Ligand source activities (1 row/activity)



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Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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ligand		 Fold
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GPCRs		 Species

 p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
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 Assay
Description		 Source

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 DOI
1251 2012 39 None 204 2 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 2012 39 None 204 2 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 2012 39 None 204 2 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 2056 7 None 251 2 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 2056 7 None 251 2 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 2056 7 None 251 2 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 2008 34 None 3 5 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 2008 34 None 3 5 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 2008 34 None 3 5 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 2008 34 None 3 5 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 2008 34 None 3 5 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 2008 34 None 3 5 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 2008 34 None 3 5 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 2008 34 None 3 5 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 162010 0 None - 1 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 162010 0 None - 1 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 162714 0 None - 1 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 162714 0 None - 1 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 176493 4 None 10 4 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 176493 4 None 10 4 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 176493 4 None 10 4 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 162010 0 None - 1 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 162010 0 None - 1 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 109741 11 None 4466 2 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 109741 11 None 4466 2 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 2008 34 None 3 5 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 2008 34 None 3 5 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 2008 34 None 3 5 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 2008 34 None 3 5 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 2012 39 None 204 2 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 2012 39 None 204 2 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 2012 39 None 204 2 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 162714 0 None - 1 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 162714 0 None - 1 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
4024 2013 20 None 3388 2 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 2013 20 None 3388 2 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 2013 20 None 3388 2 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 2013 20 None 3388 2 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 2013 20 None 3388 2 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 2013 20 None 3388 2 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 166109 0 None - 1 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 166109 0 None - 1 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 10877 0 None - 1 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 10877 0 None - 1 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
145956355 162001 0 None - 1 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 162001 0 None - 1 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 163121 0 None - 1 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 163121 0 None - 1 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 162001 0 None - 1 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 162001 0 None - 1 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 163121 0 None - 1 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 163121 0 None - 1 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 176493 4 None -11 4 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 176493 4 None -11 4 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 176493 4 None -11 4 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 2498 8 None 15848 2 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 2498 8 None 15848 2 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 2498 8 None 15848 2 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 2065 25 None -1 3 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 2065 25 None -1 3 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 2065 25 None -1 3 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 2065 25 None -1 3 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 2498 8 None 15848 2 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 2498 8 None 15848 2 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 2498 8 None 15848 2 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 2498 8 None 15848 2 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 2498 8 None 15848 2 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 2498 8 None 15848 2 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
1239 2031 24 None 1995 2 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 2031 24 None 1995 2 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 2031 24 None 1995 2 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 2031 24 None 1995 2 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 56476 0 None 50 2 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 56476 0 None 50 2 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 105493 0 None - 1 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 105493 0 None - 1 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 105494 0 None - 1 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 105494 0 None - 1 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 4061 16 None 25 2 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 4061 16 None 25 2 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 4061 16 None 25 2 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
11554040 89540 0 None 1 2 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 89540 0 None 1 2 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 89540 0 None 1 2 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 89540 0 None 1 2 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 118736 0 None - 1 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 118736 0 None - 1 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 176691 0 None - 1 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 176691 0 None - 1 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 176691 0 None - 1 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 2007 16 None 18 2 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 2007 16 None 18 2 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 2007 16 None 18 2 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
90666843 109432 0 None - 1 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
CHEMBL3220120 109432 0 None - 1 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 2012 39 None 204 2 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 2012 39 None 204 2 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 2012 39 None 204 2 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 2012 39 None 204 2 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 2012 39 None 204 2 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 2012 39 None 204 2 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
54764158 69075 0 None - 1 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 69075 0 None - 1 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 118735 0 None - 1 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 118735 0 None - 1 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 103689 0 None - 1 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 103689 0 None - 1 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 69654 0 None - 1 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 69654 0 None - 1 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 69668 0 None - 1 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 69668 0 None - 1 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 89540 0 None -1 2 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 89540 0 None -1 2 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 89540 0 None -1 2 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 89540 0 None -1 2 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 8982 0 None - 1 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 8982 0 None - 1 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 8982 0 None - 1 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 8982 0 None - 1 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 8982 0 None - 1 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 8982 0 None - 1 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 89471 0 None 3 2 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 89471 0 None 3 2 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 89471 0 None 3 2 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 89471 0 None 3 2 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 176247 0 None - 1 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 176247 0 None - 1 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 176247 0 None - 1 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 65900 0 None - 1 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 65900 0 None - 1 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 65901 0 None - 1 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 65901 0 None - 1 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 70740 0 None - 1 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 70740 0 None - 1 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 93015 0 None - 1 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 93015 0 None - 1 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 75187 0 None - 1 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 75187 0 None - 1 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
23725172 64379 0 None 2 2 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 64379 0 None 2 2 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 75174 0 None - 1 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 75174 0 None - 1 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
11957573 2008 34 None -3 5 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 2008 34 None -3 5 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 2008 34 None -3 5 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 2008 34 None -3 5 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 162204 0 None - 1 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 162204 0 None - 1 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 2013 20 None 3388 2 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 2013 20 None 3388 2 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 2013 20 None 3388 2 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 10900 0 None - 1 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 10900 0 None - 1 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 11003 0 None - 1 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 11003 0 None - 1 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 70421 0 None - 1 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 70421 0 None - 1 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 64386 0 None 1 2 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 64386 0 None 1 2 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 65383 18 None 1 2 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 65383 18 None 1 2 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 70706 0 None - 1 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 70706 0 None - 1 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 146916 0 None 4 2 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 146916 0 None 4 2 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 162204 0 None - 1 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 162204 0 None - 1 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 146916 0 None 4 2 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 146916 0 None 4 2 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
145954498 162407 0 None - 1 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
CHEMBL4165989 162407 0 None - 1 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 76517 3 None - 1 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 76517 3 None - 1 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 176246 0 None - 1 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 176246 0 None - 1 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 176246 0 None - 1 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
145959298 162305 0 None - 1 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
CHEMBL4164467 162305 0 None - 1 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 229 52 None 19 2 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 229 52 None 19 2 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 229 52 None 19 2 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 229 52 None 19 2 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 229 52 None 19 2 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 229 52 None 19 2 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
145959298 162305 0 None - 1 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
CHEMBL4164467 162305 0 None - 1 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
145954498 162407 0 None - 1 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
CHEMBL4165989 162407 0 None - 1 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 65399 0 None - 1 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 65399 0 None - 1 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 70743 0 None - 1 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 70743 0 None - 1 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 69665 0 None - 1 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 69665 0 None - 1 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
57397654 69665 0 None - 1 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 69665 0 None - 1 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 148185 0 None 2 2 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 148185 0 None 2 2 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
11603648 148185 0 None 2 2 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 148185 0 None 2 2 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 3131 64 None 10 5 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 3131 64 None 10 5 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 3131 64 None 10 5 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 3131 64 None 10 5 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 3131 64 None 10 5 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 96577 0 None 4 2 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 96577 0 None 4 2 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
11710694 96577 0 None 4 2 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 96577 0 None 4 2 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 109436 0 None - 1 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 109436 0 None - 1 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
90666846 109438 0 None - 1 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
CHEMBL3220126 109438 0 None - 1 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 8779 0 None - 1 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 8779 0 None - 1 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 10968 0 None - 1 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 10968 0 None - 1 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 70744 0 None - 1 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 70744 0 None - 1 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
156013896 178238 0 None 3 3 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
CHEMBL4635634 178238 0 None 3 3 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 178238 0 None 3 3 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 10558 0 None - 1 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 10558 0 None - 1 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 74801 0 None - 1 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 74801 0 None - 1 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 952 41 None -1 4 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 952 41 None -1 4 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 952 41 None -1 4 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 82078 0 None 3 3 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 82078 0 None 3 3 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 75177 0 None - 1 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 75177 0 None - 1 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
155540793 176280 0 None - 1 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 176280 0 None - 1 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 176280 0 None - 1 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 187641 0 None - 1 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 187641 0 None - 1 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 169392 0 None -1 2 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 169392 0 None -1 2 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
90666844 109434 0 None - 1 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
CHEMBL3220122 109434 0 None - 1 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 140542 0 None - 1 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 140542 0 None - 1 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 162946 0 None - 1 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 162946 0 None - 1 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 176387 0 None - 1 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 176387 0 None - 1 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 176387 0 None - 1 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 2080 13 None 1258 2 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 2080 13 None 1258 2 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 2080 13 None 1258 2 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
145951678 162946 0 None - 1 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 162946 0 None - 1 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
155541911 173069 0 None - 1 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 173069 0 None - 1 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 5148 1 None 7 2 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 5148 1 None 7 2 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 5360 1 None 309 2 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 5360 1 None 309 2 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 3802 49 None -9 5 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 3802 49 None -9 5 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 3802 49 None -9 5 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
10037650 5207 0 None -47 2 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 5207 0 None -47 2 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 56477 1 None 1 2 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 56477 1 None 1 2 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 109627 1 None 1 2 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 109627 1 None 1 2 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 5207 0 None -47 2 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 5207 0 None -47 2 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 162449 0 None - 1 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 162449 0 None - 1 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 162500 0 None - 1 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 162500 0 None - 1 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 162449 0 None - 1 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 162449 0 None - 1 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 5360 1 None 309 2 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 5360 1 None 309 2 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 109476 0 None 3 2 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 109476 0 None 3 2 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
1267 3802 49 None 8 5 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 3802 49 None 8 5 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 3802 49 None 8 5 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
49799507 10890 0 None - 1 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 10890 0 None - 1 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 17387 0 None - 1 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 17387 0 None - 1 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 171861 0 None - 1 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 171861 0 None - 1 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 171968 0 None - 1 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 171968 0 None - 1 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 43333 11 None - 1 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 43333 11 None - 1 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 1930 119 None -2 11 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 1930 119 None -2 11 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 1930 119 None -2 11 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 1930 119 None -2 11 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 1930 119 None -2 11 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 1930 119 None -2 11 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 121 41 None -275 6 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 121 41 None -275 6 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 121 41 None -275 6 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 171120 0 None - 1 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 171120 0 None - 1 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
145957226 162139 0 None - 1 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 162139 0 None - 1 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 1930 119 None -2 11 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 1930 119 None -2 11 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 1930 119 None -2 11 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 1930 119 None -2 11 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 1930 119 None -2 11 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 1930 119 None -2 11 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 17386 0 None - 1 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 17386 0 None - 1 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
145957226 162139 0 None - 1 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 162139 0 None - 1 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 205611 2 None 11 2 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 205611 2 None 11 2 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
11378681 11339 0 None - 1 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 11339 0 None - 1 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 11339 0 None - 1 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 17349 0 None - 1 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 17349 0 None - 1 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 17350 0 None - 1 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 17350 0 None - 1 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 17502 0 None - 1 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 17502 0 None - 1 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 162635 0 None - 1 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 162635 0 None - 1 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 162635 0 None - 1 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 162635 0 None - 1 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 16752 0 None - 1 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 16752 0 None - 1 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 16755 0 None - 1 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 16755 0 None - 1 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 205242 1 None 204 2 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 205242 1 None 204 2 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 17601 0 None - 1 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 17601 0 None - 1 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
46929551 16742 0 None - 1 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 16742 0 None - 1 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 13801 0 None - 1 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 13801 0 None - 1 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 13801 0 None - 1 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 76046 0 None - 1 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 76046 0 None - 1 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
155533291 171839 0 None - 1 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 171839 0 None - 1 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 187721 0 None - 1 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 187721 0 None - 1 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 1930 119 None -2 11 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 1930 119 None -2 11 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 1930 119 None -2 11 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 1930 119 None -2 11 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 1930 119 None -2 11 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 1930 119 None -2 11 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 63351 0 None - 1 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 63351 0 None - 1 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 132569 0 None - 1 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 132569 0 None - 1 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 109430 0 None - 1 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 109430 0 None - 1 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
127052634 140307 0 None -6 2 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 140307 0 None -6 2 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 167569 0 None - 1 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 167569 0 None - 1 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 167569 0 None - 1 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 169784 0 None - 1 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 169784 0 None - 1 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
145946358 167524 0 None - 1 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 167524 0 None - 1 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 167524 0 None - 1 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 194918 0 None - 1 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 194918 0 None - 1 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 229 52 None -19 2 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 229 52 None -19 2 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 229 52 None -19 2 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 229 52 None -19 2 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 229 52 None -19 2 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 229 52 None -19 2 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 140248 0 None -3 2 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 140248 0 None -3 2 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 10930 0 None - 1 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 10930 0 None - 1 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 10903 0 None - 1 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 10903 0 None - 1 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 17534 0 None 1 2 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 17534 0 None 1 2 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 17534 0 None -1 2 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 17534 0 None -1 2 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
145952531 162912 0 None - 1 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 162912 0 None - 1 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
145952531 162912 0 None - 1 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 162912 0 None - 1 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 8943 0 None - 1 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 8943 0 None - 1 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
11622672 75017 2 None - 1 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 75017 2 None - 1 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 108575 1 None -1 2 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 108575 1 None -1 2 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 187313 1 None - 1 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 187313 1 None - 1 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 108575 1 None -1 2 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 108575 1 None -1 2 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 63554 2 None - 1 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 63554 2 None - 1 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 169392 0 None -1 2 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 169392 0 None -1 2 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 10703 0 None - 1 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 10703 0 None - 1 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 68512 0 None - 1 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 68512 0 None - 1 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
52948255 17566 0 None - 1 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 17566 0 None - 1 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 187952 16 None - 1 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 187952 16 None - 1 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 65383 18 None -1 2 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 65383 18 None -1 2 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
56677285 65408 0 None - 1 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 65408 0 None - 1 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 68516 0 None - 1 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 68516 0 None - 1 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 64386 0 None -1 2 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 64386 0 None -1 2 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 64379 0 None -2 2 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 64379 0 None -2 2 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
11957573 2008 34 None 3 5 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 2008 34 None 3 5 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 2008 34 None 3 5 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 2008 34 None 3 5 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
1204 1930 119 None -2 11 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 1930 119 None -2 11 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 1930 119 None -2 11 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 1930 119 None -2 11 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 1930 119 None -2 11 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 1930 119 None -2 11 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 178984 0 None 6 3 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 178984 0 None 6 3 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 184223 0 None 6 3 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 184223 0 None 6 3 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
11336692 63291 1 None - 1 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 63291 1 None - 1 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
145954725 162418 0 None - 1 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 162418 0 None - 1 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
145954725 162418 0 None - 1 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 162418 0 None - 1 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
145973591 163030 0 None - 1 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 163030 0 None - 1 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
145973591 163030 0 None - 1 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 163030 0 None - 1 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 2065 25 None -1 3 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 2065 25 None -1 3 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 2065 25 None -1 3 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 2065 25 None -1 3 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
56954515 82063 0 None 2 3 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 82063 0 None 2 3 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 2008 34 None 3 5 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 2008 34 None 3 5 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 2008 34 None 3 5 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 2008 34 None 3 5 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 195749 0 None - 1 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 195749 0 None - 1 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 181602 0 None - 1 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 181602 0 None - 1 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 140313 0 None -3 2 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 140313 0 None -3 2 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 16751 0 None - 1 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 16751 0 None - 1 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
145952665 162432 0 None - 1 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
CHEMBL4166386 162432 0 None - 1 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 16756 0 None - 1 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 16756 0 None - 1 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
16678615 17317 0 None - 1 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 17317 0 None - 1 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
145951920 162956 0 None - 1 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 162956 0 None - 1 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 17631 0 None - 1 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 17631 0 None - 1 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 8909 0 None - 1 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 8909 0 None - 1 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 17812 0 None - 1 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 17812 0 None - 1 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
11694543 75797 4 None - 1 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 75797 4 None - 1 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
42623567 173689 0 None - 1 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 173689 0 None - 1 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 1930 119 None -2 11 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 1930 119 None -2 11 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 1930 119 None -2 11 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 1930 119 None -2 11 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 1930 119 None -2 11 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 1930 119 None -2 11 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
11416895 60523 0 None - 1 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 60523 0 None - 1 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 162956 0 None - 1 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 162956 0 None - 1 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 58890 0 None 1 2 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 58890 0 None 1 2 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 5674 2 None -1 2 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 5674 2 None -1 2 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 17777 0 None - 1 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 17777 0 None - 1 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 8089 1 None 89 2 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 8089 1 None 89 2 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
10702196 108566 1 None 1 2 Human 4.6 pEC50 = 4.6 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
CHEMBL320279 108566 1 None 1 2 Human 4.6 pEC50 = 4.6 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
52941269 17283 0 None - 1 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 381 5 0 4 3.8 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCN(CC3CC3)C2=O)CC1 10.1016/j.bmcl.2010.08.009
CHEMBL1257138 17283 0 None - 1 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 381 5 0 4 3.8 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCN(CC3CC3)C2=O)CC1 10.1016/j.bmcl.2010.08.009
16678514 17316 0 None - 1 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(Cc3ccccc3F)C2=O)CC1 10.1016/j.bmcl.2010.08.009
CHEMBL1257256 17316 0 None - 1 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(Cc3ccccc3F)C2=O)CC1 10.1016/j.bmcl.2010.08.009
10820929 108205 1 None 30 2 Human 5.6 pEC50 = 5.6 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
CHEMBL319658 108205 1 None 30 2 Human 5.6 pEC50 = 5.6 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
16679612 17503 0 None - 1 Human 7.5 pEC50 = 7.5 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 3.2 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3[C@H](C)CNC2=O)CC1 10.1016/j.bmcl.2010.08.009
CHEMBL1257851 17503 0 None - 1 Human 7.5 pEC50 = 7.5 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 3.2 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3[C@H](C)CNC2=O)CC1 10.1016/j.bmcl.2010.08.009
145952665 162432 0 None - 1 Human 8.5 pEC50 = 8.5 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 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
CHEMBL4166386 162432 0 None - 1 Human 8.5 pEC50 = 8.5 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 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
11647025 89471 0 None -3 2 Rat 8.5 pEC50 = 8.5 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 401 5 0 5 4.6 Cc1nc(N2CCCC2)ncc1-c1ccc2cc(CCN3CCC[C@H]3C)ccc2n1 10.1021/jm0705051
CHEMBL237191 89471 0 None -3 2 Rat 8.5 pEC50 = 8.5 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 401 5 0 5 4.6 Cc1nc(N2CCCC2)ncc1-c1ccc2cc(CCN3CCC[C@H]3C)ccc2n1 10.1021/jm0705051
155538222 176451 0 None - 1 Human 8.5 pEC50 = 8.5 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 3 2 5 0.2 CC(C)NC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4476584 176451 0 None - 1 Human 8.5 pEC50 = 8.5 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 3 2 5 0.2 CC(C)NC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4596412 176451 0 None - 1 Human 8.5 pEC50 = 8.5 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 3 2 5 0.2 CC(C)NC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
1255 3193 19 None 19 2 Human 8.5 pEC50 = 8.5 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 216 6 1 2 2.6 C(CCc1cnc[nH]1)OCc1ccccc1 10.1016/j.bmcl.2010.10.041
6421522 3193 19 None 19 2 Human 8.5 pEC50 = 8.5 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 216 6 1 2 2.6 C(CCc1cnc[nH]1)OCc1ccccc1 10.1016/j.bmcl.2010.10.041
CHEMBL19173 3193 19 None 19 2 Human 8.5 pEC50 = 8.5 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 216 6 1 2 2.6 C(CCc1cnc[nH]1)OCc1ccccc1 10.1016/j.bmcl.2010.10.041
11788475 121032 4 None - 1 Human 8.5 pEC50 = 8.5 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 163 1 2 2 1.2 C(=C1CCNCC1)c1c[nH]cn1 10.1021/jm049475h
CHEMBL356666 121032 4 None - 1 Human 8.5 pEC50 = 8.5 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 163 1 2 2 1.2 C(=C1CCNCC1)c1c[nH]cn1 10.1021/jm049475h
90666845 109437 0 None - 1 Human 8.5 pEC50 = 8.5 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 395 6 0 5 4.7 c1cc(-c2nc(CN3CCCCC3)co2)ccc1O[C@H]1C[C@H](N2CCCCC2)C1 10.1039/C0MD00056F
CHEMBL3220125 109437 0 None - 1 Human 8.5 pEC50 = 8.5 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 395 6 0 5 4.7 c1cc(-c2nc(CN3CCCCC3)co2)ccc1O[C@H]1C[C@H](N2CCCCC2)C1 10.1039/C0MD00056F
1204 1930 119 None -2 11 Human 8.5 pEC50 = 8.5 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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1247 1930 119 None -2 11 Human 8.5 pEC50 = 8.5 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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1375 1930 119 None -2 11 Human 8.5 pEC50 = 8.5 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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
774 1930 119 None -2 11 Human 8.5 pEC50 = 8.5 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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
CHEMBL90 1930 119 None -2 11 Human 8.5 pEC50 = 8.5 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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
DB05381 1930 119 None -2 11 Human 8.5 pEC50 = 8.5 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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
11603648 148185 0 None -2 2 Rat 8.4 pEC50 = 8.4 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 397 5 0 5 4.8 Cc1c(-c2ccc3cc(CCN4CCC[C@H]4C)ccc3n2)cnn1-c1ccccn1 10.1021/jm0705051
CHEMBL393581 148185 0 None -2 2 Rat 8.4 pEC50 = 8.4 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 397 5 0 5 4.8 Cc1c(-c2ccc3cc(CCN4CCC[C@H]4C)ccc3n2)cnn1-c1ccccn1 10.1021/jm0705051
11603648 148185 0 None -2 2 Rat 8.4 pEC50 = 8.4 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 397 5 0 5 4.8 Cc1c(-c2ccc3cc(CCN4CCC[C@H]4C)ccc3n2)cnn1-c1ccccn1 10.1021/jm0705051
CHEMBL393581 148185 0 None -2 2 Rat 8.4 pEC50 = 8.4 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 397 5 0 5 4.8 Cc1c(-c2ccc3cc(CCN4CCC[C@H]4C)ccc3n2)cnn1-c1ccccn1 10.1021/jm0705051
145951081 162973 0 None - 1 Human 8.4 pEC50 = 8.4 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 502 6 1 4 6.1 COc1ccc(NC2(c3cc(F)cc(F)c3)C(=O)N(C3CCCCC3)C(=O)/C2=C/c2ccccc2)cc1 10.1016/j.ejmech.2018.04.020