding assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmcl.2009.06.025
44185243 185361 0 HRH3 H3 receptor Human 7.0 pEC50 = 7.0 Binding
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
ChEMBL 389 4 1 4 3.0 CC(C)N1CCC(Oc2cc3[nH]c(C(=O)N4CCOCC4)cc3cc2F)CC1 10.1021/jm900409x
CHEMBL497632 185361 0 HRH3 H3 receptor Human 7.0 pEC50 = 7.0 Binding
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
ChEMBL 389 4 1 4 3.0 CC(C)N1CCC(Oc2cc3[nH]c(C(=O)N4CCOCC4)cc3cc2F)CC1 10.1021/jm900409x
46890592 6134 0 HRH3 H3 receptor Human 6.9 pEC50 = 6.9 Binding
Displacement of [125H]iodoproxyphan from human recombinant histamine H3 receptor expressed in human SK-N-MC cellsDisplacement of [125H]iodoproxyphan from human recombinant histamine H3 receptor expressed in human SK-N-MC cells
ChEMBL 422 6 2 4 4.4 Cc1cc(OCCCN2C[C@H]3CCCN[C@H]3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1082296 6134 0 HRH3 H3 receptor Human 6.9 pEC50 = 6.9 Binding
Displacement of [125H]iodoproxyphan from human recombinant histamine H3 receptor expressed in human SK-N-MC cellsDisplacement of [125H]iodoproxyphan from human recombinant histamine H3 receptor expressed in human SK-N-MC cells
ChEMBL 422 6 2 4 4.4 Cc1cc(OCCCN2C[C@H]3CCCN[C@H]3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
49799507 10611 0 HRH3 H3 receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 283 4 1 2 4.0 CC(C)c1ccc(N2CCC(Cc3c[nH]cn3)CC2)cc1 10.1016/j.bmc.2010.04.052
CHEMBL1172712 10611 0 HRH3 H3 receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 283 4 1 2 4.0 CC(C)c1ccc(N2CCC(Cc3c[nH]cn3)CC2)cc1 10.1016/j.bmc.2010.04.052
16678620 17021 0 HRH3 H3 receptor Human 7.9 pEC50 = 7.9 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 418 5 0 5 3.9 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCN(Cc3ccncc3)C2=O)CC1 10.1016/j.bmcl.2010.08.009
CHEMBL1257487 17021 0 HRH3 H3 receptor Human 7.9 pEC50 = 7.9 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 418 5 0 5 3.9 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCN(Cc3ccncc3)C2=O)CC1 10.1016/j.bmcl.2010.08.009
155533940 171024 0 HRH3 H3 receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 207 3 2 5 0.2 CCNC1CN(c2cc(C)nc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4469111 171024 0 HRH3 H3 receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 207 3 2 5 0.2 CCNC1CN(c2cc(C)nc(N)n2)C1 10.1021/acs.jmedchem.9b01462
42623731 171130 0 HRH3 H3 receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 221 3 2 5 0.6 CNC1CN(c2cc(C(C)C)nc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4470781 171130 0 HRH3 H3 receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 221 3 2 5 0.6 CNC1CN(c2cc(C(C)C)nc(N)n2)C1 10.1021/acs.jmedchem.9b01462
10176370 42888 10 HRH3 H3 receptor Human 7.9 pEC50 = 7.9 Functional
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
ChEMBL 179 3 2 2 1.3 c1nc(CCC2CCNCC2)c[nH]1 10.1021/jm049475h
CHEMBL150701 42888 10 HRH3 H3 receptor Human 7.9 pEC50 = 7.9 Functional
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
ChEMBL 179 3 2 2 1.3 c1nc(CCC2CCNCC2)c[nH]1 10.1021/jm049475h
1204 1806 104 HRH3 H3 receptor Human 7.9 pEC50 = 7.9 Binding
Activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 and RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 and RGS4 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.03.082
1247 1806 104 HRH3 H3 receptor Human 7.9 pEC50 = 7.9 Binding
Activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 and RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 and RGS4 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.03.082
1375 1806 104 HRH3 H3 receptor Human 7.9 pEC50 = 7.9 Binding
Activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 and RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 and RGS4 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.03.082
774 1806 104 HRH3 H3 receptor Human 7.9 pEC50 = 7.9 Binding
Activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 and RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 and RGS4 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.03.082
CHEMBL90 1806 104 HRH3 H3 receptor Human 7.9 pEC50 = 7.9 Binding
Activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 and RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 and RGS4 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.03.082
DB05381 1806 104 HRH3 H3 receptor Human 7.9 pEC50 = 7.9 Binding
Activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 and RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 and RGS4 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.03.082
1204 1806 104 HRH3 H3 receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 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 1806 104 HRH3 H3 receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 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 1806 104 HRH3 H3 receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 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 1806 104 HRH3 H3 receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 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 1806 104 HRH3 H3 receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 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 1806 104 HRH3 H3 receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 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
1269 117 26 HRH3 H3 receptor Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1021/acs.jmedchem.6b00120
37463 117 26 HRH3 H3 receptor Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1021/acs.jmedchem.6b00120
CHEMBL275443 117 26 HRH3 H3 receptor Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1021/acs.jmedchem.6b00120
155527111 170283 0 HRH3 H3 receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human H3R expressed on cells incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at recombinant human H3R expressed on cells incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 579 8 2 8 3.8 CCCCC(=O)O[C@@H]1C[C@H](C)N2C[C@]3(NC)C[C@]4(C(=O)Nc5c(C(=O)[C@H]6OC6(C)C)cccc54)[C@](C)(C=O)[C@H]3C[C@H]2C1 10.1021/acs.jmedchem.9b01462
CHEMBL4458116 170283 0 HRH3 H3 receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human H3R expressed on cells incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at recombinant human H3R expressed on cells incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 579 8 2 8 3.8 CCCCC(=O)O[C@@H]1C[C@H](C)N2C[C@]3(NC)C[C@]4(C(=O)Nc5c(C(=O)[C@H]6OC6(C)C)cccc54)[C@](C)(C=O)[C@H]3C[C@H]2C1 10.1021/acs.jmedchem.9b01462
10465285 9229 0 HRH3 H3 receptor Rat 6.9 pEC50 = 6.9 Binding
In vitro binding affinity against histamine H3 receptor from synaptosomes of rat cerebral cortexIn vitro binding affinity against histamine H3 receptor from synaptosomes of rat cerebral cortex
ChEMBL 196 7 1 2 2.4 CC(C)CCOCCCc1c[nH]cn1 10.1021/jm991068w
CHEMBL112084 9229 0 HRH3 H3 receptor Rat 6.9 pEC50 = 6.9 Binding
In vitro binding affinity against histamine H3 receptor from synaptosomes of rat cerebral cortexIn vitro binding affinity against histamine H3 receptor from synaptosomes of rat cerebral cortex
ChEMBL 196 7 1 2 2.4 CC(C)CCOCCCc1c[nH]cn1 10.1021/jm991068w
CHEMBL2145444 9229 0 HRH3 H3 receptor Rat 6.9 pEC50 = 6.9 Binding
In vitro binding affinity against histamine H3 receptor from synaptosomes of rat cerebral cortexIn vitro binding affinity against histamine H3 receptor from synaptosomes of rat cerebral cortex
ChEMBL 196 7 1 2 2.4 CC(C)CCOCCCc1c[nH]cn1 10.1021/jm991068w
145957226 161317 0 HRH3 H3 receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 686 9 1 6 7.1 COc1ccc(C(C(=O)NC2CCCCC2)N2C(=O)C(c3ccc(C(F)(F)F)cc3)=C(c3ccccc3)C23C=CC(=O)C=C3)c(OC)c1OC 10.1016/j.ejmech.2018.04.020
CHEMBL4161732 161317 0 HRH3 H3 receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 686 9 1 6 7.1 COc1ccc(C(C(=O)NC2CCCCC2)N2C(=O)C(c3ccc(C(F)(F)F)cc3)=C(c3ccccc3)C23C=CC(=O)C=C3)c(OC)c1OC 10.1016/j.ejmech.2018.04.020
1204 1806 104 HRH3 H3 receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
1247 1806 104 HRH3 H3 receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
1375 1806 104 HRH3 H3 receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
774 1806 104 HRH3 H3 receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
CHEMBL90 1806 104 HRH3 H3 receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
DB05381 1806 104 HRH3 H3 receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
16678619 17020 0 HRH3 H3 receptor Human 7.9 pEC50 = 7.9 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 418 5 0 5 3.9 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCN(Cc3cccnc3)C2=O)CC1 10.1016/j.bmcl.2010.08.009
CHEMBL1257486 17020 0 HRH3 H3 receptor Human 7.9 pEC50 = 7.9 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 418 5 0 5 3.9 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCN(Cc3cccnc3)C2=O)CC1 10.1016/j.bmcl.2010.08.009
10176370 42888 10 HRH3 H3 receptor Human 7.9 pEC50 = 7.9 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
ChEMBL 179 3 2 2 1.3 c1nc(CCC2CCNCC2)c[nH]1 10.1021/jm030905y
CHEMBL150701 42888 10 HRH3 H3 receptor Human 7.9 pEC50 = 7.9 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
ChEMBL 179 3 2 2 1.3 c1nc(CCC2CCNCC2)c[nH]1 10.1021/jm030905y
145957226 161317 0 HRH3 H3 receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 686 9 1 6 7.1 COc1ccc(C(C(=O)NC2CCCCC2)N2C(=O)C(c3ccc(C(F)(F)F)cc3)=C(c3ccccc3)C23C=CC(=O)C=C3)c(OC)c1OC 10.1016/j.ejmech.2018.04.020
CHEMBL4161732 161317 0 HRH3 H3 receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 686 9 1 6 7.1 COc1ccc(C(C(=O)NC2CCCCC2)N2C(=O)C(c3ccc(C(F)(F)F)cc3)=C(c3ccccc3)C23C=CC(=O)C=C3)c(OC)c1OC 10.1016/j.ejmech.2018.04.020
9877454 199171 1 HRH3 H3 receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 159 2 1 2 1.4 c1ccc(Cc2c[nH]cn2)nc1 10.1021/jm100643t
CHEMBL81644 199171 1 HRH3 H3 receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 159 2 1 2 1.4 c1ccc(Cc2c[nH]cn2)nc1 10.1021/jm100643t
11206058 103698 7 HRH3 H3 receptor Human 5.9 pEC50 = 5.9 Binding
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
ChEMBL 173 3 1 2 1.6 c1ccc(CCc2c[nH]cn2)nc1 10.1021/jm049932u
CHEMBL310360 103698 7 HRH3 H3 receptor Human 5.9 pEC50 = 5.9 Binding
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
ChEMBL 173 3 1 2 1.6 c1ccc(CCc2c[nH]cn2)nc1 10.1021/jm049932u
11378681 11056 0 HRH3 H3 receptor Human 6.9 pEC50 = 6.9 Functional
Effect on specific [35S]GTP-gamma-S, Binding to HEK293 cell membranes expressing the human Histamine H3 receptorEffect on specific [35S]GTP-gamma-S, Binding to HEK293 cell membranes expressing the human Histamine H3 receptor
ChEMBL 164 5 1 2 1.0 C#CCOCCCc1c[nH]cn1 10.1021/jm031065q
CHEMBL1179608 11056 0 HRH3 H3 receptor Human 6.9 pEC50 = 6.9 Functional
Effect on specific [35S]GTP-gamma-S, Binding to HEK293 cell membranes expressing the human Histamine H3 receptorEffect on specific [35S]GTP-gamma-S, Binding to HEK293 cell membranes expressing the human Histamine H3 receptor
ChEMBL 164 5 1 2 1.0 C#CCOCCCc1c[nH]cn1 10.1021/jm031065q
CHEMBL88958 11056 0 HRH3 H3 receptor Human 6.9 pEC50 = 6.9 Functional
Effect on specific [35S]GTP-gamma-S, Binding to HEK293 cell membranes expressing the human Histamine H3 receptorEffect on specific [35S]GTP-gamma-S, Binding to HEK293 cell membranes expressing the human Histamine H3 receptor
ChEMBL 164 5 1 2 1.0 C#CCOCCCc1c[nH]cn1 10.1021/jm031065q
16678616 16983 0 HRH3 H3 receptor Human 7.9 pEC50 = 7.9 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 435 5 0 4 4.7 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCN(Cc3ccc(F)cc3)C2=O)CC1 10.1016/j.bmcl.2010.08.009
CHEMBL1257376 16983 0 HRH3 H3 receptor Human 7.9 pEC50 = 7.9 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 435 5 0 4 4.7 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCN(Cc3ccc(F)cc3)C2=O)CC1 10.1016/j.bmcl.2010.08.009
16678618 16984 0 HRH3 H3 receptor Human 7.9 pEC50 = 7.9 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 418 5 0 5 3.9 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCN(Cc3ccccn3)C2=O)CC1 10.1016/j.bmcl.2010.08.009
CHEMBL1257377 16984 0 HRH3 H3 receptor Human 7.9 pEC50 = 7.9 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 418 5 0 5 3.9 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCN(Cc3ccccn3)C2=O)CC1 10.1016/j.bmcl.2010.08.009
16679616 17136 0 HRH3 H3 receptor Human 7.9 pEC50 = 7.9 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 341 3 1 4 3.0 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3C[C@H](C)NC2=O)CC1 10.1016/j.bmcl.2010.08.009
CHEMBL1257850 17136 0 HRH3 H3 receptor Human 7.9 pEC50 = 7.9 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 341 3 1 4 3.0 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3C[C@H](C)NC2=O)CC1 10.1016/j.bmcl.2010.08.009
145954176 161812 0 HRH3 H3 receptor Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 680 7 1 6 6.6 COc1ccc(C2=C(c3ccccc3)C3(C=CC(=O)C=C3)N(C(C(=O)NC3CCCCC3)c3cc4c(cc3Br)OCO4)C2=O)cc1 10.1016/j.ejmech.2018.04.020
CHEMBL4169663 161812 0 HRH3 H3 receptor Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 680 7 1 6 6.6 COc1ccc(C2=C(c3ccccc3)C3(C=CC(=O)C=C3)N(C(C(=O)NC3CCCCC3)c3cc4c(cc3Br)OCO4)C2=O)cc1 10.1016/j.ejmech.2018.04.020
145954176 161812 0 HRH3 H3 receptor Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 680 7 1 6 6.6 COc1ccc(C2=C(c3ccccc3)C3(C=CC(=O)C=C3)N(C(C(=O)NC3CCCCC3)c3cc4c(cc3Br)OCO4)C2=O)cc1 10.1016/j.ejmech.2018.04.020
CHEMBL4169663 161812 0 HRH3 H3 receptor Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 680 7 1 6 6.6 COc1ccc(C2=C(c3ccccc3)C3(C=CC(=O)C=C3)N(C(C(=O)NC3CCCCC3)c3cc4c(cc3Br)OCO4)C2=O)cc1 10.1016/j.ejmech.2018.04.020
46929554 16389 0 HRH3 H3 receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 349 5 1 3 4.7 FC(F)(F)c1ccc(SCC(c2ccncc2)c2c[nH]cn2)cc1 10.1021/jm100643t
CHEMBL1243367 16389 0 HRH3 H3 receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 349 5 1 3 4.7 FC(F)(F)c1ccc(SCC(c2ccncc2)c2c[nH]cn2)cc1 10.1021/jm100643t
46929556 16392 0 HRH3 H3 receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 337 5 1 3 5.0 CC(C)(C)c1ccc(SCC(c2ccncc2)c2c[nH]cn2)cc1 10.1021/jm100643t
CHEMBL1243393 16392 0 HRH3 H3 receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 337 5 1 3 5.0 CC(C)(C)c1ccc(SCC(c2ccncc2)c2c[nH]cn2)cc1 10.1021/jm100643t
9812843 198803 1 HRH3 H3 receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 159 2 1 2 1.4 c1cncc(Cc2c[nH]cn2)c1 10.1021/jm100643t
CHEMBL78838 198803 1 HRH3 H3 receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 159 2 1 2 1.4 c1cncc(Cc2c[nH]cn2)c1 10.1021/jm100643t
16679704 17235 0 HRH3 H3 receptor Human 6.9 pEC50 = 6.9 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 327 5 1 4 2.6 C[C@H]1CCCN1CCCOc1ccc2c(c1)cc1n2CCNC1=O 10.1016/j.bmcl.2010.08.009
CHEMBL1258194 17235 0 HRH3 H3 receptor Human 6.9 pEC50 = 6.9 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 327 5 1 4 2.6 C[C@H]1CCCN1CCCOc1ccc2c(c1)cc1n2CCNC1=O 10.1016/j.bmcl.2010.08.009
11829635 162413 3 HRH3 H3 receptor Human 5.9 pEC50 = 5.9 Binding
Inhibition of human Histamine H3 receptor using [3H]N-alpha-methyl histamineInhibition of human Histamine H3 receptor using [3H]N-alpha-methyl histamine
ChEMBL 151 3 2 2 0.9 NCC[C@H]1C[C@H]1c1c[nH]cn1 10.1021/jm020415q
CHEMBL418470 162413 3 HRH3 H3 receptor Human 5.9 pEC50 = 5.9 Binding
Inhibition of human Histamine H3 receptor using [3H]N-alpha-methyl histamineInhibition of human Histamine H3 receptor using [3H]N-alpha-methyl histamine
ChEMBL 151 3 2 2 0.9 NCC[C@H]1C[C@H]1c1c[nH]cn1 10.1021/jm020415q
46929551 16379 0 HRH3 H3 receptor Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 337 5 1 3 5.0 CC(C)(C)c1ccc(SCC(c2ccccn2)c2c[nH]cn2)cc1 10.1021/jm100643t
CHEMBL1243335 16379 0 HRH3 H3 receptor Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 337 5 1 3 5.0 CC(C)(C)c1ccc(SCC(c2ccccn2)c2c[nH]cn2)cc1 10.1021/jm100643t
10219715 13509 0 HRH3 H3 receptor Rat 7.8 pEC50 = 7.8 Functional
The compound was evaluated for agonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uMThe compound was evaluated for agonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uM
ChEMBL 184 3 3 3 0.8 CNC(=N)SCCc1c[nH]cn1 10.1016/S0960-894X(00)80219-X
CHEMBL1195600 13509 0 HRH3 H3 receptor Rat 7.8 pEC50 = 7.8 Functional
The compound was evaluated for agonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uMThe compound was evaluated for agonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uM
ChEMBL 184 3 3 3 0.8 CNC(=N)SCCc1c[nH]cn1 10.1016/S0960-894X(00)80219-X
CHEMBL554956 13509 0 HRH3 H3 receptor Rat 7.8 pEC50 = 7.8 Functional
The compound was evaluated for agonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uMThe compound was evaluated for agonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uM
ChEMBL 184 3 3 3 0.8 CNC(=N)SCCc1c[nH]cn1 10.1016/S0960-894X(00)80219-X
11600779 75456 0 HRH3 H3 receptor Human 7.8 pEC50 = 7.8 Functional
Activity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cellsActivity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cells
ChEMBL 181 7 2 2 1.7 CCCNCCCCc1c[nH]cn1 10.1021/jm0504353
CHEMBL205731 75456 0 HRH3 H3 receptor Human 7.8 pEC50 = 7.8 Functional
Activity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cellsActivity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cells
ChEMBL 181 7 2 2 1.7 CCCNCCCCc1c[nH]cn1 10.1021/jm0504353
42625222 178904 0 HRH3 H3 receptor Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 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 178904 0 HRH3 H3 receptor Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 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
155533291 171002 0 HRH3 H3 receptor Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 179 1 2 5 -0.5 Cc1cc(N2CC(N)C2)nc(N)n1 10.1021/acs.jmedchem.9b01462
CHEMBL4468827 171002 0 HRH3 H3 receptor Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 179 1 2 5 -0.5 Cc1cc(N2CC(N)C2)nc(N)n1 10.1021/acs.jmedchem.9b01462
24825510 185045 0 HRH3 H3 receptor Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 255 3 1 3 2.6 CC1(C)COC(c2cccc(Cc3c[nH]cn3)c2)=N1 10.1021/jm7014149
CHEMBL495376 185045 0 HRH3 H3 receptor Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 255 3 1 3 2.6 CC1(C)COC(c2cccc(Cc3c[nH]cn3)c2)=N1 10.1021/jm7014149
1204 1806 104 HRH3 H3 receptor Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assayAgonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm1013488
1247 1806 104 HRH3 H3 receptor Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assayAgonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm1013488
1375 1806 104 HRH3 H3 receptor Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assayAgonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm1013488
774 1806 104 HRH3 H3 receptor Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assayAgonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm1013488
CHEMBL90 1806 104 HRH3 H3 receptor Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assayAgonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm1013488
DB05381 1806 104 HRH3 H3 receptor Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assayAgonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm1013488
11418968 62799 0 HRH3 H3 receptor Human 7.8 pEC50 = 7.8 Functional
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
ChEMBL 267 4 1 2 3.1 C(=C1CCN(CCc2ccccc2)CC1)c1c[nH]cn1 10.1021/jm049475h
CHEMBL179479 62799 0 HRH3 H3 receptor Human 7.8 pEC50 = 7.8 Functional
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
ChEMBL 267 4 1 2 3.1 C(=C1CCN(CCc2ccccc2)CC1)c1c[nH]cn1 10.1021/jm049475h
11327520 131787 0 HRH3 H3 receptor Human 7.8 pEC50 = 7.8 Functional
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
ChEMBL 255 4 1 2 2.9 c1ccc(CN2CCC(Cc3c[nH]cn3)CC2)cc1 10.1021/jm049475h
CHEMBL369819 131787 0 HRH3 H3 receptor Human 7.8 pEC50 = 7.8 Functional
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
ChEMBL 255 4 1 2 2.9 c1ccc(CN2CCC(Cc3c[nH]cn3)CC2)cc1 10.1021/jm049475h
11702447 108705 0 HRH3 H3 receptor Human 7.8 pEC50 = 7.8 Functional
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation countingInverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation counting
ChEMBL 316 6 0 4 3.5 CC1(C)COC(c2ccc(OCCCN3CCCCC3)cc2)=N1 10.1039/C0MD00056F
CHEMBL3220119 108705 0 HRH3 H3 receptor Human 7.8 pEC50 = 7.8 Functional
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation countingInverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation counting
ChEMBL 316 6 0 4 3.5 CC1(C)COC(c2ccc(OCCCN3CCCCC3)cc2)=N1 10.1039/C0MD00056F
24729202 42370 5 HRH3 H3 receptor Human 5.8 pEC50 = 5.8 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
ChEMBL 149 1 2 2 0.8 C1=C(c2c[nH]cn2)CCNC1 10.1021/jm030905y
CHEMBL150243 42370 5 HRH3 H3 receptor Human 5.8 pEC50 = 5.8 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
ChEMBL 149 1 2 2 0.8 C1=C(c2c[nH]cn2)CCNC1 10.1021/jm030905y
127052634 139513 0 HRH3 H3 receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 272 4 3 3 1.5 N#C/N=C(\NC[C@@H]1CC[C@H](c2c[nH]cn2)C1)NC1CC1 10.1021/acs.jmedchem.6b00120
CHEMBL3806146 139513 0 HRH3 H3 receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 272 4 3 3 1.5 N#C/N=C(\NC[C@@H]1CC[C@H](c2c[nH]cn2)C1)NC1CC1 10.1021/acs.jmedchem.6b00120
132938089 166736 0 HRH3 H3 receptor Human 6.8 pEC50 = 6.8 Functional
Antagonist activity at recombinant human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation after 30 mins by TR-FRET TR-FRET assayAntagonist activity at recombinant human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation after 30 mins by TR-FRET TR-FRET assay
ChEMBL 317 9 0 2 5.4 CCC(C)(C)c1ccc(OCCCCCN2CCCCC2)cc1 10.1016/j.bmc.2017.03.031
CHEMBL4227989 166736 0 HRH3 H3 receptor Human 6.8 pEC50 = 6.8 Functional
Antagonist activity at recombinant human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation after 30 mins by TR-FRET TR-FRET assayAntagonist activity at recombinant human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation after 30 mins by TR-FRET TR-FRET assay
ChEMBL 317 9 0 2 5.4 CCC(C)(C)c1ccc(OCCCCCN2CCCCC2)cc1 10.1016/j.bmc.2017.03.031
CHEMBL4300613 166736 0 HRH3 H3 receptor Human 6.8 pEC50 = 6.8 Functional
Antagonist activity at recombinant human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation after 30 mins by TR-FRET TR-FRET assayAntagonist activity at recombinant human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation after 30 mins by TR-FRET TR-FRET assay
ChEMBL 317 9 0 2 5.4 CCC(C)(C)c1ccc(OCCCCCN2CCCCC2)cc1 10.1016/j.bmc.2017.03.031
155513736 168945 0 HRH3 H3 receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 235 4 2 5 1.0 CCNC1CN(c2cc(C(C)C)nc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4439165 168945 0 HRH3 H3 receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 235 4 2 5 1.0 CCNC1CN(c2cc(C(C)C)nc(N)n2)C1 10.1021/acs.jmedchem.9b01462
9923162 18565 4 HRH3 H3 receptor Human 5.8 pEC50 = 5.8 Binding
Effective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cellsEffective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cells
ChEMBL 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3cc(Br)ccc3[nH]2)CC1 10.1016/j.bmcl.2004.08.035
CHEMBL128613 18565 4 HRH3 H3 receptor Human 5.8 pEC50 = 5.8 Binding
Effective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cellsEffective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cells
ChEMBL 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3cc(Br)ccc3[nH]2)CC1 10.1016/j.bmcl.2004.08.035
145946358 166691 0 HRH3 H3 receptor Human 6.8 pEC50 = 6.8 Functional
Antagonist activity at recombinant human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation after 30 mins by TR-FRET TR-FRET assayAntagonist activity at recombinant human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation after 30 mins by TR-FRET TR-FRET assay
ChEMBL 331 9 0 2 5.7 CCC(C)(C)c1ccc(OCCCCCN2CCCC(C)C2)cc1 10.1016/j.bmc.2017.03.031
CHEMBL4225644 166691 0 HRH3 H3 receptor Human 6.8 pEC50 = 6.8 Functional
Antagonist activity at recombinant human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation after 30 mins by TR-FRET TR-FRET assayAntagonist activity at recombinant human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation after 30 mins by TR-FRET TR-FRET assay
ChEMBL 331 9 0 2 5.7 CCC(C)(C)c1ccc(OCCCCCN2CCCC(C)C2)cc1 10.1016/j.bmc.2017.03.031
CHEMBL4300100 166691 0 HRH3 H3 receptor Human 6.8 pEC50 = 6.8 Functional
Antagonist activity at recombinant human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation after 30 mins by TR-FRET TR-FRET assayAntagonist activity at recombinant human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation after 30 mins by TR-FRET TR-FRET assay
ChEMBL 331 9 0 2 5.7 CCC(C)(C)c1ccc(OCCCCCN2CCCC(C)C2)cc1 10.1016/j.bmc.2017.03.031
44249906 188519 0 HRH3 H3 receptor Human 7.8 pEC50 = 7.8 Functional
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 382 4 0 4 3.6 CC(C)N1CCC(Oc2ccc3cc(C(=O)N4CCOCC4)ccc3c2)CC1 10.1016/j.bmcl.2009.03.100
CHEMBL541483 188519 0 HRH3 H3 receptor Human 7.8 pEC50 = 7.8 Functional
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 382 4 0 4 3.6 CC(C)N1CCC(Oc2ccc3cc(C(=O)N4CCOCC4)ccc3c2)CC1 10.1016/j.bmcl.2009.03.100
1218 220 41 HRH3 H3 receptor Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 330 4 0 3 5.0 N#Cc1ccc(cc1)c1ccc2c(c1)cc(o2)CCN1CCC[C@H]1C 10.1021/jm0705051
9818903 220 41 HRH3 H3 receptor Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 330 4 0 3 5.0 N#Cc1ccc(cc1)c1ccc2c(c1)cc(o2)CCN1CCC[C@H]1C 10.1021/jm0705051
CHEMBL351231 220 41 HRH3 H3 receptor Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 330 4 0 3 5.0 N#Cc1ccc(cc1)c1ccc2c(c1)cc(o2)CCN1CCC[C@H]1C 10.1021/jm0705051
1218 220 41 HRH3 H3 receptor Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 330 4 0 3 5.0 N#Cc1ccc(cc1)c1ccc2c(c1)cc(o2)CCN1CCC[C@H]1C 10.1021/jm0705051
9818903 220 41 HRH3 H3 receptor Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 330 4 0 3 5.0 N#Cc1ccc(cc1)c1ccc2c(c1)cc(o2)CCN1CCC[C@H]1C 10.1021/jm0705051
CHEMBL351231 220 41 HRH3 H3 receptor Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 330 4 0 3 5.0 N#Cc1ccc(cc1)c1ccc2c(c1)cc(o2)CCN1CCC[C@H]1C 10.1021/jm0705051
127050434 139454 0 HRH3 H3 receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 160 3 4 3 0.2 CC(=N)SCCNC(=N)N 10.1021/acs.jmedchem.6b00120
CHEMBL3805514 139454 0 HRH3 H3 receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 160 3 4 3 0.2 CC(=N)SCCNC(=N)N 10.1021/acs.jmedchem.6b00120
49799215 10651 0 HRH3 H3 receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 242 3 1 3 2.3 c1cncc(N2CCC(Cc3c[nH]cn3)CC2)c1 10.1016/j.bmc.2010.04.052
CHEMBL1173033 10651 0 HRH3 H3 receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 242 3 1 3 2.3 c1cncc(N2CCC(Cc3c[nH]cn3)CC2)c1 10.1016/j.bmc.2010.04.052
49799509 10624 0 HRH3 H3 receptor Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 297 3 1 2 4.2 CC(C)(C)c1ccc(N2CCC(Cc3c[nH]cn3)CC2)cc1 10.1016/j.bmc.2010.04.052
CHEMBL1172776 10624 0 HRH3 H3 receptor Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 297 3 1 2 4.2 CC(C)(C)c1ccc(N2CCC(Cc3c[nH]cn3)CC2)cc1 10.1016/j.bmc.2010.04.052
46945057 17168 0 HRH3 H3 receptor Human 7.8 pEC50 = 7.8 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 395 5 0 4 4.1 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3C[C@@H](C)N(CC3CC3)C2=O)CC1 10.1016/j.bmcl.2010.08.009
CHEMBL1257965 17168 0 HRH3 H3 receptor Human 7.8 pEC50 = 7.8 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 395 5 0 4 4.1 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3C[C@@H](C)N(CC3CC3)C2=O)CC1 10.1016/j.bmcl.2010.08.009
46945057 17168 0 HRH3 H3 receptor Rat 7.8 pEC50 = 7.8 Functional
Inverse agonist activity at rat histamine H3 receptorInverse agonist activity at rat histamine H3 receptor
ChEMBL 395 5 0 4 4.1 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3C[C@@H](C)N(CC3CC3)C2=O)CC1 10.1016/j.bmcl.2010.08.009
CHEMBL1257965 17168 0 HRH3 H3 receptor Rat 7.8 pEC50 = 7.8 Functional
Inverse agonist activity at rat histamine H3 receptorInverse agonist activity at rat histamine H3 receptor
ChEMBL 395 5 0 4 4.1 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3C[C@@H](C)N(CC3CC3)C2=O)CC1 10.1016/j.bmcl.2010.08.009
10678418 120528 67 HRH3 H3 receptor Human 5.7 pEC50 = 5.7 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
ChEMBL 151 1 2 2 0.9 c1nc(C2CCNCC2)c[nH]1 10.1021/jm030905y
CHEMBL358028 120528 67 HRH3 H3 receptor Human 5.7 pEC50 = 5.7 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
ChEMBL 151 1 2 2 0.9 c1nc(C2CCNCC2)c[nH]1 10.1021/jm030905y
CHEMBL4174017 162089 0 HRH3 H3 receptor Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 534 7 1 6 5.9 COc1cc(NC2(c3ccccc3Cl)C(=O)N(C(C)(C)C)C(=O)/C2=C/c2ccccc2)cc(OC)c1OC 10.1016/j.ejmech.2018.04.020
CHEMBL4174017 162089 0 HRH3 H3 receptor Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 534 7 1 6 5.9 COc1cc(NC2(c3ccccc3Cl)C(=O)N(C(C)(C)C)C(=O)/C2=C/c2ccccc2)cc(OC)c1OC 10.1016/j.ejmech.2018.04.020
46888006 8676 0 HRH3 H3 receptor Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 272 4 1 2 3.8 FC(F)(F)c1ccc(SCCc2c[nH]cn2)cc1 10.1021/jm901890s
CHEMBL1098002 8676 0 HRH3 H3 receptor Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 272 4 1 2 3.8 FC(F)(F)c1ccc(SCCc2c[nH]cn2)cc1 10.1021/jm901890s
11469514 103453 2 HRH3 H3 receptor Human 7.7 pEC50 = 7.7 Binding
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
ChEMBL 187 4 1 2 2.0 c1cc(CCCc2c[nH]cn2)ccn1 10.1021/jm049932u
CHEMBL309654 103453 2 HRH3 H3 receptor Human 7.7 pEC50 = 7.7 Binding
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
ChEMBL 187 4 1 2 2.0 c1cc(CCCc2c[nH]cn2)ccn1 10.1021/jm049932u
9793791 45559 1 HRH3 H3 receptor Human 7.7 pEC50 = 7.7 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
ChEMBL 137 2 2 2 0.5 NCC1CC1c1c[nH]cn1 10.1021/jm030905y
CHEMBL153284 45559 1 HRH3 H3 receptor Human 7.7 pEC50 = 7.7 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
ChEMBL 137 2 2 2 0.5 NCC1CC1c1c[nH]cn1 10.1021/jm030905y
11622672 74433 2 HRH3 H3 receptor Human 7.7 pEC50 = 7.7 Functional
Activity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cellsActivity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cells
ChEMBL 221 6 1 2 2.6 c1nc(CCCCCN2CCCCC2)c[nH]1 10.1021/jm0504353
CHEMBL203389 74433 2 HRH3 H3 receptor Human 7.7 pEC50 = 7.7 Functional
Activity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cellsActivity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cells
ChEMBL 221 6 1 2 2.6 c1nc(CCCCCN2CCCCC2)c[nH]1 10.1021/jm0504353
10934158 107851 1 HRH3 H3 receptor Human 6.7 pEC50 = 6.7 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptor
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@@H]2CC[C@H](c3c[nH]cn3)O2)cc1 10.1021/jm0300025
CHEMBL320331 107851 1 HRH3 H3 receptor Human 6.7 pEC50 = 6.7 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptor
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@@H]2CC[C@H](c3c[nH]cn3)O2)cc1 10.1021/jm0300025
24738376 184638 1 HRH3 H3 receptor Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 234 3 1 1 3.7 c1ccc(-c2cccc(Cc3c[nH]cn3)c2)cc1 10.1021/jm7014149
CHEMBL493012 184638 1 HRH3 H3 receptor Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 234 3 1 1 3.7 c1ccc(-c2cccc(Cc3c[nH]cn3)c2)cc1 10.1021/jm7014149
10934158 107851 1 HRH3 H3 receptor Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@@H]2CC[C@H](c3c[nH]cn3)O2)cc1 10.1016/j.bmcl.2010.10.041
CHEMBL320331 107851 1 HRH3 H3 receptor Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@@H]2CC[C@H](c3c[nH]cn3)O2)cc1 10.1016/j.bmcl.2010.10.041
11474535 63001 2 HRH3 H3 receptor Human 6.7 pEC50 = 6.7 Functional
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
ChEMBL 221 4 1 2 2.5 CC(C)N1CCC(CCc2c[nH]cn2)CC1 10.1021/jm049475h
CHEMBL180061 63001 2 HRH3 H3 receptor Human 6.7 pEC50 = 6.7 Functional
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
ChEMBL 221 4 1 2 2.5 CC(C)N1CCC(CCc2c[nH]cn2)CC1 10.1021/jm049475h
16059780 168555 0 HRH3 H3 receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 334 4 0 4 4.0 Cc1nn(C)cc1-c1ccc2cc(CCN3CCC[C@H]3C)ccc2n1 10.1021/jm0705051
CHEMBL442242 168555 0 HRH3 H3 receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 334 4 0 4 4.0 Cc1nn(C)cc1-c1ccc2cc(CCN3CCC[C@H]3C)ccc2n1 10.1021/jm0705051
49799183 10425 0 HRH3 H3 receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 284 4 1 3 2.9 CN(C)c1ccc(N2CCC(Cc3c[nH]cn3)CC2)cc1 10.1016/j.bmc.2010.04.052
CHEMBL1170855 10425 0 HRH3 H3 receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 284 4 1 3 2.9 CN(C)c1ccc(N2CCC(Cc3c[nH]cn3)CC2)cc1 10.1016/j.bmc.2010.04.052
44539973 67941 0 HRH3 H3 receptor Human 8.7 pEC50 = 8.7 Functional
Inverse agonist activity at human H3R expressed in CHO cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human H3R expressed in CHO cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 297 4 0 4 2.5 C[C@@H]1CCCN1CCc1ccc(-c2ccc(=O)n(C)n2)cc1 10.1016/j.bmcl.2011.08.104
CHEMBL1917464 67941 0 HRH3 H3 receptor Human 8.7 pEC50 = 8.7 Functional
Inverse agonist activity at human H3R expressed in CHO cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human H3R expressed in CHO cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 297 4 0 4 2.5 C[C@@H]1CCCN1CCc1ccc(-c2ccc(=O)n(C)n2)cc1 10.1016/j.bmcl.2011.08.104
44184949 183268 0 HRH3 H3 receptor Human 8.7 pEC50 = 8.7 Binding
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
ChEMBL 451 5 0 5 3.7 O=C(c1cc2cc(OC3CCN(C4CC4)CC3)ccc2n1CC(F)(F)F)N1CCOCC1 10.1021/jm900409x
CHEMBL482844 183268 0 HRH3 H3 receptor Human 8.7 pEC50 = 8.7 Binding
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
ChEMBL 451 5 0 5 3.7 O=C(c1cc2cc(OC3CCN(C4CC4)CC3)ccc2n1CC(F)(F)F)N1CCOCC1 10.1021/jm900409x
44184902 183377 0 HRH3 H3 receptor Human 8.7 pEC50 = 8.7 Binding
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
ChEMBL 465 5 0 5 4.1 O=C(c1cc2cc(OC3CCN(C4CCC4)CC3)ccc2n1CC(F)(F)F)N1CCOCC1 10.1021/jm900409x
CHEMBL483672 183377 0 HRH3 H3 receptor Human 8.7 pEC50 = 8.7 Binding
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
ChEMBL 465 5 0 5 4.1 O=C(c1cc2cc(OC3CCN(C4CCC4)CC3)ccc2n1CC(F)(F)F)N1CCOCC1 10.1021/jm900409x
16739412 187630 0 HRH3 H3 receptor Human 8.7 pEC50 = 8.7 Binding
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
ChEMBL 444 5 0 5 4.3 CC(C)N1CCC(Oc2ccc3c(c2)cc(C(=O)N2CCC(F)(F)CC2)n3CC#N)CC1 10.1021/jm900409x
CHEMBL521710 187630 0 HRH3 H3 receptor Human 8.7 pEC50 = 8.7 Binding
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
ChEMBL 444 5 0 5 4.3 CC(C)N1CCC(Oc2ccc3c(c2)cc(C(=O)N2CCC(F)(F)CC2)n3CC#N)CC1 10.1021/jm900409x
16739525 187941 0 HRH3 H3 receptor Human 8.7 pEC50 = 8.7 Binding
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
ChEMBL 549 5 0 4 7.1 CC(C)N1CCC(Oc2ccc3c(c2)cc(C(=O)N2CCC(F)(F)CC2)n3-c2ccc(Cl)c(Cl)c2)CC1 10.1021/jm900409x
CHEMBL523948 187941 0 HRH3 H3 receptor Human 8.7 pEC50 = 8.7 Binding
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
ChEMBL 549 5 0 4 7.1 CC(C)N1CCC(Oc2ccc3c(c2)cc(C(=O)N2CCC(F)(F)CC2)n3-c2ccc(Cl)c(Cl)c2)CC1 10.1021/jm900409x
52948255 17200 0 HRH3 H3 receptor Human 8.7 pEC50 = 8.7 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 473 5 0 4 5.1 CC(C)N1CCC(Oc2cc3cc4n(c3cc2Br)[C@@H](C)CN(CC2CC2)C4=O)CC1 10.1016/j.bmcl.2010.08.009
CHEMBL1258079 17200 0 HRH3 H3 receptor Human 8.7 pEC50 = 8.7 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 473 5 0 4 5.1 CC(C)N1CCC(Oc2cc3cc4n(c3cc2Br)[C@@H](C)CN(CC2CC2)C4=O)CC1 10.1016/j.bmcl.2010.08.009
11619260 185276 10 HRH3 H3 receptor Human 8.7 pEC50 = 8.7 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 447 5 0 4 5.3 CC(C)N1CCC(Oc2ccc3c(c2)cc(C(=O)N2CCC(F)(F)CC2)n3C(C)C)CC1 10.1016/j.bmcl.2010.08.009
CHEMBL497031 185276 10 HRH3 H3 receptor Human 8.7 pEC50 = 8.7 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 447 5 0 4 5.3 CC(C)N1CCC(Oc2ccc3c(c2)cc(C(=O)N2CCC(F)(F)CC2)n3C(C)C)CC1 10.1016/j.bmcl.2010.08.009
25070031 64829 4 HRH3 H3 receptor Rat 8.7 pEC50 = 8.7 Functional
Inverse agonist activity at rat histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS bindingInverse agonist activity at rat histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS binding
ChEMBL 313 6 1 4 2.7 C[C@@H]1CCCN1CCCOc1ccc(-c2ccc(=O)[nH]n2)cc1 10.1021/jm200401v
CHEMBL1829335 64829 4 HRH3 H3 receptor Rat 8.7 pEC50 = 8.7 Functional
Inverse agonist activity at rat histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS bindingInverse agonist activity at rat histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS binding
ChEMBL 313 6 1 4 2.7 C[C@@H]1CCCN1CCCOc1ccc(-c2ccc(=O)[nH]n2)cc1 10.1021/jm200401v
44367567 168362 2 HRH3 H3 receptor Human 8.7 pEC50 = 8.7 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
ChEMBL 151 2 2 2 0.6 c1nc(C[C@H]2CCNC2)c[nH]1 10.1021/jm030905y
CHEMBL440730 168362 2 HRH3 H3 receptor Human 8.7 pEC50 = 8.7 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
ChEMBL 151 2 2 2 0.6 c1nc(C[C@H]2CCNC2)c[nH]1 10.1021/jm030905y
56677285 64854 0 HRH3 H3 receptor Human 8.7 pEC50 = 8.7 Functional
Antagonist activity at human histamine 3 receptor by [35S]GTPgammaS binding assayAntagonist activity at human histamine 3 receptor by [35S]GTPgammaS binding assay
ChEMBL 341 6 0 5 2.9 C[C@H](COc1ccc(-c2ccc(=O)n(C)n2)cc1)CN1CCC[C@H]1C 10.1016/j.bmcl.2011.06.108
CHEMBL1829485 64854 0 HRH3 H3 receptor Human 8.7 pEC50 = 8.7 Functional
Antagonist activity at human histamine 3 receptor by [35S]GTPgammaS binding assayAntagonist activity at human histamine 3 receptor by [35S]GTPgammaS binding assay
ChEMBL 341 6 0 5 2.9 C[C@H](COc1ccc(-c2ccc(=O)n(C)n2)cc1)CN1CCC[C@H]1C 10.1016/j.bmcl.2011.06.108
44540072 67945 0 HRH3 H3 receptor Human 8.7 pEC50 = 8.7 Functional
Inverse agonist activity at human H3R expressed in CHO cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human H3R expressed in CHO cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 377 5 0 4 4.1 C[C@@H]1CCCN1CCc1ccc(-c2ccc(=O)n(-c3ccc(F)cc3)n2)cc1 10.1016/j.bmcl.2011.08.104
CHEMBL1917468 67945 0 HRH3 H3 receptor Human 8.7 pEC50 = 8.7 Functional
Inverse agonist activity at human H3R expressed in CHO cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human H3R expressed in CHO cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 377 5 0 4 4.1 C[C@@H]1CCCN1CCc1ccc(-c2ccc(=O)n(-c3ccc(F)cc3)n2)cc1 10.1016/j.bmcl.2011.08.104
53363442 63832 0 HRH3 H3 receptor Rat 8.7 pEC50 = 8.7 Functional
Inverse agonist activity at rat histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS bindingInverse agonist activity at rat histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS binding
ChEMBL 313 6 1 4 2.7 C[C@@H]1CCCN1CCCOc1ccc(-c2cn[nH]c(=O)c2)cc1 10.1021/jm200401v
CHEMBL1813065 63832 0 HRH3 H3 receptor Rat 8.7 pEC50 = 8.7 Functional
Inverse agonist activity at rat histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS bindingInverse agonist activity at rat histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS binding
ChEMBL 313 6 1 4 2.7 C[C@@H]1CCCN1CCCOc1ccc(-c2cn[nH]c(=O)c2)cc1 10.1021/jm200401v
23725172 63825 0 HRH3 H3 receptor Rat 8.7 pEC50 = 8.7 Functional
Inverse agonist activity at rat histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS bindingInverse agonist activity at rat histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS binding
ChEMBL 327 6 0 5 2.7 C[C@@H]1CCCN1CCCOc1ccc(-c2ccc(=O)n(C)n2)cc1 10.1021/jm200401v
CHEMBL1813057 63825 0 HRH3 H3 receptor Rat 8.7 pEC50 = 8.7 Functional
Inverse agonist activity at rat histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS bindingInverse agonist activity at rat histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS binding
ChEMBL 327 6 0 5 2.7 C[C@@H]1CCCN1CCCOc1ccc(-c2ccc(=O)n(C)n2)cc1 10.1021/jm200401v
1252 1886 12 HRH3 H3 receptor Human 8.6 pEC50 = 8.6 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
ChEMBL 153 5 2 2 1.1 NCCCCCc1cnc[nH]1 10.1021/jm030905y
9793868 1886 12 HRH3 H3 receptor Human 8.6 pEC50 = 8.6 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
ChEMBL 153 5 2 2 1.1 NCCCCCc1cnc[nH]1 10.1021/jm030905y
CHEMBL417096 1886 12 HRH3 H3 receptor Human 8.6 pEC50 = 8.6 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
ChEMBL 153 5 2 2 1.1 NCCCCCc1cnc[nH]1 10.1021/jm030905y
11275349 45166 4 HRH3 H3 receptor Human 8.6 pEC50 = 8.6 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
ChEMBL 177 2 2 2 1.4 C=C(c1c[nH]cn1)C1CCNCC1 10.1021/jm030905y
CHEMBL152936 45166 4 HRH3 H3 receptor Human 8.6 pEC50 = 8.6 Binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
ChEMBL 177 2 2 2 1.4 C=C(c1c[nH]cn1)C1CCNCC1 10.1021/jm030905y
11957573 1879 25 HRH3 H3 receptor Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm901890s
1250 1879 25 HRH3 H3 receptor Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm901890s
3692 1879 25 HRH3 H3 receptor Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm901890s
CHEMBL19439 1879 25 HRH3 H3 receptor Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm901890s
25149335 183349 0 HRH3 H3 receptor Human 8.6 pEC50 = 8.6 Binding
Activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, G-beta-1-gamma-2 and RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, G-beta-1-gamma-2 and RGS4 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 183349 0 HRH3 H3 receptor Human 8.6 pEC50 = 8.6 Binding
Activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, G-beta-1-gamma-2 and RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, G-beta-1-gamma-2 and RGS4 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 183349 0 HRH3 H3 receptor Human 8.6 pEC50 = 8.6 Binding
Agonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 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 183349 0 HRH3 H3 receptor Human 8.6 pEC50 = 8.6 Binding
Agonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 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
1204 1806 104 HRH3 H3 receptor Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01462
1247 1806 104 HRH3 H3 receptor Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01462
1375 1806 104 HRH3 H3 receptor Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01462
774 1806 104 HRH3 H3 receptor Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01462
CHEMBL90 1806 104 HRH3 H3 receptor Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01462
DB05381 1806 104 HRH3 H3 receptor Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01462
25149712 178122 0 HRH3 H3 receptor Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gsalpha2, Gbeta1gamma2 and RGS19 by steady-state GTPase activity assayAgonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gsalpha2, Gbeta1gamma2 and RGS19 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 178122 0 HRH3 H3 receptor Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gsalpha2, Gbeta1gamma2 and RGS19 by steady-state GTPase activity assayAgonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gsalpha2, Gbeta1gamma2 and RGS19 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 183349 0 HRH3 H3 receptor Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gsalpha2, Gbeta1gamma2 and RGS19 by steady-state GTPase activity assayAgonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gsalpha2, Gbeta1gamma2 and RGS19 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 183349 0 HRH3 H3 receptor Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gsalpha2, Gbeta1gamma2 and RGS19 by steady-state GTPase activity assayAgonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gsalpha2, Gbeta1gamma2 and RGS19 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
25149335 183349 0 HRH3 H3 receptor Human 8.6 pEC50 = 8.6 Binding
Agonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 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 183349 0 HRH3 H3 receptor Human 8.6 pEC50 = 8.6 Binding
Agonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 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
11336692 62740 1 HRH3 H3 receptor Human 8.6 pEC50 = 8.6 Functional
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
ChEMBL 177 1 1 2 1.5 CN1CCC(=Cc2c[nH]cn2)CC1 10.1021/jm049475h
CHEMBL179302 62740 1 HRH3 H3 receptor Human 8.6 pEC50 = 8.6 Functional
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
ChEMBL 177 1 1 2 1.5 CN1CCC(=Cc2c[nH]cn2)CC1 10.1021/jm049475h
CHEMBL4166098 161595 0 HRH3 H3 receptor Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 534 7 1 6 5.9 COc1cc(NC2(c3cccc(Cl)c3)C(=O)N(C(C)(C)C)C(=O)/C2=C/c2ccccc2)cc(OC)c1OC 10.1016/j.ejmech.2018.04.020
CHEMBL4166098 161595 0 HRH3 H3 receptor Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 534 7 1 6 5.9 COc1cc(NC2(c3cccc(Cl)c3)C(=O)N(C(C)(C)C)C(=O)/C2=C/c2ccccc2)cc(OC)c1OC 10.1016/j.ejmech.2018.04.020
CHEMBL4175898 162207 0 HRH3 H3 receptor Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 530 7 1 5 6.5 COc1ccc(NC2(c3cccc(Cl)c3)C(=O)N(C3CCCCC3)C(=O)/C2=C/c2ccccc2)cc1OC 10.1016/j.ejmech.2018.04.020
CHEMBL4175898 162207 0 HRH3 H3 receptor Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 530 7 1 5 6.5 COc1ccc(NC2(c3cccc(Cl)c3)C(=O)N(C3CCCCC3)C(=O)/C2=C/c2ccccc2)cc1OC 10.1016/j.ejmech.2018.04.020
1236 1936 17 HRH3 H3 receptor Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1021/jm901890s
1237 1936 17 HRH3 H3 receptor Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1021/jm901890s
156615 1936 17 HRH3 H3 receptor Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1021/jm901890s
CHEMBL268229 1936 17 HRH3 H3 receptor Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1021/jm901890s
11957573 1879 25 HRH3 H3 receptor Rat 8.6 pEC50 = 8.6 Binding
In vitro binding affinity against histamine H3 receptor from synaptosomes of rat cerebral cortexIn vitro binding affinity against histamine H3 receptor from synaptosomes of rat cerebral cortex
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm991068w
1250 1879 25 HRH3 H3 receptor Rat 8.6 pEC50 = 8.6 Binding
In vitro binding affinity against histamine H3 receptor from synaptosomes of rat cerebral cortexIn vitro binding affinity against histamine H3 receptor from synaptosomes of rat cerebral cortex
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm991068w
3692 1879 25 HRH3 H3 receptor Rat 8.6 pEC50 = 8.6 Binding
In vitro binding affinity against histamine H3 receptor from synaptosomes of rat cerebral cortexIn vitro binding affinity against histamine H3 receptor from synaptosomes of rat cerebral cortex
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm991068w
CHEMBL19439 1879 25 HRH3 H3 receptor Rat 8.6 pEC50 = 8.6 Binding
In vitro binding affinity against histamine H3 receptor from synaptosomes of rat cerebral cortexIn vitro binding affinity against histamine H3 receptor from synaptosomes of rat cerebral cortex
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm991068w
46887042 8492 0 HRH3 H3 receptor Human 8.5 pEC50 = 8.5 Binding
Activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 and RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 and RGS4 by steady-state GTPase activity 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 8492 0 HRH3 H3 receptor Human 8.5 pEC50 = 8.5 Binding
Activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 and RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 and RGS4 by steady-state GTPase activity 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
56954515 81417 0 HRH3 H3 receptor Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human H3R-Galphai2-Gbeta1gamma2-RGS4 expressed in Sf9 cells 0.1 nM to 1 mM by steady state GTPase activity assayAgonist activity at human H3R-Galphai2-Gbeta1gamma2-RGS4 expressed in Sf9 cells 0.1 nM to 1 mM 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 81417 0 HRH3 H3 receptor Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human H3R-Galphai2-Gbeta1gamma2-RGS4 expressed in Sf9 cells 0.1 nM to 1 mM by steady state GTPase activity assayAgonist activity at human H3R-Galphai2-Gbeta1gamma2-RGS4 expressed in Sf9 cells 0.1 nM to 1 mM 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
11957573 1879 25 HRH3 H3 receptor Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human H3 receptor expressed in CHO cells assessed as increase in cAMP accumulation by measuring reduction in forskolin level incubated for 4 hrs by CRE/MRE-luciferase reporter gene assayAgonist activity at human H3 receptor expressed in CHO cells assessed as increase in cAMP accumulation by measuring reduction in forskolin level incubated for 4 hrs by CRE/MRE-luciferase reporter gene assay
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.ejmech.2020.112150
1250 1879 25 HRH3 H3 receptor Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human H3 receptor expressed in CHO cells assessed as increase in cAMP accumulation by measuring reduction in forskolin level incubated for 4 hrs by CRE/MRE-luciferase reporter gene assayAgonist activity at human H3 receptor expressed in CHO cells assessed as increase in cAMP accumulation by measuring reduction in forskolin level incubated for 4 hrs by CRE/MRE-luciferase reporter gene assay
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.ejmech.2020.112150
3692 1879 25 HRH3 H3 receptor Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human H3 receptor expressed in CHO cells assessed as increase in cAMP accumulation by measuring reduction in forskolin level incubated for 4 hrs by CRE/MRE-luciferase reporter gene assayAgonist activity at human H3 receptor expressed in CHO cells assessed as increase in cAMP accumulation by measuring reduction in forskolin level incubated for 4 hrs by CRE/MRE-luciferase reporter gene assay
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.ejmech.2020.112150
CHEMBL19439 1879 25 HRH3 H3 receptor Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human H3 receptor expressed in CHO cells assessed as increase in cAMP accumulation by measuring reduction in forskolin level incubated for 4 hrs by CRE/MRE-luciferase reporter gene assayAgonist activity at human H3 receptor expressed in CHO cells assessed as increase in cAMP accumulation by measuring reduction in forskolin level incubated for 4 hrs by CRE/MRE-luciferase reporter gene assay
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.ejmech.2020.112150
11610910 189346 0 HRH3 H3 receptor Human 6.7 pEC50 = 6.7 Functional
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 394 6 0 3 5.0 CC1CCN(C(=O)c2ccc3cc(OCCCN4CCCCC4)ccc3c2)CC1 10.1016/j.bmcl.2009.03.100
CHEMBL557461 189346 0 HRH3 H3 receptor Human 6.7 pEC50 = 6.7 Functional
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 394 6 0 3 5.0 CC1CCN(C(=O)c2ccc3cc(OCCCN4CCCCC4)ccc3c2)CC1 10.1016/j.bmcl.2009.03.100
44578637 180729 0 HRH3 H3 receptor Human 7.7 pEC50 = 7.7 Functional
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgammaS assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgammaS assay
ChEMBL 394 5 1 3 5.2 CC(C)N1CCC(Oc2ccc3cc(C(=O)NC4CCCCC4)ccc3c2)CC1 10.1016/j.bmcl.2008.06.062
CHEMBL477181 180729 0 HRH3 H3 receptor Human 7.7 pEC50 = 7.7 Functional
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgammaS assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgammaS assay
ChEMBL 394 5 1 3 5.2 CC(C)N1CCC(Oc2ccc3cc(C(=O)NC4CCCCC4)ccc3c2)CC1 10.1016/j.bmcl.2008.06.062
127050431 139519 0 HRH3 H3 receptor Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3806206 139519 0 HRH3 H3 receptor Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
46929553 16388 0 HRH3 H3 receptor Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 337 5 1 3 5.0 CC(C)(C)c1ccc(SCC(c2cccnc2)c2c[nH]cn2)cc1 10.1021/jm100643t
CHEMBL1243366 16388 0 HRH3 H3 receptor Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 337 5 1 3 5.0 CC(C)(C)c1ccc(SCC(c2cccnc2)c2c[nH]cn2)cc1 10.1021/jm100643t
CHEMBL4166386 161609 0 HRH3 H3 receptor Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 440 5 1 4 5.3 COc1ccc(NC2(c3ccccc3)C(=O)N(C(C)(C)C)C(=O)/C2=C/c2ccccc2)cc1 10.1016/j.ejmech.2018.04.020
46929647 16393 0 HRH3 H3 receptor Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 355 5 2 3 4.3 FC(F)(F)c1ccc(SC[C@H](c2c[nH]cn2)C2CCNCC2)cc1 10.1021/jm100643t
CHEMBL1243394 16393 0 HRH3 H3 receptor Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 355 5 2 3 4.3 FC(F)(F)c1ccc(SC[C@H](c2c[nH]cn2)C2CCNCC2)cc1 10.1021/jm100643t
11624908 187705 0 HRH3 H3 receptor Human 7.6 pEC50 = 7.6 Binding
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
ChEMBL 371 4 1 4 2.9 CC(C)N1CCC(Oc2ccc3cc(C(=O)N4CCOCC4)[nH]c3c2)CC1 10.1021/jm900409x
CHEMBL522243 187705 0 HRH3 H3 receptor Human 7.6 pEC50 = 7.6 Binding
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
ChEMBL 371 4 1 4 2.9 CC(C)N1CCC(Oc2ccc3cc(C(=O)N4CCOCC4)[nH]c3c2)CC1 10.1021/jm900409x
16678615 16951 0 HRH3 H3 receptor Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 435 5 0 4 4.7 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCN(Cc3cccc(F)c3)C2=O)CC1 10.1016/j.bmcl.2010.08.009
CHEMBL1257257 16951 0 HRH3 H3 receptor Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 435 5 0 4 4.7 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCN(Cc3cccc(F)c3)C2=O)CC1 10.1016/j.bmcl.2010.08.009
10986211 193369 0 HRH3 H3 receptor Human 5.6 pEC50 = 5.6 Binding
Inhibition of human H3-receptor using [3H]N-alpha-methyl histamineInhibition of human H3-receptor using [3H]N-alpha-methyl histamine
ChEMBL 123 1 2 2 0.2 N[C@@H]1C[C@@H]1c1c[nH]cn1 10.1021/jm020415q
CHEMBL59389 193369 0 HRH3 H3 receptor Human 5.6 pEC50 = 5.6 Binding
Inhibition of human H3-receptor using [3H]N-alpha-methyl histamineInhibition of human H3-receptor using [3H]N-alpha-methyl histamine
ChEMBL 123 1 2 2 0.2 N[C@@H]1C[C@@H]1c1c[nH]cn1 10.1021/jm020415q
145951920 162133 0 HRH3 H3 receptor Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 548 6 1 4 5.7 COc1ccc(N2C(=O)/C(=C\c3ccccc3)C2(C(=O)NC(C)(C)C)c2ccc(Br)cc2)cc1OC 10.1016/j.ejmech.2018.04.020
CHEMBL4174766 162133 0 HRH3 H3 receptor Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 548 6 1 4 5.7 COc1ccc(N2C(=O)/C(=C\c3ccccc3)C2(C(=O)NC(C)(C)C)c2ccc(Br)cc2)cc1OC 10.1016/j.ejmech.2018.04.020
16679611 17265 0 HRH3 H3 receptor Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 341 5 1 4 3.0 C[C@H]1CC[C@H](C)N1CCCOc1ccc2c(c1)cc1n2CCNC1=O 10.1016/j.bmcl.2010.08.009
CHEMBL1258309 17265 0 HRH3 H3 receptor Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 341 5 1 4 3.0 C[C@H]1CC[C@H](C)N1CCCOc1ccc2c(c1)cc1n2CCNC1=O 10.1016/j.bmcl.2010.08.009
46222044 8642 0 HRH3 H3 receptor Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 215 4 2 2 2.7 Cc1ccc(NCCc2c[nH]cn2)cc1C 10.1021/jm901890s
CHEMBL1097658 8642 0 HRH3 H3 receptor Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 215 4 2 2 2.7 Cc1ccc(NCCc2c[nH]cn2)cc1C 10.1021/jm901890s
16678214 17446 0 HRH3 H3 receptor Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 369 4 0 4 3.8 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCN(C(C)C)C2=O)CC1 10.1016/j.bmcl.2010.08.009
CHEMBL1258874 17446 0 HRH3 H3 receptor Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 369 4 0 4 3.8 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCN(C(C)C)C2=O)CC1 10.1016/j.bmcl.2010.08.009
1204 1806 104 HRH3 H3 receptor Human 7.6 pEC50 = 7.6 Binding
Activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, G-beta-1-gamma-2 and RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, G-beta-1-gamma-2 and RGS4 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm800841w
1247 1806 104 HRH3 H3 receptor Human 7.6 pEC50 = 7.6 Binding
Activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, G-beta-1-gamma-2 and RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, G-beta-1-gamma-2 and RGS4 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm800841w
1375 1806 104 HRH3 H3 receptor Human 7.6 pEC50 = 7.6 Binding
Activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, G-beta-1-gamma-2 and RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, G-beta-1-gamma-2 and RGS4 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm800841w
774 1806 104 HRH3 H3 receptor Human 7.6 pEC50 = 7.6 Binding
Activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, G-beta-1-gamma-2 and RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, G-beta-1-gamma-2 and RGS4 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm800841w
CHEMBL90 1806 104 HRH3 H3 receptor Human 7.6 pEC50 = 7.6 Binding
Activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, G-beta-1-gamma-2 and RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, G-beta-1-gamma-2 and RGS4 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm800841w
DB05381 1806 104 HRH3 H3 receptor Human 7.6 pEC50 = 7.6 Binding
Activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, G-beta-1-gamma-2 and RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, G-beta-1-gamma-2 and RGS4 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm800841w
11694543 75208 3 HRH3 H3 receptor Human 7.6 pEC50 = 7.6 Functional
Activity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cellsActivity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cells
ChEMBL 167 6 2 2 1.3 CCNCCCCc1c[nH]cn1 10.1021/jm0504353
CHEMBL204843 75208 3 HRH3 H3 receptor Human 7.6 pEC50 = 7.6 Functional
Activity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cellsActivity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cells
ChEMBL 167 6 2 2 1.3 CCNCCCCc1c[nH]cn1 10.1021/jm0504353
1204 1806 104 HRH3 H3 receptor Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm9000693
1247 1806 104 HRH3 H3 receptor Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm9000693
1375 1806 104 HRH3 H3 receptor Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm9000693
774 1806 104 HRH3 H3 receptor Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm9000693
CHEMBL90 1806 104 HRH3 H3 receptor Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm9000693
DB05381 1806 104 HRH3 H3 receptor Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm9000693
42623567 172846 0 HRH3 H3 receptor Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 207 3 2 5 0.0 CCc1cc(N2CC(NC)C2)nc(N)n1 10.1021/acs.jmedchem.9b01462
CHEMBL4535363 172846 0 HRH3 H3 receptor Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 207 3 2 5 0.0 CCc1cc(N2CC(NC)C2)nc(N)n1 10.1021/acs.jmedchem.9b01462
1204 1806 104 HRH3 H3 receptor Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gialpha-2-Gbeta-1-gamma-2 and RGS4 proteins protein by steady-state GTPase assayAgonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gialpha-2-Gbeta-1-gamma-2 and RGS4 proteins protein by steady-state GTPase assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm900526h
1247 1806 104 HRH3 H3 receptor Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gialpha-2-Gbeta-1-gamma-2 and RGS4 proteins protein by steady-state GTPase assayAgonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gialpha-2-Gbeta-1-gamma-2 and RGS4 proteins protein by steady-state GTPase assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm900526h
1375 1806 104 HRH3 H3 receptor Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gialpha-2-Gbeta-1-gamma-2 and RGS4 proteins protein by steady-state GTPase assayAgonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gialpha-2-Gbeta-1-gamma-2 and RGS4 proteins protein by steady-state GTPase assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm900526h
774 1806 104 HRH3 H3 receptor Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gialpha-2-Gbeta-1-gamma-2 and RGS4 proteins protein by steady-state GTPase assayAgonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gialpha-2-Gbeta-1-gamma-2 and RGS4 proteins protein by steady-state GTPase assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm900526h
CHEMBL90 1806 104 HRH3 H3 receptor Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gialpha-2-Gbeta-1-gamma-2 and RGS4 proteins protein by steady-state GTPase assayAgonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gialpha-2-Gbeta-1-gamma-2 and RGS4 proteins protein by steady-state GTPase assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm900526h
DB05381 1806 104 HRH3 H3 receptor Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gialpha-2-Gbeta-1-gamma-2 and RGS4 proteins protein by steady-state GTPase assayAgonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gialpha-2-Gbeta-1-gamma-2 and RGS4 proteins protein by steady-state GTPase assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm900526h
1204 1806 104 HRH3 H3 receptor Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 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 1806 104 HRH3 H3 receptor Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 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 1806 104 HRH3 H3 receptor Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 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 1806 104 HRH3 H3 receptor Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 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 1806 104 HRH3 H3 receptor Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 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 1806 104 HRH3 H3 receptor Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 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
11416895 59979 0 HRH3 H3 receptor Human 7.6 pEC50 = 7.6 Functional
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
ChEMBL 191 2 1 2 1.9 CCN1CCC(=Cc2c[nH]cn2)CC1 10.1021/jm049475h
CHEMBL175741 59979 0 HRH3 H3 receptor Human 7.6 pEC50 = 7.6 Functional
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
ChEMBL 191 2 1 2 1.9 CCN1CCC(=Cc2c[nH]cn2)CC1 10.1021/jm049475h
145951920 162133 0 HRH3 H3 receptor Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 548 6 1 4 5.7 COc1ccc(N2C(=O)/C(=C\c3ccccc3)C2(C(=O)NC(C)(C)C)c2ccc(Br)cc2)cc1OC 10.1016/j.ejmech.2018.04.020
CHEMBL4174766 162133 0 HRH3 H3 receptor Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 548 6 1 4 5.7 COc1ccc(N2C(=O)/C(=C\c3ccccc3)C2(C(=O)NC(C)(C)C)c2ccc(Br)cc2)cc1OC 10.1016/j.ejmech.2018.04.020
51354301 58363 0 HRH3 H3 receptor Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assayAgonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assay
ChEMBL 259 5 1 4 2.4 c1nc(CCn2cc(CC3CCCCC3)nn2)c[nH]1 10.1021/jm1013488
CHEMBL1688969 58363 0 HRH3 H3 receptor Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assayAgonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assay
ChEMBL 259 5 1 4 2.4 c1nc(CCn2cc(CC3CCCCC3)nn2)c[nH]1 10.1021/jm1013488
44480959 5418 2 HRH3 H3 receptor Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gialpha-2-Gbeta-1-gamma-2 and RGS4 proteins protein by steady-state GTPase assayAgonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gialpha-2-Gbeta-1-gamma-2 and RGS4 proteins protein by steady-state GTPase assay
ChEMBL 206 5 3 3 0.1 N#C/N=C(\N)NCCCCc1c[nH]cn1 10.1021/jm900526h
CHEMBL1077861 5418 2 HRH3 H3 receptor Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gialpha-2-Gbeta-1-gamma-2 and RGS4 proteins protein by steady-state GTPase assayAgonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gialpha-2-Gbeta-1-gamma-2 and RGS4 proteins protein by steady-state GTPase assay
ChEMBL 206 5 3 3 0.1 N#C/N=C(\N)NCCCCc1c[nH]cn1 10.1021/jm900526h
16679701 17411 0 HRH3 H3 receptor Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 341 3 1 4 3.0 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCCNC2=O)CC1 10.1016/j.bmcl.2010.08.009
CHEMBL1258755 17411 0 HRH3 H3 receptor Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 341 3 1 4 3.0 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCCNC2=O)CC1 10.1016/j.bmcl.2010.08.009
10773349 7826 1 HRH3 H3 receptor Human 6.6 pEC50 = 6.6 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptor
ChEMBL 165 2 2 3 0.4 NC[C@H]1C=C[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL109130 7826 1 HRH3 H3 receptor Human 6.6 pEC50 = 6.6 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptor
ChEMBL 165 2 2 3 0.4 NC[C@H]1C=C[C@H](c2c[nH]cn2)O1