Ligand source activities (1 row/activity)



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Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
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 Activity
Type		 Activity
Relation		 Activity
Value		 p-value
(-log)		 Fold
selectivity		 Tested
GPCRs		 Assay
Description		 Source

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 DOI
1251 2014 None 28 Human Functional pEC50 = 10.4 10.4 204 2
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 2014 None 28 Human Functional pEC50 = 10.4 10.4 204 2
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 2014 None 28 Human Functional pEC50 = 10.4 10.4 204 2
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 2058 None 4 Human Functional pEC50 = 10.3 10.3 251 2
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 2058 None 4 Human Functional pEC50 = 10.3 10.3 251 2
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 2058 None 4 Human Functional pEC50 = 10.3 10.3 251 2
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 2010 None 25 Human Functional pEC50 = 10.2 10.2 3 5
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 2010 None 25 Human Functional pEC50 = 10.2 10.2 3 5
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 2010 None 25 Human Functional pEC50 = 10.2 10.2 3 5
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 2010 None 25 Human Functional pEC50 = 10.2 10.2 3 5
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 2010 None 25 Human Functional pEC50 = 10.1 10.1 3 5
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 2010 None 25 Human Functional pEC50 = 10.1 10.1 3 5
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 2010 None 25 Human Functional pEC50 = 10.1 10.1 3 5
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 2010 None 25 Human Functional pEC50 = 10.1 10.1 3 5
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 162106 None 0 Human Functional pEC50 = 10 10.0 - 1
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 162106 None 0 Human Functional pEC50 = 10 10.0 - 1
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 162811 None 0 Human Functional pEC50 = 10 10.0 - 1
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 162811 None 0 Human Functional pEC50 = 10 10.0 - 1
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 176600 None 5 Mouse Functional pEC50 = 10 10.0 10 4
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 176600 None 5 Mouse Functional pEC50 = 10 10.0 10 4
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 176600 None 5 Mouse Functional pEC50 = 10 10.0 10 4
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 162106 None 0 Human Functional pEC50 = 9.9 9.9 - 1
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 162106 None 0 Human Functional pEC50 = 9.9 9.9 - 1
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 109799 None 8 Human Functional pEC50 = 9.9 9.9 4466 2
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 109799 None 8 Human Functional pEC50 = 9.9 9.9 4466 2
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 2010 None 25 Human Functional pEC50 = 9.9 9.9 3 5
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 2010 None 25 Human Functional pEC50 = 9.9 9.9 3 5
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 2010 None 25 Human Functional pEC50 = 9.9 9.9 3 5
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 2010 None 25 Human Functional pEC50 = 9.9 9.9 3 5
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 2014 None 28 Human Functional pEC50 = 9.9 9.9 204 2
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 2014 None 28 Human Functional pEC50 = 9.9 9.9 204 2
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 2014 None 28 Human Functional pEC50 = 9.9 9.9 204 2
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 162811 None 0 Human Functional pEC50 = 9.9 9.9 - 1
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 162811 None 0 Human Functional pEC50 = 9.9 9.9 - 1
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 2015 None 18 Human Functional pEC50 = 9.8 9.8 3388 2
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 2015 None 18 Human Functional pEC50 = 9.8 9.8 3388 2
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 2015 None 18 Human Functional pEC50 = 9.8 9.8 3388 2
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 2015 None 18 Human Functional pEC50 = 9.7 9.7 3388 2
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 2015 None 18 Human Functional pEC50 = 9.7 9.7 3388 2
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 2015 None 18 Human Functional pEC50 = 9.7 9.7 3388 2
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 166206 None 0 Human Functional pEC50 = 9.7 9.7 - 1
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 166206 None 0 Human Functional pEC50 = 9.7 9.7 - 1
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 10883 None 0 Human Functional pEC50 = 9.7 9.7 - 1
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 10883 None 0 Human Functional pEC50 = 9.7 9.7 - 1
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 162097 None 0 Human Functional pEC50 = 9.6 9.6 - 1
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 162097 None 0 Human Functional pEC50 = 9.6 9.6 - 1
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 163218 None 0 Human Functional pEC50 = 9.6 9.6 - 1
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 163218 None 0 Human Functional pEC50 = 9.6 9.6 - 1
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 162097 None 0 Human Functional pEC50 = 9.5 9.5 - 1
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 162097 None 0 Human Functional pEC50 = 9.5 9.5 - 1
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 163218 None 0 Human Functional pEC50 = 9.5 9.5 - 1
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 163218 None 0 Human Functional pEC50 = 9.5 9.5 - 1
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 176600 None 5 Human Functional pEC50 = 9.5 9.5 -11 4
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 176600 None 5 Human Functional pEC50 = 9.5 9.5 -11 4
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 176600 None 5 Human Functional pEC50 = 9.5 9.5 -11 4
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 2500 None 6 Human Functional pEC50 = 9.5 9.5 15848 2
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 2500 None 6 Human Functional pEC50 = 9.5 9.5 15848 2
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 2500 None 6 Human Functional pEC50 = 9.5 9.5 15848 2
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 2067 None 16 Human Functional pEC50 = 9.5 9.5 -1 3
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 2067 None 16 Human Functional pEC50 = 9.5 9.5 -1 3
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 2067 None 16 Human Functional pEC50 = 9.5 9.5 -1 3
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 2067 None 16 Human Functional pEC50 = 9.5 9.5 -1 3
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 2500 None 6 Human Functional pEC50 = 9.5 9.5 15848 2
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 2500 None 6 Human Functional pEC50 = 9.5 9.5 15848 2
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 2500 None 6 Human Functional pEC50 = 9.5 9.5 15848 2
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 2500 None 6 Human Functional pEC50 = 9.5 9.5 15848 2
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 2500 None 6 Human Functional pEC50 = 9.5 9.5 15848 2
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 2500 None 6 Human Functional pEC50 = 9.5 9.5 15848 2
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 2033 None 15 Human Functional pEC50 = 9.4 9.4 1995 2
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 2033 None 15 Human Functional pEC50 = 9.4 9.4 1995 2
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 2033 None 15 Human Functional pEC50 = 9.4 9.4 1995 2
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 2033 None 15 Human Functional pEC50 = 9.4 9.4 1995 2
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 56494 None 0 Human Functional pEC50 = 9.4 9.4 50 2
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 56494 None 0 Human Functional pEC50 = 9.4 9.4 50 2
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 105551 None 0 Human Functional pEC50 = 9.4 9.4 - 1
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 105551 None 0 Human Functional pEC50 = 9.4 9.4 - 1
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 105552 None 0 Human Functional pEC50 = 9.3 9.3 - 1
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 105552 None 0 Human Functional pEC50 = 9.3 9.3 - 1
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 4063 None 15 Human Functional pEC50 = 9.3 9.3 25 2
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 4063 None 15 Human Functional pEC50 = 9.3 9.3 25 2
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 4063 None 15 Human Functional pEC50 = 9.3 9.3 25 2
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 89576 None 0 Human Functional pEC50 = 9.2 9.2 1 2
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 89576 None 0 Human Functional pEC50 = 9.2 9.2 1 2
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 89576 None 0 Human Functional pEC50 = 9.2 9.2 1 2
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 89576 None 0 Human Functional pEC50 = 9.2 9.2 1 2
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 118802 None 0 Human Functional pEC50 = 9.2 9.2 - 1
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 118802 None 0 Human Functional pEC50 = 9.2 9.2 - 1
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 176798 None 0 Human Functional pEC50 = 9.2 9.2 - 1
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 176798 None 0 Human Functional pEC50 = 9.2 9.2 - 1
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 176798 None 0 Human Functional pEC50 = 9.2 9.2 - 1
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 2009 None 10 Human Functional pEC50 = 9.2 9.2 18 2
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 2009 None 10 Human Functional pEC50 = 9.2 9.2 18 2
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 2009 None 10 Human Functional pEC50 = 9.2 9.2 18 2
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 109490 None 0 Human Functional pEC50 = 9.2 9.2 - 1
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 109490 None 0 Human Functional pEC50 = 9.2 9.2 - 1
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 2014 None 28 Human Functional pEC50 = 9.2 9.2 204 2
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 2014 None 28 Human Functional pEC50 = 9.2 9.2 204 2
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 2014 None 28 Human Functional pEC50 = 9.2 9.2 204 2
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 2014 None 28 Human Functional pEC50 = 9.2 9.2 204 2
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 2014 None 28 Human Functional pEC50 = 9.2 9.2 204 2
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 2014 None 28 Human Functional pEC50 = 9.2 9.2 204 2
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 69099 None 0 Human Functional pEC50 = 9.2 9.2 - 1
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 69099 None 0 Human Functional pEC50 = 9.2 9.2 - 1
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 118801 None 0 Human Functional pEC50 = 9.2 9.2 - 1
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 118801 None 0 Human Functional pEC50 = 9.2 9.2 - 1
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 103746 None 0 Human Functional pEC50 = 9.2 9.2 - 1
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 103746 None 0 Human Functional pEC50 = 9.2 9.2 - 1
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 69678 None 0 Human Functional pEC50 = 9.2 9.2 - 1
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 69678 None 0 Human Functional pEC50 = 9.2 9.2 - 1
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 69692 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 69692 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 89576 None 0 Rat Functional pEC50 = 9.1 9.1 -1 2
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 89576 None 0 Rat Functional pEC50 = 9.1 9.1 -1 2
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 89576 None 0 Rat Functional pEC50 = 9.1 9.1 -1 2
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 89576 None 0 Rat Functional pEC50 = 9.1 9.1 -1 2
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 8986 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 8986 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 8986 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 8986 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 8986 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 8986 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 89507 None 0 Human Functional pEC50 = 9.1 9.1 3 2
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 89507 None 0 Human Functional pEC50 = 9.1 9.1 3 2
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 89507 None 0 Human Functional pEC50 = 9.1 9.1 3 2
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 89507 None 0 Human Functional pEC50 = 9.1 9.1 3 2
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 176354 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 176354 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 176354 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 65923 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 65923 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 65924 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 65924 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 70766 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 70766 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 93070 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 93070 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 75215 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 75215 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 64402 None 0 Human Functional pEC50 = 9 9.0 2 2
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 64402 None 0 Human Functional pEC50 = 9 9.0 2 2
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 75202 None 0 Human Functional pEC50 = 9 9.0 - 1
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 75202 None 0 Human Functional pEC50 = 9 9.0 - 1
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 2010 None 25 Rat Functional pEC50 = 9 9.0 -3 5
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 2010 None 25 Rat Functional pEC50 = 9 9.0 -3 5
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 2010 None 25 Rat Functional pEC50 = 9 9.0 -3 5
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 2010 None 25 Rat Functional pEC50 = 9 9.0 -3 5
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 162300 None 0 Human Functional pEC50 = 9.0 9.0 - 1
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 162300 None 0 Human Functional pEC50 = 9.0 9.0 - 1
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 2015 None 18 Human Functional pEC50 = 9.0 9.0 3388 2
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 2015 None 18 Human Functional pEC50 = 9.0 9.0 3388 2
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 2015 None 18 Human Functional pEC50 = 9.0 9.0 3388 2
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 10906 None 0 Human Functional pEC50 = 9.0 9.0 - 1
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 10906 None 0 Human Functional pEC50 = 9.0 9.0 - 1
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 11009 None 0 Human Functional pEC50 = 9.0 9.0 - 1
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 11009 None 0 Human Functional pEC50 = 9.0 9.0 - 1
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 70447 None 0 Human Functional pEC50 = 9.0 9.0 - 1
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 70447 None 0 Human Functional pEC50 = 9.0 9.0 - 1
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 64409 None 0 Human Functional pEC50 = 9.0 9.0 1 2
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 64409 None 0 Human Functional pEC50 = 9.0 9.0 1 2
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 65406 None 23 Human Functional pEC50 = 9.0 9.0 1 2
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 65406 None 23 Human Functional pEC50 = 9.0 9.0 1 2
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 70732 None 0 Human Functional pEC50 = 9.0 9.0 - 1
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 70732 None 0 Human Functional pEC50 = 9.0 9.0 - 1
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 147006 None 0 Human Functional pEC50 = 9.0 9.0 4 2
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 147006 None 0 Human Functional pEC50 = 9.0 9.0 4 2
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 162300 None 0 Human Functional pEC50 = 9.0 9.0 - 1
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 162300 None 0 Human Functional pEC50 = 9.0 9.0 - 1
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 147006 None 0 Human Functional pEC50 = 9.0 9.0 4 2
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 147006 None 0 Human Functional pEC50 = 9.0 9.0 4 2
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 162504 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 162504 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 76546 None 2 Human Functional pEC50 = 8.9 8.9 - 1
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 76546 None 2 Human Functional pEC50 = 8.9 8.9 - 1
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 176353 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 176353 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 176353 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 162401 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 162401 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 None 35 Human Functional pEC50 = 8.9 8.9 19 2
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 None 35 Human Functional pEC50 = 8.9 8.9 19 2
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 None 35 Human Functional pEC50 = 8.9 8.9 19 2
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 None 35 Human Functional pEC50 = 8.9 8.9 19 2
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 None 35 Human Functional pEC50 = 8.9 8.9 19 2
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 None 35 Human Functional pEC50 = 8.9 8.9 19 2
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 162401 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 162401 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 162504 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 162504 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 65422 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 65422 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 70769 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 70769 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 69689 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 69689 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 69689 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 69689 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 148275 None 0 Human Functional pEC50 = 8.9 8.9 2 2
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 148275 None 0 Human Functional pEC50 = 8.9 8.9 2 2
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 148275 None 0 Human Functional pEC50 = 8.9 8.9 2 2
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 148275 None 0 Human Functional pEC50 = 8.9 8.9 2 2
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 3133 None 50 Guinea pig Functional pEC50 = 8.8 8.8 11 5
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 3133 None 50 Guinea pig Functional pEC50 = 8.8 8.8 11 5
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 3133 None 50 Guinea pig Functional pEC50 = 8.8 8.8 11 5
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
9948102.0 3133 None 50 Guinea pig Functional pEC50 = 8.8 8.8 11 5
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 3133 None 50 Guinea pig Functional pEC50 = 8.8 8.8 11 5
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 3133 None 50 Guinea pig Functional pEC50 = 8.8 8.8 11 5
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
5048 3133 None 50 Human Functional pEC50 = 8.8 8.8 -11 5
Inverse agonist activity at human H3RInverse agonist activity at human H3R
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.1016/j.ejmech.2022.114742
8924 3133 None 50 Human Functional pEC50 = 8.8 8.8 -11 5
Inverse agonist activity at human H3RInverse agonist activity at human H3R
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.1016/j.ejmech.2022.114742
9948102 3133 None 50 Human Functional pEC50 = 8.8 8.8 -11 5
Inverse agonist activity at human H3RInverse agonist activity at human H3R
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.1016/j.ejmech.2022.114742
9948102.0 3133 None 50 Human Functional pEC50 = 8.8 8.8 -11 5
Inverse agonist activity at human H3RInverse agonist activity at human H3R
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.1016/j.ejmech.2022.114742
CHEMBL462605 3133 None 50 Human Functional pEC50 = 8.8 8.8 -11 5
Inverse agonist activity at human H3RInverse agonist activity at human H3R
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.1016/j.ejmech.2022.114742
DB11642 3133 None 50 Human Functional pEC50 = 8.8 8.8 -11 5
Inverse agonist activity at human H3RInverse agonist activity at human H3R
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.1016/j.ejmech.2022.114742
11710694 96632 None 0 Human Functional pEC50 = 8.8 8.8 4 2
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 96632 None 0 Human Functional pEC50 = 8.8 8.8 4 2
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 96632 None 0 Human Functional pEC50 = 8.8 8.8 4 2
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 96632 None 0 Human Functional pEC50 = 8.8 8.8 4 2
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 109494 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 109494 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 109496 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 109496 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 8783 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 8783 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 10974 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 10974 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 70770 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 70770 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 178345 None 0 Human Functional pEC50 = 8.8 8.8 3 3
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 178345 None 0 Human Functional pEC50 = 8.8 8.8 3 3
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 178345 None 0 Human Functional pEC50 = 8.8 8.8 3 3
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 10563 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 10563 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 74829 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 74829 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 953 None 33 Mouse Functional pEC50 = 8.8 8.8 -1 4
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 953 None 33 Mouse Functional pEC50 = 8.8 8.8 -1 4
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 953 None 33 Mouse Functional pEC50 = 8.8 8.8 -1 4
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 82111 None 0 Human Functional pEC50 = 8.8 8.8 3 3
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 82111 None 0 Human Functional pEC50 = 8.8 8.8 3 3
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 75205 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 75205 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 176387 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 176387 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 176387 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 187749 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 187749 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 169497 None 0 Human Functional pEC50 = 8.7 8.7 -1 2
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 169497 None 0 Human Functional pEC50 = 8.7 8.7 -1 2
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 109492 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 109492 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 140631 None 0 Human Functional pEC50 = 8 8.0 - 1
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 140631 None 0 Human Functional pEC50 = 8 8.0 - 1
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 163043 None 0 Human Functional pEC50 = 8 8.0 - 1
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 163043 None 0 Human Functional pEC50 = 8 8.0 - 1
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 176494 None 0 Human Functional pEC50 = 8 8.0 - 1
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 176494 None 0 Human Functional pEC50 = 8 8.0 - 1
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 176494 None 0 Human Functional pEC50 = 8 8.0 - 1
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 2082 None 7 Human Functional pEC50 = 8 8.0 1258 2
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 2082 None 7 Human Functional pEC50 = 8 8.0 1258 2
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 2082 None 7 Human Functional pEC50 = 8 8.0 1258 2
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 163043 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 163043 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 173174 None 0 Human Functional pEC50 = 7 7.0 - 1
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 173174 None 0 Human Functional pEC50 = 7 7.0 - 1
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 5152 None 0 Human Functional pEC50 = 7 7.0 7 2
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 5152 None 0 Human Functional pEC50 = 7 7.0 7 2
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 5364 None 1 Human Functional pEC50 = 7 7.0 309 2
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 5364 None 1 Human Functional pEC50 = 7 7.0 309 2
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 3804 None 32 Human Functional pEC50 = 7 7.0 -6 5
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 3804 None 32 Human Functional pEC50 = 7 7.0 -6 5
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 3804 None 32 Human Functional pEC50 = 7 7.0 -6 5
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 5211 None 0 Human Functional pEC50 = 5 5.0 -47 2
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 5211 None 0 Human Functional pEC50 = 5 5.0 -47 2
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 56495 None 0 Human Functional pEC50 = 5 5.0 1 2
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 56495 None 0 Human Functional pEC50 = 5 5.0 1 2
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 109685 None 0 Human Functional pEC50 = 5 5.0 1 2
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 109685 None 0 Human Functional pEC50 = 5 5.0 1 2
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 5211 None 0 Human Functional pEC50 = 5.0 5.0 -47 2
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 5211 None 0 Human Functional pEC50 = 5.0 5.0 -47 2
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 162546 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 162546 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 162597 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 162597 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 162546 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 162546 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 5364 None 1 Human Functional pEC50 = 7.0 7.0 309 2
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 5364 None 1 Human Functional pEC50 = 7.0 7.0 309 2
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 109534 None 0 Human Functional pEC50 = 6.0 6.0 3 2
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 109534 None 0 Human Functional pEC50 = 6.0 6.0 3 2
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 3804 None 32 Mouse Functional pEC50 = 8.0 8.0 6 5
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 3804 None 32 Mouse Functional pEC50 = 8.0 8.0 6 5
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 3804 None 32 Mouse Functional pEC50 = 8.0 8.0 6 5
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 10896 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 10896 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 17396 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 17396 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 171966 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 171966 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 172073 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 172073 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 43349 None 4 Human Functional pEC50 = 7.9 7.9 - 1
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 43349 None 4 Human Functional pEC50 = 7.9 7.9 - 1
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 1932 None 74 Human Functional pEC50 = 7.9 7.9 -2 11
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 1932 None 74 Human Functional pEC50 = 7.9 7.9 -2 11
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 1932 None 74 Human Functional pEC50 = 7.9 7.9 -2 11
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 1932 None 74 Human Functional pEC50 = 7.9 7.9 -2 11
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
774.0 1932 None 74 Human Functional pEC50 = 7.9 7.9 -2 11
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 1932 None 74 Human Functional pEC50 = 7.9 7.9 -2 11
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 1932 None 74 Human Functional pEC50 = 7.9 7.9 -2 11
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 None 34 Human Functional pEC50 = 4.9 4.9 -275 6
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 None 34 Human Functional pEC50 = 4.9 4.9 -275 6
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 None 34 Human Functional pEC50 = 4.9 4.9 -275 6
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 171225 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 171225 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 162235 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 162235 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 1932 None 74 Human Functional pEC50 = 7.9 7.9 -2 11
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 1932 None 74 Human Functional pEC50 = 7.9 7.9 -2 11
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 1932 None 74 Human Functional pEC50 = 7.9 7.9 -2 11
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 1932 None 74 Human Functional pEC50 = 7.9 7.9 -2 11
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
774.0 1932 None 74 Human Functional pEC50 = 7.9 7.9 -2 11
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 1932 None 74 Human Functional pEC50 = 7.9 7.9 -2 11
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 1932 None 74 Human Functional pEC50 = 7.9 7.9 -2 11
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 17395 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 17395 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 162235 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 162235 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 208071 None 2 Human Functional pEC50 = 5.9 5.9 11 2
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 208071 None 2 Human Functional pEC50 = 5.9 5.9 11 2
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 11345 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 11345 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 11345 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 17358 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 17358 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 17359 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 17359 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 17511 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 17511 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 162732 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 162732 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 162732 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 162732 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 16761 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 16761 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 16764 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 16764 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 207702 None 1 Human Functional pEC50 = 6.9 6.9 204 2
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 207702 None 1 Human Functional pEC50 = 6.9 6.9 204 2
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 17610 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 17610 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 16751 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 16751 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 13808 None 0 Rat Functional pEC50 = 7.8 7.8 - 1
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 13808 None 0 Rat Functional pEC50 = 7.8 7.8 - 1
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 13808 None 0 Rat Functional pEC50 = 7.8 7.8 - 1
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 76075 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 76075 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 171944 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 171944 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 187829 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 187829 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 1932 None 74 Human Functional pEC50 = 7.8 7.8 -2 11
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 1932 None 74 Human Functional pEC50 = 7.8 7.8 -2 11
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 1932 None 74 Human Functional pEC50 = 7.8 7.8 -2 11
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 1932 None 74 Human Functional pEC50 = 7.8 7.8 -2 11
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
774.0 1932 None 74 Human Functional pEC50 = 7.8 7.8 -2 11
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 1932 None 74 Human Functional pEC50 = 7.8 7.8 -2 11
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 1932 None 74 Human Functional pEC50 = 7.8 7.8 -2 11
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 63373 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 63373 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 132639 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 132639 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 109488 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 109488 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 140396 None 0 Human Functional pEC50 = 5.8 5.8 -6 2
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 140396 None 0 Human Functional pEC50 = 5.8 5.8 -6 2
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 167670 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 167670 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 167670 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 169889 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 169889 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 167624 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 167624 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 167624 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 195993 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 195993 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 None 35 Rat Functional pEC50 = 7.8 7.8 -19 2
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 None 35 Rat Functional pEC50 = 7.8 7.8 -19 2
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 None 35 Rat Functional pEC50 = 7.8 7.8 -19 2
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 None 35 Rat Functional pEC50 = 7.8 7.8 -19 2
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 None 35 Rat Functional pEC50 = 7.8 7.8 -19 2
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 None 35 Rat Functional pEC50 = 7.8 7.8 -19 2
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 140337 None 0 Human Functional pEC50 = 6.8 6.8 -3 2
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 140337 None 0 Human Functional pEC50 = 6.8 6.8 -3 2
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 10936 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 10936 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 10909 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 10909 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 17543 None 0 Human Functional pEC50 = 7.8 7.8 1 2
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 17543 None 0 Human Functional pEC50 = 7.8 7.8 1 2
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 17543 None 0 Rat Functional pEC50 = 7.8 7.8 -1 2
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 17543 None 0 Rat Functional pEC50 = 7.8 7.8 -1 2
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 163009 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 163009 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 163009 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 163009 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 8947 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 8947 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 75045 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 75045 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 108633 None 0 Human Functional pEC50 = 6.7 6.7 -1 2
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 108633 None 0 Human Functional pEC50 = 6.7 6.7 -1 2
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 187421 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 187421 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 108633 None 0 Human Functional pEC50 = 6.7 6.7 -1 2
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 108633 None 0 Human Functional pEC50 = 6.7 6.7 -1 2
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 63577 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 63577 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 169497 None 0 Human Functional pEC50 = 8.7 8.7 -1 2
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 169497 None 0 Human Functional pEC50 = 8.7 8.7 -1 2
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 10709 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 10709 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 68536 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 68536 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 17575 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 17575 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 188060 None 12 Human Functional pEC50 = 8.7 8.7 - 1
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 188060 None 12 Human Functional pEC50 = 8.7 8.7 - 1
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 65406 None 23 Rat Functional pEC50 = 8.7 8.7 -1 2
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 65406 None 23 Rat Functional pEC50 = 8.7 8.7 -1 2
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 65431 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 65431 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 68540 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 68540 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 64409 None 0 Rat Functional pEC50 = 8.7 8.7 -1 2
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 64409 None 0 Rat Functional pEC50 = 8.7 8.7 -1 2
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 64402 None 0 Rat Functional pEC50 = 8.7 8.7 -2 2
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 64402 None 0 Rat Functional pEC50 = 8.7 8.7 -2 2
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 2010 None 25 Human Functional pEC50 = 8.6 8.6 3 5
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 2010 None 25 Human Functional pEC50 = 8.6 8.6 3 5
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 2010 None 25 Human Functional pEC50 = 8.6 8.6 3 5
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 2010 None 25 Human Functional pEC50 = 8.6 8.6 3 5
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 1932 None 74 Human Functional pEC50 = 8.6 8.6 -2 11
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 1932 None 74 Human Functional pEC50 = 8.6 8.6 -2 11
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 1932 None 74 Human Functional pEC50 = 8.6 8.6 -2 11
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 1932 None 74 Human Functional pEC50 = 8.6 8.6 -2 11
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
774.0 1932 None 74 Human Functional pEC50 = 8.6 8.6 -2 11
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 1932 None 74 Human Functional pEC50 = 8.6 8.6 -2 11
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 1932 None 74 Human Functional pEC50 = 8.6 8.6 -2 11
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 179092 None 0 Human Functional pEC50 = 8.6 8.6 6 3
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 179092 None 0 Human Functional pEC50 = 8.6 8.6 6 3
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 184331 None 0 Human Functional pEC50 = 8.6 8.6 6 3
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 184331 None 0 Human Functional pEC50 = 8.6 8.6 6 3
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 63313 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 63313 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 162515 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 162515 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 162515 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 162515 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 163127 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 163127 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 163127 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 163127 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 2067 None 16 Human Functional pEC50 = 8.6 8.6 -1 3
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 2067 None 16 Human Functional pEC50 = 8.6 8.6 -1 3
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 2067 None 16 Human Functional pEC50 = 8.6 8.6 -1 3
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 2067 None 16 Human Functional pEC50 = 8.6 8.6 -1 3
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 82096 None 0 Human Functional pEC50 = 8.5 8.5 2 3
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 82096 None 0 Human Functional pEC50 = 8.5 8.5 2 3
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 2010 None 25 Human Functional pEC50 = 8.5 8.5 3 5
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 2010 None 25 Human Functional pEC50 = 8.5 8.5 3 5
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 2010 None 25 Human Functional pEC50 = 8.5 8.5 3 5
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 2010 None 25 Human Functional pEC50 = 8.5 8.5 3 5
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 198207 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 198207 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 181710 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 181710 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 140402 None 0 Human Functional pEC50 = 6.7 6.7 -3 2
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 140402 None 0 Human Functional pEC50 = 6.7 6.7 -3 2
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 16760 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 16760 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 162529 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 162529 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 16765 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 16765 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 17326 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 17326 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 163053 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 163053 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 17640 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 17640 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 8913 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 8913 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 17821 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 17821 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 75826 None 2 Human Functional pEC50 = 7.6 7.6 - 1
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 75826 None 2 Human Functional pEC50 = 7.6 7.6 - 1
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 173795 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 173795 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 1932 None 74 Human Functional pEC50 = 7.6 7.6 -2 11
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 1932 None 74 Human Functional pEC50 = 7.6 7.6 -2 11
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 1932 None 74 Human Functional pEC50 = 7.6 7.6 -2 11
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 1932 None 74 Human Functional pEC50 = 7.6 7.6 -2 11
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
774.0 1932 None 74 Human Functional pEC50 = 7.6 7.6 -2 11
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 1932 None 74 Human Functional pEC50 = 7.6 7.6 -2 11
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 1932 None 74 Human Functional pEC50 = 7.6 7.6 -2 11
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 60545 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 60545 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 163053 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 163053 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 58909 None 0 Human Functional pEC50 = 6.6 6.6 1 2
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 58909 None 0 Human Functional pEC50 = 6.6 6.6 1 2
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 5678 None 0 Human Functional pEC50 = 6.6 6.6 -1 2
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 5678 None 0 Human Functional pEC50 = 6.6 6.6 -1 2
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 17786 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 17786 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 8093 None 1 Human Functional pEC50 = 6.6 6.6 89 2
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 8093 None 1 Human Functional pEC50 = 6.6 6.6 89 2
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 108624 None 1 Human Functional pEC50 = 4.6 4.6 1 2
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 108624 None 1 Human Functional pEC50 = 4.6 4.6 1 2
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 17292 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 17292 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 17325 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 17325 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 108263 None 1 Human Functional pEC50 = 5.6 5.6 30 2
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 108263 None 1 Human Functional pEC50 = 5.6 5.6 30 2
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 17512 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 17512 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 162529 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 162529 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 89507 None 0 Rat Functional pEC50 = 8.5 8.5 -3 2
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 89507 None 0 Rat Functional pEC50 = 8.5 8.5 -3 2
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 176558 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 176558 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 176558 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 3195 None 17 Human Functional pEC50 = 8.5 8.5 19 2
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 3195 None 17 Human Functional pEC50 = 8.5 8.5 19 2
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 3195 None 17 Human Functional pEC50 = 8.5 8.5 19 2
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 121098 None 2 Human Functional pEC50 = 8.5 8.5 - 1
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 121098 None 2 Human Functional pEC50 = 8.5 8.5 - 1
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 109495 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 109495 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 1932 None 74 Human Functional pEC50 = 8.5 8.5 -2 11
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 1932 None 74 Human Functional pEC50 = 8.5 8.5 -2 11
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 1932 None 74 Human Functional pEC50 = 8.5 8.5 -2 11
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 1932 None 74 Human Functional pEC50 = 8.5 8.5 -2 11
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
774.0 1932 None 74 Human Functional pEC50 = 8.5 8.5 -2 11
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 1932 None 74 Human Functional pEC50 = 8.5 8.5 -2 11
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 1932 None 74 Human Functional pEC50 = 8.5 8.5 -2 11
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 148275 None 0 Rat Functional pEC50 = 8.4 8.4 -2 2
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 148275 None 0 Rat Functional pEC50 = 8.4 8.4 -2 2
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 148275 None 0 Rat Functional pEC50 = 8.4 8.4 -2 2
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 148275 None 0 Rat Functional pEC50 = 8.4 8.4 -2 2
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 163070 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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
CHEMBL4175106 163070 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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
145951081 163070 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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
CHEMBL4175106 163070 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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
127004182 176495 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 1 5 -0.2 CN(C)C1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4455352 176495 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 1 5 -0.2 CN(C)C1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4595913 176495 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 1 5 -0.2 CN(C)C1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
155491015 176600 None 5 Human Functional pEC50 = 8.4 8.4 -11 4
Agonist activity at human H3R expressed on HEK293T cells by [35S]GTPgammaS binding assayAgonist activity at human H3R expressed on HEK293T cells by [35S]GTPgammaS binding assay
ChEMBL 207 4 2 5 0.2 CCCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4441731 176600 None 5 Human Functional pEC50 = 8.4 8.4 -11 4
Agonist activity at human H3R expressed on HEK293T cells by [35S]GTPgammaS binding assayAgonist activity at human H3R expressed on HEK293T cells by [35S]GTPgammaS binding assay
ChEMBL 207 4 2 5 0.2 CCCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4596734 176600 None 5 Human Functional pEC50 = 8.4 8.4 -11 4
Agonist activity at human H3R expressed on HEK293T cells by [35S]GTPgammaS binding assayAgonist activity at human H3R expressed on HEK293T cells by [35S]GTPgammaS binding assay
ChEMBL 207 4 2 5 0.2 CCCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
1252 2017 None 16 Human Functional pEC50 = 8.4 8.4 - 1
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 153 5 2 2 1.1 NCCCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
9793868 2017 None 16 Human Functional pEC50 = 8.4 8.4 - 1
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 153 5 2 2 1.1 NCCCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL417096 2017 None 16 Human Functional pEC50 = 8.4 8.4 - 1
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 153 5 2 2 1.1 NCCCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
11395725 60827 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 247 3 1 2 3.0 c1nc(CC2CCN(C3CCCCC3)CC2)c[nH]1 10.1021/jm049475h
CHEMBL176178 60827 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 247 3 1 2 3.0 c1nc(CC2CCN(C3CCCCC3)CC2)c[nH]1 10.1021/jm049475h
11164099 61029 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 193 3 1 2 1.7 CCN1CCC(Cc2c[nH]cn2)CC1 10.1021/jm049475h
CHEMBL176269 61029 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 193 3 1 2 1.7 CCN1CCC(Cc2c[nH]cn2)CC1 10.1021/jm049475h
1204 1932 None 74 Human Functional pEC50 = 7.5 7.5 -2 11
Agonist activity at human H3 receptor stably transfected in CHO-DUKX cells assessed as increase in cAMP accumulation by measuring reduction in forskolin level by HitHunter-cAMP assayAgonist activity at human H3 receptor stably transfected in CHO-DUKX cells assessed as increase in cAMP accumulation by measuring reduction in forskolin level by HitHunter-cAMP assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2020.112150
1247 1932 None 74 Human Functional pEC50 = 7.5 7.5 -2 11
Agonist activity at human H3 receptor stably transfected in CHO-DUKX cells assessed as increase in cAMP accumulation by measuring reduction in forskolin level by HitHunter-cAMP assayAgonist activity at human H3 receptor stably transfected in CHO-DUKX cells assessed as increase in cAMP accumulation by measuring reduction in forskolin level by HitHunter-cAMP assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2020.112150
1375 1932 None 74 Human Functional pEC50 = 7.5 7.5 -2 11
Agonist activity at human H3 receptor stably transfected in CHO-DUKX cells assessed as increase in cAMP accumulation by measuring reduction in forskolin level by HitHunter-cAMP assayAgonist activity at human H3 receptor stably transfected in CHO-DUKX cells assessed as increase in cAMP accumulation by measuring reduction in forskolin level by HitHunter-cAMP assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2020.112150
774 1932 None 74 Human Functional pEC50 = 7.5 7.5 -2 11
Agonist activity at human H3 receptor stably transfected in CHO-DUKX cells assessed as increase in cAMP accumulation by measuring reduction in forskolin level by HitHunter-cAMP assayAgonist activity at human H3 receptor stably transfected in CHO-DUKX cells assessed as increase in cAMP accumulation by measuring reduction in forskolin level by HitHunter-cAMP assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2020.112150
774.0 1932 None 74 Human Functional pEC50 = 7.5 7.5 -2 11
Agonist activity at human H3 receptor stably transfected in CHO-DUKX cells assessed as increase in cAMP accumulation by measuring reduction in forskolin level by HitHunter-cAMP assayAgonist activity at human H3 receptor stably transfected in CHO-DUKX cells assessed as increase in cAMP accumulation by measuring reduction in forskolin level by HitHunter-cAMP assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2020.112150
CHEMBL90 1932 None 74 Human Functional pEC50 = 7.5 7.5 -2 11
Agonist activity at human H3 receptor stably transfected in CHO-DUKX cells assessed as increase in cAMP accumulation by measuring reduction in forskolin level by HitHunter-cAMP assayAgonist activity at human H3 receptor stably transfected in CHO-DUKX cells assessed as increase in cAMP accumulation by measuring reduction in forskolin level by HitHunter-cAMP assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2020.112150
DB05381 1932 None 74 Human Functional pEC50 = 7.5 7.5 -2 11
Agonist activity at human H3 receptor stably transfected in CHO-DUKX cells assessed as increase in cAMP accumulation by measuring reduction in forskolin level by HitHunter-cAMP assayAgonist activity at human H3 receptor stably transfected in CHO-DUKX cells assessed as increase in cAMP accumulation by measuring reduction in forskolin level by HitHunter-cAMP assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2020.112150
11672774 4061 None 11 Human Functional pEC50 = 7.5 7.5 - 1
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 6 1 2 1.7 CN(CCCCCc1[nH]cnc1)C 10.1021/jm0504353
1245 4061 None 11 Human Functional pEC50 = 7.5 7.5 - 1
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 6 1 2 1.7 CN(CCCCCc1[nH]cnc1)C 10.1021/jm0504353
CHEMBL206548 4061 None 11 Human Functional pEC50 = 7.5 7.5 - 1
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 6 1 2 1.7 CN(CCCCCc1[nH]cnc1)C 10.1021/jm0504353
11637064 74980 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 207 6 1 2 2.2 c1nc(CCCCCN2CCCC2)c[nH]1 10.1021/jm0504353
CHEMBL203228 74980 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 207 6 1 2 2.2 c1nc(CCCCCN2CCCC2)c[nH]1 10.1021/jm0504353
11629829 76049 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 207 5 1 2 2.2 c1nc(CCCCN2CCCCC2)c[nH]1 10.1021/jm0504353
CHEMBL205583 76049 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 207 5 1 2 2.2 c1nc(CCCCN2CCCCC2)c[nH]1 10.1021/jm0504353
155527319 171335 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 CCc1cc(N2CC(N)C2)nc(N)n1 10.1021/acs.jmedchem.9b01462
CHEMBL4459723 171335 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 CCc1cc(N2CC(N)C2)nc(N)n1 10.1021/acs.jmedchem.9b01462
155562440 175268 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 0.4 CCNC1CN(c2cc(CC)nc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4570258 175268 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 0.4 CCNC1CN(c2cc(CC)nc(N)n2)C1 10.1021/acs.jmedchem.9b01462
14717864 173750 None 8 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human histamine H3 receptor assessed as beta galactosidase activityAgonist activity at human histamine H3 receptor assessed as beta galactosidase activity
ChEMBL 124 3 1 1 1.8 CCCCc1c[nH]cn1 10.1021/jm7014149
CHEMBL453433 173750 None 8 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human histamine H3 receptor assessed as beta galactosidase activityAgonist activity at human histamine H3 receptor assessed as beta galactosidase activity
ChEMBL 124 3 1 1 1.8 CCCCc1c[nH]cn1 10.1021/jm7014149
11178286 131514 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 283 6 1 2 3.3 c1ccc(CCCN2CCC(Cc3c[nH]cn3)CC2)cc1 10.1021/jm049475h
CHEMBL369096 131514 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 283 6 1 2 3.3 c1ccc(CCCN2CCC(Cc3c[nH]cn3)CC2)cc1 10.1021/jm049475h
11435330 12079 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 182 7 1 2 2.2 CCCCOCCCc1c[nH]cn1 10.1021/jm031065q
CHEMBL1183715 12079 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 182 7 1 2 2.2 CCCCOCCCc1c[nH]cn1 10.1021/jm031065q
CHEMBL314526 12079 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 182 7 1 2 2.2 CCCCOCCCc1c[nH]cn1 10.1021/jm031065q
1274 4064 None 14 Human Functional pEC50 = 6.5 6.5 -7 4
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 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1016/j.bmcl.2010.10.041
3063228 4064 None 14 Human Functional pEC50 = 6.5 6.5 -7 4
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 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1016/j.bmcl.2010.10.041
CHEMBL1196470 4064 None 14 Human Functional pEC50 = 6.5 6.5 -7 4
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 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1016/j.bmcl.2010.10.041
1274 4064 None 14 Human Functional pEC50 = 6.5 6.5 -7 4
Agonist activity at human histamine H3 receptor in SK-N-MC cells assessed as inhibition of forskolin-induced cAMP-mediated CRE-beta galactosidase activityAgonist activity at human histamine H3 receptor in SK-N-MC cells assessed as inhibition of forskolin-induced cAMP-mediated CRE-beta galactosidase activity
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1021/jm060880d
3063228 4064 None 14 Human Functional pEC50 = 6.5 6.5 -7 4
Agonist activity at human histamine H3 receptor in SK-N-MC cells assessed as inhibition of forskolin-induced cAMP-mediated CRE-beta galactosidase activityAgonist activity at human histamine H3 receptor in SK-N-MC cells assessed as inhibition of forskolin-induced cAMP-mediated CRE-beta galactosidase activity
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1021/jm060880d
CHEMBL1196470 4064 None 14 Human Functional pEC50 = 6.5 6.5 -7 4
Agonist activity at human histamine H3 receptor in SK-N-MC cells assessed as inhibition of forskolin-induced cAMP-mediated CRE-beta galactosidase activityAgonist activity at human histamine H3 receptor in SK-N-MC cells assessed as inhibition of forskolin-induced cAMP-mediated CRE-beta galactosidase activity
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1021/jm060880d
11166138 131525 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 261 4 1 2 3.4 c1nc(CCC2CCN(C3CCCCC3)CC2)c[nH]1 10.1021/jm049475h
CHEMBL369158 131525 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 261 4 1 2 3.4 c1nc(CCC2CCN(C3CCCCC3)CC2)c[nH]1 10.1021/jm049475h
10106063 109327 None 11 Human Functional pEC50 = 5.5 5.5 -40 2
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
CHEMBL321860 109327 None 11 Human Functional pEC50 = 5.5 5.5 -40 2
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
10106063 109327 None 11 Human Functional pEC50 = 5.5 5.5 -40 2
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
CHEMBL321860 109327 None 11 Human Functional pEC50 = 5.5 5.5 -40 2
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
46222042 8781 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 187 4 2 2 2.1 c1ccc(NCCc2c[nH]cn2)cc1 10.1021/jm901890s
CHEMBL1096514 8781 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 187 4 2 2 2.1 c1ccc(NCCc2c[nH]cn2)cc1 10.1021/jm901890s
12647300 8780 None 1 Human Functional pEC50 = 5.5 5.5 - 1
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 193 4 2 2 1.9 c1nc(CCNC2CCCCC2)c[nH]1 10.1021/jm901890s
CHEMBL1096513 8780 None 1 Human Functional pEC50 = 5.5 5.5 - 1
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 193 4 2 2 1.9 c1nc(CCNC2CCCCC2)c[nH]1 10.1021/jm901890s
52948008 17476 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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)cc2n3CCCN(CC3CC3)C2=O)CC1 10.1016/j.bmcl.2010.08.009
CHEMBL1257728 17476 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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)cc2n3CCCN(CC3CC3)C2=O)CC1 10.1016/j.bmcl.2010.08.009
11171181 11351 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 166 6 1 2 1.5 C=CCOCCCc1c[nH]cn1 10.1021/jm031065q
CHEMBL1179642 11351 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 166 6 1 2 1.5 C=CCOCCCc1c[nH]cn1 10.1021/jm031065q
CHEMBL91361 11351 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 166 6 1 2 1.5 C=CCOCCCc1c[nH]cn1 10.1021/jm031065q
127051301 140287 None 0 Human Functional pEC50 = 6.4 6.4 -5 3
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
CHEMBL3804906 140287 None 0 Human Functional pEC50 = 6.4 6.4 -5 3
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
46929447 16746 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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(SCC(c2c[nH]cn2)C2CCNCC2)cc1 10.1021/jm100643t
CHEMBL1243305 16746 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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(SCC(c2c[nH]cn2)C2CCNCC2)cc1 10.1021/jm100643t
16679518 17785 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 3 1 4 2.6 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCNC2=O)CC1 10.1016/j.bmcl.2010.08.009
CHEMBL1258754 17785 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 3 1 4 2.6 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCNC2=O)CC1 10.1016/j.bmcl.2010.08.009
11564628 75558 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 193 5 1 2 1.8 c1nc(CCCCN2CCCC2)c[nH]1 10.1021/jm0504353
CHEMBL204360 75558 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 193 5 1 2 1.8 c1nc(CCCCN2CCCC2)c[nH]1 10.1021/jm0504353
155565634 175677 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 2 1 5 0.1 Cc1cc(N2CC(N(C)C)C2)nc(N)n1 10.1021/acs.jmedchem.9b01462
CHEMBL4579385 175677 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 2 1 5 0.1 Cc1cc(N2CC(N(C)C)C2)nc(N)n1 10.1021/acs.jmedchem.9b01462
10197870 5303 None 0 Human Functional pEC50 = 7.4 7.4 47 2
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
CHEMBL106612 5303 None 0 Human Functional pEC50 = 7.4 7.4 47 2
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
170389 209439 None 25 Human Functional pEC50 = 7.4 7.4 4 2
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 0.3 NCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL4634086 209439 None 25 Human Functional pEC50 = 7.4 7.4 4 2
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 0.3 NCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL91353 209439 None 25 Human Functional pEC50 = 7.4 7.4 4 2
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 0.3 NCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
1267 3804 None 32 Human Functional pEC50 = 7.4 7.4 -6 5
Inverse agonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assayInverse agonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm1013488
3035905 3804 None 32 Human Functional pEC50 = 7.4 7.4 -6 5
Inverse agonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assayInverse agonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm1013488
CHEMBL260374 3804 None 32 Human Functional pEC50 = 7.4 7.4 -6 5
Inverse agonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assayInverse agonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm1013488
1204 1932 None 74 Human Functional pEC50 = 8.4 8.4 -2 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2020.112150
1247 1932 None 74 Human Functional pEC50 = 8.4 8.4 -2 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2020.112150
1375 1932 None 74 Human Functional pEC50 = 8.4 8.4 -2 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2020.112150
774 1932 None 74 Human Functional pEC50 = 8.4 8.4 -2 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2020.112150
774.0 1932 None 74 Human Functional pEC50 = 8.4 8.4 -2 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2020.112150
CHEMBL90 1932 None 74 Human Functional pEC50 = 8.4 8.4 -2 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2020.112150
DB05381 1932 None 74 Human Functional pEC50 = 8.4 8.4 -2 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2020.112150
44273932 13566 None 4 Rat Functional pEC50 = 8.4 8.4 - 1
Compound was evaluated for agonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uMCompound was evaluated for agonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uM
ChEMBL 125 2 2 2 0.5 C[C@H](CN)c1c[nH]cn1 10.1016/S0960-894X(00)80219-X
CHEMBL1193901 13566 None 4 Rat Functional pEC50 = 8.4 8.4 - 1
Compound was evaluated for agonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uMCompound was evaluated for agonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uM
ChEMBL 125 2 2 2 0.5 C[C@H](CN)c1c[nH]cn1 10.1016/S0960-894X(00)80219-X
CHEMBL545378 13566 None 4 Rat Functional pEC50 = 8.4 8.4 - 1
Compound was evaluated for agonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uMCompound was evaluated for agonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uM
ChEMBL 125 2 2 2 0.5 C[C@H](CN)c1c[nH]cn1 10.1016/S0960-894X(00)80219-X
52944579 17574 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 419 3 1 4 4.0 CC(C)N1CCC(Oc2cc3cc4n(c3cc2Br)[C@@H](C)CNC4=O)CC1 10.1016/j.bmcl.2010.08.009
CHEMBL1258078 17574 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 419 3 1 4 4.0 CC(C)N1CCC(Oc2cc3cc4n(c3cc2Br)[C@@H](C)CNC4=O)CC1 10.1016/j.bmcl.2010.08.009
16122898 17639 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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
CHEMBL1258308 17639 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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
1204 1932 None 74 Human Functional pEC50 = 8.4 8.4 -2 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0300025
1247 1932 None 74 Human Functional pEC50 = 8.4 8.4 -2 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0300025
1375 1932 None 74 Human Functional pEC50 = 8.4 8.4 -2 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0300025
774 1932 None 74 Human Functional pEC50 = 8.4 8.4 -2 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0300025
774.0 1932 None 74 Human Functional pEC50 = 8.4 8.4 -2 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0300025
CHEMBL90 1932 None 74 Human Functional pEC50 = 8.4 8.4 -2 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0300025
DB05381 1932 None 74 Human Functional pEC50 = 8.4 8.4 -2 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0300025
56954320 82110 None 0 Human Functional pEC50 = 8.4 8.4 10 3
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 472 15 6 4 0.9 N/C(=N\C(=O)CCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1 10.1021/jm201128q
CHEMBL2165641 82110 None 0 Human Functional pEC50 = 8.4 8.4 10 3
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 472 15 6 4 0.9 N/C(=N\C(=O)CCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1 10.1021/jm201128q
46222046 8784 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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)c1cccc(NCCc2c[nH]cn2)c1 10.1021/jm901890s
CHEMBL1096517 8784 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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)c1cccc(NCCc2c[nH]cn2)c1 10.1021/jm901890s
1236 2067 None 16 Human Functional pEC50 = 7.4 7.4 -1 3
Agonist activity at human H3 receptor expressed in HEK293 cells preincubated for 30 mins followed by [35S]-GTPgammaS addition and measured after 30 mins by liquid scintillation counting methodAgonist activity at human H3 receptor expressed in HEK293 cells preincubated for 30 mins followed by [35S]-GTPgammaS addition and measured after 30 mins by liquid scintillation counting method
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1016/j.ejmech.2020.112150
1237 2067 None 16 Human Functional pEC50 = 7.4 7.4 -1 3
Agonist activity at human H3 receptor expressed in HEK293 cells preincubated for 30 mins followed by [35S]-GTPgammaS addition and measured after 30 mins by liquid scintillation counting methodAgonist activity at human H3 receptor expressed in HEK293 cells preincubated for 30 mins followed by [35S]-GTPgammaS addition and measured after 30 mins by liquid scintillation counting method
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1016/j.ejmech.2020.112150
156615 2067 None 16 Human Functional pEC50 = 7.4 7.4 -1 3
Agonist activity at human H3 receptor expressed in HEK293 cells preincubated for 30 mins followed by [35S]-GTPgammaS addition and measured after 30 mins by liquid scintillation counting methodAgonist activity at human H3 receptor expressed in HEK293 cells preincubated for 30 mins followed by [35S]-GTPgammaS addition and measured after 30 mins by liquid scintillation counting method
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1016/j.ejmech.2020.112150
CHEMBL268229 2067 None 16 Human Functional pEC50 = 7.4 7.4 -1 3
Agonist activity at human H3 receptor expressed in HEK293 cells preincubated for 30 mins followed by [35S]-GTPgammaS addition and measured after 30 mins by liquid scintillation counting methodAgonist activity at human H3 receptor expressed in HEK293 cells preincubated for 30 mins followed by [35S]-GTPgammaS addition and measured after 30 mins by liquid scintillation counting method
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1016/j.ejmech.2020.112150
11413171 12114 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 210 9 1 2 2.9 CCCCCCOCCCc1c[nH]cn1 10.1021/jm031065q
CHEMBL1184057 12114 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 210 9 1 2 2.9 CCCCCCOCCCc1c[nH]cn1 10.1021/jm031065q
CHEMBL330688 12114 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 210 9 1 2 2.9 CCCCCCOCCCc1c[nH]cn1 10.1021/jm031065q
16679706 17293 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 409 4 0 4 3.9 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCN(CC(F)(F)F)C2=O)CC1 10.1016/j.bmcl.2010.08.009
CHEMBL1257139 17293 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 409 4 0 4 3.9 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCN(CC(F)(F)F)C2=O)CC1 10.1016/j.bmcl.2010.08.009
49799252 10764 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 241 3 1 2 2.9 c1ccc(N2CCC(Cc3c[nH]cn3)CC2)cc1 10.1016/j.bmc.2010.04.052
CHEMBL1171443 10764 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 241 3 1 2 2.9 c1ccc(N2CCC(Cc3c[nH]cn3)CC2)cc1 10.1016/j.bmc.2010.04.052
10197870 5303 None 0 Human Functional pEC50 = 7.4 7.4 47 2
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
CHEMBL106612 5303 None 0 Human Functional pEC50 = 7.4 7.4 47 2
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
56954427 82113 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 669 29 6 4 6.4 N/C(=N\C(=O)CCCCCCCCCCCCCCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1 10.1021/jm201128q
CHEMBL2165644 82113 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 669 29 6 4 6.4 N/C(=N\C(=O)CCCCCCCCCCCCCCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1 10.1021/jm201128q
16679617 17477 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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
CHEMBL1257729 17477 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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
46929550 16750 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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(c2ccccn2)c2c[nH]cn2)cc1 10.1021/jm100643t
CHEMBL1243334 16750 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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(c2ccccn2)c2c[nH]cn2)cc1 10.1021/jm100643t
16679707 17820 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 0 4 3.0 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCN(C)C2=O)CC1 10.1016/j.bmcl.2010.08.009
CHEMBL1258873 17820 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 0 4 3.0 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCN(C)C2=O)CC1 10.1016/j.bmcl.2010.08.009
11538251 147006 None 0 Rat Functional pEC50 = 8.3 8.3 -4 2
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 385 4 0 5 4.6 Cc1cc2ncc(-c3ccc4cc(CCN5CCC[C@H]5C)ccc4n3)c(C)n2n1 10.1021/jm0705051
CHEMBL392573 147006 None 0 Rat Functional pEC50 = 8.3 8.3 -4 2
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 385 4 0 5 4.6 Cc1cc2ncc(-c3ccc4cc(CCN5CCC[C@H]5C)ccc4n3)c(C)n2n1 10.1021/jm0705051
1249 2009 None 10 Human Functional pEC50 = 8.3 8.3 18 2
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 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1021/jm0504353
13499360 2009 None 10 Human Functional pEC50 = 8.3 8.3 18 2
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 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1021/jm0504353
CHEMBL90019 2009 None 10 Human Functional pEC50 = 8.3 8.3 18 2
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 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1021/jm0504353
1252 2017 None 16 Human Functional pEC50 = 8.3 8.3 - 1
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 153 5 2 2 1.1 NCCCCCc1cnc[nH]1 10.1021/jm0504353
9793868 2017 None 16 Human Functional pEC50 = 8.3 8.3 - 1
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 153 5 2 2 1.1 NCCCCCc1cnc[nH]1 10.1021/jm0504353
CHEMBL417096 2017 None 16 Human Functional pEC50 = 8.3 8.3 - 1
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 153 5 2 2 1.1 NCCCCCc1cnc[nH]1 10.1021/jm0504353
11572015 75056 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 209 9 2 2 2.5 CCCCNCCCCCc1c[nH]cn1 10.1021/jm0504353
CHEMBL203441 75056 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 209 9 2 2 2.5 CCCCNCCCCCc1c[nH]cn1 10.1021/jm0504353
11622495 76605 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 CCCCNCCCCc1c[nH]cn1 10.1021/jm0504353
CHEMBL206303 76605 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 CCCCNCCCCc1c[nH]cn1 10.1021/jm0504353
155565577 176331 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 0.5 CC(C)CNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4579823 176331 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 0.5 CC(C)CNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4594651 176331 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 0.5 CC(C)CNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
59631598 176525 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 165 1 2 5 -0.8 Nc1nccc(N2CC(N)C2)n1 10.1021/acs.jmedchem.9b01462
CHEMBL4459469 176525 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 165 1 2 5 -0.8 Nc1nccc(N2CC(N)C2)n1 10.1021/acs.jmedchem.9b01462
CHEMBL4596157 176525 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 165 1 2 5 -0.8 Nc1nccc(N2CC(N)C2)n1 10.1021/acs.jmedchem.9b01462
1204 1932 None 74 Human Functional pEC50 = 8.3 8.3 -2 11
Agonist activity at human H3R expressed on SK-N-MC cells assessed as inhibition of forskolin-induced beta galactosidase activity preincubated with forskolin for 6 hrs followed compound addition by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on SK-N-MC cells assessed as inhibition of forskolin-induced beta galactosidase activity preincubated with forskolin for 6 hrs followed compound addition by CRE-luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01462
1247 1932 None 74 Human Functional pEC50 = 8.3 8.3 -2 11
Agonist activity at human H3R expressed on SK-N-MC cells assessed as inhibition of forskolin-induced beta galactosidase activity preincubated with forskolin for 6 hrs followed compound addition by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on SK-N-MC cells assessed as inhibition of forskolin-induced beta galactosidase activity preincubated with forskolin for 6 hrs followed compound addition by CRE-luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01462
1375 1932 None 74 Human Functional pEC50 = 8.3 8.3 -2 11
Agonist activity at human H3R expressed on SK-N-MC cells assessed as inhibition of forskolin-induced beta galactosidase activity preincubated with forskolin for 6 hrs followed compound addition by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on SK-N-MC cells assessed as inhibition of forskolin-induced beta galactosidase activity preincubated with forskolin for 6 hrs followed compound addition by CRE-luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01462
774 1932 None 74 Human Functional pEC50 = 8.3 8.3 -2 11
Agonist activity at human H3R expressed on SK-N-MC cells assessed as inhibition of forskolin-induced beta galactosidase activity preincubated with forskolin for 6 hrs followed compound addition by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on SK-N-MC cells assessed as inhibition of forskolin-induced beta galactosidase activity preincubated with forskolin for 6 hrs followed compound addition by CRE-luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01462
774.0 1932 None 74 Human Functional pEC50 = 8.3 8.3 -2 11
Agonist activity at human H3R expressed on SK-N-MC cells assessed as inhibition of forskolin-induced beta galactosidase activity preincubated with forskolin for 6 hrs followed compound addition by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on SK-N-MC cells assessed as inhibition of forskolin-induced beta galactosidase activity preincubated with forskolin for 6 hrs followed compound addition by CRE-luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01462
CHEMBL90 1932 None 74 Human Functional pEC50 = 8.3 8.3 -2 11
Agonist activity at human H3R expressed on SK-N-MC cells assessed as inhibition of forskolin-induced beta galactosidase activity preincubated with forskolin for 6 hrs followed compound addition by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on SK-N-MC cells assessed as inhibition of forskolin-induced beta galactosidase activity preincubated with forskolin for 6 hrs followed compound addition by CRE-luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01462
DB05381 1932 None 74 Human Functional pEC50 = 8.3 8.3 -2 11
Agonist activity at human H3R expressed on SK-N-MC cells assessed as inhibition of forskolin-induced beta galactosidase activity preincubated with forskolin for 6 hrs followed compound addition by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on SK-N-MC cells assessed as inhibition of forskolin-induced beta galactosidase activity preincubated with forskolin for 6 hrs followed compound addition by CRE-luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01462
1204 1932 None 74 Human Functional pEC50 = 8.3 8.3 -2 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1247 1932 None 74 Human Functional pEC50 = 8.3 8.3 -2 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1375 1932 None 74 Human Functional pEC50 = 8.3 8.3 -2 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
774 1932 None 74 Human Functional pEC50 = 8.3 8.3 -2 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
774.0 1932 None 74 Human Functional pEC50 = 8.3 8.3 -2 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL90 1932 None 74 Human Functional pEC50 = 8.3 8.3 -2 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
DB05381 1932 None 74 Human Functional pEC50 = 8.3 8.3 -2 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
11538251 147006 None 0 Rat Functional pEC50 = 8.3 8.3 -4 2
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 385 4 0 5 4.6 Cc1cc2ncc(-c3ccc4cc(CCN5CCC[C@H]5C)ccc4n3)c(C)n2n1 10.1021/jm0705051
CHEMBL392573 147006 None 0 Rat Functional pEC50 = 8.3 8.3 -4 2
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 385 4 0 5 4.6 Cc1cc2ncc(-c3ccc4cc(CCN5CCC[C@H]5C)ccc4n3)c(C)n2n1 10.1021/jm0705051
49857811 70872 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Inverse agonist activity at histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgamma bindingInverse agonist activity at histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgamma binding
ChEMBL 346 8 0 5 2.5 C[C@@H]1CCCN1CCCOc1ccc(C(=O)CN2CCOCC2)cc1 10.1016/j.bmcl.2012.01.004
CHEMBL1951055 70872 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Inverse agonist activity at histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgamma bindingInverse agonist activity at histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgamma binding
ChEMBL 346 8 0 5 2.5 C[C@@H]1CCCN1CCCOc1ccc(C(=O)CN2CCOCC2)cc1 10.1016/j.bmcl.2012.01.004
145974564 163174 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 578 7 1 6 6.0 COc1cc(NC2(c3ccc(Br)cc3)C(=O)N(C(C)(C)C)C(=O)/C2=C/c2ccccc2)cc(OC)c1OC 10.1016/j.ejmech.2018.04.020
CHEMBL4176601 163174 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 578 7 1 6 6.0 COc1cc(NC2(c3ccc(Br)cc3)C(=O)N(C(C)(C)C)C(=O)/C2=C/c2ccccc2)cc(OC)c1OC 10.1016/j.ejmech.2018.04.020
145974564 163174 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 578 7 1 6 6.0 COc1cc(NC2(c3ccc(Br)cc3)C(=O)N(C(C)(C)C)C(=O)/C2=C/c2ccccc2)cc(OC)c1OC 10.1016/j.ejmech.2018.04.020
CHEMBL4176601 163174 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 578 7 1 6 6.0 COc1cc(NC2(c3ccc(Br)cc3)C(=O)N(C(C)(C)C)C(=O)/C2=C/c2ccccc2)cc(OC)c1OC 10.1016/j.ejmech.2018.04.020
16059780 169497 None 0 Rat Functional pEC50 = 8.2 8.2 1 2
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 334 4 0 4 4.0 Cc1nn(C)cc1-c1ccc2cc(CCN3CCC[C@H]3C)ccc2n1 10.1021/jm0705051
CHEMBL442242 169497 None 0 Rat Functional pEC50 = 8.2 8.2 1 2
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 334 4 0 4 4.0 Cc1nn(C)cc1-c1ccc2cc(CCN3CCC[C@H]3C)ccc2n1 10.1021/jm0705051
16059780 169497 None 0 Rat Functional pEC50 = 8.2 8.2 1 2
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 334 4 0 4 4.0 Cc1nn(C)cc1-c1ccc2cc(CCN3CCC[C@H]3C)ccc2n1 10.1021/jm0705051
CHEMBL442242 169497 None 0 Rat Functional pEC50 = 8.2 8.2 1 2
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 334 4 0 4 4.0 Cc1nn(C)cc1-c1ccc2cc(CCN3CCC[C@H]3C)ccc2n1 10.1021/jm0705051
11615601 75046 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 235 6 1 2 3.0 c1nc(CCCCCN2CCCCCC2)c[nH]1 10.1021/jm0504353
CHEMBL203390 75046 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 235 6 1 2 3.0 c1nc(CCCCCN2CCCCCC2)c[nH]1 10.1021/jm0504353
11629931 76338 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 5 1 2 2.6 c1nc(CCCCN2CCCCCC2)c[nH]1 10.1021/jm0504353
CHEMBL205868 76338 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 5 1 2 2.6 c1nc(CCCCN2CCCCCC2)c[nH]1 10.1021/jm0504353
11739735 60552 None 1 Human Functional pEC50 = 7.3 7.3 - 1
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 193 3 1 2 1.7 CN1CCC(CCc2c[nH]cn2)CC1 10.1021/jm049475h
CHEMBL175800 60552 None 1 Human Functional pEC50 = 7.3 7.3 - 1
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 193 3 1 2 1.7 CN1CCC(CCc2c[nH]cn2)CC1 10.1021/jm049475h
11223503 62137 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 245 2 1 2 3.2 C(=C1CCN(C2CCCCC2)CC1)c1c[nH]cn1 10.1021/jm049475h
CHEMBL177612 62137 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 245 2 1 2 3.2 C(=C1CCN(C2CCCCC2)CC1)c1c[nH]cn1 10.1021/jm049475h
16679705 17438 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 385 6 0 5 3.0 COCCN1CCn2c(cc3cc(OC4CCN(C(C)C)CC4)ccc32)C1=O 10.1016/j.bmcl.2010.08.009
CHEMBL1257608 17438 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 385 6 0 5 3.0 COCCN1CCn2c(cc3cc(OC4CCN(C(C)C)CC4)ccc32)C1=O 10.1016/j.bmcl.2010.08.009
46929548 16749 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 343 5 2 3 4.6 CC(C)(C)c1ccc(SCC(c2c[nH]cn2)C2CCNCC2)cc1 10.1021/jm100643t
CHEMBL1243333 16749 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 343 5 2 3 4.6 CC(C)(C)c1ccc(SCC(c2c[nH]cn2)C2CCNCC2)cc1 10.1021/jm100643t
127050431 140402 None 0 Human Functional pEC50 = 6.3 6.3 -3 2
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 140402 None 0 Human Functional pEC50 = 6.3 6.3 -3 2
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
16678725 17437 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 371 5 1 5 2.3 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCN(CCO)C2=O)CC1 10.1016/j.bmcl.2010.08.009
CHEMBL1257607 17437 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 371 5 1 5 2.3 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCN(CCO)C2=O)CC1 10.1016/j.bmcl.2010.08.009
127048828 140407 None 0 Human Functional pEC50 = 6.2 6.2 -38 2
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 288 5 3 3 2.0 CC(C)CN/C(=N/C#N)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3806255 140407 None 0 Human Functional pEC50 = 6.2 6.2 -38 2
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 288 5 3 3 2.0 CC(C)CN/C(=N/C#N)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
145961641 162460 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 746 11 1 8 7.1 COC1=CC2(C=C(OC)C1=O)C(c1ccccc1)=C(c1ccc(C(F)(F)F)cc1)C(=O)N2C(C(=O)NC1CCCCC1)c1ccc(OC)c(OC)c1OC 10.1016/j.ejmech.2018.04.020
CHEMBL4165167 162460 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 746 11 1 8 7.1 COC1=CC2(C=C(OC)C1=O)C(c1ccccc1)=C(c1ccc(C(F)(F)F)cc1)C(=O)N2C(C(=O)NC1CCCCC1)c1ccc(OC)c(OC)c1OC 10.1016/j.ejmech.2018.04.020
145961641 162460 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 746 11 1 8 7.1 COC1=CC2(C=C(OC)C1=O)C(c1ccccc1)=C(c1ccc(C(F)(F)F)cc1)C(=O)N2C(C(=O)NC1CCCCC1)c1ccc(OC)c(OC)c1OC 10.1016/j.ejmech.2018.04.020
CHEMBL4165167 162460 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 746 11 1 8 7.1 COC1=CC2(C=C(OC)C1=O)C(c1ccccc1)=C(c1ccc(C(F)(F)F)cc1)C(=O)N2C(C(=O)NC1CCCCC1)c1ccc(OC)c(OC)c1OC 10.1016/j.ejmech.2018.04.020
145952741 162597 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 162597 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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
1204 1932 None 74 Rat Functional pEC50 = 7.2 7.2 -10 11
Compound was evaluated for antagonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uMCompound was evaluated for antagonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uM
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/S0960-894X(00)80219-X
1247 1932 None 74 Rat Functional pEC50 = 7.2 7.2 -10 11
Compound was evaluated for antagonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uMCompound was evaluated for antagonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uM
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/S0960-894X(00)80219-X
1375 1932 None 74 Rat Functional pEC50 = 7.2 7.2 -10 11
Compound was evaluated for antagonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uMCompound was evaluated for antagonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uM
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/S0960-894X(00)80219-X
774 1932 None 74 Rat Functional pEC50 = 7.2 7.2 -10 11
Compound was evaluated for antagonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uMCompound was evaluated for antagonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uM
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/S0960-894X(00)80219-X
774.0 1932 None 74 Rat Functional pEC50 = 7.2 7.2 -10 11
Compound was evaluated for antagonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uMCompound was evaluated for antagonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uM
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/S0960-894X(00)80219-X
CHEMBL90 1932 None 74 Rat Functional pEC50 = 7.2 7.2 -10 11
Compound was evaluated for antagonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uMCompound was evaluated for antagonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uM
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/S0960-894X(00)80219-X
DB05381 1932 None 74 Rat Functional pEC50 = 7.2 7.2 -10 11
Compound was evaluated for antagonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uMCompound was evaluated for antagonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uM
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/S0960-894X(00)80219-X
155528291 171436 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 1 5 0.4 CCc1cc(N2CC(N(C)C)C2)nc(N)n1 10.1021/acs.jmedchem.9b01462
CHEMBL4461302 171436 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 1 5 0.4 CCc1cc(N2CC(N(C)C)C2)nc(N)n1 10.1021/acs.jmedchem.9b01462
1204 1932 None 74 Human Functional pEC50 = 7.2 7.2 -2 11
Agonist activity at human H3R expressed on HEK293T cells by [35S]GTPgammaS binding assayAgonist activity at human H3R expressed on HEK293T cells by [35S]GTPgammaS binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01462
1247 1932 None 74 Human Functional pEC50 = 7.2 7.2 -2 11
Agonist activity at human H3R expressed on HEK293T cells by [35S]GTPgammaS binding assayAgonist activity at human H3R expressed on HEK293T cells by [35S]GTPgammaS binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01462
1375 1932 None 74 Human Functional pEC50 = 7.2 7.2 -2 11
Agonist activity at human H3R expressed on HEK293T cells by [35S]GTPgammaS binding assayAgonist activity at human H3R expressed on HEK293T cells by [35S]GTPgammaS binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01462
774 1932 None 74 Human Functional pEC50 = 7.2 7.2 -2 11
Agonist activity at human H3R expressed on HEK293T cells by [35S]GTPgammaS binding assayAgonist activity at human H3R expressed on HEK293T cells by [35S]GTPgammaS binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01462
774.0 1932 None 74 Human Functional pEC50 = 7.2 7.2 -2 11
Agonist activity at human H3R expressed on HEK293T cells by [35S]GTPgammaS binding assayAgonist activity at human H3R expressed on HEK293T cells by [35S]GTPgammaS binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01462
CHEMBL90 1932 None 74 Human Functional pEC50 = 7.2 7.2 -2 11
Agonist activity at human H3R expressed on HEK293T cells by [35S]GTPgammaS binding assayAgonist activity at human H3R expressed on HEK293T cells by [35S]GTPgammaS binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01462
DB05381 1932 None 74 Human Functional pEC50 = 7.2 7.2 -2 11
Agonist activity at human H3R expressed on HEK293T cells by [35S]GTPgammaS binding assayAgonist activity at human H3R expressed on HEK293T cells by [35S]GTPgammaS binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01462
11291550 131413 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 205 2 1 2 2.3 CC(C)N1CCC(=Cc2c[nH]cn2)CC1 10.1021/jm049475h
CHEMBL368774 131413 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 205 2 1 2 2.3 CC(C)N1CCC(=Cc2c[nH]cn2)CC1 10.1021/jm049475h
24825520 171358 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 236 2 1 1 2.8 Brc1ccc(Cc2c[nH]cn2)cc1 10.1021/jm7014149
CHEMBL446011 171358 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 236 2 1 1 2.8 Brc1ccc(Cc2c[nH]cn2)cc1 10.1021/jm7014149
1204 1932 None 74 Human Functional pEC50 = 6.2 6.2 -2 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm901890s
1247 1932 None 74 Human Functional pEC50 = 6.2 6.2 -2 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm901890s
1375 1932 None 74 Human Functional pEC50 = 6.2 6.2 -2 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm901890s
774 1932 None 74 Human Functional pEC50 = 6.2 6.2 -2 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm901890s
774.0 1932 None 74 Human Functional pEC50 = 6.2 6.2 -2 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm901890s
CHEMBL90 1932 None 74 Human Functional pEC50 = 6.2 6.2 -2 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm901890s
DB05381 1932 None 74 Human Functional pEC50 = 6.2 6.2 -2 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm901890s
46888007 9030 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 234 5 1 3 2.8 COc1ccc(SCCc2c[nH]cn2)cc1 10.1021/jm901890s
CHEMBL1098527 9030 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 234 5 1 3 2.8 COc1ccc(SCCc2c[nH]cn2)cc1 10.1021/jm901890s
46929552 16759 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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(c2cccnc2)c2c[nH]cn2)cc1 10.1021/jm100643t
CHEMBL1243365 16759 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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(c2cccnc2)c2c[nH]cn2)cc1 10.1021/jm100643t
11710694 96632 None 0 Rat Functional pEC50 = 8.1 8.1 -4 2
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 382 4 0 4 5.2 Cc1nc2ncccc2cc1-c1ccc2cc(CCN3CCC[C@H]3C)ccc2n1 10.1021/jm0705051
CHEMBL263101 96632 None 0 Rat Functional pEC50 = 8.1 8.1 -4 2
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 382 4 0 4 5.2 Cc1nc2ncccc2cc1-c1ccc2cc(CCN3CCC[C@H]3C)ccc2n1 10.1021/jm0705051
11710694 96632 None 0 Rat Functional pEC50 = 8.1 8.1 -4 2
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 382 4 0 4 5.2 Cc1nc2ncccc2cc1-c1ccc2cc(CCN3CCC[C@H]3C)ccc2n1 10.1021/jm0705051
CHEMBL263101 96632 None 0 Rat Functional pEC50 = 8.1 8.1 -4 2
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 382 4 0 4 5.2 Cc1nc2ncccc2cc1-c1ccc2cc(CCN3CCC[C@H]3C)ccc2n1 10.1021/jm0705051
46912442 10908 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 271 4 1 3 2.9 COc1ccc(N2CCC(Cc3c[nH]cn3)CC2)cc1 10.1016/j.bmc.2010.04.052
CHEMBL1172775 10908 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 271 4 1 3 2.9 COc1ccc(N2CCC(Cc3c[nH]cn3)CC2)cc1 10.1016/j.bmc.2010.04.052
11499453 76238 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 209 8 2 2 2.4 CC(C)CNCCCCCc1c[nH]cn1 10.1021/jm0504353
CHEMBL205834 76238 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 209 8 2 2 2.4 CC(C)CNCCCCCc1c[nH]cn1 10.1021/jm0504353
155557369 176573 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 1 5 0.6 CCN(CC)C1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4555457 176573 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 1 5 0.6 CCN(CC)C1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4596532 176573 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 1 5 0.6 CCN(CC)C1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
155544433 176722 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 219 2 1 5 0.3 Nc1nccc(N2CC(N3CCCC3)C2)n1 10.1021/acs.jmedchem.9b01462
CHEMBL4539015 176722 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 219 2 1 5 0.3 Nc1nccc(N2CC(N3CCCC3)C2)n1 10.1021/acs.jmedchem.9b01462
CHEMBL4597818 176722 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 219 2 1 5 0.3 Nc1nccc(N2CC(N3CCCC3)C2)n1 10.1021/acs.jmedchem.9b01462
24825515 187423 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 238 2 1 1 3.4 CC(C)(C)C#Cc1cccc(Cc2c[nH]cn2)c1 10.1021/jm7014149
CHEMBL493014 187423 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 238 2 1 1 3.4 CC(C)(C)C#Cc1cccc(Cc2c[nH]cn2)c1 10.1021/jm7014149
11210869 60785 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 207 3 1 2 2.1 CC(C)N1CCC(Cc2c[nH]cn2)CC1 10.1021/jm049475h
CHEMBL176105 60785 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 207 3 1 2 2.1 CC(C)N1CCC(Cc2c[nH]cn2)CC1 10.1021/jm049475h
11407784 63495 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 269 5 1 2 2.9 c1ccc(CCN2CCC(Cc3c[nH]cn3)CC2)cc1 10.1021/jm049475h
CHEMBL179873 63495 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 269 5 1 2 2.9 c1ccc(CCN2CCC(Cc3c[nH]cn3)CC2)cc1 10.1021/jm049475h
11951972 109491 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 356 6 0 4 4.4 c1cc(C2=NC3(CCCCC3)CO2)ccc1OCCCN1CCCCC1 10.1039/C0MD00056F
CHEMBL3220121 109491 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 356 6 0 4 4.4 c1cc(C2=NC3(CCCCC3)CO2)ccc1OCCCN1CCCCC1 10.1039/C0MD00056F
127040267 137239 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Antagonist activity at human recombinant histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin/(R)(-)-alpha-methylhistamine-induced cAMP accumulation after 1 hr by TR-FRET immunoassayAntagonist activity at human recombinant histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin/(R)(-)-alpha-methylhistamine-induced cAMP accumulation after 1 hr by TR-FRET immunoassay
ChEMBL 295 7 0 2 4.6 CC1CCCN(CCCCCOc2ccc(Cl)cc2)C1 10.1016/j.bmc.2015.11.021
CHEMBL3745760 137239 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Antagonist activity at human recombinant histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin/(R)(-)-alpha-methylhistamine-induced cAMP accumulation after 1 hr by TR-FRET immunoassayAntagonist activity at human recombinant histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin/(R)(-)-alpha-methylhistamine-induced cAMP accumulation after 1 hr by TR-FRET immunoassay
ChEMBL 295 7 0 2 4.6 CC1CCCN(CCCCCOc2ccc(Cl)cc2)C1 10.1016/j.bmc.2015.11.021
CHEMBL3747892 137239 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Antagonist activity at human recombinant histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin/(R)(-)-alpha-methylhistamine-induced cAMP accumulation after 1 hr by TR-FRET immunoassayAntagonist activity at human recombinant histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin/(R)(-)-alpha-methylhistamine-induced cAMP accumulation after 1 hr by TR-FRET immunoassay
ChEMBL 295 7 0 2 4.6 CC1CCCN(CCCCCOc2ccc(Cl)cc2)C1 10.1016/j.bmc.2015.11.021
44478385 5778 None 7 Human Functional pEC50 = 6.1 6.1 -20 2
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 342 9 3 4 2.5 N#C/N=C(/NCCCCc1c[nH]cn1)NCCSc1ccccc1 10.1021/acs.jmedchem.6b00120
CHEMBL1078642 5778 None 7 Human Functional pEC50 = 6.1 6.1 -20 2
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 342 9 3 4 2.5 N#C/N=C(/NCCCCc1c[nH]cn1)NCCSc1ccccc1 10.1021/acs.jmedchem.6b00120
46929648 16766 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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
CHEMBL1243395 16766 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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
16679519 17609 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 O=C1NCCn2c1cc1cc(OCCCN3CCCCC3)ccc12 10.1016/j.bmcl.2010.08.009
CHEMBL1258193 17609 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 O=C1NCCn2c1cc1cc(OCCCN3CCCCC3)ccc12 10.1016/j.bmcl.2010.08.009
127040592 137253 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Antagonist activity at human recombinant histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin/(R)(-)-alpha-methylhistamine-induced cAMP accumulation after 1 hr by TR-FRET immunoassayAntagonist activity at human recombinant histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin/(R)(-)-alpha-methylhistamine-induced cAMP accumulation after 1 hr by TR-FRET immunoassay
ChEMBL 309 9 0 2 5.2 Clc1ccc(OCCCCCCCN2CCCCC2)cc1 10.1016/j.bmc.2015.11.021
CHEMBL3747062 137253 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Antagonist activity at human recombinant histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin/(R)(-)-alpha-methylhistamine-induced cAMP accumulation after 1 hr by TR-FRET immunoassayAntagonist activity at human recombinant histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin/(R)(-)-alpha-methylhistamine-induced cAMP accumulation after 1 hr by TR-FRET immunoassay
ChEMBL 309 9 0 2 5.2 Clc1ccc(OCCCCCCCN2CCCCC2)cc1 10.1016/j.bmc.2015.11.021
CHEMBL3747907 137253 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Antagonist activity at human recombinant histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin/(R)(-)-alpha-methylhistamine-induced cAMP accumulation after 1 hr by TR-FRET immunoassayAntagonist activity at human recombinant histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin/(R)(-)-alpha-methylhistamine-induced cAMP accumulation after 1 hr by TR-FRET immunoassay
ChEMBL 309 9 0 2 5.2 Clc1ccc(OCCCCCCCN2CCCCC2)cc1 10.1016/j.bmc.2015.11.021
10583206 109416 None 0 Human Functional pEC50 = 6.1 6.1 6 2
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
CHEMBL321920 109416 None 0 Human Functional pEC50 = 6.1 6.1 6 2
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
59777245 170834 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 2 2 5 0.3 CC(C)c1cc(N2CC(N)C2)nc(N)n1 10.1021/acs.jmedchem.9b01462
CHEMBL4452204 170834 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 2 2 5 0.3 CC(C)c1cc(N2CC(N)C2)nc(N)n1 10.1021/acs.jmedchem.9b01462
24825526 174514 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 317 5 1 3 3.4 c1ccc(C[C@@H]2COC(c3cccc(Cc4c[nH]cn4)c3)=N2)cc1 10.1021/jm7014149
CHEMBL455266 174514 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 317 5 1 3 3.4 c1ccc(C[C@@H]2COC(c3cccc(Cc4c[nH]cn4)c3)=N2)cc1 10.1021/jm7014149
24825514 186961 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 256 4 1 2 3.6 CC(C)(C)CC(=O)c1cccc(Cc2c[nH]cn2)c1 10.1021/jm7014149
CHEMBL489493 186961 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 256 4 1 2 3.6 CC(C)(C)CC(=O)c1cccc(Cc2c[nH]cn2)c1 10.1021/jm7014149
11189201 63447 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 253 3 1 2 3.1 C(=C1CCN(Cc2ccccc2)CC1)c1c[nH]cn1 10.1021/jm049475h
CHEMBL179747 63447 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 253 3 1 2 3.1 C(=C1CCN(Cc2ccccc2)CC1)c1c[nH]cn1 10.1021/jm049475h
90666844 109493 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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
CHEMBL3220123 109493 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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
10419556 5360 None 0 Human Functional pEC50 = 6.1 6.1 9 2
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
CHEMBL106913 5360 None 0 Human Functional pEC50 = 6.1 6.1 9 2
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
10583206 109416 None 0 Human Functional pEC50 = 6.1 6.1 6 2
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
CHEMBL321920 109416 None 0 Human Functional pEC50 = 6.1 6.1 6 2
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
49799254 10905 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 286 4 1 4 2.8 O=[N+]([O-])c1ccc(N2CCC(Cc3c[nH]cn3)CC2)cc1 10.1016/j.bmc.2010.04.052
CHEMBL1172753 10905 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 286 4 1 4 2.8 O=[N+]([O-])c1ccc(N2CCC(Cc3c[nH]cn3)CC2)cc1 10.1016/j.bmc.2010.04.052
10419556 5360 None 0 Human Functional pEC50 = 6.1 6.1 9 2
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
CHEMBL106913 5360 None 0 Human Functional pEC50 = 6.1 6.1 9 2
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
127052635 140294 None 0 Human Functional pEC50 = 6.1 6.1 -4 2
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 288 5 3 3 2.0 CC(C)CN/C(=N/C#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3805003 140294 None 0 Human Functional pEC50 = 6.1 6.1 -4 2
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 288 5 3 3 2.0 CC(C)CN/C(=N/C#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
1204 1932 None 74 Human Functional pEC50 = 7.1 7.1 -2 11
Agonist activity at human H3 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H3 receptor expressed in 293-EBNA cells by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0603318
1247 1932 None 74 Human Functional pEC50 = 7.1 7.1 -2 11
Agonist activity at human H3 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H3 receptor expressed in 293-EBNA cells by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0603318
1375 1932 None 74 Human Functional pEC50 = 7.1 7.1 -2 11
Agonist activity at human H3 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H3 receptor expressed in 293-EBNA cells by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0603318
774 1932 None 74 Human Functional pEC50 = 7.1 7.1 -2 11
Agonist activity at human H3 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H3 receptor expressed in 293-EBNA cells by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0603318
774.0 1932 None 74 Human Functional pEC50 = 7.1 7.1 -2 11
Agonist activity at human H3 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H3 receptor expressed in 293-EBNA cells by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0603318
CHEMBL90 1932 None 74 Human Functional pEC50 = 7.1 7.1 -2 11
Agonist activity at human H3 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H3 receptor expressed in 293-EBNA cells by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0603318
DB05381 1932 None 74 Human Functional pEC50 = 7.1 7.1 -2 11
Agonist activity at human H3 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H3 receptor expressed in 293-EBNA cells by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0603318
46222043 8782 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 201 4 2 2 2.4 Cc1ccc(NCCc2c[nH]cn2)cc1 10.1021/jm901890s
CHEMBL1096515 8782 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 201 4 2 2 2.4 Cc1ccc(NCCc2c[nH]cn2)cc1 10.1021/jm901890s
11581337 186778 None 0 Mouse Functional pEC50 = 8.0 8.0 -14 3
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 363 6 0 5 3.5 Cn1c(-c2ccc(OCCCN3CCCC3)cc2)nc2ccccc2c1=O 10.1016/j.bmcl.2009.06.025
CHEMBL488248 186778 None 0 Mouse Functional pEC50 = 8.0 8.0 -14 3
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 363 6 0 5 3.5 Cn1c(-c2ccc(OCCCN3CCCC3)cc2)nc2ccccc2c1=O 10.1016/j.bmcl.2009.06.025
CHEMBL557214 186778 None 0 Mouse Functional pEC50 = 8.0 8.0 -14 3
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 363 6 0 5 3.5 Cn1c(-c2ccc(OCCCN3CCCC3)cc2)nc2ccccc2c1=O 10.1016/j.bmcl.2009.06.025
10978141 5152 None 0 Human Functional pEC50 = 7.0 7.0 7 2
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
CHEMBL105803 5152 None 0 Human Functional pEC50 = 7.0 7.0 7 2
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
127050776 140334 None 0 Human Functional pEC50 = 5.0 5.0 -8 3
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
CHEMBL3805437 140334 None 0 Human Functional pEC50 = 5.0 5.0 -8 3
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
145954741 162548 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 438 2 1 3 3.4 O=C1C=C[C@]23C(c4ccccc4)=CC(=O)N2[C@H](c2ccc(C(F)(F)F)cc2)C(=O)N[C@@H]3C1 10.1016/j.ejmech.2018.04.020
CHEMBL4166675 162548 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 438 2 1 3 3.4 O=C1C=C[C@]23C(c4ccccc4)=CC(=O)N2[C@H](c2ccc(C(F)(F)F)cc2)C(=O)N[C@@H]3C1 10.1016/j.ejmech.2018.04.020
145954741 162548 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 438 2 1 3 3.4 O=C1C=C[C@]23C(c4ccccc4)=CC(=O)N2[C@H](c2ccc(C(F)(F)F)cc2)C(=O)N[C@@H]3C1 10.1016/j.ejmech.2018.04.020
CHEMBL4166675 162548 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 438 2 1 3 3.4 O=C1C=C[C@]23C(c4ccccc4)=CC(=O)N2[C@H](c2ccc(C(F)(F)F)cc2)C(=O)N[C@@H]3C1 10.1016/j.ejmech.2018.04.020
16679614 17542 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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
CHEMBL1257964 17542 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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
10945113 109685 None 0 Human Functional pEC50 = 5.0 5.0 1 2
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
CHEMBL322256 109685 None 0 Human Functional pEC50 = 5.0 5.0 1 2
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
10375442 11344 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 196 8 1 2 2.5 CCCCCOCCCc1c[nH]cn1 10.1021/jm031065q
CHEMBL1179604 11344 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 196 8 1 2 2.5 CCCCCOCCCc1c[nH]cn1 10.1021/jm031065q
CHEMBL88746 11344 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 196 8 1 2 2.5 CCCCCOCCCc1c[nH]cn1 10.1021/jm031065q
1267 3804 None 32 Human Functional pEC50 = 7.0 7.0 -6 5
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm900526h
3035905 3804 None 32 Human Functional pEC50 = 7.0 7.0 -6 5
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm900526h
CHEMBL260374 3804 None 32 Human Functional pEC50 = 7.0 7.0 -6 5
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm900526h
11043445 56495 None 0 Human Functional pEC50 = 5.0 5.0 1 2
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
CHEMBL1632410 56495 None 0 Human Functional pEC50 = 5.0 5.0 1 2
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
127051301 140287 None 0 Human Functional pEC50 = 6 6.0 -5 3
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
CHEMBL3804906 140287 None 0 Human Functional pEC50 = 6 6.0 -5 3
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
25229699 90556 None 0 Human Functional pIC50 = 10 10.0 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 384 5 2 4 4.1 CC1CCCN1C1CCN(c2ccc(NC(=O)NCc3cccs3)cc2)C1 10.1016/j.bmcl.2013.03.080
CHEMBL2387288 90556 None 0 Human Functional pIC50 = 10 10.0 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 384 5 2 4 4.1 CC1CCCN1C1CCN(c2ccc(NC(=O)NCc3cccs3)cc2)C1 10.1016/j.bmcl.2013.03.080
25263989 90585 None 0 Human Functional pIC50 = 10 10.0 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 370 4 2 3 4.2 CC1CCCN1C1CCN(c2ccc(NC(=O)NC3CCCCC3)cc2)C1 10.1016/j.bmcl.2013.03.080
CHEMBL2387314 90585 None 0 Human Functional pIC50 = 10 10.0 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 370 4 2 3 4.2 CC1CCCN1C1CCN(c2ccc(NC(=O)NC3CCCCC3)cc2)C1 10.1016/j.bmcl.2013.03.080
11524225 189107 None 0 Human Functional pIC50 = 10 10.0 100000 2
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 403 4 0 5 4.3 Cc1cccc2c(=O)n(C)c(-c3ccc(OC4CCN(C5CCC5)CC4)cc3)nc12 10.1016/j.bmcl.2008.10.034
CHEMBL508712 189107 None 0 Human Functional pIC50 = 10 10.0 100000 2
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 403 4 0 5 4.3 Cc1cccc2c(=O)n(C)c(-c3ccc(OC4CCN(C5CCC5)CC4)cc3)nc12 10.1016/j.bmcl.2008.10.034
45271712 197640 None 0 Human Functional pIC50 = 9.8 9.8 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
ChEMBL 459 7 0 6 4.5 COc1cccc2c1OC(c1ccc(OCCCN3CCC[C@H](C)C3)cc1)C(C)S2(=O)=O 10.1016/j.bmcl.2009.05.101
CHEMBL550517 197640 None 0 Human Functional pIC50 = 9.8 9.8 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
ChEMBL 459 7 0 6 4.5 COc1cccc2c1OC(c1ccc(OCCCN3CCC[C@H](C)C3)cc1)C(C)S2(=O)=O 10.1016/j.bmcl.2009.05.101
45271713 198869 None 0 Human Functional pIC50 = 9.8 9.8 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
ChEMBL 457 5 0 6 4.4 COc1cccc2c1OC(c1ccc(OC3CCN(C4CCC4)CC3)cc1)C(C)S2(=O)=O 10.1016/j.bmcl.2009.05.101
CHEMBL562870 198869 None 0 Human Functional pIC50 = 9.8 9.8 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
ChEMBL 457 5 0 6 4.4 COc1cccc2c1OC(c1ccc(OC3CCN(C4CCC4)CC3)cc1)C(C)S2(=O)=O 10.1016/j.bmcl.2009.05.101
11618702 173948 None 0 Human Functional pIC50 = 9.7 9.7 35481 2
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 423 4 0 5 4.7 Cn1c(-c2ccc(OC3CCN(C4CCC4)CC3)cc2)nc2c(Cl)cccc2c1=O 10.1016/j.bmcl.2008.10.034
CHEMBL453893 173948 None 0 Human Functional pIC50 = 9.7 9.7 35481 2
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 423 4 0 5 4.7 Cn1c(-c2ccc(OC3CCN(C4CCC4)CC3)cc2)nc2c(Cl)cccc2c1=O 10.1016/j.bmcl.2008.10.034
44158811 15729 None 0 Human Functional pIC50 = 9.7 9.7 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 482 7 0 8 3.9 Cc1nccn1-c1ccc(C(c2nnnn2Cc2ccccc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
CHEMBL1222499 15729 None 0 Human Functional pIC50 = 9.7 9.7 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 482 7 0 8 3.9 Cc1nccn1-c1ccc(C(c2nnnn2Cc2ccccc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
25263992 90557 None 0 Human Functional pIC50 = 9.7 9.7 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 398 5 2 4 4.4 Cc1cc(NC(=O)NCc2cccs2)ccc1N1CCC(N2CCCC2C)C1 10.1016/j.bmcl.2013.03.080
CHEMBL2387289 90557 None 0 Human Functional pIC50 = 9.7 9.7 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 398 5 2 4 4.4 Cc1cc(NC(=O)NCc2cccs2)ccc1N1CCC(N2CCCC2C)C1 10.1016/j.bmcl.2013.03.080
71625826 90559 None 0 Human Functional pIC50 = 9.7 9.7 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 446 5 2 3 5.4 CC1CCCN1C1CCN(c2ccc(NC(=O)NCc3cc(Cl)cc(Cl)c3)cc2)C1 10.1016/j.bmcl.2013.03.080
CHEMBL2387290 90559 None 0 Human Functional pIC50 = 9.7 9.7 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 446 5 2 3 5.4 CC1CCCN1C1CCN(c2ccc(NC(=O)NCc3cc(Cl)cc(Cl)c3)cc2)C1 10.1016/j.bmcl.2013.03.080
71625712 90577 None 0 Human Functional pIC50 = 9.7 9.7 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 435 7 2 3 6.2 Cc1c(Cl)cc(NC(=O)Nc2ccc(OCCCN3CCCCC3)cc2)cc1Cl 10.1016/j.bmcl.2013.03.080
CHEMBL2387307 90577 None 0 Human Functional pIC50 = 9.7 9.7 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 435 7 2 3 6.2 Cc1c(Cl)cc(NC(=O)Nc2ccc(OCCCN3CCCCC3)cc2)cc1Cl 10.1016/j.bmcl.2013.03.080
25263991 90586 None 0 Human Functional pIC50 = 9.7 9.7 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 384 4 2 3 4.5 Cc1cc(N2CCC(N3CCCC3C)C2)ccc1NC(=O)NC1CCCCC1 10.1016/j.bmcl.2013.03.080
CHEMBL2387315 90586 None 0 Human Functional pIC50 = 9.7 9.7 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 384 4 2 3 4.5 Cc1cc(N2CCC(N3CCCC3C)C2)ccc1NC(=O)NC1CCCCC1 10.1016/j.bmcl.2013.03.080
25263990 90587 None 0 Human Functional pIC50 = 9.7 9.7 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 384 4 2 3 4.5 Cc1cc(NC(=O)NC2CCCCC2)ccc1N1CCC(N2CCCC2C)C1 10.1016/j.bmcl.2013.03.080
CHEMBL2387316 90587 None 0 Human Functional pIC50 = 9.7 9.7 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 384 4 2 3 4.5 Cc1cc(NC(=O)NC2CCCCC2)ccc1N1CCC(N2CCCC2C)C1 10.1016/j.bmcl.2013.03.080
25264121 90588 None 0 Human Functional pIC50 = 9.7 9.7 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 371 3 1 4 2.5 CC1CCCN1C1CCN(c2ccc(NC(=O)N3CCN(C)CC3)cc2)C1 10.1016/j.bmcl.2013.03.080
CHEMBL2387317 90588 None 0 Human Functional pIC50 = 9.7 9.7 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 371 3 1 4 2.5 CC1CCCN1C1CCN(c2ccc(NC(=O)N3CCN(C)CC3)cc2)C1 10.1016/j.bmcl.2013.03.080
45267459 198551 None 0 Human Functional pIC50 = 9.7 9.7 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
ChEMBL 445 7 0 6 4.2 COc1cccc2c1OC(c1ccc(OCCCN3CCC[C@H]3C)cc1)C(C)S2(=O)=O 10.1016/j.bmcl.2009.05.101
CHEMBL560863 198551 None 0 Human Functional pIC50 = 9.7 9.7 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
ChEMBL 445 7 0 6 4.2 COc1cccc2c1OC(c1ccc(OCCCN3CCC[C@H]3C)cc1)C(C)S2(=O)=O 10.1016/j.bmcl.2009.05.101
11618024 186779 None 0 Human Functional pIC50 = 9.7 9.7 28840 2
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 389 4 0 5 4.0 Cn1c(-c2ccc(OC3CCN(C4CCC4)CC3)cc2)nc2ccccc2c1=O 10.1016/j.bmcl.2008.10.034
CHEMBL488249 186779 None 0 Human Functional pIC50 = 9.7 9.7 28840 2
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 389 4 0 5 4.0 Cn1c(-c2ccc(OC3CCN(C4CCC4)CC3)cc2)nc2ccccc2c1=O 10.1016/j.bmcl.2008.10.034
11502381 174248 None 0 Human Functional pIC50 = 9.6 9.6 17782 2
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 407 4 0 5 4.1 Cn1c(-c2ccc(OC3CCN(C4CCC4)CC3)cc2)nc2c(F)cccc2c1=O 10.1016/j.bmcl.2008.10.034
CHEMBL454642 174248 None 0 Human Functional pIC50 = 9.6 9.6 17782 2
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 407 4 0 5 4.1 Cn1c(-c2ccc(OC3CCN(C4CCC4)CC3)cc2)nc2c(F)cccc2c1=O 10.1016/j.bmcl.2008.10.034
23151367 184735 None 0 Human Functional pIC50 = 9.6 9.6 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 403 4 0 5 4.4 Cc1cccc2nc(C)n(-c3ccc(OC4CCN(C5CCC5)CC4)cc3)c(=O)c12 10.1021/jm800569w
CHEMBL484946 184735 None 0 Human Functional pIC50 = 9.6 9.6 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 403 4 0 5 4.4 Cc1cccc2nc(C)n(-c3ccc(OC4CCN(C5CCC5)CC4)cc3)c(=O)c12 10.1021/jm800569w
49865537 16008 None 0 Human Functional pIC50 = 9.5 9.5 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 521 8 1 7 4.6 O=C(Nc1ccccc1)c1ccc(C(c2nnnn2Cc2ccccc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
CHEMBL1223513 16008 None 0 Human Functional pIC50 = 9.5 9.5 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 521 8 1 7 4.6 O=C(Nc1ccccc1)c1ccc(C(c2nnnn2Cc2ccccc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
25264119 90553 None 0 Human Functional pIC50 = 9.5 9.5 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 356 3 1 3 3.8 CC1CCCN1C1CCN(c2ccc(NC(=O)N3CCCCC3)cc2)C1 10.1016/j.bmcl.2013.03.080
CHEMBL2387285 90553 None 0 Human Functional pIC50 = 9.5 9.5 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 356 3 1 3 3.8 CC1CCCN1C1CCN(c2ccc(NC(=O)N3CCCCC3)cc2)C1 10.1016/j.bmcl.2013.03.080
11502638 173847 None 0 Human Functional pIC50 = 9.5 9.5 19054 2
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 419 5 0 6 4.0 COc1ccc2nc(-c3ccc(OC4CCN(C5CCC5)CC4)cc3)n(C)c(=O)c2c1 10.1016/j.bmcl.2008.10.034
CHEMBL453654 173847 None 0 Human Functional pIC50 = 9.5 9.5 19054 2
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 419 5 0 6 4.0 COc1ccc2nc(-c3ccc(OC4CCN(C5CCC5)CC4)cc3)n(C)c(=O)c2c1 10.1016/j.bmcl.2008.10.034
11641036 186129 None 0 Human Functional pIC50 = 9.5 9.5 23442 2
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 453 8 0 5 5.4 O=c1c2ccccc2nc(-c2ccc(OCCCN3CCCCC3)cc2)n1Cc1ccccc1 10.1016/j.bmcl.2008.10.034
CHEMBL487059 186129 None 0 Human Functional pIC50 = 9.5 9.5 23442 2
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 453 8 0 5 5.4 O=c1c2ccccc2nc(-c2ccc(OCCCN3CCCCC3)cc2)n1Cc1ccccc1 10.1016/j.bmcl.2008.10.034
11539020 188998 None 7 Human Functional pIC50 = 9.5 9.5 - 1
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 420 5 0 7 3.4 COc1nccc2c(=O)n(C)c(-c3ccc(OC4CCN(C5CCC5)CC4)cc3)nc12 10.1016/j.bmcl.2008.10.034
CHEMBL507360 188998 None 7 Human Functional pIC50 = 9.5 9.5 - 1
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 420 5 0 7 3.4 COc1nccc2c(=O)n(C)c(-c3ccc(OC4CCN(C5CCC5)CC4)cc3)nc12 10.1016/j.bmcl.2008.10.034
162644991 179518 None 0 Human Functional pIC50 = 9.5 9.5 - 1
Antagonist activity at human H3 receptor expressed in HEK293 cells centrifuged for 3 mins followed by 60 mins incubation by LANCE Ultra cAMP assayAntagonist activity at human H3 receptor expressed in HEK293 cells centrifuged for 3 mins followed by 60 mins incubation by LANCE Ultra cAMP assay
ChEMBL 234 5 1 4 0.8 C#CCN(C)CCCn1ccc(=O)c(O)c1C 10.1021/acs.jmedchem.0c01480
CHEMBL4740154 179518 None 0 Human Functional pIC50 = 9.5 9.5 - 1
Antagonist activity at human H3 receptor expressed in HEK293 cells centrifuged for 3 mins followed by 60 mins incubation by LANCE Ultra cAMP assayAntagonist activity at human H3 receptor expressed in HEK293 cells centrifuged for 3 mins followed by 60 mins incubation by LANCE Ultra cAMP assay
ChEMBL 234 5 1 4 0.8 C#CCN(C)CCCn1ccc(=O)c(O)c1C 10.1021/acs.jmedchem.0c01480
45268300 198627 None 0 Human Functional pIC50 = 9.5 9.5 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
ChEMBL 431 7 0 6 3.9 COc1ccc2c(c1)OC(c1ccc(OCCCN3CCCC3)cc1)C(C)S2(=O)=O 10.1016/j.bmcl.2009.05.101
CHEMBL561324 198627 None 0 Human Functional pIC50 = 9.5 9.5 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
ChEMBL 431 7 0 6 3.9 COc1ccc2c(c1)OC(c1ccc(OCCCN3CCCC3)cc1)C(C)S2(=O)=O 10.1016/j.bmcl.2009.05.101
11973780 185166 None 3 Human Functional pIC50 = 9.5 9.5 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 457 4 0 5 5.1 Cc1nc2cccc(C(F)(F)F)c2c(=O)n1-c1ccc(OC2CCN(C3CCC3)CC2)cc1 10.1021/jm800569w
CHEMBL485543 185166 None 3 Human Functional pIC50 = 9.5 9.5 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 457 4 0 5 5.1 Cc1nc2cccc(C(F)(F)F)c2c(=O)n1-c1ccc(OC2CCN(C3CCC3)CC2)cc1 10.1021/jm800569w
23151229 175781 None 0 Human Functional pIC50 = 9.5 9.5 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 423 4 0 5 4.7 Cc1nc2cccc(Cl)c2c(=O)n1-c1ccc(OC2CCN(C3CCC3)CC2)cc1 10.1021/jm800569w
CHEMBL458176 175781 None 0 Human Functional pIC50 = 9.5 9.5 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 423 4 0 5 4.7 Cc1nc2cccc(Cl)c2c(=O)n1-c1ccc(OC2CCN(C3CCC3)CC2)cc1 10.1021/jm800569w
45270870 197578 None 0 Human Functional pIC50 = 9.5 9.5 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
ChEMBL 445 7 0 6 4.2 COc1cccc2c1OC(c1ccc(OCCCN3CCCCC3)cc1)C(C)S2(=O)=O 10.1016/j.bmcl.2009.05.101
CHEMBL550050 197578 None 0 Human Functional pIC50 = 9.5 9.5 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
ChEMBL 445 7 0 6 4.2 COc1cccc2c1OC(c1ccc(OCCCN3CCCCC3)cc1)C(C)S2(=O)=O 10.1016/j.bmcl.2009.05.101
11567952 174332 None 0 Human Functional pIC50 = 9.5 9.5 - 1
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 419 5 0 6 4.0 COc1ccc2c(=O)n(C)c(-c3ccc(OC4CCN(C5CCC5)CC4)cc3)nc2c1 10.1016/j.bmcl.2008.10.034
CHEMBL454879 174332 None 0 Human Functional pIC50 = 9.5 9.5 - 1
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 419 5 0 6 4.0 COc1ccc2c(=O)n(C)c(-c3ccc(OC4CCN(C5CCC5)CC4)cc3)nc2c1 10.1016/j.bmcl.2008.10.034
45270044 198849 None 0 Human Functional pIC50 = 9.4 9.4 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
ChEMBL 431 7 0 6 3.9 COc1cccc2c1OC(c1ccc(OCCCN3CCCC3)cc1)C(C)S2(=O)=O 10.1016/j.bmcl.2009.05.101
CHEMBL562722 198849 None 0 Human Functional pIC50 = 9.4 9.4 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
ChEMBL 431 7 0 6 3.9 COc1cccc2c1OC(c1ccc(OCCCN3CCCC3)cc1)C(C)S2(=O)=O 10.1016/j.bmcl.2009.05.101
44159047 15731 None 0 Human Functional pIC50 = 9.4 9.4 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 499 7 0 8 4.8 Cc1nc(-c2ccc(C(c3nnnn3Cc3ccccc3)N3CCCN(C4CCC4)CC3)cc2)cs1 10.1016/j.bmcl.2010.07.009
CHEMBL1222501 15731 None 0 Human Functional pIC50 = 9.4 9.4 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 499 7 0 8 4.8 Cc1nc(-c2ccc(C(c3nnnn3Cc3ccccc3)N3CCCN(C4CCC4)CC3)cc2)cs1 10.1016/j.bmcl.2010.07.009
44158698 15894 None 0 Human Functional pIC50 = 9.4 9.4 1 2
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 514 8 0 8 3.1 CN1CCN(Cc2ccc(C(c3nnnn3Cc3ccccc3)N3CCCN(C4CCC4)CC3)cc2)CC1 10.1016/j.bmcl.2010.07.009
CHEMBL1223158 15894 None 0 Human Functional pIC50 = 9.4 9.4 1 2
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 514 8 0 8 3.1 CN1CCN(Cc2ccc(C(c3nnnn3Cc3ccccc3)N3CCCN(C4CCC4)CC3)cc2)CC1 10.1016/j.bmcl.2010.07.009
25264261 90552 None 0 Human Functional pIC50 = 9.4 9.4 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 433 4 1 4 4.1 CC1CCCN1C1CCN(c2ccc(NC(=O)N3CCN(c4ccccc4)CC3)cc2)C1 10.1016/j.bmcl.2013.03.080
CHEMBL2387284 90552 None 0 Human Functional pIC50 = 9.4 9.4 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 433 4 1 4 4.1 CC1CCCN1C1CCN(c2ccc(NC(=O)N3CCN(c4ccccc4)CC3)cc2)C1 10.1016/j.bmcl.2013.03.080
44158698 15894 None 0 Rat Functional pIC50 = 9.4 9.4 -1 2
Antagonist activity at rat histamine H3 receptorAntagonist activity at rat histamine H3 receptor
ChEMBL 514 8 0 8 3.1 CN1CCN(Cc2ccc(C(c3nnnn3Cc3ccccc3)N3CCCN(C4CCC4)CC3)cc2)CC1 10.1016/j.bmcl.2010.07.009
CHEMBL1223158 15894 None 0 Rat Functional pIC50 = 9.4 9.4 -1 2
Antagonist activity at rat histamine H3 receptorAntagonist activity at rat histamine H3 receptor
ChEMBL 514 8 0 8 3.1 CN1CCN(Cc2ccc(C(c3nnnn3Cc3ccccc3)N3CCCN(C4CCC4)CC3)cc2)CC1 10.1016/j.bmcl.2010.07.009
45268299 199182 None 0 Human Functional pIC50 = 9.4 9.4 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
ChEMBL 431 7 0 6 3.9 COc1ccc2c(c1)S(=O)(=O)C(C)C(c1ccc(OCCCN3CCCC3)cc1)O2 10.1016/j.bmcl.2009.05.101
CHEMBL565007 199182 None 0 Human Functional pIC50 = 9.4 9.4 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
ChEMBL 431 7 0 6 3.9 COc1ccc2c(c1)S(=O)(=O)C(C)C(c1ccc(OCCCN3CCCC3)cc1)O2 10.1016/j.bmcl.2009.05.101
44250288 198508 None 0 Human Functional pIC50 = 9.4 9.4 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
ChEMBL 431 7 0 6 3.9 COc1cccc2c1O[C@@H](c1ccc(OCCCN3CCCC3)cc1)[C@H](C)S2(=O)=O 10.1016/j.bmcl.2009.05.101
CHEMBL560386 198508 None 0 Human Functional pIC50 = 9.4 9.4 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
ChEMBL 431 7 0 6 3.9 COc1cccc2c1O[C@@H](c1ccc(OCCCN3CCCC3)cc1)[C@H](C)S2(=O)=O 10.1016/j.bmcl.2009.05.101
45270863 197328 None 0 Human Functional pIC50 = 9.4 9.4 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
ChEMBL 431 7 0 6 3.9 COc1cccc2c1S(=O)(=O)C(C)C(c1ccc(OCCCN3CCCC3)cc1)O2 10.1016/j.bmcl.2009.05.101
CHEMBL549639 197328 None 0 Human Functional pIC50 = 9.4 9.4 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
ChEMBL 431 7 0 6 3.9 COc1cccc2c1S(=O)(=O)C(C)C(c1ccc(OCCCN3CCCC3)cc1)O2 10.1016/j.bmcl.2009.05.101
162653341 180527 None 0 Human Functional pIC50 = 9.3 9.3 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 368 5 0 5 3.6 COc1cn(-c2ccc(OC3CCN(C4CCCC4)CC3)cc2)ccc1=O 10.1016/j.ejmech.2020.113096
CHEMBL4752329 180527 None 0 Human Functional pIC50 = 9.3 9.3 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 368 5 0 5 3.6 COc1cn(-c2ccc(OC3CCN(C4CCCC4)CC3)cc2)ccc1=O 10.1016/j.ejmech.2020.113096
11502343 186256 None 0 Human Functional pIC50 = 9.3 9.3 3801 2
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 405 8 0 5 4.7 CCCn1c(-c2ccc(OCCCN3CCCCC3)cc2)nc2ccccc2c1=O 10.1016/j.bmcl.2008.10.034
CHEMBL487230 186256 None 0 Human Functional pIC50 = 9.3 9.3 3801 2
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 405 8 0 5 4.7 CCCn1c(-c2ccc(OCCCN3CCCCC3)cc2)nc2ccccc2c1=O 10.1016/j.bmcl.2008.10.034
11517340 173947 None 5 Human Functional pIC50 = 9.3 9.3 - 1
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 419 5 0 6 4.0 COc1cccc2c(=O)n(C)c(-c3ccc(OC4CCN(C5CCC5)CC4)cc3)nc12 10.1016/j.bmcl.2008.10.034
CHEMBL453892 173947 None 5 Human Functional pIC50 = 9.3 9.3 - 1
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 419 5 0 6 4.0 COc1cccc2c(=O)n(C)c(-c3ccc(OC4CCN(C5CCC5)CC4)cc3)nc12 10.1016/j.bmcl.2008.10.034
44159636 15715 None 0 Human Functional pIC50 = 9.3 9.3 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 500 7 0 8 3.1 CN1CCN(c2ccc(C(c3nnnn3Cc3ccccc3)N3CCCN(C4CCC4)CC3)cc2)CC1 10.1016/j.bmcl.2010.07.009
CHEMBL1222434 15715 None 0 Human Functional pIC50 = 9.3 9.3 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 500 7 0 8 3.1 CN1CCN(c2ccc(C(c3nnnn3Cc3ccccc3)N3CCCN(C4CCC4)CC3)cc2)CC1 10.1016/j.bmcl.2010.07.009
25264262 90550 None 0 Human Functional pIC50 = 9.3 9.3 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 399 3 1 4 2.4 CC(=O)N1CCN(C(=O)Nc2ccc(N3CCC(N4CCCC4C)C3)cc2)CC1 10.1016/j.bmcl.2013.03.080
CHEMBL2387282 90550 None 0 Human Functional pIC50 = 9.3 9.3 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 399 3 1 4 2.4 CC(=O)N1CCN(C(=O)Nc2ccc(N3CCC(N4CCCC4C)C3)cc2)CC1 10.1016/j.bmcl.2013.03.080
71625711 90576 None 0 Human Functional pIC50 = 9.3 9.3 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 421 7 2 3 5.9 O=C(Nc1ccc(OCCCN2CCCCC2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2013.03.080
CHEMBL2387306 90576 None 0 Human Functional pIC50 = 9.3 9.3 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 421 7 2 3 5.9 O=C(Nc1ccc(OCCCN2CCCCC2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2013.03.080
73348918 90579 None 0 Human Functional pIC50 = 9.3 9.3 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 389 7 2 3 4.9 O=C(Nc1ccc(OCCCN2CCCCC2)cc1)Nc1ccc(F)cc1F 10.1016/j.bmcl.2013.03.080
CHEMBL2387309 90579 None 0 Human Functional pIC50 = 9.3 9.3 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 389 7 2 3 4.9 O=C(Nc1ccc(OCCCN2CCCCC2)cc1)Nc1ccc(F)cc1F 10.1016/j.bmcl.2013.03.080
141419107 180201 None 0 Human Functional pIC50 = 9.3 9.3 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 328 7 0 5 2.7 COc1cn(-c2ccc(OCCCN3CCCC3)cc2)ccc1=O 10.1016/j.ejmech.2020.113096
CHEMBL4748265 180201 None 0 Human Functional pIC50 = 9.3 9.3 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 328 7 0 5 2.7 COc1cn(-c2ccc(OCCCN3CCCC3)cc2)ccc1=O 10.1016/j.ejmech.2020.113096
25099115 189600 None 0 Human Functional pIC50 = 9.3 9.3 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 400 5 0 5 3.2 COc1ccc2c(c1)C(=O)O[C@]21CC[C@H](C(=O)N(C)CCN2CCCCC2)CC1 10.1016/j.bmcl.2008.07.125
CHEMBL513893 189600 None 0 Human Functional pIC50 = 9.3 9.3 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 400 5 0 5 3.2 COc1ccc2c(c1)C(=O)O[C@]21CC[C@H](C(=O)N(C)CCN2CCCCC2)CC1 10.1016/j.bmcl.2008.07.125
11517341 173843 None 0 Human Functional pIC50 = 9.3 9.3 7762 2
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 419 5 0 6 4.0 COc1cccc2nc(-c3ccc(OC4CCN(C5CCC5)CC4)cc3)n(C)c(=O)c12 10.1016/j.bmcl.2008.10.034
CHEMBL453653 173843 None 0 Human Functional pIC50 = 9.3 9.3 7762 2
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 419 5 0 6 4.0 COc1cccc2nc(-c3ccc(OC4CCN(C5CCC5)CC4)cc3)n(C)c(=O)c12 10.1016/j.bmcl.2008.10.034
10736 1876 None 46 Human Functional pIC50 = 9.3 9.3 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 351 4 1 4 3.2 CNC(=O)c1ccc(nc1)Oc1ccc2c(c1)CCN(CC2)C1CCC1 10.1021/jm800569w
9798547 1876 None 46 Human Functional pIC50 = 9.3 9.3 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 351 4 1 4 3.2 CNC(=O)c1ccc(nc1)Oc1ccc2c(c1)CCN(CC2)C1CCC1 10.1021/jm800569w
CHEMBL517140 1876 None 46 Human Functional pIC50 = 9.3 9.3 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 351 4 1 4 3.2 CNC(=O)c1ccc(nc1)Oc1ccc2c(c1)CCN(CC2)C1CCC1 10.1021/jm800569w
23151209 184330 None 0 Human Functional pIC50 = 9.3 9.3 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 407 4 0 5 4.2 Cc1nc2cccc(F)c2c(=O)n1-c1ccc(OC2CCN(C3CCC3)CC2)cc1 10.1021/jm800569w
CHEMBL483400 184330 None 0 Human Functional pIC50 = 9.3 9.3 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 407 4 0 5 4.2 Cc1nc2cccc(F)c2c(=O)n1-c1ccc(OC2CCN(C3CCC3)CC2)cc1 10.1021/jm800569w
44159523 15714 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 501 8 0 8 3.2 c1ccc(Cn2nnnc2C(c2ccc(CN3CCOCC3)cc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
CHEMBL1222433 15714 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 501 8 0 8 3.2 c1ccc(Cn2nnnc2C(c2ccc(CN3CCOCC3)cc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
71625828 90562 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 470 6 2 4 6.5 Cc1cc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)ccc1N1CCC(N2CCCC2C)C1 10.1016/j.bmcl.2013.03.080
CHEMBL2387293 90562 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 470 6 2 4 6.5 Cc1cc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)ccc1N1CCC(N2CCCC2C)C1 10.1016/j.bmcl.2013.03.080
3002005 90581 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 415 11 2 4 5.3 CCN(CC)CCOc1ccc(NC(=S)Nc2ccc(OCC(C)C)cc2)cc1 10.1016/j.bmcl.2013.03.080
CHEMBL2387310 90581 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 415 11 2 4 5.3 CCN(CC)CCOc1ccc(NC(=S)Nc2ccc(OCC(C)C)cc2)cc1 10.1016/j.bmcl.2013.03.080
45272583 198276 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
ChEMBL 401 6 0 5 3.8 C[C@@H]1[C@@H](c2ccc(OCCCN3CCCC3)cc2)Oc2ccccc2S1(=O)=O 10.1016/j.bmcl.2009.05.101
CHEMBL558248 198276 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
ChEMBL 401 6 0 5 3.8 C[C@@H]1[C@@H](c2ccc(OCCCN3CCCC3)cc2)Oc2ccccc2S1(=O)=O 10.1016/j.bmcl.2009.05.101
45268315 198781 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
ChEMBL 401 6 0 5 3.8 CC1C(c2ccc(OCCCN3CCCC3)cc2)Oc2ccccc2S1(=O)=O 10.1016/j.bmcl.2009.05.101
CHEMBL562326 198781 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
ChEMBL 401 6 0 5 3.8 CC1C(c2ccc(OCCCN3CCCC3)cc2)Oc2ccccc2S1(=O)=O 10.1016/j.bmcl.2009.05.101
45273485 198230 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
ChEMBL 431 7 0 6 3.9 COc1cccc2c1O[C@H](c1ccc(OCCCN3CCCC3)cc1)[C@@H](C)S2(=O)=O 10.1016/j.bmcl.2009.05.101
CHEMBL557718 198230 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
ChEMBL 431 7 0 6 3.9 COc1cccc2c1O[C@H](c1ccc(OCCCN3CCCC3)cc1)[C@@H](C)S2(=O)=O 10.1016/j.bmcl.2009.05.101
1218 229 None 35 Human Functional pIC50 = 9.2 9.2 19 2
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 330 4 0 3 5.0 N#Cc1ccc(cc1)c1ccc2c(c1)cc(o2)CCN1CCC[C@H]1C 10.1021/jm800569w
9818903 229 None 35 Human Functional pIC50 = 9.2 9.2 19 2
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 330 4 0 3 5.0 N#Cc1ccc(cc1)c1ccc2c(c1)cc(o2)CCN1CCC[C@H]1C 10.1021/jm800569w
CHEMBL351231 229 None 35 Human Functional pIC50 = 9.2 9.2 19 2
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 330 4 0 3 5.0 N#Cc1ccc(cc1)c1ccc2c(c1)cc(o2)CCN1CCC[C@H]1C 10.1021/jm800569w
10473209 62694 None 3 Human Functional pIC50 = 9.2 9.2 - 1
Inverse agonist activity at human histamine H3 receptor by GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor by GTPgammaS binding assay
ChEMBL 352 4 1 5 2.6 CNC(=O)c1cnc(Oc2ccc3c(c2)CCN(C2CCC2)CC3)cn1 10.1021/jm100064d
CHEMBL1783890 62694 None 3 Human Functional pIC50 = 9.2 9.2 - 1
Inverse agonist activity at human histamine H3 receptor by GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor by GTPgammaS binding assay
ChEMBL 352 4 1 5 2.6 CNC(=O)c1cnc(Oc2ccc3c(c2)CCN(C2CCC2)CC3)cn1 10.1021/jm100064d
24948946 183018 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 425 7 0 5 4.9 O=c1c2ccccc2nc(-c2ccccc2)n1-c1ccc(OCCCN2CCCC2)cc1 10.1021/jm8003834
CHEMBL479241 183018 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 425 7 0 5 4.9 O=c1c2ccccc2nc(-c2ccccc2)n1-c1ccc(OCCCN2CCCC2)cc1 10.1021/jm8003834
78324475 119162 None 0 Human Functional pIC50 = 9.2 9.2 - 1
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
ChEMBL 381 9 0 4 4.5 CCOC(=O)COCc1ccc(-c2ccc(CCN3CCC[C@H]3C)cc2)cc1 nan
CHEMBL3427228 119162 None 0 Human Functional pIC50 = 9.2 9.2 - 1
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
ChEMBL 381 9 0 4 4.5 CCOC(=O)COCc1ccc(-c2ccc(CCN3CCC[C@H]3C)cc2)cc1 nan
78324475 119162 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
ChEMBL 381 9 0 4 4.5 CCOC(=O)COCc1ccc(-c2ccc(CCN3CCC[C@H]3C)cc2)cc1 10.1021/acsmedchemlett.5b00002
CHEMBL3427228 119162 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
ChEMBL 381 9 0 4 4.5 CCOC(=O)COCc1ccc(-c2ccc(CCN3CCC[C@H]3C)cc2)cc1 10.1021/acsmedchemlett.5b00002
11581337 186778 None 0 Human Functional pIC50 = 9.2 9.2 14 3
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 363 6 0 5 3.5 Cn1c(-c2ccc(OCCCN3CCCC3)cc2)nc2ccccc2c1=O 10.1016/j.bmcl.2008.10.034
CHEMBL488248 186778 None 0 Human Functional pIC50 = 9.2 9.2 14 3
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 363 6 0 5 3.5 Cn1c(-c2ccc(OCCCN3CCCC3)cc2)nc2ccccc2c1=O 10.1016/j.bmcl.2008.10.034
CHEMBL557214 186778 None 0 Human Functional pIC50 = 9.2 9.2 14 3
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 363 6 0 5 3.5 Cn1c(-c2ccc(OCCCN3CCCC3)cc2)nc2ccccc2c1=O 10.1016/j.bmcl.2008.10.034
24951351 189746 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 391 8 0 5 4.2 CCCc1nc2ccccc2c(=O)n1-c1ccc(OCCCN2CCCC2)cc1 10.1021/jm8003834
CHEMBL515004 189746 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 391 8 0 5 4.2 CCCc1nc2ccccc2c(=O)n1-c1ccc(OCCCN2CCCC2)cc1 10.1021/jm8003834
44160131 15743 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 482 8 0 8 3.6 c1ccc(Cn2nnnc2C(c2ccc(Cn3cccn3)cc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
CHEMBL1222593 15743 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 482 8 0 8 3.6 c1ccc(Cn2nnnc2C(c2ccc(Cn3cccn3)cc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
71625710 90575 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 387 7 2 3 5.2 O=C(Nc1ccc(Cl)cc1)Nc1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2013.03.080
CHEMBL2387305 90575 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 387 7 2 3 5.2 O=C(Nc1ccc(Cl)cc1)Nc1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2013.03.080
24900259 69626 None 5 Human Functional pIC50 = 9.2 9.2 - 1
Inverse agonist activity at human cloned histamine H3 receptor by [35S]GTPgammaS binding assayInverse agonist activity at human cloned histamine H3 receptor by [35S]GTPgammaS binding assay
ChEMBL 401 9 0 4 4.2 COCCCS(=O)(=O)c1ccc(-c2ccc(CCN3CCC[C@H]3C)cc2)cc1 10.1016/j.bmcl.2011.11.075
CHEMBL1934523 69626 None 5 Human Functional pIC50 = 9.2 9.2 - 1
Inverse agonist activity at human cloned histamine H3 receptor by [35S]GTPgammaS binding assayInverse agonist activity at human cloned histamine H3 receptor by [35S]GTPgammaS binding assay
ChEMBL 401 9 0 4 4.2 COCCCS(=O)(=O)c1ccc(-c2ccc(CCN3CCC[C@H]3C)cc2)cc1 10.1016/j.bmcl.2011.11.075
44563137 173949 None 0 Human Functional pIC50 = 9.2 9.2 - 1
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 457 4 0 5 5.0 Cn1c(-c2ccc(OC3CCN(C4CCC4)CC3)cc2)nc2c(C(F)(F)F)cccc2c1=O 10.1016/j.bmcl.2008.10.034
CHEMBL453894 173949 None 0 Human Functional pIC50 = 9.2 9.2 - 1
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 457 4 0 5 5.0 Cn1c(-c2ccc(OC3CCN(C4CCC4)CC3)cc2)nc2c(C(F)(F)F)cccc2c1=O 10.1016/j.bmcl.2008.10.034
11632103 189645 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 370 4 0 4 3.2 CN(CCN1CCCCC1)C(=O)[C@H]1CC[C@@]2(CC1)OC(=O)c1ccccc12 10.1016/j.bmcl.2008.07.125
CHEMBL514217 189645 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 370 4 0 4 3.2 CN(CCN1CCCCC1)C(=O)[C@H]1CC[C@@]2(CC1)OC(=O)c1ccccc12 10.1016/j.bmcl.2008.07.125
24951038 182387 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 391 6 0 5 4.2 Cc1nc2ccccc2c(=O)n1-c1ccc(OCCCN2CCC[C@H](C)C2)cc1 10.1021/jm8003834
CHEMBL478395 182387 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 391 6 0 5 4.2 Cc1nc2ccccc2c(=O)n1-c1ccc(OCCCN2CCC[C@H](C)C2)cc1 10.1021/jm8003834
162660913 181527 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 354 5 0 5 3.2 COc1cn(-c2ccc(OC3CCN(C4CCC4)CC3)cc2)ccc1=O 10.1016/j.ejmech.2020.113096
CHEMBL4763867 181527 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 354 5 0 5 3.2 COc1cn(-c2ccc(OC3CCN(C4CCC4)CC3)cc2)ccc1=O 10.1016/j.ejmech.2020.113096
11567596 174686 None 0 Human Functional pIC50 = 9.1 9.1 8317 2
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 403 4 0 5 4.4 Cn1c(-c2ccc(OC3CCN(C4CCCC4)CC3)cc2)nc2ccccc2c1=O 10.1016/j.bmcl.2008.10.034
CHEMBL455681 174686 None 0 Human Functional pIC50 = 9.1 9.1 8317 2
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 403 4 0 5 4.4 Cn1c(-c2ccc(OC3CCN(C4CCCC4)CC3)cc2)nc2ccccc2c1=O 10.1016/j.bmcl.2008.10.034
78321037 119176 None 0 Human Functional pIC50 = 9.1 9.1 - 1
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
ChEMBL 347 6 1 4 3.5 C[C@@H]1CCCN1CCc1ccc(-c2ccc(Cc3nnn[nH]3)cc2)cc1 nan
CHEMBL3427242 119176 None 0 Human Functional pIC50 = 9.1 9.1 - 1
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
ChEMBL 347 6 1 4 3.5 C[C@@H]1CCCN1CCc1ccc(-c2ccc(Cc3nnn[nH]3)cc2)cc1 nan
78321037 119176 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
ChEMBL 347 6 1 4 3.5 C[C@@H]1CCCN1CCc1ccc(-c2ccc(Cc3nnn[nH]3)cc2)cc1 10.1021/acsmedchemlett.5b00002
CHEMBL3427242 119176 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
ChEMBL 347 6 1 4 3.5 C[C@@H]1CCCN1CCc1ccc(-c2ccc(Cc3nnn[nH]3)cc2)cc1 10.1021/acsmedchemlett.5b00002
78320394 160655 None 0 Human Functional pIC50 = 9.1 9.1 - 1
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
ChEMBL 408 9 2 3 3.9 C[C@H](NC(=O)CCc1ccc(-c2ccc(CCN3CCC[C@H]3C)cc2)cc1)C(=O)O nan
CHEMBL4112593 160655 None 0 Human Functional pIC50 = 9.1 9.1 - 1
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
ChEMBL 408 9 2 3 3.9 C[C@H](NC(=O)CCc1ccc(-c2ccc(CCN3CCC[C@H]3C)cc2)cc1)C(=O)O nan
1223 953 None 33 Human Functional pIC50 = 9.1 9.1 1 4
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1016/j.bmcl.2013.09.052
2790 953 None 33 Human Functional pIC50 = 9.1 9.1 1 4
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1016/j.bmcl.2013.09.052
CHEMBL14690 953 None 33 Human Functional pIC50 = 9.1 9.1 1 4
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1016/j.bmcl.2013.09.052
25264122 90589 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 385 3 1 4 2.8 Cc1cc(N2CCC(N3CCCC3C)C2)ccc1NC(=O)N1CCN(C)CC1 10.1016/j.bmcl.2013.03.080
CHEMBL2387318 90589 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 385 3 1 4 2.8 Cc1cc(N2CCC(N3CCCC3C)C2)ccc1NC(=O)N1CCN(C)CC1 10.1016/j.bmcl.2013.03.080
76329181 105921 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 389 3 0 4 2.7 O=C(C1CC2(CCN(C3CCOCC3)CC2)C1)N1CCCN(C2CCC2)CC1 10.1021/jm4014828
CHEMBL3127674 105921 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 389 3 0 4 2.7 O=C(C1CC2(CCN(C3CCOCC3)CC2)C1)N1CCCN(C2CCC2)CC1 10.1021/jm4014828
24948945 182885 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 391 7 0 5 4.4 CC(C)c1nc2ccccc2c(=O)n1-c1ccc(OCCCN2CCCC2)cc1 10.1021/jm8003834
CHEMBL479036 182885 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 391 7 0 5 4.4 CC(C)c1nc2ccccc2c(=O)n1-c1ccc(OCCCN2CCCC2)cc1 10.1021/jm8003834
45272592 199009 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
ChEMBL 445 7 0 6 4.2 COc1cccc2c1OC(c1ccc(OCCCN3CCC[C@@H]3C)cc1)C(C)S2(=O)=O 10.1016/j.bmcl.2009.05.101
CHEMBL563779 199009 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
ChEMBL 445 7 0 6 4.2 COc1cccc2c1OC(c1ccc(OCCCN3CCC[C@@H]3C)cc1)C(C)S2(=O)=O 10.1016/j.bmcl.2009.05.101
23151210 178077 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 407 4 0 5 4.2 Cc1nc2c(F)cccc2c(=O)n1-c1ccc(OC2CCN(C3CCC3)CC2)cc1 10.1021/jm800569w
CHEMBL464599 178077 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 407 4 0 5 4.2 Cc1nc2c(F)cccc2c(=O)n1-c1ccc(OC2CCN(C3CCC3)CC2)cc1 10.1021/jm800569w
45270862 198072 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
ChEMBL 399 6 0 5 4.1 CC1=C(c2ccc(OCCCN3CCCC3)cc2)Oc2ccccc2S1(=O)=O 10.1016/j.bmcl.2009.05.101
CHEMBL556100 198072 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
ChEMBL 399 6 0 5 4.1 CC1=C(c2ccc(OCCCN3CCCC3)cc2)Oc2ccccc2S1(=O)=O 10.1016/j.bmcl.2009.05.101
11668594 186780 None 0 Human Functional pIC50 = 9.1 9.1 1258 2
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 405 7 0 5 4.9 CC(C)n1c(-c2ccc(OCCCN3CCCCC3)cc2)nc2ccccc2c1=O 10.1016/j.bmcl.2008.10.034
CHEMBL488251 186780 None 0 Human Functional pIC50 = 9.1 9.1 1258 2
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 405 7 0 5 4.9 CC(C)n1c(-c2ccc(OCCCN3CCCCC3)cc2)nc2ccccc2c1=O 10.1016/j.bmcl.2008.10.034
11689687 191388 None 0 Human Functional pIC50 = 9.1 9.1 1479 2
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 391 7 0 5 4.3 CCn1c(-c2ccc(OCCCN3CCCCC3)cc2)nc2ccccc2c1=O 10.1016/j.bmcl.2008.10.034
CHEMBL519067 191388 None 0 Human Functional pIC50 = 9.1 9.1 1479 2
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 391 7 0 5 4.3 CCn1c(-c2ccc(OCCCN3CCCCC3)cc2)nc2ccccc2c1=O 10.1016/j.bmcl.2008.10.034
44158699 15745 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 495 8 0 8 4.6 c1ccc(Cn2nnnc2C(c2ccc(Oc3ccccn3)cc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
CHEMBL1222595 15745 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 495 8 0 8 4.6 c1ccc(Cn2nnnc2C(c2ccc(Oc3ccccn3)cc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
25263865 90583 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 446 4 2 3 6.0 Cc1cc(N2CCC(N3CCCC3C)C2)ccc1NC(=O)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2013.03.080
CHEMBL2387312 90583 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 446 4 2 3 6.0 Cc1cc(N2CCC(N3CCCC3C)C2)ccc1NC(=O)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2013.03.080
23151246 189958 None 0 Human Functional pIC50 = 9.0 9.0 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 425 4 0 5 4.4 Cc1nc2cc(F)c(F)cc2c(=O)n1-c1ccc(OC2CCN(C3CCC3)CC2)cc1 10.1021/jm800569w
CHEMBL516697 189958 None 0 Human Functional pIC50 = 9.0 9.0 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 425 4 0 5 4.4 Cc1nc2cc(F)c(F)cc2c(=O)n1-c1ccc(OC2CCN(C3CCC3)CC2)cc1 10.1021/jm800569w
78324785 119164 None 0 Human Functional pIC50 = 9.0 9.0 - 1
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
ChEMBL 361 7 0 5 3.6 C[C@@H]1CCCN1CCc1ccc(-c2ccc(CCn3cnnn3)cc2)cc1 nan
CHEMBL3427230 119164 None 0 Human Functional pIC50 = 9.0 9.0 - 1
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
ChEMBL 361 7 0 5 3.6 C[C@@H]1CCCN1CCc1ccc(-c2ccc(CCn3cnnn3)cc2)cc1 nan
78324785 119164 None 0 Human Functional pIC50 = 9.0 9.0 - 1
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
ChEMBL 361 7 0 5 3.6 C[C@@H]1CCCN1CCc1ccc(-c2ccc(CCn3cnnn3)cc2)cc1 10.1021/acsmedchemlett.5b00002
CHEMBL3427230 119164 None 0 Human Functional pIC50 = 9.0 9.0 - 1
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
ChEMBL 361 7 0 5 3.6 C[C@@H]1CCCN1CCc1ccc(-c2ccc(CCn3cnnn3)cc2)cc1 10.1021/acsmedchemlett.5b00002
78324790 160447 None 0 Human Functional pIC50 = 9.0 9.0 - 1
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
ChEMBL 478 9 1 4 5.6 C[C@@H]1CCCN1CCc1ccc(-c2ccc(CCC(=O)NC(C)(C)C(=O)OC(C)(C)C)cc2)cc1 nan
CHEMBL4110820 160447 None 0 Human Functional pIC50 = 9.0 9.0 - 1
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
ChEMBL 478 9 1 4 5.6 C[C@@H]1CCCN1CCc1ccc(-c2ccc(CCC(=O)NC(C)(C)C(=O)OC(C)(C)C)cc2)cc1 nan
118737697 119169 None 0 Human Functional pIC50 = 9.0 9.0 - 1
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
ChEMBL 478 9 1 4 5.4 C[C@@H]1CCCN1CCc1ccc(-c2ccc(CCNC(=O)C(C)(C)C(=O)OC(C)(C)C)cc2)cc1 10.1021/acsmedchemlett.5b00002
CHEMBL3427235 119169 None 0 Human Functional pIC50 = 9.0 9.0 - 1
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
ChEMBL 478 9 1 4 5.4 C[C@@H]1CCCN1CCc1ccc(-c2ccc(CCNC(=O)C(C)(C)C(=O)OC(C)(C)C)cc2)cc1 10.1021/acsmedchemlett.5b00002
78321036 160440 None 0 Human Functional pIC50 = 9.0 9.0 - 1
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
ChEMBL 476 9 0 4 5.1 CCOC(=O)C1CCN(C(=O)CCc2ccc(-c3ccc(CCN4CCC[C@H]4C)cc3)cc2)CC1 nan
CHEMBL4110757 160440 None 0 Human Functional pIC50 = 9.0 9.0 - 1
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
ChEMBL 476 9 0 4 5.1 CCOC(=O)C1CCN(C(=O)CCc2ccc(-c3ccc(CCN4CCC[C@H]4C)cc3)cc2)CC1 nan
24951349 181725 None 0 Human Functional pIC50 = 9.0 9.0 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 431 6 0 5 4.6 Cc1nc2cc(C(F)(F)F)ccc2c(=O)n1-c1ccc(OCCCN2CCCC2)cc1 10.1021/jm8003834
CHEMBL477364 181725 None 0 Human Functional pIC50 = 9.0 9.0 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 431 6 0 5 4.6 Cc1nc2cc(C(F)(F)F)ccc2c(=O)n1-c1ccc(OCCCN2CCCC2)cc1 10.1021/jm8003834
78321360 119179 None 0 Human Functional pIC50 = 9.0 9.0 - 1
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
ChEMBL 351 8 1 2 4.8 C[C@@H]1CCCN1CCc1ccc(-c2ccc(CCCC(=O)O)cc2)cc1 nan
CHEMBL3427245 119179 None 0 Human Functional pIC50 = 9.0 9.0 - 1
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
ChEMBL 351 8 1 2 4.8 C[C@@H]1CCCN1CCc1ccc(-c2ccc(CCCC(=O)O)cc2)cc1 nan
78321360 119179 None 0 Human Functional pIC50 = 9.0 9.0 - 1
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
ChEMBL 351 8 1 2 4.8 C[C@@H]1CCCN1CCc1ccc(-c2ccc(CCCC(=O)O)cc2)cc1 10.1021/acsmedchemlett.5b00002
CHEMBL3427245 119179 None 0 Human Functional pIC50 = 9.0 9.0 - 1
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
ChEMBL 351 8 1 2 4.8 C[C@@H]1CCCN1CCc1ccc(-c2ccc(CCCC(=O)O)cc2)cc1 10.1021/acsmedchemlett.5b00002
11667985 183019 None 0 Human Functional pIC50 = 9.0 9.0 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 377 6 0 5 3.9 Cc1cccc2nc(C)n(-c3ccc(OCCCN4CCCC4)cc3)c(=O)c12 10.1021/jm8003834
CHEMBL479242 183019 None 0 Human Functional pIC50 = 9.0 9.0 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 377 6 0 5 3.9 Cc1cccc2nc(C)n(-c3ccc(OCCCN4CCCC4)cc3)c(=O)c12 10.1021/jm8003834
78321673 160533 None 0 Human Functional pIC50 = 9 9.0 - 1
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
ChEMBL 408 9 1 4 3.6 COC(=O)CNC(=O)CCc1ccc(-c2ccc(CCN3CCC[C@H]3C)cc2)cc1 nan
CHEMBL4111575 160533 None 0 Human Functional pIC50 = 9 9.0 - 1
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
ChEMBL 408 9 1 4 3.6 COC(=O)CNC(=O)CCc1ccc(-c2ccc(CCN3CCC[C@H]3C)cc2)cc1 nan
118737700 119172 None 0 Human Functional pIC50 = 9 9.0 - 1
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
ChEMBL 408 9 1 4 3.6 COC(=O)CC(=O)NCCc1ccc(-c2ccc(CCN3CCC[C@H]3C)cc2)cc1 10.1021/acsmedchemlett.5b00002
CHEMBL3427238 119172 None 0 Human Functional pIC50 = 9 9.0 - 1
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
ChEMBL 408 9 1 4 3.6 COC(=O)CC(=O)NCCc1ccc(-c2ccc(CCN3CCC[C@H]3C)cc2)cc1 10.1021/acsmedchemlett.5b00002
1223 953 None 33 Human Functional pIC50 = 9 9.0 1 4
Antagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1016/j.bmcl.2010.08.099
2790 953 None 33 Human Functional pIC50 = 9 9.0 1 4
Antagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1016/j.bmcl.2010.08.099
CHEMBL14690 953 None 33 Human Functional pIC50 = 9 9.0 1 4
Antagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1016/j.bmcl.2010.08.099
1223 953 None 33 Mouse Functional pIC50 = 9 9.0 -1 4
Antagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1016/j.bmcl.2010.08.099
2790 953 None 33 Mouse Functional pIC50 = 9 9.0 -1 4
Antagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1016/j.bmcl.2010.08.099
CHEMBL14690 953 None 33 Mouse Functional pIC50 = 9 9.0 -1 4
Antagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1016/j.bmcl.2010.08.099
71625599 90573 None 0 Human Functional pIC50 = 9 9.0 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 395 8 2 3 5.4 CCN(CC)CCOc1ccc(NC(=O)Nc2c(Cl)cccc2Cl)cc1 10.1016/j.bmcl.2013.03.080
CHEMBL2387303 90573 None 0 Human Functional pIC50 = 9 9.0 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 395 8 2 3 5.4 CCN(CC)CCOc1ccc(NC(=O)Nc2c(Cl)cccc2Cl)cc1 10.1016/j.bmcl.2013.03.080
25264118 90554 None 0 Human Functional pIC50 = 9.0 9.0 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 413 4 1 4 2.8 CC(=O)N(C)C1CCN(C(=O)Nc2ccc(N3CCC(N4CCCC4C)C3)cc2)C1 10.1016/j.bmcl.2013.03.080
CHEMBL2387286 90554 None 0 Human Functional pIC50 = 9.0 9.0 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 413 4 1 4 2.8 CC(=O)N(C)C1CCN(C(=O)Nc2ccc(N3CCC(N4CCCC4C)C3)cc2)C1 10.1016/j.bmcl.2013.03.080
25264117 90555 None 0 Human Functional pIC50 = 9.0 9.0 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 427 4 1 4 3.1 CC(=O)N(C)C1CCN(C(=O)Nc2ccc(N3CCC(N4CCCC4C)C3)c(C)c2)C1 10.1016/j.bmcl.2013.03.080
CHEMBL2387287 90555 None 0 Human Functional pIC50 = 9.0 9.0 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 427 4 1 4 3.1 CC(=O)N(C)C1CCN(C(=O)Nc2ccc(N3CCC(N4CCCC4C)C3)c(C)c2)C1 10.1016/j.bmcl.2013.03.080
25263867 90560 None 0 Human Functional pIC50 = 9.0 9.0 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 460 5 2 3 5.7 Cc1cc(NC(=O)NCc2cc(Cl)cc(Cl)c2)ccc1N1CCC(N2CCCC2C)C1 10.1016/j.bmcl.2013.03.080
CHEMBL2387291 90560 None 0 Human Functional pIC50 = 9.0 9.0 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 460 5 2 3 5.7 Cc1cc(NC(=O)NCc2cc(Cl)cc(Cl)c2)ccc1N1CCC(N2CCCC2C)C1 10.1016/j.bmcl.2013.03.080
25264260 90590 None 0 Human Functional pIC50 = 9.0 9.0 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 385 3 1 4 2.8 Cc1cc(NC(=O)N2CCN(C)CC2)ccc1N1CCC(N2CCCC2C)C1 10.1016/j.bmcl.2013.03.080
CHEMBL2387319 90590 None 0 Human Functional pIC50 = 9.0 9.0 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 385 3 1 4 2.8 Cc1cc(NC(=O)N2CCN(C)CC2)ccc1N1CCC(N2CCCC2C)C1 10.1016/j.bmcl.2013.03.080
78324787 119166 None 0 Human Functional pIC50 = 9.0 9.0 - 1
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
ChEMBL 351 7 0 3 4.5 COC(=O)CCc1ccc(-c2ccc(CCN3CCC[C@H]3C)cc2)cc1 nan
CHEMBL3427232 119166 None 0 Human Functional pIC50 = 9.0 9.0 - 1
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
ChEMBL 351 7 0 3 4.5 COC(=O)CCc1ccc(-c2ccc(CCN3CCC[C@H]3C)cc2)cc1 nan
10176219 206891 None 2 Guinea pig Functional pIC50 = 9.0 9.0 - 1
Histamine H3 receptor agonist activity was assessed by the inhibition of the electrically evoked twitch response of the guinea-pig ileum.Histamine H3 receptor agonist activity was assessed by the inhibition of the electrically evoked twitch response of the guinea-pig ileum.
ChEMBL 152 4 3 2 0.7 N=C(N)CCCc1c[nH]cn1 10.1016/S0960-894X(00)80659-9
CHEMBL72156 206891 None 2 Guinea pig Functional pIC50 = 9.0 9.0 - 1
Histamine H3 receptor agonist activity was assessed by the inhibition of the electrically evoked twitch response of the guinea-pig ileum.Histamine H3 receptor agonist activity was assessed by the inhibition of the electrically evoked twitch response of the guinea-pig ileum.
ChEMBL 152 4 3 2 0.7 N=C(N)CCCc1c[nH]cn1 10.1016/S0960-894X(00)80659-9
23151224 182053 None 0 Human Functional pIC50 = 9.0 9.0 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 393 7 0 6 3.6 COc1ccc2nc(C)n(-c3ccc(OCCCN4CCCC4)cc3)c(=O)c2c1 10.1021/jm8003834
CHEMBL477991 182053 None 0 Human Functional pIC50 = 9.0 9.0 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 393 7 0 6 3.6 COc1ccc2nc(C)n(-c3ccc(OCCCN4CCCC4)cc3)c(=O)c2c1 10.1021/jm8003834
78324787 119166 None 0 Human Functional pIC50 = 9.0 9.0 - 1
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
ChEMBL 351 7 0 3 4.5 COC(=O)CCc1ccc(-c2ccc(CCN3CCC[C@H]3C)cc2)cc1 10.1021/acsmedchemlett.5b00002
CHEMBL3427232 119166 None 0 Human Functional pIC50 = 9.0 9.0 - 1
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
ChEMBL 351 7 0 3 4.5 COC(=O)CCc1ccc(-c2ccc(CCN3CCC[C@H]3C)cc2)cc1 10.1021/acsmedchemlett.5b00002
141419106 179911 None 0 Human Functional pIC50 = 9.0 9.0 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 356 8 0 5 3.3 CCc1c(OC)c(=O)ccn1-c1ccc(OCCCN2CCCC2)cc1 10.1016/j.ejmech.2020.113096
CHEMBL4744905 179911 None 0 Human Functional pIC50 = 9.0 9.0 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 356 8 0 5 3.3 CCc1c(OC)c(=O)ccn1-c1ccc(OCCCN2CCCC2)cc1 10.1016/j.ejmech.2020.113096
1223 953 None 33 Human Functional pIC50 = 8.9 8.9 1 4
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1016/j.ejmech.2020.113096
2790 953 None 33 Human Functional pIC50 = 8.9 8.9 1 4
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1016/j.ejmech.2020.113096
CHEMBL14690 953 None 33 Human Functional pIC50 = 8.9 8.9 1 4
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1016/j.ejmech.2020.113096
23151160 190616 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 407 4 0 5 4.2 Cc1nc2ccc(F)cc2c(=O)n1-c1ccc(OC2CCN(C3CCC3)CC2)cc1 10.1021/jm800569w
CHEMBL517937 190616 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 407 4 0 5 4.2 Cc1nc2ccc(F)cc2c(=O)n1-c1ccc(OC2CCN(C3CCC3)CC2)cc1 10.1021/jm800569w
23151169 192418 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 419 5 0 6 4.1 COc1cccc2nc(C)n(-c3ccc(OC4CCN(C5CCC5)CC4)cc3)c(=O)c12 10.1021/jm800569w
CHEMBL520629 192418 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 419 5 0 6 4.1 COc1cccc2nc(C)n(-c3ccc(OC4CCN(C5CCC5)CC4)cc3)c(=O)c12 10.1021/jm800569w
44160010 15717 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 468 7 0 8 3.6 c1ccc(Cn2nnnc2C(c2ccc(-n3cccn3)cc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
CHEMBL1222436 15717 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 468 7 0 8 3.6 c1ccc(Cn2nnnc2C(c2ccc(-n3cccn3)cc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
25263864 90582 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 432 4 2 3 5.7 CC1CCCN1C1CCN(c2ccc(NC(=O)Nc3cc(Cl)cc(Cl)c3)cc2)C1 10.1016/j.bmcl.2013.03.080
CHEMBL2387311 90582 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 432 4 2 3 5.7 CC1CCCN1C1CCN(c2ccc(NC(=O)Nc3cc(Cl)cc(Cl)c3)cc2)C1 10.1016/j.bmcl.2013.03.080
78324786 119165 None 0 Human Functional pIC50 = 8.9 8.9 - 1
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
ChEMBL 361 7 0 5 3.6 C[C@@H]1CCCN1CCc1ccc(-c2ccc(CCn3ncnn3)cc2)cc1 nan
CHEMBL3427231 119165 None 0 Human Functional pIC50 = 8.9 8.9 - 1
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
ChEMBL 361 7 0 5 3.6 C[C@@H]1CCCN1CCc1ccc(-c2ccc(CCn3ncnn3)cc2)cc1 nan
78321038 160839 None 0 Human Functional pIC50 = 8.9 8.9 - 1
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
ChEMBL 408 7 1 4 4.1 COC(=O)C(C)(C)NC(=O)c1ccc(-c2ccc(CCN3CCC[C@H]3C)cc2)cc1 nan
CHEMBL4113958 160839 None 0 Human Functional pIC50 = 8.9 8.9 - 1
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
ChEMBL 408 7 1 4 4.1 COC(=O)C(C)(C)NC(=O)c1ccc(-c2ccc(CCN3CCC[C@H]3C)cc2)cc1 nan
11516386 186137 None 0 Human Functional pIC50 = 8.9 8.9 2398 2
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 377 6 0 5 3.9 Cn1c(-c2ccc(OCCCN3CCCCC3)cc2)nc2ccccc2c1=O 10.1016/j.bmcl.2008.10.034
CHEMBL487064 186137 None 0 Human Functional pIC50 = 8.9 8.9 2398 2
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 377 6 0 5 3.9 Cn1c(-c2ccc(OCCCN3CCCCC3)cc2)nc2ccccc2c1=O 10.1016/j.bmcl.2008.10.034
24951191 182541 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 377 6 0 5 3.9 Cc1ccc2c(=O)n(-c3ccc(OCCCN4CCCC4)cc3)c(C)nc2c1 10.1021/jm8003834
CHEMBL478615 182541 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 377 6 0 5 3.9 Cc1ccc2c(=O)n(-c3ccc(OCCCN4CCCC4)cc3)c(C)nc2c1 10.1021/jm8003834
78324786 119165 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
ChEMBL 361 7 0 5 3.6 C[C@@H]1CCCN1CCc1ccc(-c2ccc(CCn3ncnn3)cc2)cc1 10.1021/acsmedchemlett.5b00002
CHEMBL3427231 119165 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
ChEMBL 361 7 0 5 3.6 C[C@@H]1CCCN1CCc1ccc(-c2ccc(CCn3ncnn3)cc2)cc1 10.1021/acsmedchemlett.5b00002
118737703 119177 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
ChEMBL 408 7 1 4 4.5 COC(=O)C(C)(C)C(=O)Nc1ccc(-c2ccc(CCN3CCC[C@H]3C)cc2)cc1 10.1021/acsmedchemlett.5b00002
CHEMBL3427243 119177 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
ChEMBL 408 7 1 4 4.5 COC(=O)C(C)(C)C(=O)Nc1ccc(-c2ccc(CCN3CCC[C@H]3C)cc2)cc1 10.1021/acsmedchemlett.5b00002
10446240 75024 None 0 Human Functional pIC50 = 8.9 8.9 - 1
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 277 8 2 2 3.6 Clc1ccc(CNCCCCCc2c[nH]cn2)cc1 10.1021/jm0504353
CHEMBL203263 75024 None 0 Human Functional pIC50 = 8.9 8.9 - 1
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 277 8 2 2 3.6 Clc1ccc(CNCCCCCc2c[nH]cn2)cc1 10.1021/jm0504353
23151327 178074 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 407 4 0 5 4.2 Cc1nc2cc(F)ccc2c(=O)n1-c1ccc(OC2CCN(C3CCC3)CC2)cc1 10.1021/jm800569w
CHEMBL464598 178074 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 407 4 0 5 4.2 Cc1nc2cc(F)ccc2c(=O)n1-c1ccc(OC2CCN(C3CCC3)CC2)cc1 10.1021/jm800569w
11596426 181724 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 397 6 0 5 4.2 Cc1nc2cccc(Cl)c2c(=O)n1-c1ccc(OCCCN2CCCC2)cc1 10.1021/jm8003834
CHEMBL477363 181724 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 397 6 0 5 4.2 Cc1nc2cccc(Cl)c2c(=O)n1-c1ccc(OCCCN2CCCC2)cc1 10.1021/jm8003834
24951193 182052 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 393 7 0 6 3.6 COc1cccc2nc(C)n(-c3ccc(OCCCN4CCCC4)cc3)c(=O)c12 10.1021/jm8003834
CHEMBL477990 182052 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 393 7 0 6 3.6 COc1cccc2nc(C)n(-c3ccc(OCCCN4CCCC4)cc3)c(=O)c12 10.1021/jm8003834
1223 953 None 33 Human Functional pIC50 = 8.9 8.9 1 4
Antagonist activity at human H3 receptor by TR-FRET assayAntagonist activity at human H3 receptor by TR-FRET assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1016/j.bmc.2021.116306
2790 953 None 33 Human Functional pIC50 = 8.9 8.9 1 4
Antagonist activity at human H3 receptor by TR-FRET assayAntagonist activity at human H3 receptor by TR-FRET assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1016/j.bmc.2021.116306
CHEMBL14690 953 None 33 Human Functional pIC50 = 8.9 8.9 1 4
Antagonist activity at human H3 receptor by TR-FRET assayAntagonist activity at human H3 receptor by TR-FRET assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1016/j.bmc.2021.116306
162654981 180666 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 382 5 0 5 3.9 COc1c(C)n(-c2ccc(OC3CCN(C4CCCC4)CC3)cc2)ccc1=O 10.1016/j.ejmech.2020.113096
CHEMBL4753961 180666 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 382 5 0 5 3.9 COc1c(C)n(-c2ccc(OC3CCN(C4CCCC4)CC3)cc2)ccc1=O 10.1016/j.ejmech.2020.113096
71625827 90561 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 456 6 2 4 6.2 CC1CCCN1C1CCN(c2ccc(NC(=O)Nc3ccc(Oc4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2013.03.080
CHEMBL2387292 90561 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 456 6 2 4 6.2 CC1CCCN1C1CCN(c2ccc(NC(=O)Nc3ccc(Oc4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2013.03.080
25139757 175868 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 423 4 0 5 4.7 Cc1nc2ccc(Cl)cc2c(=O)n1-c1ccc(OC2CCN(C3CCC3)CC2)cc1 10.1021/jm800569w
CHEMBL458359 175868 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 423 4 0 5 4.7 Cc1nc2ccc(Cl)cc2c(=O)n1-c1ccc(OC2CCN(C3CCC3)CC2)cc1 10.1021/jm800569w
11501983 184302 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 389 4 0 5 4.1 Cc1nc2ccccc2c(=O)n1-c1ccc(OC2CCN(C3CCC3)CC2)cc1 10.1021/jm800569w
CHEMBL483199 184302 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 389 4 0 5 4.1 Cc1nc2ccccc2c(=O)n1-c1ccc(OC2CCN(C3CCC3)CC2)cc1 10.1021/jm800569w
23151250 184419 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 419 5 0 6 4.1 COc1ccc2nc(C)n(-c3ccc(OC4CCN(C5CCC5)CC4)cc3)c(=O)c2c1 10.1021/jm800569w
CHEMBL484189 184419 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 419 5 0 6 4.1 COc1ccc2nc(C)n(-c3ccc(OC4CCN(C5CCC5)CC4)cc3)c(=O)c2c1 10.1021/jm800569w
78320095 160417 None 0 Human Functional pIC50 = 8.8 8.8 - 1
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
ChEMBL 476 10 1 4 5.3 COC(=O)CCCNC(=O)C1(c2ccc(-c3ccc(CCN4CCC[C@H]4C)cc3)cc2)CCCC1 nan
CHEMBL4110626 160417 None 0 Human Functional pIC50 = 8.8 8.8 - 1
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
ChEMBL 476 10 1 4 5.3 COC(=O)CCCNC(=O)C1(c2ccc(-c3ccc(CCN4CCC[C@H]4C)cc3)cc2)CCCC1 nan
23151331 189766 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 381 6 0 5 3.7 Cc1nc2c(F)cccc2c(=O)n1-c1ccc(OCCCN2CCCC2)cc1 10.1021/jm8003834
CHEMBL515150 189766 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 381 6 0 5 3.7 Cc1nc2c(F)cccc2c(=O)n1-c1ccc(OCCCN2CCCC2)cc1 10.1021/jm8003834
11610816 184523 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 390 4 0 6 3.5 Cc1nc2ncccc2c(=O)n1-c1ccc(OC2CCN(C3CCC3)CC2)cc1 10.1021/jm800569w
CHEMBL484611 184523 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 390 4 0 6 3.5 Cc1nc2ncccc2c(=O)n1-c1ccc(OC2CCN(C3CCC3)CC2)cc1 10.1021/jm800569w
44160248 15893 None 0 Human Functional pIC50 = 8.8 8.8 10 2
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 480 7 0 8 2.8 CS(=O)(=O)c1ccc(C(c2nnnn2Cc2ccccc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
CHEMBL1223157 15893 None 0 Human Functional pIC50 = 8.8 8.8 10 2
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 480 7 0 8 2.8 CS(=O)(=O)c1ccc(C(c2nnnn2Cc2ccccc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
44159759 15923 None 0 Human Functional pIC50 = 8.8 8.8 5 2
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 469 7 0 9 3.0 c1ccc(Cn2nnnc2C(c2ccc(-n3cncn3)cc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
CHEMBL1223235 15923 None 0 Human Functional pIC50 = 8.8 8.8 5 2
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 469 7 0 9 3.0 c1ccc(Cn2nnnc2C(c2ccc(-n3cncn3)cc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
76336463 105923 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 403 3 0 4 3.1 O=C(C1CC2(CCN(C3CCOCC3)CC2)C1)N1CCN(C2CCCCC2)CC1 10.1021/jm4014828
CHEMBL3127676 105923 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 403 3 0 4 3.1 O=C(C1CC2(CCN(C3CCOCC3)CC2)C1)N1CCN(C2CCCCC2)CC1 10.1021/jm4014828
44563063 186131 None 0 Human Functional pIC50 = 8.8 8.8 1513 2
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 439 7 0 5 5.3 O=c1c2ccccc2nc(-c2ccc(OCCCN3CCCCC3)cc2)n1-c1ccccc1 10.1016/j.bmcl.2008.10.034
CHEMBL487060 186131 None 0 Human Functional pIC50 = 8.8 8.8 1513 2
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 439 7 0 5 5.3 O=c1c2ccccc2nc(-c2ccc(OCCCN3CCCCC3)cc2)n1-c1ccccc1 10.1016/j.bmcl.2008.10.034
11581919 181652 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 391 6 0 5 4.3 Cc1nc2ccccc2c(=O)n1-c1ccc(OCCCN2CCCCCC2)cc1 10.1021/jm8003834
CHEMBL476579 181652 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 391 6 0 5 4.3 Cc1nc2ccccc2c(=O)n1-c1ccc(OCCCN2CCCCCC2)cc1 10.1021/jm8003834
11516387 181666 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 377 7 0 5 3.8 CCc1nc2ccccc2c(=O)n1-c1ccc(OCCCN2CCCC2)cc1 10.1021/jm8003834
CHEMBL476723 181666 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 377 7 0 5 3.8 CCc1nc2ccccc2c(=O)n1-c1ccc(OCCCN2CCCC2)cc1 10.1021/jm8003834
24951348 183031 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 381 6 0 5 3.7 Cc1nc2ccc(F)cc2c(=O)n1-c1ccc(OCCCN2CCCC2)cc1 10.1021/jm8003834
CHEMBL479252 183031 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 381 6 0 5 3.7 Cc1nc2ccc(F)cc2c(=O)n1-c1ccc(OCCCN2CCCC2)cc1 10.1021/jm8003834
141351665 179589 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 342 5 0 5 3.1 COc1cn(-c2ccc(OC3CCN(C(C)C)CC3)cc2)ccc1=O 10.1016/j.ejmech.2020.113096
CHEMBL4740932 179589 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 342 5 0 5 3.1 COc1cn(-c2ccc(OC3CCN(C(C)C)CC3)cc2)ccc1=O 10.1016/j.ejmech.2020.113096
25139758 176112 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 423 4 0 5 4.7 Cc1nc2c(Cl)cccc2c(=O)n1-c1ccc(OC2CCN(C3CCC3)CC2)cc1 10.1021/jm800569w
CHEMBL458954 176112 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 423 4 0 5 4.7 Cc1nc2c(Cl)cccc2c(=O)n1-c1ccc(OC2CCN(C3CCC3)CC2)cc1 10.1021/jm800569w
11682068 181518 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 363 6 0 5 3.6 Cc1nc2ccccc2c(=O)n1-c1ccc(OCCCN2CCCC2)cc1 10.1021/jm800569w
CHEMBL476373 181518 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 363 6 0 5 3.6 Cc1nc2ccccc2c(=O)n1-c1ccc(OCCCN2CCCC2)cc1 10.1021/jm800569w
76325615 105926 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 363 3 0 4 2.2 CC(C)N1CCN(C(=O)C2CC3(CCN(C4CCOCC4)CC3)C2)CC1 10.1021/jm4014828
CHEMBL3127679 105926 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 363 3 0 4 2.2 CC(C)N1CCN(C(=O)C2CC3(CCN(C4CCOCC4)CC3)C2)CC1 10.1021/jm4014828
11697697 2547 None 25 Human Functional pIC50 = 8.8 8.8 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 431 6 0 5 4.6 Cc1nc2cccc(c2c(=O)n1c1ccc(cc1)OCCCN1CCCC1)C(F)(F)F 10.1021/jm8003834
7346 2547 None 25 Human Functional pIC50 = 8.8 8.8 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 431 6 0 5 4.6 Cc1nc2cccc(c2c(=O)n1c1ccc(cc1)OCCCN1CCCC1)C(F)(F)F 10.1021/jm8003834
CHEMBL476323 2547 None 25 Human Functional pIC50 = 8.8 8.8 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 431 6 0 5 4.6 Cc1nc2cccc(c2c(=O)n1c1ccc(cc1)OCCCN1CCCC1)C(F)(F)F 10.1021/jm8003834
DB11910 2547 None 25 Human Functional pIC50 = 8.8 8.8 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 431 6 0 5 4.6 Cc1nc2cccc(c2c(=O)n1c1ccc(cc1)OCCCN1CCCC1)C(F)(F)F 10.1021/jm8003834
24951192 182543 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 377 6 0 5 3.9 Cc1cccc2c(=O)n(-c3ccc(OCCCN4CCCC4)cc3)c(C)nc12 10.1021/jm8003834
CHEMBL478616 182543 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 377 6 0 5 3.9 Cc1cccc2c(=O)n(-c3ccc(OCCCN4CCCC4)cc3)c(C)nc12 10.1021/jm8003834
23151323 185064 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 419 5 0 6 4.1 COc1ccc2c(=O)n(-c3ccc(OC4CCN(C5CCC5)CC4)cc3)c(C)nc2c1 10.1021/jm800569w
CHEMBL485388 185064 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 419 5 0 6 4.1 COc1ccc2c(=O)n(-c3ccc(OC4CCN(C5CCC5)CC4)cc3)c(C)nc2c1 10.1021/jm800569w
23151312 192680 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 390 4 0 6 3.5 Cc1nc2cnccc2c(=O)n1-c1ccc(OC2CCN(C3CCC3)CC2)cc1 10.1021/jm800569w
CHEMBL521327 192680 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 390 4 0 6 3.5 Cc1nc2cnccc2c(=O)n1-c1ccc(OC2CCN(C3CCC3)CC2)cc1 10.1021/jm800569w
78324789 119168 None 0 Human Functional pIC50 = 8.7 8.7 - 1
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
ChEMBL 365 8 0 3 4.9 CCOC(=O)CCc1ccc(-c2ccc(CCN3CCC[C@H]3C)cc2)cc1 nan
CHEMBL3427234 119168 None 0 Human Functional pIC50 = 8.7 8.7 - 1
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
ChEMBL 365 8 0 3 4.9 CCOC(=O)CCc1ccc(-c2ccc(CCN3CCC[C@H]3C)cc2)cc1 nan
45270025 197621 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
ChEMBL 369 6 0 4 5.2 C[C@H]1Sc2ccccc2O[C@@H]1c1ccc(OCCCN2CCCC2)cc1 10.1016/j.bmcl.2009.05.101
CHEMBL550393 197621 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
ChEMBL 369 6 0 4 5.2 C[C@H]1Sc2ccccc2O[C@@H]1c1ccc(OCCCN2CCCC2)cc1 10.1016/j.bmcl.2009.05.101
24948948 181293 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 381 6 0 5 3.7 Cc1nc2cc(F)ccc2c(=O)n1-c1ccc(OCCCN2CCCC2)cc1 10.1021/jm8003834
CHEMBL476106 181293 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 381 6 0 5 3.7 Cc1nc2cc(F)ccc2c(=O)n1-c1ccc(OCCCN2CCCC2)cc1 10.1021/jm8003834
78324789 119168 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
ChEMBL 365 8 0 3 4.9 CCOC(=O)CCc1ccc(-c2ccc(CCN3CCC[C@H]3C)cc2)cc1 10.1021/acsmedchemlett.5b00002
CHEMBL3427234 119168 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
ChEMBL 365 8 0 3 4.9 CCOC(=O)CCc1ccc(-c2ccc(CCN3CCC[C@H]3C)cc2)cc1 10.1021/acsmedchemlett.5b00002
44447988 95662 None 1 Rat Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at histamine H3 receptor in rat forebrain assessed as inhibition of [3H]histamine release from synaptosomesAntagonist activity at histamine H3 receptor in rat forebrain assessed as inhibition of [3H]histamine release from synaptosomes
ChEMBL 356 6 0 6 1.8 C[C@H]1CCCN1CCN1CCN(CCN2CCC[C@@H]2C)C1=C(C#N)C#N 10.1016/j.bmcl.2008.03.006
CHEMBL257812 95662 None 1 Rat Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at histamine H3 receptor in rat forebrain assessed as inhibition of [3H]histamine release from synaptosomesAntagonist activity at histamine H3 receptor in rat forebrain assessed as inhibition of [3H]histamine release from synaptosomes
ChEMBL 356 6 0 6 1.8 C[C@H]1CCCN1CCN1CCN(CCN2CCC[C@@H]2C)C1=C(C#N)C#N 10.1016/j.bmcl.2008.03.006
76325614 105922 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 375 3 0 4 2.4 O=C(C1CC2(CCN(C3CCOCC3)CC2)C1)N1CCN(C2CCC2)CC1 10.1021/jm4014828
CHEMBL3127675 105922 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 375 3 0 4 2.4 O=C(C1CC2(CCN(C3CCOCC3)CC2)C1)N1CCN(C2CCC2)CC1 10.1021/jm4014828
78320715 159954 None 0 Human Functional pIC50 = 8.7 8.7 - 1
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
ChEMBL 448 8 1 4 4.5 COC(=O)CNC(=O)C1(c2ccc(-c3ccc(CCN4CCC[C@H]4C)cc3)cc2)CCCC1 nan
CHEMBL4106702 159954 None 0 Human Functional pIC50 = 8.7 8.7 - 1
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
ChEMBL 448 8 1 4 4.5 COC(=O)CNC(=O)C1(c2ccc(-c3ccc(CCN4CCC[C@H]4C)cc3)cc2)CCCC1 nan
118737701 119174 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
ChEMBL 448 8 1 4 4.8 COC(=O)CC(=O)NC1(c2ccc(-c3ccc(CCN4CCC[C@H]4C)cc3)cc2)CCCC1 10.1021/acsmedchemlett.5b00002
CHEMBL3427240 119174 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
ChEMBL 448 8 1 4 4.8 COC(=O)CC(=O)NC1(c2ccc(-c3ccc(CCN4CCC[C@H]4C)cc3)cc2)CCCC1 10.1021/acsmedchemlett.5b00002
141419108 179604 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 342 7 0 5 3.0 COc1cn(-c2ccc(OCCCN3CCCC3)cc2)c(C)cc1=O 10.1016/j.ejmech.2020.113096
CHEMBL4741097 179604 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 342 7 0 5 3.0 COc1cn(-c2ccc(OCCCN3CCCC3)cc2)c(C)cc1=O 10.1016/j.ejmech.2020.113096
1267 3804 None 32 Human Functional pIC50 = 8.7 8.7 -6 5
Inhibition of recombinant human histamine H3 receptor stably expressed in HEK293 cells assessed as increase in cAMP accumulation in presence of forskolin incubated for 30 mins by TR-FRET LANCE assayInhibition of recombinant human histamine H3 receptor stably expressed in HEK293 cells assessed as increase in cAMP accumulation in presence of forskolin incubated for 30 mins by TR-FRET LANCE assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.3c00430
3035905 3804 None 32 Human Functional pIC50 = 8.7 8.7 -6 5
Inhibition of recombinant human histamine H3 receptor stably expressed in HEK293 cells assessed as increase in cAMP accumulation in presence of forskolin incubated for 30 mins by TR-FRET LANCE assayInhibition of recombinant human histamine H3 receptor stably expressed in HEK293 cells assessed as increase in cAMP accumulation in presence of forskolin incubated for 30 mins by TR-FRET LANCE assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.3c00430
CHEMBL260374 3804 None 32 Human Functional pIC50 = 8.7 8.7 -6 5
Inhibition of recombinant human histamine H3 receptor stably expressed in HEK293 cells assessed as increase in cAMP accumulation in presence of forskolin incubated for 30 mins by TR-FRET LANCE assayInhibition of recombinant human histamine H3 receptor stably expressed in HEK293 cells assessed as increase in cAMP accumulation in presence of forskolin incubated for 30 mins by TR-FRET LANCE assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.3c00430
72546762 102619 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 358 9 2 4 4.0 N#Cc1ccc(CCCCNC(=N)SCCCN2CCCCC2)cc1 10.1016/j.bmcl.2013.09.052
CHEMBL2441945 102619 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 358 9 2 4 4.0 N#Cc1ccc(CCCCNC(=N)SCCCN2CCCCC2)cc1 10.1016/j.bmcl.2013.09.052
CHEMBL3040738 102619 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 358 9 2 4 4.0 N#Cc1ccc(CCCCNC(=N)SCCCN2CCCCC2)cc1 10.1016/j.bmcl.2013.09.052
11536119 138794 None 0 Human Functional pIC50 = 8 8.0 - 1
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 249 7 2 2 3.4 c1nc(CCCCCNC2CCCCCC2)c[nH]1 10.1021/jm0504353
CHEMBL377954 138794 None 0 Human Functional pIC50 = 8 8.0 - 1
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 249 7 2 2 3.4 c1nc(CCCCCNC2CCCCCC2)c[nH]1 10.1021/jm0504353
25139625 184962 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 403 4 0 5 4.5 Cc1nc2ccccc2c(=O)n1-c1ccc(OC2CCCN(C3CCC3)CC2)cc1 10.1021/jm800569w
CHEMBL485242 184962 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 403 4 0 5 4.5 Cc1nc2ccccc2c(=O)n1-c1ccc(OC2CCCN(C3CCC3)CC2)cc1 10.1021/jm800569w
23151329 192643 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 403 4 0 5 4.5 Cc1nc2ccccc2c(=O)n1-c1ccc(O[C@H]2CC[C@@H](N3CCCC3)CC2)cc1 10.1021/jm800569w
CHEMBL521022 192643 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 403 4 0 5 4.5 Cc1nc2ccccc2c(=O)n1-c1ccc(O[C@H]2CC[C@@H](N3CCCC3)CC2)cc1 10.1021/jm800569w
25118477 105955 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 387 3 0 3 3.9 O=C(C1CC12CCN(C1CCCCC1)CC2)N1CCN(C2CCCCC2)CC1 10.1021/jm4014828
CHEMBL3127708 105955 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 387 3 0 3 3.9 O=C(C1CC12CCN(C1CCCCC1)CC2)N1CCN(C2CCCCC2)CC1 10.1021/jm4014828
11704156 182550 None 0 Human Functional pIC50 = 8 8.0 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 405 6 0 5 4.7 Cc1nc2ccccc2c(=O)n1-c1ccc(OCCCN2CCCCCCC2)cc1 10.1021/jm8003834
CHEMBL478621 182550 None 0 Human Functional pIC50 = 8 8.0 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 405 6 0 5 4.7 Cc1nc2ccccc2c(=O)n1-c1ccc(OCCCN2CCCCCCC2)cc1 10.1021/jm8003834
44159287 15779 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 453 6 0 7 3.9 c1ccc(Cn2nnnc2C(c2ccc3ncccc3c2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
CHEMBL1222730 15779 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 453 6 0 7 3.9 c1ccc(Cn2nnnc2C(c2ccc3ncccc3c2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
23151143 184954 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 375 4 0 5 3.7 Cc1nc2ccccc2c(=O)n1-c1ccc(OC2CCN(C3CCC3)C2)cc1 10.1021/jm800569w
CHEMBL485234 184954 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 375 4 0 5 3.7 Cc1nc2ccccc2c(=O)n1-c1ccc(OC2CCN(C3CCC3)C2)cc1 10.1021/jm800569w
164613249 184665 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human H3 receptor by TR-FRET assayAntagonist activity at human H3 receptor by TR-FRET assay
ChEMBL 315 7 1 5 2.8 CN(C)CCCOc1ccc(/C=C/c2cc(=O)c(O)co2)cc1 10.1016/j.bmc.2021.116306
CHEMBL4848375 184665 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human H3 receptor by TR-FRET assayAntagonist activity at human H3 receptor by TR-FRET assay
ChEMBL 315 7 1 5 2.8 CN(C)CCCOc1ccc(/C=C/c2cc(=O)c(O)co2)cc1 10.1016/j.bmc.2021.116306
72164842 92152 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assay
ChEMBL 348 5 1 3 4.3 O=C(Cc1c[nH]c2ccccc12)Oc1ccc(CN2CCCCC2)cc1 10.1016/j.bmc.2013.07.051
CHEMBL2419585 92152 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assay
ChEMBL 348 5 1 3 4.3 O=C(Cc1c[nH]c2ccccc12)Oc1ccc(CN2CCCCC2)cc1 10.1016/j.bmc.2013.07.051
162661522 181637 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 358 7 0 6 2.3 COc1c(C)n(-c2ccc(OCCCN3CCOCC3)cc2)ccc1=O 10.1016/j.ejmech.2020.113096
CHEMBL4765168 181637 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 358 7 0 6 2.3 COc1c(C)n(-c2ccc(OCCCN3CCOCC3)cc2)ccc1=O 10.1016/j.ejmech.2020.113096
550705 18190 None 1 Human Functional pIC50 = 8.0 8.0 25 2
Antagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 293 0 1 2 3.3 CC1CC(O)(C#Cc2cccc3ccccc23)C(C)CN1C 10.1016/j.bmcl.2010.08.099
CHEMBL1269843 18190 None 1 Human Functional pIC50 = 8.0 8.0 25 2
Antagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 293 0 1 2 3.3 CC1CC(O)(C#Cc2cccc3ccccc23)C(C)CN1C 10.1016/j.bmcl.2010.08.099
46212866 105931 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 369 3 0 4 1.1 CS(=O)(=O)N1CCC2(CC1)CC(C(=O)N1CCN(C3CCC3)CC1)C2 10.1021/jm4014828
CHEMBL3127684 105931 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 369 3 0 4 1.1 CS(=O)(=O)N1CCC2(CC1)CC(C(=O)N1CCN(C3CCC3)CC1)C2 10.1021/jm4014828
11560214 182557 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 391 6 0 5 4.3 Cc1nc2ccccc2c(=O)n1-c1ccc(OCCCN2CCCCC2C)cc1 10.1021/jm8003834
CHEMBL478628 182557 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 391 6 0 5 4.3 Cc1nc2ccccc2c(=O)n1-c1ccc(OCCCN2CCCCC2C)cc1 10.1021/jm8003834
44579387 187222 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 379 4 0 2 4.6 CN(CCN1CCCCC1)C(=O)N1CCC(c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2008.07.125
CHEMBL491614 187222 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 379 4 0 2 4.6 CN(CCN1CCCCC1)C(=O)N1CCC(c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2008.07.125
25118123 105944 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 321 2 0 4 1.0 CN1CCN(C(=O)C2CC23CCN(C2CCOCC2)CC3)CC1 10.1021/jm4014828
CHEMBL3127697 105944 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 321 2 0 4 1.0 CN1CCN(C(=O)C2CC23CCN(C2CCOCC2)CC3)CC1 10.1021/jm4014828
71625596 90570 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 363 8 2 3 4.3 CCN(CC)CCOc1ccc(NC(=O)Nc2ccc(F)cc2F)cc1 10.1016/j.bmcl.2013.03.080
CHEMBL2387300 90570 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 363 8 2 3 4.3 CCN(CC)CCOc1ccc(NC(=O)Nc2ccc(F)cc2F)cc1 10.1016/j.bmcl.2013.03.080
44159760 15992 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 480 6 0 6 4.1 Brc1ccc(C(c2nnnn2Cc2ccccc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
CHEMBL1223449 15992 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 480 6 0 6 4.1 Brc1ccc(C(c2nnnn2Cc2ccccc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
52941057 18191 None 0 Mouse Functional pIC50 = 6.9 6.9 -13 2
Antagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 293 0 1 2 3.3 C[C@H]1CN(C)[C@H](C)C[C@@]1(O)C#Cc1cccc2ccccc12 10.1016/j.bmcl.2010.08.099
CHEMBL1269844 18191 None 0 Mouse Functional pIC50 = 6.9 6.9 -13 2
Antagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 293 0 1 2 3.3 C[C@H]1CN(C)[C@H](C)C[C@@]1(O)C#Cc1cccc2ccccc12 10.1016/j.bmcl.2010.08.099
44159173 15758 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 441 6 1 6 3.9 c1ccc(Cn2nnnc2C(c2ccc3[nH]ccc3c2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
CHEMBL1222662 15758 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 441 6 1 6 3.9 c1ccc(Cn2nnnc2C(c2ccc3[nH]ccc3c2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
52944521 18253 None 0 Human Functional pIC50 = 7.9 7.9 57 2
Antagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 294 0 1 3 2.7 CC1CC(O)(C#Cc2cccc3ncccc23)C(C)CN1C 10.1016/j.bmcl.2010.08.099
CHEMBL1270264 18253 None 0 Human Functional pIC50 = 7.9 7.9 57 2
Antagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 294 0 1 3 2.7 CC1CC(O)(C#Cc2cccc3ncccc23)C(C)CN1C 10.1016/j.bmcl.2010.08.099
5048 3133 None 50 Human Functional pIC50 = 7.9 7.9 -11 5
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.1021/jm800569w
8924 3133 None 50 Human Functional pIC50 = 7.9 7.9 -11 5
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.1021/jm800569w
9948102 3133 None 50 Human Functional pIC50 = 7.9 7.9 -11 5
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.1021/jm800569w
9948102.0 3133 None 50 Human Functional pIC50 = 7.9 7.9 -11 5
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.1021/jm800569w
CHEMBL462605 3133 None 50 Human Functional pIC50 = 7.9 7.9 -11 5
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.1021/jm800569w
DB11642 3133 None 50 Human Functional pIC50 = 7.9 7.9 -11 5
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.1021/jm800569w
44158482 15746 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 496 8 0 9 4.0 c1ccc(Cn2nnnc2C(c2ccc(Oc3ncccn3)cc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
CHEMBL1222596 15746 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 496 8 0 9 4.0 c1ccc(Cn2nnnc2C(c2ccc(Oc3ncccn3)cc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
76311112 105934 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 397 3 0 3 3.3 CC(C)N1CCCN(C(=O)C2CC3(CCN(C(=O)c4ccccc4)CC3)C2)CC1 10.1021/jm4014828
CHEMBL3127687 105934 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 397 3 0 3 3.3 CC(C)N1CCCN(C(=O)C2CC3(CCN(C(=O)c4ccccc4)CC3)C2)CC1 10.1021/jm4014828
25117760 105949 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 389 3 0 4 2.7 O=C(C1CC12CCN(C1CCOCC1)CC2)N1CCN(C2CCCCC2)CC1 10.1021/jm4014828
CHEMBL3127702 105949 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 389 3 0 4 2.7 O=C(C1CC12CCN(C1CCOCC1)CC2)N1CCN(C2CCCCC2)CC1 10.1021/jm4014828
49865290 15597 None 0 Rat Functional pIC50 = 7.9 7.9 -3 2
Antagonist activity at rat histamine H3 receptorAntagonist activity at rat histamine H3 receptor
ChEMBL 459 7 1 7 2.7 CNC(=O)c1ccc(C(c2nnnn2Cc2ccccc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
CHEMBL1221429 15597 None 0 Rat Functional pIC50 = 7.9 7.9 -3 2
Antagonist activity at rat histamine H3 receptorAntagonist activity at rat histamine H3 receptor
ChEMBL 459 7 1 7 2.7 CNC(=O)c1ccc(C(c2nnnn2Cc2ccccc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
11492393 4060 None 7 Human Functional pIC50 = 7.9 7.9 - 1
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 235 7 2 2 3.0 C(CCc1cnc[nH]1)CCNC1CCCCC1 10.1021/jm0504353
1263 4060 None 7 Human Functional pIC50 = 7.9 7.9 - 1
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 235 7 2 2 3.0 C(CCc1cnc[nH]1)CCNC1CCCCC1 10.1021/jm0504353
CHEMBL206346 4060 None 7 Human Functional pIC50 = 7.9 7.9 - 1
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 235 7 2 2 3.0 C(CCc1cnc[nH]1)CCNC1CCCCC1 10.1021/jm0504353
155529365 171516 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human histamine H3 receptor stably expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human histamine H3 receptor stably expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 330 8 1 5 3.0 CCN(CC)CCCOc1ccc(-n2ccc(=O)c(O)c2C)cc1 10.1021/acs.jmedchem.9b00017
CHEMBL4462662 171516 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human histamine H3 receptor stably expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human histamine H3 receptor stably expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 330 8 1 5 3.0 CCN(CC)CCCOc1ccc(-n2ccc(=O)c(O)c2C)cc1 10.1021/acs.jmedchem.9b00017
1267 3804 None 32 Human Functional pIC50 = 6.9 6.9 -6 5
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2013.07.051
3035905 3804 None 32 Human Functional pIC50 = 6.9 6.9 -6 5
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2013.07.051
CHEMBL260374 3804 None 32 Human Functional pIC50 = 6.9 6.9 -6 5
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2013.07.051
72164593 92140 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assay
ChEMBL 333 4 2 2 4.4 O=C(Nc1ccc(CN2CCCCC2)cc1)c1c[nH]c2ccccc12 10.1016/j.bmc.2013.07.051
CHEMBL2419569 92140 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assay
ChEMBL 333 4 2 2 4.4 O=C(Nc1ccc(CN2CCCCC2)cc1)c1c[nH]c2ccccc12 10.1016/j.bmc.2013.07.051
52942843 18233 None 0 Mouse Functional pIC50 = 6.9 6.9 -61 2
Antagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 297 3 1 2 3.9 CC1CC(O)(CCc2ccc3ccccc3c2)C(C)CN1C 10.1016/j.bmcl.2010.08.099
CHEMBL1270165 18233 None 0 Mouse Functional pIC50 = 6.9 6.9 -61 2
Antagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 297 3 1 2 3.9 CC1CC(O)(CCc2ccc3ccccc3c2)C(C)CN1C 10.1016/j.bmcl.2010.08.099
155544839 175047 None 0 Human Functional pIC50 = 4.9 4.9 -2 2
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 284 2 1 5 3.1 CC1CCCc2c(-c3ccc([N+](=O)[O-])cc3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
CHEMBL4565419 175047 None 0 Human Functional pIC50 = 4.9 4.9 -2 2
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 284 2 1 5 3.1 CC1CCCc2c(-c3ccc([N+](=O)[O-])cc3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
155544839 175047 None 0 Human Functional pIC50 = 4.9 4.9 -2 2
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 284 2 1 5 3.1 CC1CCCc2c(-c3ccc([N+](=O)[O-])cc3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
CHEMBL4565419 175047 None 0 Human Functional pIC50 = 4.9 4.9 -2 2
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 284 2 1 5 3.1 CC1CCCc2c(-c3ccc([N+](=O)[O-])cc3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
72546764 102593 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 336 9 1 2 4.0 O=C(CCCN1CCCCC1)NCCCCc1ccc(Cl)cc1 10.1016/j.bmcl.2013.09.052
CHEMBL2441947 102593 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 336 9 1 2 4.0 O=C(CCCN1CCCCC1)NCCCCc1ccc(Cl)cc1 10.1016/j.bmcl.2013.09.052
CHEMBL3040649 102593 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 336 9 1 2 4.0 O=C(CCCN1CCCCC1)NCCCCc1ccc(Cl)cc1 10.1016/j.bmcl.2013.09.052
72547016 102610 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 370 9 1 2 4.4 O=C(CCCN1CCCCC1)NCCCCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2013.09.052
CHEMBL2441948 102610 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 370 9 1 2 4.4 O=C(CCCN1CCCCC1)NCCCCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2013.09.052
CHEMBL3040708 102610 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 370 9 1 2 4.4 O=C(CCCN1CCCCC1)NCCCCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2013.09.052
72546517 102603 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 340 6 2 4 2.7 CN1CCN(CCCSC(=N)NCc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2013.09.052
CHEMBL2441936 102603 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 340 6 2 4 2.7 CN1CCN(CCCSC(=N)NCc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2013.09.052
CHEMBL3040671 102603 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 340 6 2 4 2.7 CN1CCN(CCCSC(=N)NCc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2013.09.052
57391869 63140 None 0 Guinea pig Functional pIC50 = 6.9 6.9 - 1
Antagonist activity against histamine H3 receptor in guinea pig ileum assessed as inhibition of electrically-evoked twitches after 30 mins in presence of (R)-alpha-methyl-histamineAntagonist activity against histamine H3 receptor in guinea pig ileum assessed as inhibition of electrically-evoked twitches after 30 mins in presence of (R)-alpha-methyl-histamine
ChEMBL 223 6 2 3 1.6 CC=CCNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
CHEMBL1774589 63140 None 0 Guinea pig Functional pIC50 = 6.9 6.9 - 1
Antagonist activity against histamine H3 receptor in guinea pig ileum assessed as inhibition of electrically-evoked twitches after 30 mins in presence of (R)-alpha-methyl-histamineAntagonist activity against histamine H3 receptor in guinea pig ileum assessed as inhibition of electrically-evoked twitches after 30 mins in presence of (R)-alpha-methyl-histamine
ChEMBL 223 6 2 3 1.6 CC=CCNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
CHEMBL1789349 63140 None 0 Guinea pig Functional pIC50 = 6.9 6.9 - 1
Antagonist activity against histamine H3 receptor in guinea pig ileum assessed as inhibition of electrically-evoked twitches after 30 mins in presence of (R)-alpha-methyl-histamineAntagonist activity against histamine H3 receptor in guinea pig ileum assessed as inhibition of electrically-evoked twitches after 30 mins in presence of (R)-alpha-methyl-histamine
ChEMBL 223 6 2 3 1.6 CC=CCNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
155559319 174967 None 0 Human Functional pIC50 = 5.9 5.9 -13 2
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 239 1 1 3 3.2 CC1CCCc2c(-c3ccccc3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
CHEMBL4563363 174967 None 0 Human Functional pIC50 = 5.9 5.9 -13 2
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 239 1 1 3 3.2 CC1CCCc2c(-c3ccccc3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
57394133 69366 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assayAntagonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assay
ChEMBL 347 5 2 5 3.8 Nc1nc2ccccc2nc1CNc1ccc(CN2CCCCC2)cc1 10.1016/j.bmc.2011.09.061
CHEMBL1929412 69366 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assayAntagonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assay
ChEMBL 347 5 2 5 3.8 Nc1nc2ccccc2nc1CNc1ccc(CN2CCCCC2)cc1 10.1016/j.bmc.2011.09.061
76329185 105940 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 410 2 0 3 2.9 O=C(c1ccccc1)N1CCC2(CC1)CCN(C(=O)N1CCN(C3CCC3)CC1)C2 10.1021/jm4014828
CHEMBL3127693 105940 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 410 2 0 3 2.9 O=C(c1ccccc1)N1CCC2(CC1)CCN(C(=O)N1CCN(C3CCC3)CC1)C2 10.1021/jm4014828
155559319 174967 None 0 Human Functional pIC50 = 5.9 5.9 -13 2
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 239 1 1 3 3.2 CC1CCCc2c(-c3ccccc3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
CHEMBL4563363 174967 None 0 Human Functional pIC50 = 5.9 5.9 -13 2
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 239 1 1 3 3.2 CC1CCCc2c(-c3ccccc3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
52941061 18200 None 0 Mouse Functional pIC50 = 5.9 5.9 -32 2
Antagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 293 0 1 2 3.3 C[C@H]1C[C@](O)(C#Cc2cccc3ccccc23)[C@H](C)CN1C 10.1016/j.bmcl.2010.08.099
CHEMBL1269950 18200 None 0 Mouse Functional pIC50 = 5.9 5.9 -32 2
Antagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 293 0 1 2 3.3 C[C@H]1C[C@](O)(C#Cc2cccc3ccccc23)[C@H](C)CN1C 10.1016/j.bmcl.2010.08.099
9119245 92142 None 2 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assay
ChEMBL 333 5 2 2 3.9 O=C(Cc1c[nH]c2ccccc12)Nc1ccc(CN2CCCC2)cc1 10.1016/j.bmc.2013.07.051
CHEMBL2419571 92142 None 2 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assay
ChEMBL 333 5 2 2 3.9 O=C(Cc1c[nH]c2ccccc12)Nc1ccc(CN2CCCC2)cc1 10.1016/j.bmc.2013.07.051
44159044 15925 None 0 Rat Functional pIC50 = 6.9 6.9 -3 2
Antagonist activity at rat histamine H3 receptorAntagonist activity at rat histamine H3 receptor
ChEMBL 442 6 0 7 4.1 c1ccc(Cn2nnnc2C(c2ccc3occc3c2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
CHEMBL1223237 15925 None 0 Rat Functional pIC50 = 6.9 6.9 -3 2
Antagonist activity at rat histamine H3 receptorAntagonist activity at rat histamine H3 receptor
ChEMBL 442 6 0 7 4.1 c1ccc(Cn2nnnc2C(c2ccc3occc3c2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
52945858 18235 None 0 Human Functional pIC50 = 7.9 7.9 24 2
Antagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 309 3 1 2 4.0 CC1CN2CCCC2CC1(O)CCc1cccc2ccccc12 10.1016/j.bmcl.2010.08.099
CHEMBL1270167 18235 None 0 Human Functional pIC50 = 7.9 7.9 24 2
Antagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 309 3 1 2 4.0 CC1CN2CCCC2CC1(O)CCc1cccc2ccccc12 10.1016/j.bmcl.2010.08.099
23151337 184301 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 390 4 0 6 3.5 Cc1nc2cccnc2c(=O)n1-c1ccc(OC2CCN(C3CCC3)CC2)cc1 10.1021/jm800569w
CHEMBL483194 184301 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 390 4 0 6 3.5 Cc1nc2cccnc2c(=O)n1-c1ccc(OC2CCN(C3CCC3)CC2)cc1 10.1021/jm800569w
11581640 191917 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 377 4 0 5 3.9 Cc1nc2ccccc2c(=O)n1-c1ccc(OC2CCN(C(C)C)CC2)cc1 10.1021/jm800569w
CHEMBL519839 191917 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 377 4 0 5 3.9 Cc1nc2ccccc2c(=O)n1-c1ccc(OC2CCN(C(C)C)CC2)cc1 10.1021/jm800569w
49865449 15975 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 446 8 0 7 3.8 CCOc1ccc(C(c2nnnn2Cc2ccccc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
CHEMBL1223379 15975 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 446 8 0 7 3.8 CCOc1ccc(C(c2nnnn2Cc2ccccc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
76329182 105925 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 377 3 0 4 2.6 CC(C)N1CCCN(C(=O)C2CC3(CCN(C4CCOCC4)CC3)C2)CC1 10.1021/jm4014828
CHEMBL3127678 105925 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 377 3 0 4 2.6 CC(C)N1CCCN(C(=O)C2CC3(CCN(C4CCOCC4)CC3)C2)CC1 10.1021/jm4014828
127036598 137570 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at recombinant human H3 receptor expressed on CHO-K1 cells assessed as cAMP level by luciferase gene reporter assayAntagonist activity at recombinant human H3 receptor expressed on CHO-K1 cells assessed as cAMP level by luciferase gene reporter assay
ChEMBL 399 5 0 4 3.4 CC(C)N1CCC(Oc2ccc3c(c2)CCN(C2CCN(C(C)C)C2)C3=O)CC1 10.1016/j.ejmech.2015.12.005
CHEMBL3753901 137570 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at recombinant human H3 receptor expressed on CHO-K1 cells assessed as cAMP level by luciferase gene reporter assayAntagonist activity at recombinant human H3 receptor expressed on CHO-K1 cells assessed as cAMP level by luciferase gene reporter assay
ChEMBL 399 5 0 4 3.4 CC(C)N1CCC(Oc2ccc3c(c2)CCN(C2CCN(C(C)C)C2)C3=O)CC1 10.1016/j.ejmech.2015.12.005
164609531 184586 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human H3 receptor by TR-FRET assayAntagonist activity at human H3 receptor by TR-FRET assay
ChEMBL 388 7 1 4 5.4 Oc1cccc2ccc(/C=C/c3ccc(OCCCN4CCCCC4)cc3)nc12 10.1016/j.bmc.2021.116306
CHEMBL4847024 184586 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human H3 receptor by TR-FRET assayAntagonist activity at human H3 receptor by TR-FRET assay
ChEMBL 388 7 1 4 5.4 Oc1cccc2ccc(/C=C/c3ccc(OCCCN4CCCCC4)cc3)nc12 10.1016/j.bmc.2021.116306
71625481 90565 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 341 7 2 3 4.3 Cc1cccc(NC(=O)Nc2ccc(OCCCN(C)C)cc2)c1C 10.1016/j.bmcl.2013.03.080
CHEMBL2387296 90565 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 341 7 2 3 4.3 Cc1cccc(NC(=O)Nc2ccc(OCCCN(C)C)cc2)c1C 10.1016/j.bmcl.2013.03.080
76314723 105929 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 378 2 0 4 2.1 CC(C)N1CCN(C(=O)N2CCC3(CCCN(C4CCOCC4)C3)C2)CC1 10.1021/jm4014828
CHEMBL3127682 105929 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 378 2 0 4 2.1 CC(C)N1CCN(C(=O)N2CCC3(CCCN(C4CCOCC4)C3)C2)CC1 10.1021/jm4014828
25118474 105952 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 384 3 0 5 2.0 O=C(C1CC12CCN(C1CCOCC1)CC2)N1CCN(c2ccncc2)CC1 10.1021/jm4014828
CHEMBL3127705 105952 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 384 3 0 5 2.0 O=C(C1CC12CCN(C1CCOCC1)CC2)N1CCN(c2ccncc2)CC1 10.1021/jm4014828
1267 3804 None 32 Human Functional pIC50 = 6.9 6.9 -6 5
Inverse agonist activity at recombinant human Histamine 3 receptor expressed in CHO-K1 cells assessed as inhibition of RAMH-induced agonist activity preincubated for 20 mins and measured after 60 mins by [35S]-GTPgammaS binding assayInverse agonist activity at recombinant human Histamine 3 receptor expressed in CHO-K1 cells assessed as inhibition of RAMH-induced agonist activity preincubated for 20 mins and measured after 60 mins by [35S]-GTPgammaS binding assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.8b01280
3035905 3804 None 32 Human Functional pIC50 = 6.9 6.9 -6 5
Inverse agonist activity at recombinant human Histamine 3 receptor expressed in CHO-K1 cells assessed as inhibition of RAMH-induced agonist activity preincubated for 20 mins and measured after 60 mins by [35S]-GTPgammaS binding assayInverse agonist activity at recombinant human Histamine 3 receptor expressed in CHO-K1 cells assessed as inhibition of RAMH-induced agonist activity preincubated for 20 mins and measured after 60 mins by [35S]-GTPgammaS binding assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.8b01280
CHEMBL260374 3804 None 32 Human Functional pIC50 = 6.9 6.9 -6 5
Inverse agonist activity at recombinant human Histamine 3 receptor expressed in CHO-K1 cells assessed as inhibition of RAMH-induced agonist activity preincubated for 20 mins and measured after 60 mins by [35S]-GTPgammaS binding assayInverse agonist activity at recombinant human Histamine 3 receptor expressed in CHO-K1 cells assessed as inhibition of RAMH-induced agonist activity preincubated for 20 mins and measured after 60 mins by [35S]-GTPgammaS binding assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.8b01280
49865289 15892 None 0 Human Functional pIC50 = 4.9 4.9 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 449 6 0 7 2.7 CN1CCC(N2CCN(C(c3ccc(F)cc3)c3nnnn3Cc3ccccc3)CC2)CC1 10.1016/j.bmcl.2010.07.009
CHEMBL1223156 15892 None 0 Human Functional pIC50 = 4.9 4.9 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 449 6 0 7 2.7 CN1CCC(N2CCN(C(c3ccc(F)cc3)c3nnnn3Cc3ccccc3)CC2)CC1 10.1016/j.bmcl.2010.07.009
71625595 90568 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 335 6 2 3 3.5 CN(C)CCOc1ccc(NC(=O)Nc2ccc(F)cc2F)cc1 10.1016/j.bmcl.2013.03.080
CHEMBL2387299 90568 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 335 6 2 3 3.5 CN(C)CCOc1ccc(NC(=O)Nc2ccc(F)cc2F)cc1 10.1016/j.bmcl.2013.03.080
118737699 119171 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
ChEMBL 476 10 1 4 5.6 COC(=O)CCCC(=O)NC1(c2ccc(-c3ccc(CCN4CCC[C@H]4C)cc3)cc2)CCCC1 10.1021/acsmedchemlett.5b00002
CHEMBL3427237 119171 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
ChEMBL 476 10 1 4 5.6 COC(=O)CCCC(=O)NC1(c2ccc(-c3ccc(CCN4CCC[C@H]4C)cc3)cc2)CCCC1 10.1021/acsmedchemlett.5b00002
72546761 102599 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 401 9 2 3 5.2 N=C(NCCCCc1ccc(C(F)(F)F)cc1)SCCCN1CCCCC1 10.1016/j.bmcl.2013.09.052
CHEMBL2441944 102599 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 401 9 2 3 5.2 N=C(NCCCCc1ccc(C(F)(F)F)cc1)SCCCN1CCCCC1 10.1016/j.bmcl.2013.09.052
CHEMBL3040666 102599 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 401 9 2 3 5.2 N=C(NCCCCc1ccc(C(F)(F)F)cc1)SCCCN1CCCCC1 10.1016/j.bmcl.2013.09.052
73348063 102612 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 327 6 2 4 2.8 N=C(NCc1ccc(Cl)cc1)SCCCN1CCOCC1 10.1016/j.bmcl.2013.09.052
CHEMBL2441934 102612 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 327 6 2 4 2.8 N=C(NCc1ccc(Cl)cc1)SCCCN1CCOCC1 10.1016/j.bmcl.2013.09.052
CHEMBL3040711 102612 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 327 6 2 4 2.8 N=C(NCc1ccc(Cl)cc1)SCCCN1CCOCC1 10.1016/j.bmcl.2013.09.052
164611458 185350 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human H3 receptor by TR-FRET assayAntagonist activity at human H3 receptor by TR-FRET assay
ChEMBL 374 7 1 4 5.0 Oc1cccc2ccc(/C=C/c3ccc(OCCCN4CCCC4)cc3)nc12 10.1016/j.bmc.2021.116306
CHEMBL4858290 185350 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human H3 receptor by TR-FRET assayAntagonist activity at human H3 receptor by TR-FRET assay
ChEMBL 374 7 1 4 5.0 Oc1cccc2ccc(/C=C/c3ccc(OCCCN4CCCC4)cc3)nc12 10.1016/j.bmc.2021.116306
1267 3804 None 32 Human Functional pIC50 = 7.8 7.8 -6 5
Antagonist activity at human H3 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assayAntagonist activity at human H3 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm0603318
3035905 3804 None 32 Human Functional pIC50 = 7.8 7.8 -6 5
Antagonist activity at human H3 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assayAntagonist activity at human H3 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm0603318
CHEMBL260374 3804 None 32 Human Functional pIC50 = 7.8 7.8 -6 5
Antagonist activity at human H3 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assayAntagonist activity at human H3 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm0603318
25118476 105918 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 409 5 0 3 3.8 O=C(C1CC12CCN(CCc1ccccc1)CC2)N1CCN(C2CCCCC2)CC1 10.1021/jm4014828
CHEMBL3127670 105918 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 409 5 0 3 3.8 O=C(C1CC12CCN(CCc1ccccc1)CC2)N1CCN(C2CCCCC2)CC1 10.1021/jm4014828
71625482 90566 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 333 6 2 3 3.9 CN(C)CCOc1ccc(NC(=O)Nc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2013.03.080
CHEMBL2387297 90566 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 333 6 2 3 3.9 CN(C)CCOc1ccc(NC(=O)Nc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2013.03.080
164609802 185322 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human H3 receptor by TR-FRET assayAntagonist activity at human H3 receptor by TR-FRET assay
ChEMBL 343 9 1 5 3.6 CCN(CC)CCCOc1ccc(/C=C/c2cc(=O)c(O)co2)cc1 10.1016/j.bmc.2021.116306
CHEMBL4857779 185322 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human H3 receptor by TR-FRET assayAntagonist activity at human H3 receptor by TR-FRET assay
ChEMBL 343 9 1 5 3.6 CCN(CC)CCCOc1ccc(/C=C/c2cc(=O)c(O)co2)cc1 10.1016/j.bmc.2021.116306
44579547 187123 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 364 4 0 3 3.0 CN(CCN1CCCCC1)C(=O)N1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2008.07.125
CHEMBL490786 187123 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 364 4 0 3 3.0 CN(CCN1CCCCC1)C(=O)N1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2008.07.125
2232766 161465 None 4 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human H3 receptor expressed in HEK293 cells assessed as inhibition of RAMH-induced reduction of forskolin-stimulated cAMP accumulation after 30 mins by Ulight-based TR-FRET assayAntagonist activity at human H3 receptor expressed in HEK293 cells assessed as inhibition of RAMH-induced reduction of forskolin-stimulated cAMP accumulation after 30 mins by Ulight-based TR-FRET assay
ChEMBL 297 7 0 2 4.9 c1ccc2c(OCCCCCN3CCCCC3)cccc2c1 10.1016/j.bmc.2018.04.023
CHEMBL4126145 161465 None 4 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human H3 receptor expressed in HEK293 cells assessed as inhibition of RAMH-induced reduction of forskolin-stimulated cAMP accumulation after 30 mins by Ulight-based TR-FRET assayAntagonist activity at human H3 receptor expressed in HEK293 cells assessed as inhibition of RAMH-induced reduction of forskolin-stimulated cAMP accumulation after 30 mins by Ulight-based TR-FRET assay
ChEMBL 297 7 0 2 4.9 c1ccc2c(OCCCCCN3CCCCC3)cccc2c1 10.1016/j.bmc.2018.04.023
162645948 179707 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 371 7 0 6 2.2 COc1c(C)n(-c2ccc(OCCCN3CCN(C)CC3)cc2)ccc1=O 10.1016/j.ejmech.2020.113096
CHEMBL4742244 179707 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 371 7 0 6 2.2 COc1c(C)n(-c2ccc(OCCCN3CCN(C)CC3)cc2)ccc1=O 10.1016/j.ejmech.2020.113096
52943448 18215 None 0 Human Functional pIC50 = 7.8 7.8 28 2
Antagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 297 3 1 2 3.9 CC1CC(O)(CCc2cccc3ccccc23)C(C)CN1C 10.1016/j.bmcl.2010.08.099
CHEMBL1270058 18215 None 0 Human Functional pIC50 = 7.8 7.8 28 2
Antagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 297 3 1 2 3.9 CC1CC(O)(CCc2cccc3ccccc23)C(C)CN1C 10.1016/j.bmcl.2010.08.099
16082828 80291 None 0 Human Functional pIC50 = 7.8 7.8 6 3
Antagonist activity at human H3 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assayAntagonist activity at human H3 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assay
ChEMBL 275 6 2 2 3.3 Clc1ccc(CNCC[C@@H]2C[C@H]2c2c[nH]cn2)cc1 10.1021/jm0603318
CHEMBL213886 80291 None 0 Human Functional pIC50 = 7.8 7.8 6 3
Antagonist activity at human H3 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assayAntagonist activity at human H3 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assay
ChEMBL 275 6 2 2 3.3 Clc1ccc(CNCC[C@@H]2C[C@H]2c2c[nH]cn2)cc1 10.1021/jm0603318
44159170 15953 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 402 6 0 6 3.4 c1ccc(Cn2nnnc2C(c2ccccc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
CHEMBL1223311 15953 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 402 6 0 6 3.4 c1ccc(Cn2nnnc2C(c2ccccc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
76314726 105951 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 375 3 0 4 2.4 O=C(C1CC12CCN(C1CCOCC1)CC2)N1CCCN(C2CCC2)CC1 10.1021/jm4014828
CHEMBL3127704 105951 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 375 3 0 4 2.4 O=C(C1CC12CCN(C1CCOCC1)CC2)N1CCCN(C2CCC2)CC1 10.1021/jm4014828
44160248 15893 None 0 Rat Functional pIC50 = 7.8 7.8 -10 2
Antagonist activity at rat histamine H3 receptorAntagonist activity at rat histamine H3 receptor
ChEMBL 480 7 0 8 2.8 CS(=O)(=O)c1ccc(C(c2nnnn2Cc2ccccc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
CHEMBL1223157 15893 None 0 Rat Functional pIC50 = 7.8 7.8 -10 2
Antagonist activity at rat histamine H3 receptorAntagonist activity at rat histamine H3 receptor
ChEMBL 480 7 0 8 2.8 CS(=O)(=O)c1ccc(C(c2nnnn2Cc2ccccc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
44159640 15924 None 0 Rat Functional pIC50 = 7.8 7.8 -3 2
Antagonist activity at rat histamine H3 receptorAntagonist activity at rat histamine H3 receptor
ChEMBL 483 8 0 9 3.0 c1ccc(Cn2nnnc2C(c2ccc(Cn3cncn3)cc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
CHEMBL1223236 15924 None 0 Rat Functional pIC50 = 7.8 7.8 -3 2
Antagonist activity at rat histamine H3 receptorAntagonist activity at rat histamine H3 receptor
ChEMBL 483 8 0 9 3.0 c1ccc(Cn2nnnc2C(c2ccc(Cn3cncn3)cc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
54765288 69361 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Inverse agonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assayInverse agonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assay
ChEMBL 361 4 2 5 3.5 Nc1nc2ccccc2nc1NC(=O)c1ccc(CN2CCCCC2)cc1 10.1016/j.bmc.2011.09.061
CHEMBL1929400 69361 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Inverse agonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assayInverse agonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assay
ChEMBL 361 4 2 5 3.5 Nc1nc2ccccc2nc1NC(=O)c1ccc(CN2CCCCC2)cc1 10.1016/j.bmc.2011.09.061
CHEMBL1929401 69361 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Inverse agonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assayInverse agonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assay
ChEMBL 361 4 2 5 3.5 Nc1nc2ccccc2nc1NC(=O)c1ccc(CN2CCCCC2)cc1 10.1016/j.bmc.2011.09.061
49865112 15829 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 366 5 1 6 2.2 C[C@@H]1CN(C(c2ccc(F)cc2)c2nnnn2Cc2ccccc2)CCN1 10.1016/j.bmcl.2010.07.009
CHEMBL1222948 15829 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 366 5 1 6 2.2 C[C@@H]1CN(C(c2ccc(F)cc2)c2nnnn2Cc2ccccc2)CCN1 10.1016/j.bmcl.2010.07.009
164625990 186578 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human H3 receptor by TR-FRET assayAntagonist activity at human H3 receptor by TR-FRET assay
ChEMBL 370 7 1 6 2.5 CN1CCN(CCCOc2ccc(/C=C/c3cc(=O)c(O)co3)cc2)CC1 10.1016/j.bmc.2021.116306
CHEMBL4876778 186578 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human H3 receptor by TR-FRET assayAntagonist activity at human H3 receptor by TR-FRET assay
ChEMBL 370 7 1 6 2.5 CN1CCN(CCCOc2ccc(/C=C/c3cc(=O)c(O)co3)cc2)CC1 10.1016/j.bmc.2021.116306
162651994 180361 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 328 6 0 5 2.6 COc1c(C)n(-c2ccc(OCCN3CCCC3)cc2)ccc1=O 10.1016/j.ejmech.2020.113096
CHEMBL4750326 180361 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 328 6 0 5 2.6 COc1c(C)n(-c2ccc(OCCN3CCCC3)cc2)ccc1=O 10.1016/j.ejmech.2020.113096
76314725 105943 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 438 2 0 3 3.7 O=C(c1ccccc1)N1CCC2(CCCN(C(=O)N3CCCN(C4CCC4)CC3)C2)CC1 10.1021/jm4014828
CHEMBL3127696 105943 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 438 2 0 3 3.7 O=C(c1ccccc1)N1CCC2(CCCN(C(=O)N3CCCN(C4CCC4)CC3)C2)CC1 10.1021/jm4014828
11682779 189035 None 6 Human Functional pIC50 = 7.8 7.8 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 400 5 0 5 3.2 COc1ccc2c(c1)[C@]1(CC[C@@H](C(=O)N(C)CCN3CCCCC3)CC1)OC2=O 10.1016/j.bmcl.2008.07.125
CHEMBL507921 189035 None 6 Human Functional pIC50 = 7.8 7.8 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 400 5 0 5 3.2 COc1ccc2c(c1)[C@]1(CC[C@@H](C(=O)N(C)CCN3CCCCC3)CC1)OC2=O 10.1016/j.bmcl.2008.07.125
72164839 92147 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assay
ChEMBL 319 6 2 2 4.4 c1ccc2c(CCNc3ccc(CN4CCCC4)cc3)c[nH]c2c1 10.1016/j.bmc.2013.07.051
CHEMBL2419580 92147 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assay
ChEMBL 319 6 2 2 4.4 c1ccc2c(CCNc3ccc(CN4CCCC4)cc3)c[nH]c2c1 10.1016/j.bmc.2013.07.051
57392413 69363 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assayAntagonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assay
ChEMBL 365 9 2 6 3.5 CCN(CC)Cc1ccc(OCCNc2nc3ccccc3nc2N)cc1 10.1016/j.bmc.2011.09.061
CHEMBL1929407 69363 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assayAntagonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assay
ChEMBL 365 9 2 6 3.5 CCN(CC)Cc1ccc(OCCNc2nc3ccccc3nc2N)cc1 10.1016/j.bmc.2011.09.061
49865171 15846 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 390 6 0 6 2.2 C#CCN1CCN(C(c2ccc(F)cc2)c2nnnn2Cc2ccccc2)CC1 10.1016/j.bmcl.2010.07.009
CHEMBL1223010 15846 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 390 6 0 6 2.2 C#CCN1CCN(C(c2ccc(F)cc2)c2nnnn2Cc2ccccc2)CC1 10.1016/j.bmcl.2010.07.009
54765288 69361 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Inverse agonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assayInverse agonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assay
ChEMBL 361 4 2 5 3.5 Nc1nc2ccccc2nc1NC(=O)c1ccc(CN2CCCCC2)cc1 10.1016/j.bmc.2011.09.061
CHEMBL1929400 69361 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Inverse agonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assayInverse agonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assay
ChEMBL 361 4 2 5 3.5 Nc1nc2ccccc2nc1NC(=O)c1ccc(CN2CCCCC2)cc1 10.1016/j.bmc.2011.09.061
CHEMBL1929401 69361 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Inverse agonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assayInverse agonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assay
ChEMBL 361 4 2 5 3.5 Nc1nc2ccccc2nc1NC(=O)c1ccc(CN2CCCCC2)cc1 10.1016/j.bmc.2011.09.061
49865396 15951 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 468 8 0 7 4.0 FC(F)Oc1ccccc1C(c1nnnn1Cc1ccccc1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.07.009
CHEMBL1223309 15951 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 468 8 0 7 4.0 FC(F)Oc1ccccc1C(c1nnnn1Cc1ccccc1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.07.009
49865489 15994 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 445 7 1 7 2.5 NC(=O)c1ccc(C(c2nnnn2Cc2ccccc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
CHEMBL1223450 15994 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 445 7 1 7 2.5 NC(=O)c1ccc(C(c2nnnn2Cc2ccccc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
25118124 105946 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 347 3 0 4 1.6 O=C(C1CC12CCN(C1CCOCC1)CC2)N1CCN(C2CC2)CC1 10.1021/jm4014828
CHEMBL3127699 105946 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 347 3 0 4 1.6 O=C(C1CC12CCN(C1CCOCC1)CC2)N1CCN(C2CC2)CC1 10.1021/jm4014828
25118479 105956 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 347 3 0 3 3.0 CC(C)N1CCC2(CC1)CC2C(=O)N1CCN(C2CCCCC2)CC1 10.1021/jm4014828
CHEMBL3127709 105956 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 347 3 0 3 3.0 CC(C)N1CCC2(CC1)CC2C(=O)N1CCN(C2CCCCC2)CC1 10.1021/jm4014828
73357179 102592 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 311 6 2 3 3.6 N=C(NCc1ccc(Cl)cc1)SCCCN1CCCC1 10.1016/j.bmcl.2013.09.052
CHEMBL2441933 102592 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 311 6 2 3 3.6 N=C(NCc1ccc(Cl)cc1)SCCCN1CCCC1 10.1016/j.bmcl.2013.09.052
CHEMBL3040646 102592 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 311 6 2 3 3.6 N=C(NCc1ccc(Cl)cc1)SCCCN1CCCC1 10.1016/j.bmcl.2013.09.052
1267 3804 None 32 Human Functional pIC50 = 7.7 7.7 -6 5
Inverse agonist activity at human H3R expressed in HEK293T-SP-FLAG-hH3R-CRE-CBR cells assessed as reduction in histamine-induced inhibition of forskolin stimulated luciferase activity by luciferase reporter gene assayInverse agonist activity at human H3R expressed in HEK293T-SP-FLAG-hH3R-CRE-CBR cells assessed as reduction in histamine-induced inhibition of forskolin stimulated luciferase activity by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
3035905 3804 None 32 Human Functional pIC50 = 7.7 7.7 -6 5
Inverse agonist activity at human H3R expressed in HEK293T-SP-FLAG-hH3R-CRE-CBR cells assessed as reduction in histamine-induced inhibition of forskolin stimulated luciferase activity by luciferase reporter gene assayInverse agonist activity at human H3R expressed in HEK293T-SP-FLAG-hH3R-CRE-CBR cells assessed as reduction in histamine-induced inhibition of forskolin stimulated luciferase activity by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
CHEMBL260374 3804 None 32 Human Functional pIC50 = 7.7 7.7 -6 5
Inverse agonist activity at human H3R expressed in HEK293T-SP-FLAG-hH3R-CRE-CBR cells assessed as reduction in histamine-induced inhibition of forskolin stimulated luciferase activity by luciferase reporter gene assayInverse agonist activity at human H3R expressed in HEK293T-SP-FLAG-hH3R-CRE-CBR cells assessed as reduction in histamine-induced inhibition of forskolin stimulated luciferase activity by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
52941024 18216 None 0 Human Functional pIC50 = 8.7 8.7 42 2
Antagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 297 3 1 2 3.9 C[C@H]1CN(C)[C@H](C)C[C@@]1(O)CCc1cccc2ccccc12 10.1016/j.bmcl.2010.08.099
CHEMBL1270059 18216 None 0 Human Functional pIC50 = 8.7 8.7 42 2
Antagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 297 3 1 2 3.9 C[C@H]1CN(C)[C@H](C)C[C@@]1(O)CCc1cccc2ccccc12 10.1016/j.bmcl.2010.08.099
52942843 18233 None 0 Human Functional pIC50 = 8.7 8.7 61 2
Antagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 297 3 1 2 3.9 CC1CC(O)(CCc2ccc3ccccc3c2)C(C)CN1C 10.1016/j.bmcl.2010.08.099
CHEMBL1270165 18233 None 0 Human Functional pIC50 = 8.7 8.7 61 2
Antagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 297 3 1 2 3.9 CC1CC(O)(CCc2ccc3ccccc3c2)C(C)CN1C 10.1016/j.bmcl.2010.08.099
23151208 184521 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 390 4 0 6 3.5 Cc1nc2ccncc2c(=O)n1-c1ccc(OC2CCN(C3CCC3)CC2)cc1 10.1021/jm800569w
CHEMBL484610 184521 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 390 4 0 6 3.5 Cc1nc2ccncc2c(=O)n1-c1ccc(OC2CCN(C3CCC3)CC2)cc1 10.1021/jm800569w
78320092 160065 None 0 Human Functional pIC50 = 8.7 8.7 - 1
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
ChEMBL 464 9 1 4 5.2 C[C@H](NC(=O)CCc1ccc(-c2ccc(CCN3CCC[C@H]3C)cc2)cc1)C(=O)OC(C)(C)C nan
CHEMBL4107566 160065 None 0 Human Functional pIC50 = 8.7 8.7 - 1
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
ChEMBL 464 9 1 4 5.2 C[C@H](NC(=O)CCc1ccc(-c2ccc(CCN3CCC[C@H]3C)cc2)cc1)C(=O)OC(C)(C)C nan
78321034 160624 None 0 Human Functional pIC50 = 8.7 8.7 - 1
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
ChEMBL 462 10 2 3 5.2 C[C@@H]1CCCN1CCc1ccc(-c2ccc(C3(C(=O)NCCCC(=O)O)CCCC3)cc2)cc1 nan
CHEMBL4112348 160624 None 0 Human Functional pIC50 = 8.7 8.7 - 1
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
ChEMBL 462 10 2 3 5.2 C[C@@H]1CCCN1CCc1ccc(-c2ccc(C3(C(=O)NCCCC(=O)O)CCCC3)cc2)cc1 nan
118737698 119170 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
ChEMBL 464 9 1 4 5.0 C[C@@H](C(=O)NCCc1ccc(-c2ccc(CCN3CCC[C@H]3C)cc2)cc1)C(=O)OC(C)(C)C 10.1021/acsmedchemlett.5b00002
CHEMBL3427236 119170 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
ChEMBL 464 9 1 4 5.0 C[C@@H](C(=O)NCCc1ccc(-c2ccc(CCN3CCC[C@H]3C)cc2)cc1)C(=O)OC(C)(C)C 10.1021/acsmedchemlett.5b00002
118737702 119175 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
ChEMBL 462 10 2 3 5.5 C[C@@H]1CCCN1CCc1ccc(-c2ccc(C3(NC(=O)CCCC(=O)O)CCCC3)cc2)cc1 10.1021/acsmedchemlett.5b00002
CHEMBL3427241 119175 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
ChEMBL 462 10 2 3 5.5 C[C@@H]1CCCN1CCc1ccc(-c2ccc(C3(NC(=O)CCCC(=O)O)CCCC3)cc2)cc1 10.1021/acsmedchemlett.5b00002
164627029 186549 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human H3 receptor by TR-FRET assayAntagonist activity at human H3 receptor by TR-FRET assay
ChEMBL 368 8 1 5 3.6 CCn1cc(O)c(=O)cc1/C=C/c1ccc(OCCCN2CCCC2)cc1 10.1016/j.bmc.2021.116306
CHEMBL4876429 186549 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human H3 receptor by TR-FRET assayAntagonist activity at human H3 receptor by TR-FRET assay
ChEMBL 368 8 1 5 3.6 CCn1cc(O)c(=O)cc1/C=C/c1ccc(OCCCN2CCCC2)cc1 10.1016/j.bmc.2021.116306
49865110 15827 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 420 6 0 6 3.5 C[C@@H]1CN(C(c2ccc(F)cc2)c2nnnn2Cc2ccccc2)CCN1C1CCC1 10.1016/j.bmcl.2010.07.009
CHEMBL1222946 15827 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 420 6 0 6 3.5 C[C@@H]1CN(C(c2ccc(F)cc2)c2nnnn2Cc2ccccc2)CCN1C1CCC1 10.1016/j.bmcl.2010.07.009
24951350 181470 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 431 6 0 5 4.6 Cc1nc2c(C(F)(F)F)cccc2c(=O)n1-c1ccc(OCCCN2CCCC2)cc1 10.1021/jm8003834
CHEMBL476322 181470 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 431 6 0 5 4.6 Cc1nc2c(C(F)(F)F)cccc2c(=O)n1-c1ccc(OCCCN2CCCC2)cc1 10.1021/jm8003834
11675333 181721 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 381 6 0 5 3.7 Cc1nc2cccc(F)c2c(=O)n1-c1ccc(OCCCN2CCCC2)cc1 10.1021/jm8003834
CHEMBL477356 181721 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 381 6 0 5 3.7 Cc1nc2cccc(F)c2c(=O)n1-c1ccc(OCCCN2CCCC2)cc1 10.1021/jm8003834
24951035 181722 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 377 6 0 5 3.9 Cc1nc2ccccc2c(=O)n1-c1ccc(OCCCN2CCC[C@@H]2C)cc1 10.1021/jm8003834
CHEMBL477360 181722 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 377 6 0 5 3.9 Cc1nc2ccccc2c(=O)n1-c1ccc(OCCCN2CCC[C@@H]2C)cc1 10.1021/jm8003834
25264263 90551 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 413 3 1 4 2.8 CC(=O)N1CCN(C(=O)Nc2ccc(N3CCC(N4CCCC4C)C3)c(C)c2)CC1 10.1016/j.bmcl.2013.03.080
CHEMBL2387283 90551 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 413 3 1 4 2.8 CC(=O)N1CCN(C(=O)Nc2ccc(N3CCC(N4CCCC4C)C3)c(C)c2)CC1 10.1016/j.bmcl.2013.03.080
23151248 181713 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 393 7 0 6 3.6 COc1ccc2c(=O)n(-c3ccc(OCCCN4CCCC4)cc3)c(C)nc2c1 10.1021/jm8003834
CHEMBL477201 181713 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 393 7 0 6 3.6 COc1ccc2c(=O)n(-c3ccc(OCCCN4CCCC4)cc3)c(C)nc2c1 10.1021/jm8003834
162669227 182887 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 368 5 0 5 3.6 COc1c(C)n(-c2ccc(OC3CCN(C4CCC4)CC3)cc2)ccc1=O 10.1016/j.ejmech.2020.113096
CHEMBL4790392 182887 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 368 5 0 5 3.6 COc1c(C)n(-c2ccc(OC3CCN(C4CCC4)CC3)cc2)ccc1=O 10.1016/j.ejmech.2020.113096
76286162 119161 None 0 Human Functional pIC50 = 8.6 8.6 - 1
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
ChEMBL 337 7 1 2 4.4 C[C@@H]1CCCN1CCc1ccc(-c2ccc(CCC(=O)O)cc2)cc1 nan
CHEMBL3427227 119161 None 0 Human Functional pIC50 = 8.6 8.6 - 1
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
ChEMBL 337 7 1 2 4.4 C[C@@H]1CCCN1CCc1ccc(-c2ccc(CCC(=O)O)cc2)cc1 nan
78321358 160285 None 0 Human Functional pIC50 = 8.6 8.6 - 1
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
ChEMBL 380 8 2 3 3.6 C[C@@H]1CCCN1CCc1ccc(-c2ccc(C(=O)NCCC(=O)O)cc2)cc1 nan
CHEMBL4109418 160285 None 0 Human Functional pIC50 = 8.6 8.6 - 1
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
ChEMBL 380 8 2 3 3.6 C[C@@H]1CCCN1CCc1ccc(-c2ccc(C(=O)NCCC(=O)O)cc2)cc1 nan
76286162 119161 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
ChEMBL 337 7 1 2 4.4 C[C@@H]1CCCN1CCc1ccc(-c2ccc(CCC(=O)O)cc2)cc1 10.1021/acsmedchemlett.5b00002
CHEMBL3427227 119161 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
ChEMBL 337 7 1 2 4.4 C[C@@H]1CCCN1CCc1ccc(-c2ccc(CCC(=O)O)cc2)cc1 10.1021/acsmedchemlett.5b00002
118737704 119178 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
ChEMBL 380 8 2 3 4.2 C[C@@H]1CCCN1CCc1ccc(-c2ccc(NC(=O)CCC(=O)O)cc2)cc1 10.1021/acsmedchemlett.5b00002
CHEMBL3427244 119178 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
ChEMBL 380 8 2 3 4.2 C[C@@H]1CCCN1CCc1ccc(-c2ccc(NC(=O)CCC(=O)O)cc2)cc1 10.1021/acsmedchemlett.5b00002
11452311 1882 None 6 Human Functional pIC50 = 8.6 8.6 - 1
Inverse agonist activity at human histamine H3 receptor by GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor by GTPgammaS binding assay
ChEMBL 398 3 0 4 3.3 CC(N1CCCN(CC1)C(=O)C1CCN(CC1)c1ccc(nc1)C(F)(F)F)C 10.1021/jm100064d
9103 1882 None 6 Human Functional pIC50 = 8.6 8.6 - 1
Inverse agonist activity at human histamine H3 receptor by GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor by GTPgammaS binding assay
ChEMBL 398 3 0 4 3.3 CC(N1CCCN(CC1)C(=O)C1CCN(CC1)c1ccc(nc1)C(F)(F)F)C 10.1021/jm100064d
CHEMBL2151157 1882 None 6 Human Functional pIC50 = 8.6 8.6 - 1
Inverse agonist activity at human histamine H3 receptor by GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor by GTPgammaS binding assay
ChEMBL 398 3 0 4 3.3 CC(N1CCCN(CC1)C(=O)C1CCN(CC1)c1ccc(nc1)C(F)(F)F)C 10.1021/jm100064d
164610977 185442 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human H3 receptor by TR-FRET assayAntagonist activity at human H3 receptor by TR-FRET assay
ChEMBL 369 7 1 5 4.1 Cc1oc(/C=C/c2ccc(OCCCN3CCCCC3)cc2)cc(=O)c1O 10.1016/j.bmc.2021.116306
CHEMBL4859825 185442 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human H3 receptor by TR-FRET assayAntagonist activity at human H3 receptor by TR-FRET assay
ChEMBL 369 7 1 5 4.1 Cc1oc(/C=C/c2ccc(OCCCN3CCCCC3)cc2)cc(=O)c1O 10.1016/j.bmc.2021.116306
76314724 105938 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 460 3 0 4 2.8 O=C(N1CCCN(C2CCC2)CC1)N1CCC2(CCN(S(=O)(=O)c3ccccc3)CC2)C1 10.1021/jm4014828
CHEMBL3127691 105938 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 460 3 0 4 2.8 O=C(N1CCCN(C2CCC2)CC1)N1CCC2(CCN(S(=O)(=O)c3ccccc3)CC2)C1 10.1021/jm4014828
164617396 184978 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human H3 receptor by TR-FRET assayAntagonist activity at human H3 receptor by TR-FRET assay
ChEMBL 355 7 1 5 3.8 O=c1cc(/C=C/c2ccc(OCCCN3CCCCC3)cc2)occ1O 10.1016/j.bmc.2021.116306
CHEMBL4852639 184978 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human H3 receptor by TR-FRET assayAntagonist activity at human H3 receptor by TR-FRET assay
ChEMBL 355 7 1 5 3.8 O=c1cc(/C=C/c2ccc(OCCCN3CCCCC3)cc2)occ1O 10.1016/j.bmc.2021.116306
52944686 18202 None 0 Human Functional pIC50 = 7.7 7.7 28 2
Antagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 295 2 1 2 3.9 CC1CC(O)(/C=C/c2cccc3ccccc23)C(C)CN1C 10.1016/j.bmcl.2010.08.099
CHEMBL1269952 18202 None 0 Human Functional pIC50 = 7.7 7.7 28 2
Antagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 295 2 1 2 3.9 CC1CC(O)(/C=C/c2cccc3ccccc23)C(C)CN1C 10.1016/j.bmcl.2010.08.099
24951037 169923 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 391 6 0 5 4.3 Cc1nc2ccccc2c(=O)n1-c1ccc(OCCCN2[C@H](C)CC[C@H]2C)cc1 10.1021/jm8003834
CHEMBL443958 169923 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 391 6 0 5 4.3 Cc1nc2ccccc2c(=O)n1-c1ccc(OCCCN2[C@H](C)CC[C@H]2C)cc1 10.1021/jm8003834
10232 3713 None 17 Human Functional pIC50 = 7.7 7.7 - 1
Inverse agonist activity at recombinant human Histamine 3 receptor expressed in CHO-K1 cells assessed as inhibition of RAMH-induced agonist activity preincubated for 20 mins and measured after 60 mins by [35S]-GTPgammaS binding assayInverse agonist activity at recombinant human Histamine 3 receptor expressed in CHO-K1 cells assessed as inhibition of RAMH-induced agonist activity preincubated for 20 mins and measured after 60 mins by [35S]-GTPgammaS binding assay
ChEMBL 373 6 1 5 2.4 O=C(Nc1ccc(cc1)OC1CCN(CC1)C1CCC1)CN1CCOCC1 10.1021/acs.jmedchem.8b01280
60151477 3713 None 17 Human Functional pIC50 = 7.7 7.7 - 1
Inverse agonist activity at recombinant human Histamine 3 receptor expressed in CHO-K1 cells assessed as inhibition of RAMH-induced agonist activity preincubated for 20 mins and measured after 60 mins by [35S]-GTPgammaS binding assayInverse agonist activity at recombinant human Histamine 3 receptor expressed in CHO-K1 cells assessed as inhibition of RAMH-induced agonist activity preincubated for 20 mins and measured after 60 mins by [35S]-GTPgammaS binding assay
ChEMBL 373 6 1 5 2.4 O=C(Nc1ccc(cc1)OC1CCN(CC1)C1CCC1)CN1CCOCC1 10.1021/acs.jmedchem.8b01280
60151477.0 3713 None 17 Human Functional pIC50 = 7.7 7.7 - 1
Inverse agonist activity at recombinant human Histamine 3 receptor expressed in CHO-K1 cells assessed as inhibition of RAMH-induced agonist activity preincubated for 20 mins and measured after 60 mins by [35S]-GTPgammaS binding assayInverse agonist activity at recombinant human Histamine 3 receptor expressed in CHO-K1 cells assessed as inhibition of RAMH-induced agonist activity preincubated for 20 mins and measured after 60 mins by [35S]-GTPgammaS binding assay
ChEMBL 373 6 1 5 2.4 O=C(Nc1ccc(cc1)OC1CCN(CC1)C1CCC1)CN1CCOCC1 10.1021/acs.jmedchem.8b01280
CHEMBL4297328 3713 None 17 Human Functional pIC50 = 7.7 7.7 - 1
Inverse agonist activity at recombinant human Histamine 3 receptor expressed in CHO-K1 cells assessed as inhibition of RAMH-induced agonist activity preincubated for 20 mins and measured after 60 mins by [35S]-GTPgammaS binding assayInverse agonist activity at recombinant human Histamine 3 receptor expressed in CHO-K1 cells assessed as inhibition of RAMH-induced agonist activity preincubated for 20 mins and measured after 60 mins by [35S]-GTPgammaS binding assay
ChEMBL 373 6 1 5 2.4 O=C(Nc1ccc(cc1)OC1CCN(CC1)C1CCC1)CN1CCOCC1 10.1021/acs.jmedchem.8b01280
DB14835 3713 None 17 Human Functional pIC50 = 7.7 7.7 - 1
Inverse agonist activity at recombinant human Histamine 3 receptor expressed in CHO-K1 cells assessed as inhibition of RAMH-induced agonist activity preincubated for 20 mins and measured after 60 mins by [35S]-GTPgammaS binding assayInverse agonist activity at recombinant human Histamine 3 receptor expressed in CHO-K1 cells assessed as inhibition of RAMH-induced agonist activity preincubated for 20 mins and measured after 60 mins by [35S]-GTPgammaS binding assay
ChEMBL 373 6 1 5 2.4 O=C(Nc1ccc(cc1)OC1CCN(CC1)C1CCC1)CN1CCOCC1 10.1021/acs.jmedchem.8b01280
49864994 15803 None 0 Human Functional pIC50 = 4.7 4.7 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 351 5 0 5 3.4 Fc1ccc(C(c2nnnn2Cc2ccccc2)N2CCCCC2)cc1 10.1016/j.bmcl.2010.07.009
CHEMBL1222805 15803 None 0 Human Functional pIC50 = 4.7 4.7 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 351 5 0 5 3.4 Fc1ccc(C(c2nnnn2Cc2ccccc2)N2CCCCC2)cc1 10.1016/j.bmcl.2010.07.009
49864995 15804 None 0 Human Functional pIC50 = 4.7 4.7 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 353 5 0 6 2.3 Fc1ccc(C(c2nnnn2Cc2ccccc2)N2CCOCC2)cc1 10.1016/j.bmcl.2010.07.009
CHEMBL1222806 15804 None 0 Human Functional pIC50 = 4.7 4.7 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 353 5 0 6 2.3 Fc1ccc(C(c2nnnn2Cc2ccccc2)N2CCOCC2)cc1 10.1016/j.bmcl.2010.07.009
49865226 15868 None 0 Human Functional pIC50 = 4.7 4.7 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 390 5 0 8 2.1 Fc1ccc(C(c2nnnn2Cc2ccccc2)N2CCn3cnnc3C2)cc1 10.1016/j.bmcl.2010.07.009
CHEMBL1223079 15868 None 0 Human Functional pIC50 = 4.7 4.7 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 390 5 0 8 2.1 Fc1ccc(C(c2nnnn2Cc2ccccc2)N2CCn3cnnc3C2)cc1 10.1016/j.bmcl.2010.07.009
72164841 92151 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assay
ChEMBL 334 4 1 3 4.4 O=C(Oc1ccc(CN2CCCCC2)cc1)c1c[nH]c2ccccc12 10.1016/j.bmc.2013.07.051
CHEMBL2419584 92151 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assay
ChEMBL 334 4 1 3 4.4 O=C(Oc1ccc(CN2CCCCC2)cc1)c1c[nH]c2ccccc12 10.1016/j.bmc.2013.07.051
44159883 16009 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 485 7 0 7 3.5 O=C1CCCN1c1ccc(C(c2nnnn2Cc2ccccc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
CHEMBL1223514 16009 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 485 7 0 7 3.5 O=C1CCCN1c1ccc(C(c2nnnn2Cc2ccccc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
76325616 105941 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 446 3 0 4 2.5 O=C(N1CCN(C2CCC2)CC1)N1CCC2(CCN(S(=O)(=O)c3ccccc3)CC2)C1 10.1021/jm4014828
CHEMBL3127694 105941 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 446 3 0 4 2.5 O=C(N1CCN(C2CCC2)CC1)N1CCC2(CCN(S(=O)(=O)c3ccccc3)CC2)C1 10.1021/jm4014828
11538747 181689 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 371 3 0 4 2.7 CN(CCN1CCCCC1)C(=O)N1CCC2(CC1)OC(=O)c1ccccc12 10.1016/j.bmcl.2008.07.125
CHEMBL476962 181689 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 371 3 0 4 2.7 CN(CCN1CCCCC1)C(=O)N1CCC2(CC1)OC(=O)c1ccccc12 10.1016/j.bmcl.2008.07.125
168475864 196877 None 2 Human Functional pIC50 = 6.7 6.7 - 1
Inhibition of recombinant human histamine H3 receptor stably expressed in HEK293 cells assessed as increase in cAMP accumulation in presence of forskolin incubated for 30 mins by TR-FRET LANCE assayInhibition of recombinant human histamine H3 receptor stably expressed in HEK293 cells assessed as increase in cAMP accumulation in presence of forskolin incubated for 30 mins by TR-FRET LANCE assay
ChEMBL 397 7 0 4 5.3 N#Cc1ccc(-c2ccc(OCCCN3CCC(c4ccncc4)CC3)cc2)cc1 10.1021/acs.jmedchem.3c00430
CHEMBL5433976 196877 None 2 Human Functional pIC50 = 6.7 6.7 - 1
Inhibition of recombinant human histamine H3 receptor stably expressed in HEK293 cells assessed as increase in cAMP accumulation in presence of forskolin incubated for 30 mins by TR-FRET LANCE assayInhibition of recombinant human histamine H3 receptor stably expressed in HEK293 cells assessed as increase in cAMP accumulation in presence of forskolin incubated for 30 mins by TR-FRET LANCE assay
ChEMBL 397 7 0 4 5.3 N#Cc1ccc(-c2ccc(OCCCN3CCC(c4ccncc4)CC3)cc2)cc1 10.1021/acs.jmedchem.3c00430
53530230 92143 None 3 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assay
ChEMBL 349 5 2 3 3.2 O=C(Cc1c[nH]c2ccccc12)Nc1ccc(CN2CCOCC2)cc1 10.1016/j.bmc.2013.07.051
CHEMBL2419572 92143 None 3 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assay
ChEMBL 349 5 2 3 3.2 O=C(Cc1c[nH]c2ccccc12)Nc1ccc(CN2CCOCC2)cc1 10.1016/j.bmc.2013.07.051
162651175 180474 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 431 5 0 6 2.4 COc1c(C)n(-c2ccc(S(=O)(=O)N3CCN(C4CCCC4)CC3)cc2)ccc1=O 10.1016/j.ejmech.2020.113096
CHEMBL4751577 180474 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 431 5 0 6 2.4 COc1c(C)n(-c2ccc(S(=O)(=O)N3CCN(C4CCCC4)CC3)cc2)ccc1=O 10.1016/j.ejmech.2020.113096
11531261 181751 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 391 6 0 5 4.2 Cc1nc2ccccc2c(=O)n1-c1ccc(OCCCN2CCC(C)CC2)cc1 10.1021/jm8003834
CHEMBL477556 181751 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 391 6 0 5 4.2 Cc1nc2ccccc2c(=O)n1-c1ccc(OCCCN2CCC(C)CC2)cc1 10.1021/jm8003834
44579429 188897 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 357 5 0 3 3.1 CN(CCN1CCCCC1)C(=O)N1CCC(C(=O)c2ccccc2)CC1 10.1016/j.bmcl.2008.07.125
CHEMBL505783 188897 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 357 5 0 3 3.1 CN(CCN1CCCCC1)C(=O)N1CCC(C(=O)c2ccccc2)CC1 10.1016/j.bmcl.2008.07.125
155567151 175956 None 0 Human Functional pIC50 = 6.6 6.6 1 2
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 245 1 1 3 3.5 CC1CCCc2c1nc(N)nc2C1CCCCC1 10.1021/acs.jmedchem.9b00241
CHEMBL4585616 175956 None 0 Human Functional pIC50 = 6.6 6.6 1 2
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 245 1 1 3 3.5 CC1CCCc2c1nc(N)nc2C1CCCCC1 10.1021/acs.jmedchem.9b00241
49865169 15844 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 418 6 0 6 3.3 Fc1ccc(C(c2nnnn2Cc2ccccc2)N2C[C@@H]3C[C@H]2CN3C2CCC2)cc1 10.1016/j.bmcl.2010.07.009
CHEMBL1223008 15844 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 418 6 0 6 3.3 Fc1ccc(C(c2nnnn2Cc2ccccc2)N2C[C@@H]3C[C@H]2CN3C2CCC2)cc1 10.1016/j.bmcl.2010.07.009
49865228 15870 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 420 6 0 6 3.5 Fc1ccc(C(c2nnnn2Cc2ccccc2)N2CCC(N3CCCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
CHEMBL1223081 15870 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 420 6 0 6 3.5 Fc1ccc(C(c2nnnn2Cc2ccccc2)N2CCC(N3CCCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
155567151 175956 None 0 Human Functional pIC50 = 6.6 6.6 1 2
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 245 1 1 3 3.5 CC1CCCc2c1nc(N)nc2C1CCCCC1 10.1021/acs.jmedchem.9b00241
CHEMBL4585616 175956 None 0 Human Functional pIC50 = 6.6 6.6 1 2
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 245 1 1 3 3.5 CC1CCCc2c1nc(N)nc2C1CCCCC1 10.1021/acs.jmedchem.9b00241
72164843 92153 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assay
ChEMBL 334 5 1 3 3.9 O=C(Cc1c[nH]c2ccccc12)Oc1ccc(CN2CCCC2)cc1 10.1016/j.bmc.2013.07.051
CHEMBL2419586 92153 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assay
ChEMBL 334 5 1 3 3.9 O=C(Cc1c[nH]c2ccccc12)Oc1ccc(CN2CCCC2)cc1 10.1016/j.bmc.2013.07.051
49865229 15871 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 394 6 0 6 3.0 CN(C)C1CCCN(C(c2ccc(F)cc2)c2nnnn2Cc2ccccc2)C1 10.1016/j.bmcl.2010.07.009
CHEMBL1223082 15871 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 394 6 0 6 3.0 CN(C)C1CCCN(C(c2ccc(F)cc2)c2nnnn2Cc2ccccc2)C1 10.1016/j.bmcl.2010.07.009
49864997 15806 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 406 6 0 6 3.1 Fc1ccc(C(c2nnnn2Cc2ccccc2)N2CCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
CHEMBL1222808 15806 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 406 6 0 6 3.1 Fc1ccc(C(c2nnnn2Cc2ccccc2)N2CCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
57399371 69365 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assayAntagonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assay
ChEMBL 347 4 2 5 3.1 Nc1nc2ccccc2nc1C(=O)Nc1ccc(CN2CCCC2)cc1 10.1016/j.bmc.2011.09.061
CHEMBL1929411 69365 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assayAntagonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assay
ChEMBL 347 4 2 5 3.1 Nc1nc2ccccc2nc1C(=O)Nc1ccc(CN2CCCC2)cc1 10.1016/j.bmc.2011.09.061
44579472 172628 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 354 4 0 3 3.1 CN(CCN1CCCCC1)C(=O)N1CCC(C#N)(c2ccccc2)CC1 10.1016/j.bmcl.2008.07.125
CHEMBL448362 172628 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 354 4 0 3 3.1 CN(CCN1CCCCC1)C(=O)N1CCC(C#N)(c2ccccc2)CC1 10.1016/j.bmcl.2008.07.125
155544071 173417 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 289 1 1 3 4.3 CC1CCCc2c(-c3cccc4ccccc34)nc(N)nc21 10.1021/acs.jmedchem.9b00241
CHEMBL4526205 173417 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 289 1 1 3 4.3 CC1CCCc2c(-c3cccc4ccccc34)nc(N)nc21 10.1021/acs.jmedchem.9b00241
71625825 90574 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 373 6 2 3 4.8 O=C(Nc1ccc(Cl)cc1)Nc1ccc(OCCN2CCCCC2)cc1 10.1016/j.bmcl.2013.03.080
CHEMBL2387304 90574 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 373 6 2 3 4.8 O=C(Nc1ccc(Cl)cc1)Nc1ccc(OCCN2CCCCC2)cc1 10.1016/j.bmcl.2013.03.080
164622805 185969 None 0 Human Functional pIC50 = 7.6 7.6 -2 6
Antagonist activity at histamine H3 receptor (unknown origin)Antagonist activity at histamine H3 receptor (unknown origin)
ChEMBL 467 9 0 6 4.5 Fc1ccc2c(C3CCN(CCCOc4ccc(CCN5CCOCC5)cc4)CC3)noc2c1 10.1016/j.bmcl.2021.127909
CHEMBL4867978 185969 None 0 Human Functional pIC50 = 7.6 7.6 -2 6
Antagonist activity at histamine H3 receptor (unknown origin)Antagonist activity at histamine H3 receptor (unknown origin)
ChEMBL 467 9 0 6 4.5 Fc1ccc2c(C3CCN(CCCOc4ccc(CCN5CCOCC5)cc4)CC3)noc2c1 10.1016/j.bmcl.2021.127909
155544071 173417 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 289 1 1 3 4.3 CC1CCCc2c(-c3cccc4ccccc34)nc(N)nc21 10.1021/acs.jmedchem.9b00241
CHEMBL4526205 173417 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 289 1 1 3 4.3 CC1CCCc2c(-c3cccc4ccccc34)nc(N)nc21 10.1021/acs.jmedchem.9b00241
127036360 137412 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at recombinant human H3 receptor expressed on CHO-K1 cells assessed as cAMP level by luciferase gene reporter assayAntagonist activity at recombinant human H3 receptor expressed on CHO-K1 cells assessed as cAMP level by luciferase gene reporter assay
ChEMBL 399 6 1 4 3.7 CC(C)N1CCC(NC(=O)c2ccc(OC3CCN(C4CCCC4)CC3)cc2)C1 10.1016/j.ejmech.2015.12.005
CHEMBL3752655 137412 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at recombinant human H3 receptor expressed on CHO-K1 cells assessed as cAMP level by luciferase gene reporter assayAntagonist activity at recombinant human H3 receptor expressed on CHO-K1 cells assessed as cAMP level by luciferase gene reporter assay
ChEMBL 399 6 1 4 3.7 CC(C)N1CCC(NC(=O)c2ccc(OC3CCN(C4CCCC4)CC3)cc2)C1 10.1016/j.ejmech.2015.12.005
49864996 15805 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 368 8 0 6 2.4 CN(C)CCN(C)C(c1ccc(F)cc1)c1nnnn1Cc1ccccc1 10.1016/j.bmcl.2010.07.009
CHEMBL1222807 15805 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 368 8 0 6 2.4 CN(C)CCN(C)C(c1ccc(F)cc1)c1nnnn1Cc1ccccc1 10.1016/j.bmcl.2010.07.009
13170764 175183 None 0 Human Functional pIC50 = 5.6 5.6 -2 2
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 255 2 1 4 2.6 COc1ccc(-c2nc(N)nc3c2CCCC3)cc1 10.1021/acs.jmedchem.9b00241
CHEMBL4568452 175183 None 0 Human Functional pIC50 = 5.6 5.6 -2 2
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 255 2 1 4 2.6 COc1ccc(-c2nc(N)nc3c2CCCC3)cc1 10.1021/acs.jmedchem.9b00241
13170764 175183 None 0 Human Functional pIC50 = 5.6 5.6 -2 2
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 255 2 1 4 2.6 COc1ccc(-c2nc(N)nc3c2CCCC3)cc1 10.1021/acs.jmedchem.9b00241
CHEMBL4568452 175183 None 0 Human Functional pIC50 = 5.6 5.6 -2 2
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 255 2 1 4 2.6 COc1ccc(-c2nc(N)nc3c2CCCC3)cc1 10.1021/acs.jmedchem.9b00241
44447979 95567 None 0 Rat Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at histamine H3 receptor in rat forebrain assessed as inhibition of [3H]histamine release from synaptosomesAntagonist activity at histamine H3 receptor in rat forebrain assessed as inhibition of [3H]histamine release from synaptosomes
ChEMBL 384 8 0 6 2.6 N#CC(C#N)=C1N(CCCN2CCCCC2)CCN1CCCN1CCCCC1 10.1016/j.bmcl.2008.03.006
CHEMBL257391 95567 None 0 Rat Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at histamine H3 receptor in rat forebrain assessed as inhibition of [3H]histamine release from synaptosomesAntagonist activity at histamine H3 receptor in rat forebrain assessed as inhibition of [3H]histamine release from synaptosomes
ChEMBL 384 8 0 6 2.6 N#CC(C#N)=C1N(CCCN2CCCCC2)CCN1CCCN1CCCCC1 10.1016/j.bmcl.2008.03.006
49865448 15973 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 444 7 0 6 4.5 CC(C)c1ccc(C(c2nnnn2Cc2ccccc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
CHEMBL1223377 15973 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 444 7 0 6 4.5 CC(C)c1ccc(C(c2nnnn2Cc2ccccc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
44158590 15976 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 468 8 0 7 4.0 FC(F)Oc1ccc(C(c2nnnn2Cc2ccccc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
CHEMBL1223380 15976 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 468 8 0 7 4.0 FC(F)Oc1ccc(C(c2nnnn2Cc2ccccc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
11509682 171696 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 405 6 0 5 4.4 Cc1nc2ccccc2c(=O)n1-c1ccc(OCCCN2CC(C)CC(C)C2)cc1 10.1021/jm8003834
CHEMBL446516 171696 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 405 6 0 5 4.4 Cc1nc2ccccc2c(=O)n1-c1ccc(OCCCN2CC(C)CC(C)C2)cc1 10.1021/jm8003834
550705 18190 None 1 Mouse Functional pIC50 = 6.6 6.6 -25 2
Antagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 293 0 1 2 3.3 CC1CC(O)(C#Cc2cccc3ccccc23)C(C)CN1C 10.1016/j.bmcl.2010.08.099
CHEMBL1269843 18190 None 1 Mouse Functional pIC50 = 6.6 6.6 -25 2
Antagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 293 0 1 2 3.3 CC1CC(O)(C#Cc2cccc3ccccc23)C(C)CN1C 10.1016/j.bmcl.2010.08.099
11507778 18234 None 0 Mouse Functional pIC50 = 6.6 6.6 -56 2
Antagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 305 0 1 2 3.4 CC1CN2CCCC2CC1(O)C#Cc1cccc2ccccc12 10.1016/j.bmcl.2010.08.099
CHEMBL1270166 18234 None 0 Mouse Functional pIC50 = 6.6 6.6 -56 2
Antagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 305 0 1 2 3.4 CC1CN2CCCC2CC1(O)C#Cc1cccc2ccccc12 10.1016/j.bmcl.2010.08.099
54765288 69361 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assayAntagonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assay
ChEMBL 361 4 2 5 3.5 Nc1nc2ccccc2nc1NC(=O)c1ccc(CN2CCCCC2)cc1 10.1016/j.bmc.2011.09.061
CHEMBL1929400 69361 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assayAntagonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assay
ChEMBL 361 4 2 5 3.5 Nc1nc2ccccc2nc1NC(=O)c1ccc(CN2CCCCC2)cc1 10.1016/j.bmc.2011.09.061
CHEMBL1929401 69361 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assayAntagonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assay
ChEMBL 361 4 2 5 3.5 Nc1nc2ccccc2nc1NC(=O)c1ccc(CN2CCCCC2)cc1 10.1016/j.bmc.2011.09.061
72164594 92141 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assay
ChEMBL 347 5 2 2 4.3 O=C(Cc1c[nH]c2ccccc12)Nc1ccc(CN2CCCCC2)cc1 10.1016/j.bmc.2013.07.051
CHEMBL2419570 92141 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assay
ChEMBL 347 5 2 2 4.3 O=C(Cc1c[nH]c2ccccc12)Nc1ccc(CN2CCCCC2)cc1 10.1016/j.bmc.2013.07.051
3209694 15815 None 3 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 434 6 0 6 3.9 Fc1ccc(C(c2nnnn2Cc2ccccc2)N2CCN(C3CCCCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
CHEMBL1222870 15815 None 3 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 434 6 0 6 3.9 Fc1ccc(C(c2nnnn2Cc2ccccc2)N2CCN(C3CCCCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
54587323 63136 None 0 Guinea pig Functional pIC50 = 7.5 7.5 - 1
Antagonist activity against histamine H3 receptor in guinea pig ileum assessed as inhibition of electrically-evoked twitches after 30 mins in presence of (R)-alpha-methyl-histamineAntagonist activity against histamine H3 receptor in guinea pig ileum assessed as inhibition of electrically-evoked twitches after 30 mins in presence of (R)-alpha-methyl-histamine
ChEMBL 277 7 2 3 3.0 O=C(NCCC1=CCCCC1)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
CHEMBL1774596 63136 None 0 Guinea pig Functional pIC50 = 7.5 7.5 - 1
Antagonist activity against histamine H3 receptor in guinea pig ileum assessed as inhibition of electrically-evoked twitches after 30 mins in presence of (R)-alpha-methyl-histamineAntagonist activity against histamine H3 receptor in guinea pig ileum assessed as inhibition of electrically-evoked twitches after 30 mins in presence of (R)-alpha-methyl-histamine
ChEMBL 277 7 2 3 3.0 O=C(NCCC1=CCCCC1)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
CHEMBL1789341 63136 None 0 Guinea pig Functional pIC50 = 7.5 7.5 - 1
Antagonist activity against histamine H3 receptor in guinea pig ileum assessed as inhibition of electrically-evoked twitches after 30 mins in presence of (R)-alpha-methyl-histamineAntagonist activity against histamine H3 receptor in guinea pig ileum assessed as inhibition of electrically-evoked twitches after 30 mins in presence of (R)-alpha-methyl-histamine
ChEMBL 277 7 2 3 3.0 O=C(NCCC1=CCCCC1)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
72164840 92149 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assay
ChEMBL 321 8 2 2 4.7 CCN(CC)Cc1ccc(NCCc2c[nH]c3ccccc23)cc1 10.1016/j.bmc.2013.07.051
CHEMBL2419582 92149 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assay
ChEMBL 321 8 2 2 4.7 CCN(CC)Cc1ccc(NCCc2c[nH]c3ccccc23)cc1 10.1016/j.bmc.2013.07.051
155532722 171888 None 0 Human Functional pIC50 = 5.5 5.5 -3 2
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 253 1 1 3 3.5 Cc1ccc(-c2nc(N)nc3c2CCCC3C)cc1 10.1021/acs.jmedchem.9b00241
CHEMBL4467878 171888 None 0 Human Functional pIC50 = 5.5 5.5 -3 2
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 253 1 1 3 3.5 Cc1ccc(-c2nc(N)nc3c2CCCC3C)cc1 10.1021/acs.jmedchem.9b00241
155532722 171888 None 0 Human Functional pIC50 = 5.5 5.5 -3 2
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 253 1 1 3 3.5 Cc1ccc(-c2nc(N)nc3c2CCCC3C)cc1 10.1021/acs.jmedchem.9b00241
CHEMBL4467878 171888 None 0 Human Functional pIC50 = 5.5 5.5 -3 2
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 253 1 1 3 3.5 Cc1ccc(-c2nc(N)nc3c2CCCC3C)cc1 10.1021/acs.jmedchem.9b00241
44579476 186974 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 364 4 0 3 3.0 CN(CCN1CCCCC1)C(=O)N1CCN(c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2008.07.125
CHEMBL489590 186974 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 364 4 0 3 3.0 CN(CCN1CCCCC1)C(=O)N1CCN(c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2008.07.125
25139490 176111 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 423 4 0 5 4.7 Cc1nc2cc(Cl)ccc2c(=O)n1-c1ccc(OC2CCN(C3CCC3)CC2)cc1 10.1021/jm800569w
CHEMBL458953 176111 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 423 4 0 5 4.7 Cc1nc2cc(Cl)ccc2c(=O)n1-c1ccc(OC2CCN(C3CCC3)CC2)cc1 10.1021/jm800569w
49865290 15597 None 0 Human Functional pIC50 = 8.5 8.5 3 2
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 459 7 1 7 2.7 CNC(=O)c1ccc(C(c2nnnn2Cc2ccccc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
CHEMBL1221429 15597 None 0 Human Functional pIC50 = 8.5 8.5 3 2
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 459 7 1 7 2.7 CNC(=O)c1ccc(C(c2nnnn2Cc2ccccc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
90290274 160690 None 0 Human Functional pIC50 = 8.5 8.5 - 1
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
ChEMBL 530 9 1 4 6.4 CCOC(=O)[C@H]1CCCC[C@H]1NC(=O)C1(c2ccc(-c3ccc(CCN4CCC[C@H]4C)cc3)cc2)CCCC1 nan
CHEMBL4112815 160690 None 0 Human Functional pIC50 = 8.5 8.5 - 1
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
ChEMBL 530 9 1 4 6.4 CCOC(=O)[C@H]1CCCC[C@H]1NC(=O)C1(c2ccc(-c3ccc(CCN4CCC[C@H]4C)cc3)cc2)CCCC1 nan
45268283 199124 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
ChEMBL 431 7 0 4 6.5 c1ccc([C@@H]2Sc3ccccc3O[C@@H]2c2ccc(OCCCN3CCCC3)cc2)cc1 10.1016/j.bmcl.2009.05.101
CHEMBL564514 199124 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
ChEMBL 431 7 0 4 6.5 c1ccc([C@@H]2Sc3ccccc3O[C@@H]2c2ccc(OCCCN3CCCC3)cc2)cc1 10.1016/j.bmcl.2009.05.101
25263866 90584 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 446 4 2 3 6.0 Cc1cc(NC(=O)Nc2cc(Cl)cc(Cl)c2)ccc1N1CCC(N2CCCC2C)C1 10.1016/j.bmcl.2013.03.080
CHEMBL2387313 90584 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 446 4 2 3 6.0 Cc1cc(NC(=O)Nc2cc(Cl)cc(Cl)c2)ccc1N1CCC(N2CCCC2C)C1 10.1016/j.bmcl.2013.03.080
78324788 119167 None 0 Human Functional pIC50 = 8.5 8.5 - 1
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
ChEMBL 351 6 1 2 4.7 C[C@@H]1CCCN1CCc1ccc(-c2ccc(C(C)(C)C(=O)O)cc2)cc1 nan
CHEMBL3427233 119167 None 0 Human Functional pIC50 = 8.5 8.5 - 1
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
ChEMBL 351 6 1 2 4.7 C[C@@H]1CCCN1CCc1ccc(-c2ccc(C(C)(C)C(=O)O)cc2)cc1 nan
23151199 186134 None 0 Human Functional pIC50 = 8.5 8.5 2089 2
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 377 6 0 5 3.9 Cc1nc2ccccc2c(=O)n1-c1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.10.034
CHEMBL487063 186134 None 0 Human Functional pIC50 = 8.5 8.5 2089 2
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 377 6 0 5 3.9 Cc1nc2ccccc2c(=O)n1-c1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.10.034
23151199 186134 None 0 Human Functional pIC50 = 8.5 8.5 2089 2
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 377 6 0 5 3.9 Cc1nc2ccccc2c(=O)n1-c1ccc(OCCCN2CCCCC2)cc1 10.1021/jm8003834
CHEMBL487063 186134 None 0 Human Functional pIC50 = 8.5 8.5 2089 2
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 377 6 0 5 3.9 Cc1nc2ccccc2c(=O)n1-c1ccc(OCCCN2CCCCC2)cc1 10.1021/jm8003834
78324788 119167 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
ChEMBL 351 6 1 2 4.7 C[C@@H]1CCCN1CCc1ccc(-c2ccc(C(C)(C)C(=O)O)cc2)cc1 10.1021/acsmedchemlett.5b00002
CHEMBL3427233 119167 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
ChEMBL 351 6 1 2 4.7 C[C@@H]1CCCN1CCc1ccc(-c2ccc(C(C)(C)C(=O)O)cc2)cc1 10.1021/acsmedchemlett.5b00002
11661358 184326 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 403 4 0 5 4.5 Cc1nc2ccccc2c(=O)n1-c1ccc(OC2CCN(C3CCCC3)CC2)cc1 10.1021/jm800569w
CHEMBL483366 184326 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 403 4 0 5 4.5 Cc1nc2ccccc2c(=O)n1-c1ccc(OC2CCN(C3CCCC3)CC2)cc1 10.1021/jm800569w
76318298 105939 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 426 3 0 4 2.2 CC(C)S(=O)(=O)N1CCC2(CCN(C(=O)N3CCCN(C4CCC4)CC3)C2)CC1 10.1021/jm4014828
CHEMBL3127692 105939 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 426 3 0 4 2.2 CC(C)S(=O)(=O)N1CCC2(CCN(C(=O)N3CCCN(C4CCC4)CC3)C2)CC1 10.1021/jm4014828
25118125 105945 None 1 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 349 3 0 4 1.8 CC(C)N1CCN(C(=O)C2CC23CCN(C2CCOCC2)CC3)CC1 10.1021/jm4014828
CHEMBL3127698 105945 None 1 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 349 3 0 4 1.8 CC(C)N1CCN(C(=O)C2CC23CCN(C2CCOCC2)CC3)CC1 10.1021/jm4014828
78320398 119173 None 0 Human Functional pIC50 = 8.5 8.5 - 1
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
ChEMBL 391 6 0 3 5.4 COC(=O)C1(c2ccc(-c3ccc(CCN4CCC[C@H]4C)cc3)cc2)CCCC1 nan
CHEMBL3427239 119173 None 0 Human Functional pIC50 = 8.5 8.5 - 1
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
ChEMBL 391 6 0 3 5.4 COC(=O)C1(c2ccc(-c3ccc(CCN4CCC[C@H]4C)cc3)cc2)CCCC1 nan
78320398 119173 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
ChEMBL 391 6 0 3 5.4 COC(=O)C1(c2ccc(-c3ccc(CCN4CCC[C@H]4C)cc3)cc2)CCCC1 10.1021/acsmedchemlett.5b00002
CHEMBL3427239 119173 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
ChEMBL 391 6 0 3 5.4 COC(=O)C1(c2ccc(-c3ccc(CCN4CCC[C@H]4C)cc3)cc2)CCCC1 10.1021/acsmedchemlett.5b00002
164611350 185211 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human H3 receptor by TR-FRET assayAntagonist activity at human H3 receptor by TR-FRET assay
ChEMBL 354 7 1 5 3.1 Cn1cc(O)c(=O)cc1/C=C/c1ccc(OCCCN2CCCC2)cc1 10.1016/j.bmc.2021.116306
CHEMBL4856094 185211 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human H3 receptor by TR-FRET assayAntagonist activity at human H3 receptor by TR-FRET assay
ChEMBL 354 7 1 5 3.1 Cn1cc(O)c(=O)cc1/C=C/c1ccc(OCCCN2CCCC2)cc1 10.1016/j.bmc.2021.116306
23151223 184608 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 389 4 0 5 4.1 Cc1nc2ccccc2c(=O)n1-c1ccc(OC2CCC(N3CCCC3)C2)cc1 10.1021/jm800569w
CHEMBL484740 184608 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 389 4 0 5 4.1 Cc1nc2ccccc2c(=O)n1-c1ccc(OC2CCC(N3CCCC3)C2)cc1 10.1021/jm800569w
49865111 15828 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 434 6 0 6 3.9 C[C@H]1CN(C(c2ccc(F)cc2)c2nnnn2Cc2ccccc2)C[C@@H](C)N1C1CCC1 10.1016/j.bmcl.2010.07.009
CHEMBL1222947 15828 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 434 6 0 6 3.9 C[C@H]1CN(C(c2ccc(F)cc2)c2nnnn2Cc2ccccc2)C[C@@H](C)N1C1CCC1 10.1016/j.bmcl.2010.07.009
11682068 181518 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 363 6 0 5 3.6 Cc1nc2ccccc2c(=O)n1-c1ccc(OCCCN2CCCC2)cc1 10.1021/jm8003834
CHEMBL476373 181518 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 363 6 0 5 3.6 Cc1nc2ccccc2c(=O)n1-c1ccc(OCCCN2CCCC2)cc1 10.1021/jm8003834
44578389 190949 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 349 6 0 5 3.3 O=c1c2ccccc2ncn1-c1ccc(OCCCN2CCCC2)cc1 10.1021/jm8003834
CHEMBL518431 190949 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 349 6 0 5 3.3 O=c1c2ccccc2ncn1-c1ccc(OCCCN2CCCC2)cc1 10.1021/jm8003834
49864803 15732 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 486 7 0 9 3.9 c1ccc(Cn2nnnc2C(c2ccc(-c3csnn3)cc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
CHEMBL1222502 15732 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 486 7 0 9 3.9 c1ccc(Cn2nnnc2C(c2ccc(-c3csnn3)cc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
76336464 105937 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 424 2 0 3 3.3 O=C(c1ccccc1)N1CCC2(CC1)CCN(C(=O)N1CCCN(C3CCC3)CC1)C2 10.1021/jm4014828
CHEMBL3127690 105937 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 424 2 0 3 3.3 O=C(c1ccccc1)N1CCC2(CC1)CCN(C(=O)N1CCCN(C3CCC3)CC1)C2 10.1021/jm4014828
25095678 105947 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 361 3 0 4 2.0 O=C(C1CC12CCN(C1CCOCC1)CC2)N1CCN(C2CCC2)CC1 10.1021/jm4014828
CHEMBL3127700 105947 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 361 3 0 4 2.0 O=C(C1CC12CCN(C1CCOCC1)CC2)N1CCN(C2CCC2)CC1 10.1021/jm4014828
11611851 182429 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 400 5 0 5 3.2 COc1cccc2c1[C@]1(CC[C@@H](C(=O)N(C)CCN3CCCCC3)CC1)OC2=O 10.1016/j.bmcl.2008.07.125
CHEMBL478434 182429 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 400 5 0 5 3.2 COc1cccc2c1[C@]1(CC[C@@H](C(=O)N(C)CCN3CCCCC3)CC1)OC2=O 10.1016/j.bmcl.2008.07.125
24950873 181706 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 393 7 0 6 3.6 COc1cccc2c(=O)n(-c3ccc(OCCCN4CCCC4)cc3)c(C)nc12 10.1021/jm8003834
CHEMBL477152 181706 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 393 7 0 6 3.6 COc1cccc2c(=O)n(-c3ccc(OCCCN4CCCC4)cc3)c(C)nc12 10.1021/jm8003834
90281088 119159 None 0 Human Functional pIC50 = 8.4 8.4 - 1
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
ChEMBL 309 5 1 2 4.1 C[C@@H]1CCCN1CCc1ccc(-c2ccc(C(=O)O)cc2)cc1 nan
CHEMBL3427225 119159 None 0 Human Functional pIC50 = 8.4 8.4 - 1
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
ChEMBL 309 5 1 2 4.1 C[C@@H]1CCCN1CCc1ccc(-c2ccc(C(=O)O)cc2)cc1 nan
78320399 160321 None 0 Human Functional pIC50 = 8.4 8.4 - 1
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
ChEMBL 450 9 1 4 4.8 C[C@@H]1CCCN1CCc1ccc(-c2ccc(CCC(=O)NCC(=O)OC(C)(C)C)cc2)cc1 nan
CHEMBL4109781 160321 None 0 Human Functional pIC50 = 8.4 8.4 - 1
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
ChEMBL 450 9 1 4 4.8 C[C@@H]1CCCN1CCc1ccc(-c2ccc(CCC(=O)NCC(=O)OC(C)(C)C)cc2)cc1 nan
90281088 119159 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
ChEMBL 309 5 1 2 4.1 C[C@@H]1CCCN1CCc1ccc(-c2ccc(C(=O)O)cc2)cc1 10.1021/acsmedchemlett.5b00002
CHEMBL3427225 119159 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
ChEMBL 309 5 1 2 4.1 C[C@@H]1CCCN1CCc1ccc(-c2ccc(C(=O)O)cc2)cc1 10.1021/acsmedchemlett.5b00002
45271701 197419 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
ChEMBL 401 6 0 5 3.8 C[C@H]1[C@@H](c2ccc(OCCCN3CCCC3)cc2)Oc2ccccc2S1(=O)=O 10.1016/j.bmcl.2009.05.101
CHEMBL549908 197419 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
ChEMBL 401 6 0 5 3.8 C[C@H]1[C@@H](c2ccc(OCCCN3CCCC3)cc2)Oc2ccccc2S1(=O)=O 10.1016/j.bmcl.2009.05.101
11646541 182403 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 377 6 0 5 3.9 Cc1ccc2nc(C)n(-c3ccc(OCCCN4CCCC4)cc3)c(=O)c2c1 10.1021/jm8003834
CHEMBL478406 182403 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 377 6 0 5 3.9 Cc1ccc2nc(C)n(-c3ccc(OCCCN4CCCC4)cc3)c(=O)c2c1 10.1021/jm8003834
164622056 186301 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human H3 receptor by TR-FRET assayAntagonist activity at human H3 receptor by TR-FRET assay
ChEMBL 370 7 1 6 2.4 Cn1cc(O)c(=O)cc1/C=C/c1ccc(OCCCN2CCOCC2)cc1 10.1016/j.bmc.2021.116306
CHEMBL4872910 186301 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human H3 receptor by TR-FRET assayAntagonist activity at human H3 receptor by TR-FRET assay
ChEMBL 370 7 1 6 2.4 Cn1cc(O)c(=O)cc1/C=C/c1ccc(OCCCN2CCOCC2)cc1 10.1016/j.bmc.2021.116306
155529822 171598 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 317 1 1 3 3.9 CC1CCCc2c(-c3ccc(Br)cc3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
CHEMBL4463811 171598 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 317 1 1 3 3.9 CC1CCCc2c(-c3ccc(Br)cc3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
3209702 15807 None 2 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 420 6 0 6 3.5 Fc1ccc(C(c2nnnn2Cc2ccccc2)N2CCN(C3CCCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
CHEMBL1222809 15807 None 2 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 420 6 0 6 3.5 Fc1ccc(C(c2nnnn2Cc2ccccc2)N2CCN(C3CCCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
73354133 102615 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 347 10 2 3 4.5 N=C(NCCCCCc1ccccc1)SCCCN1CCCCC1 10.1016/j.bmcl.2013.09.052
CHEMBL2441943 102615 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 347 10 2 3 4.5 N=C(NCCCCCc1ccccc1)SCCCN1CCCCC1 10.1016/j.bmcl.2013.09.052
CHEMBL3040720 102615 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 347 10 2 3 4.5 N=C(NCCCCCc1ccccc1)SCCCN1CCCCC1 10.1016/j.bmcl.2013.09.052
72546519 102630 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 325 7 2 3 3.6 N=C(NCCc1ccc(Cl)cc1)SCCCN1CCCC1 10.1016/j.bmcl.2013.09.052
CHEMBL2441938 102630 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 325 7 2 3 3.6 N=C(NCCc1ccc(Cl)cc1)SCCCN1CCCC1 10.1016/j.bmcl.2013.09.052
CHEMBL3040778 102630 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 325 7 2 3 3.6 N=C(NCCc1ccc(Cl)cc1)SCCCN1CCCC1 10.1016/j.bmcl.2013.09.052
155529822 171598 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 317 1 1 3 3.9 CC1CCCc2c(-c3ccc(Br)cc3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
CHEMBL4463811 171598 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 317 1 1 3 3.9 CC1CCCc2c(-c3ccc(Br)cc3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
145961372 161701 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human H3 receptor expressed in HEK293 cells assessed as inhibition of RAMH-induced reduction of forskolin-stimulated cAMP accumulation after 30 mins by Ulight-based TR-FRET assayAntagonist activity at human H3 receptor expressed in HEK293 cells assessed as inhibition of RAMH-induced reduction of forskolin-stimulated cAMP accumulation after 30 mins by Ulight-based TR-FRET assay
ChEMBL 311 7 0 2 5.3 c1ccc2c(OCCCCCN3CCCCCC3)cccc2c1 10.1016/j.bmc.2018.04.023
CHEMBL4129589 161701 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human H3 receptor expressed in HEK293 cells assessed as inhibition of RAMH-induced reduction of forskolin-stimulated cAMP accumulation after 30 mins by Ulight-based TR-FRET assayAntagonist activity at human H3 receptor expressed in HEK293 cells assessed as inhibition of RAMH-induced reduction of forskolin-stimulated cAMP accumulation after 30 mins by Ulight-based TR-FRET assay
ChEMBL 311 7 0 2 5.3 c1ccc2c(OCCCCCN3CCCCCC3)cccc2c1 10.1016/j.bmc.2018.04.023
72546520 102596 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 341 7 2 4 2.9 N=C(NCCc1ccc(Cl)cc1)SCCCN1CCOCC1 10.1016/j.bmcl.2013.09.052
CHEMBL2441939 102596 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 341 7 2 4 2.9 N=C(NCCc1ccc(Cl)cc1)SCCCN1CCOCC1 10.1016/j.bmcl.2013.09.052
CHEMBL3040655 102596 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 341 7 2 4 2.9 N=C(NCCc1ccc(Cl)cc1)SCCCN1CCOCC1 10.1016/j.bmcl.2013.09.052
72547017 102624 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 336 9 1 2 4.0 O=C(CCCCc1ccc(Cl)cc1)NCCCN1CCCCC1 10.1016/j.bmcl.2013.09.052
CHEMBL2441949 102624 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 336 9 1 2 4.0 O=C(CCCCc1ccc(Cl)cc1)NCCCN1CCCCC1 10.1016/j.bmcl.2013.09.052
CHEMBL3040755 102624 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 336 9 1 2 4.0 O=C(CCCCc1ccc(Cl)cc1)NCCCN1CCCCC1 10.1016/j.bmcl.2013.09.052
10063835 63143 None 0 Guinea pig Functional pIC50 = 7.5 7.5 - 1
Antagonist activity against histamine H3 receptor in guinea pig ileum assessed as inhibition of electrically-evoked twitches after 30 mins in presence of (R)-alpha-methyl-histamineAntagonist activity against histamine H3 receptor in guinea pig ileum assessed as inhibition of electrically-evoked twitches after 30 mins in presence of (R)-alpha-methyl-histamine
ChEMBL 307 9 2 3 3.8 O=C(NCCCCC1CCCCC1)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
CHEMBL1774601 63143 None 0 Guinea pig Functional pIC50 = 7.5 7.5 - 1
Antagonist activity against histamine H3 receptor in guinea pig ileum assessed as inhibition of electrically-evoked twitches after 30 mins in presence of (R)-alpha-methyl-histamineAntagonist activity against histamine H3 receptor in guinea pig ileum assessed as inhibition of electrically-evoked twitches after 30 mins in presence of (R)-alpha-methyl-histamine
ChEMBL 307 9 2 3 3.8 O=C(NCCCCC1CCCCC1)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
CHEMBL1789356 63143 None 0 Guinea pig Functional pIC50 = 7.5 7.5 - 1
Antagonist activity against histamine H3 receptor in guinea pig ileum assessed as inhibition of electrically-evoked twitches after 30 mins in presence of (R)-alpha-methyl-histamineAntagonist activity against histamine H3 receptor in guinea pig ileum assessed as inhibition of electrically-evoked twitches after 30 mins in presence of (R)-alpha-methyl-histamine
ChEMBL 307 9 2 3 3.8 O=C(NCCCCC1CCCCC1)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
44158486 15760 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 441 6 1 6 3.9 c1ccc(Cn2nnnc2C(c2ccc3cc[nH]c3c2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
CHEMBL1222664 15760 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 441 6 1 6 3.9 c1ccc(Cn2nnnc2C(c2ccc3cc[nH]c3c2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
76329183 105930 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 378 2 0 4 2.1 CC(C)N1CCN(C(=O)N2CCC3(CCN(C4CCOCC4)CC3)C2)CC1 10.1021/jm4014828
CHEMBL3127683 105930 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 378 2 0 4 2.1 CC(C)N1CCN(C(=O)N2CCC3(CCN(C4CCOCC4)CC3)C2)CC1 10.1021/jm4014828
127036359 137464 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at recombinant human H3 receptor expressed on CHO-K1 cells assessed as cAMP level by luciferase gene reporter assayAntagonist activity at recombinant human H3 receptor expressed on CHO-K1 cells assessed as cAMP level by luciferase gene reporter assay
ChEMBL 373 6 1 4 3.2 CC(C)N1CCC(Oc2ccc(C(=O)NC3CCN(C(C)C)C3)cc2)CC1 10.1016/j.ejmech.2015.12.005
CHEMBL3753093 137464 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at recombinant human H3 receptor expressed on CHO-K1 cells assessed as cAMP level by luciferase gene reporter assayAntagonist activity at recombinant human H3 receptor expressed on CHO-K1 cells assessed as cAMP level by luciferase gene reporter assay
ChEMBL 373 6 1 4 3.2 CC(C)N1CCC(Oc2ccc(C(=O)NC3CCN(C(C)C)C3)cc2)CC1 10.1016/j.ejmech.2015.12.005
10107667 63185 None 0 Guinea pig Functional pIC50 = 7.5 7.5 - 1
Antagonist activity against histamine H3 receptor in guinea pig ileum assessed as inhibition of electrically-evoked twitches after 30 mins in presence of (R)-alpha-methyl-histamineAntagonist activity against histamine H3 receptor in guinea pig ileum assessed as inhibition of electrically-evoked twitches after 30 mins in presence of (R)-alpha-methyl-histamine
ChEMBL 279 7 2 3 3.0 O=C(NCCC1CCCCC1)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
CHEMBL1774599 63185 None 0 Guinea pig Functional pIC50 = 7.5 7.5 - 1
Antagonist activity against histamine H3 receptor in guinea pig ileum assessed as inhibition of electrically-evoked twitches after 30 mins in presence of (R)-alpha-methyl-histamineAntagonist activity against histamine H3 receptor in guinea pig ileum assessed as inhibition of electrically-evoked twitches after 30 mins in presence of (R)-alpha-methyl-histamine
ChEMBL 279 7 2 3 3.0 O=C(NCCC1CCCCC1)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
CHEMBL1789800 63185 None 0 Guinea pig Functional pIC50 = 7.5 7.5 - 1
Antagonist activity against histamine H3 receptor in guinea pig ileum assessed as inhibition of electrically-evoked twitches after 30 mins in presence of (R)-alpha-methyl-histamineAntagonist activity against histamine H3 receptor in guinea pig ileum assessed as inhibition of electrically-evoked twitches after 30 mins in presence of (R)-alpha-methyl-histamine
ChEMBL 279 7 2 3 3.0 O=C(NCCC1CCCCC1)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
44159763 15777 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 457 6 0 9 2.7 Cn1nnc2cc(C(c3nnnn3Cc3ccccc3)N3CCCN(C4CCC4)CC3)ccc21 10.1016/j.bmcl.2010.07.009
CHEMBL1222729 15777 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 457 6 0 9 2.7 Cn1nnc2cc(C(c3nnnn3Cc3ccccc3)N3CCCN(C4CCC4)CC3)ccc21 10.1016/j.bmcl.2010.07.009
11703337 189961 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 365 8 0 5 3.8 CCN(CC)CCCOc1ccc(-n2c(C)nc3ccccc3c2=O)cc1 10.1021/jm8003834
CHEMBL516725 189961 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 365 8 0 5 3.8 CCN(CC)CCCOc1ccc(-n2c(C)nc3ccccc3c2=O)cc1 10.1021/jm8003834
49865488 15991 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 436 6 0 6 4.0 Clc1ccc(C(c2nnnn2Cc2ccccc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
CHEMBL1223448 15991 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 436 6 0 6 4.0 Clc1ccc(C(c2nnnn2Cc2ccccc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
76325617 105942 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 409 3 0 3 3.4 O=C(c1ccccc1)N1CCC2(CC1)CCN(C(=O)C1CCN(C3CCC3)CC1)C2 10.1021/jm4014828
CHEMBL3127695 105942 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 409 3 0 3 3.4 O=C(c1ccccc1)N1CCC2(CC1)CCN(C(=O)C1CCN(C3CCC3)CC1)C2 10.1021/jm4014828
44579388 187050 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 379 4 0 2 4.6 CN(CCN1CCCCC1)C(=O)N1CCC(c2cccc3ccccc23)CC1 10.1016/j.bmcl.2008.07.125
CHEMBL490195 187050 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 379 4 0 2 4.6 CN(CCN1CCCCC1)C(=O)N1CCC(c2cccc3ccccc23)CC1 10.1016/j.bmcl.2008.07.125
52945858 18235 None 0 Mouse Functional pIC50 = 6.5 6.5 -24 2
Antagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 309 3 1 2 4.0 CC1CN2CCCC2CC1(O)CCc1cccc2ccccc12 10.1016/j.bmcl.2010.08.099
CHEMBL1270167 18235 None 0 Mouse Functional pIC50 = 6.5 6.5 -24 2
Antagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 309 3 1 2 4.0 CC1CN2CCCC2CC1(O)CCc1cccc2ccccc12 10.1016/j.bmcl.2010.08.099
49799185 10975 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of RAHM-induced [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAntagonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of RAHM-induced [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 317 4 1 2 4.5 c1ccc(-c2ccc(N3CCC(Cc4c[nH]cn4)CC3)cc2)cc1 10.1016/j.bmc.2010.04.052
CHEMBL1173391 10975 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of RAHM-induced [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAntagonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of RAHM-induced [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 317 4 1 2 4.5 c1ccc(-c2ccc(N3CCC(Cc4c[nH]cn4)CC3)cc2)cc1 10.1016/j.bmc.2010.04.052
162653703 180625 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 417 5 0 6 2.0 COc1c(C)n(-c2ccc(S(=O)(=O)N3CCN(C4CCC4)CC3)cc2)ccc1=O 10.1016/j.ejmech.2020.113096
CHEMBL4753396 180625 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 417 5 0 6 2.0 COc1c(C)n(-c2ccc(S(=O)(=O)N3CCN(C4CCC4)CC3)cc2)ccc1=O 10.1016/j.ejmech.2020.113096
162661133 181611 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 369 4 0 5 2.3 COc1c(C)n(-c2ccc(C(=O)N3CCN(C(C)C)CC3)cc2)ccc1=O 10.1016/j.ejmech.2020.113096
CHEMBL4764966 181611 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 369 4 0 5 2.3 COc1c(C)n(-c2ccc(C(=O)N3CCN(C(C)C)CC3)cc2)ccc1=O 10.1016/j.ejmech.2020.113096
46866435 92144 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assay
ChEMBL 335 7 2 2 4.2 CCN(CC)Cc1ccc(NC(=O)Cc2c[nH]c3ccccc23)cc1 10.1016/j.bmc.2013.07.051
CHEMBL2419573 92144 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assay
ChEMBL 335 7 2 2 4.2 CCN(CC)Cc1ccc(NC(=O)Cc2c[nH]c3ccccc23)cc1 10.1016/j.bmc.2013.07.051
164618302 184680 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human H3 receptor by TR-FRET assayAntagonist activity at human H3 receptor by TR-FRET assay
ChEMBL 383 7 1 6 2.3 CN1CCN(CCCOc2ccc(/C=C/c3cc(=O)c(O)cn3C)cc2)CC1 10.1016/j.bmc.2021.116306
CHEMBL4848524 184680 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human H3 receptor by TR-FRET assayAntagonist activity at human H3 receptor by TR-FRET assay
ChEMBL 383 7 1 6 2.3 CN1CCN(CCCOc2ccc(/C=C/c3cc(=O)c(O)cn3C)cc2)CC1 10.1016/j.bmc.2021.116306
49865109 15826 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 434 6 0 6 3.9 Fc1ccc(C(c2nnnn2Cc2ccccc2)N2CCCN(C3CCCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
CHEMBL1222945 15826 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 434 6 0 6 3.9 Fc1ccc(C(c2nnnn2Cc2ccccc2)N2CCCN(C3CCCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
59395224 105954 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 305 2 1 3 1.9 O=C(C1CC12CCNCC2)N1CCN(C2CCCCC2)CC1 10.1021/jm4014828
CHEMBL3127707 105954 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 305 2 1 3 1.9 O=C(C1CC12CCNCC2)N1CCN(C2CCCCC2)CC1 10.1021/jm4014828
49865227 15869 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 394 6 0 6 3.0 CN(C)C1CCN(C(c2ccc(F)cc2)c2nnnn2Cc2ccccc2)CC1 10.1016/j.bmcl.2010.07.009
CHEMBL1223080 15869 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 394 6 0 6 3.0 CN(C)C1CCN(C(c2ccc(F)cc2)c2nnnn2Cc2ccccc2)CC1 10.1016/j.bmcl.2010.07.009
16082833 80378 None 0 Human Functional pIC50 = 7.4 7.4 40 2
Antagonist activity at human H3 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assayAntagonist activity at human H3 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assay
ChEMBL 247 6 2 2 3.1 c1nc([C@H]2C[C@@H]2CCNCC2CCCCC2)c[nH]1 10.1021/jm0603318
CHEMBL214312 80378 None 0 Human Functional pIC50 = 7.4 7.4 40 2
Antagonist activity at human H3 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assayAntagonist activity at human H3 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assay
ChEMBL 247 6 2 2 3.1 c1nc([C@H]2C[C@@H]2CCNCC2CCCCC2)c[nH]1 10.1021/jm0603318
23151225 192706 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 389 4 0 5 4.1 Cc1nc2ccccc2c(=O)n1-c1ccc(OC2CCN(C3CCCC3)C2)cc1 10.1021/jm800569w
CHEMBL521503 192706 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 389 4 0 5 4.1 Cc1nc2ccccc2c(=O)n1-c1ccc(OC2CCN(C3CCCC3)C2)cc1 10.1021/jm800569w
5048 3133 None 50 Human Functional pIC50 = 6.4 6.4 -11 5
Inhibition of recombinant human histamine H3 receptor stably expressed in HEK293 cells assessed as increase in cAMP accumulation in presence of forskolin incubated for 30 mins by TR-FRET LANCE assayInhibition of recombinant human histamine H3 receptor stably expressed in HEK293 cells assessed as increase in cAMP accumulation in presence of forskolin incubated for 30 mins by TR-FRET LANCE assay
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.1021/acs.jmedchem.3c00430
8924 3133 None 50 Human Functional pIC50 = 6.4 6.4 -11 5
Inhibition of recombinant human histamine H3 receptor stably expressed in HEK293 cells assessed as increase in cAMP accumulation in presence of forskolin incubated for 30 mins by TR-FRET LANCE assayInhibition of recombinant human histamine H3 receptor stably expressed in HEK293 cells assessed as increase in cAMP accumulation in presence of forskolin incubated for 30 mins by TR-FRET LANCE assay
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.1021/acs.jmedchem.3c00430
9948102 3133 None 50 Human Functional pIC50 = 6.4 6.4 -11 5
Inhibition of recombinant human histamine H3 receptor stably expressed in HEK293 cells assessed as increase in cAMP accumulation in presence of forskolin incubated for 30 mins by TR-FRET LANCE assayInhibition of recombinant human histamine H3 receptor stably expressed in HEK293 cells assessed as increase in cAMP accumulation in presence of forskolin incubated for 30 mins by TR-FRET LANCE assay
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.1021/acs.jmedchem.3c00430
9948102.0 3133 None 50 Human Functional pIC50 = 6.4 6.4 -11 5
Inhibition of recombinant human histamine H3 receptor stably expressed in HEK293 cells assessed as increase in cAMP accumulation in presence of forskolin incubated for 30 mins by TR-FRET LANCE assayInhibition of recombinant human histamine H3 receptor stably expressed in HEK293 cells assessed as increase in cAMP accumulation in presence of forskolin incubated for 30 mins by TR-FRET LANCE assay
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.1021/acs.jmedchem.3c00430
CHEMBL462605 3133 None 50 Human Functional pIC50 = 6.4 6.4 -11 5
Inhibition of recombinant human histamine H3 receptor stably expressed in HEK293 cells assessed as increase in cAMP accumulation in presence of forskolin incubated for 30 mins by TR-FRET LANCE assayInhibition of recombinant human histamine H3 receptor stably expressed in HEK293 cells assessed as increase in cAMP accumulation in presence of forskolin incubated for 30 mins by TR-FRET LANCE assay
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.1021/acs.jmedchem.3c00430
DB11642 3133 None 50 Human Functional pIC50 = 6.4 6.4 -11 5
Inhibition of recombinant human histamine H3 receptor stably expressed in HEK293 cells assessed as increase in cAMP accumulation in presence of forskolin incubated for 30 mins by TR-FRET LANCE assayInhibition of recombinant human histamine H3 receptor stably expressed in HEK293 cells assessed as increase in cAMP accumulation in presence of forskolin incubated for 30 mins by TR-FRET LANCE assay
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.1021/acs.jmedchem.3c00430
57399371 69365 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Inverse agonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assayInverse agonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assay
ChEMBL 347 4 2 5 3.1 Nc1nc2ccccc2nc1C(=O)Nc1ccc(CN2CCCC2)cc1 10.1016/j.bmc.2011.09.061
CHEMBL1929411 69365 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Inverse agonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assayInverse agonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assay
ChEMBL 347 4 2 5 3.1 Nc1nc2ccccc2nc1C(=O)Nc1ccc(CN2CCCC2)cc1 10.1016/j.bmc.2011.09.061
44579606 187025 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 385 3 0 4 2.8 CN(CCN1CCCCC1)C(=O)N1CCC2(CC1)Cc1ccccc1C(=O)O2 10.1016/j.bmcl.2008.07.125
CHEMBL489973 187025 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 385 3 0 4 2.8 CN(CCN1CCCCC1)C(=O)N1CCC2(CC1)Cc1ccccc1C(=O)O2 10.1016/j.bmcl.2008.07.125
162664073 182248 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 405 5 0 6 1.9 COc1c(C)n(-c2ccc(S(=O)(=O)N3CCN(C(C)C)CC3)cc2)ccc1=O 10.1016/j.ejmech.2020.113096
CHEMBL4782278 182248 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 405 5 0 6 1.9 COc1c(C)n(-c2ccc(S(=O)(=O)N3CCN(C(C)C)CC3)cc2)ccc1=O 10.1016/j.ejmech.2020.113096
11625356 181690 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 357 3 0 3 3.0 CN(CCN1CCCCC1)C(=O)N1CCC2(CC1)OCc1ccccc12 10.1016/j.bmcl.2008.07.125
CHEMBL476963 181690 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 357 3 0 3 3.0 CN(CCN1CCCCC1)C(=O)N1CCC2(CC1)OCc1ccccc12 10.1016/j.bmcl.2008.07.125
71625594 90567 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 395 8 2 3 5.4 CCN(CC)CCOc1ccc(NC(=O)Nc2ccc(Cl)cc2Cl)cc1 10.1016/j.bmcl.2013.03.080
CHEMBL2387298 90567 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 395 8 2 3 5.4 CCN(CC)CCOc1ccc(NC(=O)Nc2ccc(Cl)cc2Cl)cc1 10.1016/j.bmcl.2013.03.080
11672850 76701 None 2 Human Functional pIC50 = 7.4 7.4 - 1
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 7 2 2 2.1 CC(C)NCCCCCc1c[nH]cn1 10.1021/jm0504353
CHEMBL206451 76701 None 2 Human Functional pIC50 = 7.4 7.4 - 1
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 7 2 2 2.1 CC(C)NCCCCCc1c[nH]cn1 10.1021/jm0504353
44579428 186969 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 343 5 0 2 3.5 CN(CCN1CCCCC1)C(=O)N1CCC(Cc2ccccc2)CC1 10.1016/j.bmcl.2008.07.125
CHEMBL489580 186969 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 343 5 0 2 3.5 CN(CCN1CCCCC1)C(=O)N1CCC(Cc2ccccc2)CC1 10.1016/j.bmcl.2008.07.125
76311113 105935 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 424 2 0 3 3.3 O=C(c1ccccc1)N1CCCC2(CCN(C(=O)N3CCCN(C4CCC4)CC3)C2)C1 10.1021/jm4014828
CHEMBL3127688 105935 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 424 2 0 3 3.3 O=C(c1ccccc1)N1CCCC2(CCN(C(=O)N3CCCN(C4CCC4)CC3)C2)C1 10.1021/jm4014828
155550732 176734 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human H3R expressed in HEK293 cells assessed as reduction in R)(-)-alpha methylhistamine-induced inhibition of forskolin-induced cAMP accumulation by TR-FRET based LANCE ultra cAMP immunoassayAntagonist activity at human H3R expressed in HEK293 cells assessed as reduction in R)(-)-alpha methylhistamine-induced inhibition of forskolin-induced cAMP accumulation by TR-FRET based LANCE ultra cAMP immunoassay
ChEMBL 323 8 0 2 5.4 c1ccc(-c2ccc(OCCCCCN3CCCCC3)cc2)cc1 10.1016/j.bmc.2017.07.058
CHEMBL4540849 176734 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human H3R expressed in HEK293 cells assessed as reduction in R)(-)-alpha methylhistamine-induced inhibition of forskolin-induced cAMP accumulation by TR-FRET based LANCE ultra cAMP immunoassayAntagonist activity at human H3R expressed in HEK293 cells assessed as reduction in R)(-)-alpha methylhistamine-induced inhibition of forskolin-induced cAMP accumulation by TR-FRET based LANCE ultra cAMP immunoassay
ChEMBL 323 8 0 2 5.4 c1ccc(-c2ccc(OCCCCCN3CCCCC3)cc2)cc1 10.1016/j.bmc.2017.07.058
CHEMBL4597895 176734 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human H3R expressed in HEK293 cells assessed as reduction in R)(-)-alpha methylhistamine-induced inhibition of forskolin-induced cAMP accumulation by TR-FRET based LANCE ultra cAMP immunoassayAntagonist activity at human H3R expressed in HEK293 cells assessed as reduction in R)(-)-alpha methylhistamine-induced inhibition of forskolin-induced cAMP accumulation by TR-FRET based LANCE ultra cAMP immunoassay
ChEMBL 323 8 0 2 5.4 c1ccc(-c2ccc(OCCCCCN3CCCCC3)cc2)cc1 10.1016/j.bmc.2017.07.058
25139491 185065 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 419 5 0 6 4.1 COc1cccc2c(=O)n(-c3ccc(OC4CCN(C5CCC5)CC4)cc3)c(C)nc12 10.1021/jm800569w
CHEMBL485389 185065 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 419 5 0 6 4.1 COc1cccc2c(=O)n(-c3ccc(OC4CCN(C5CCC5)CC4)cc3)c(C)nc12 10.1021/jm800569w
24951036 181723 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 377 6 0 5 3.9 Cc1nc2ccccc2c(=O)n1-c1ccc(OCCCN2CCC[C@H]2C)cc1 10.1021/jm8003834
CHEMBL477361 181723 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 377 6 0 5 3.9 Cc1nc2ccccc2c(=O)n1-c1ccc(OCCCN2CCC[C@H]2C)cc1 10.1021/jm8003834
162661045 181594 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 356 8 0 5 3.4 COc1c(C)n(-c2ccc(OCCCCN3CCCC3)cc2)ccc1=O 10.1016/j.ejmech.2020.113096
CHEMBL4764747 181594 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 356 8 0 5 3.4 COc1c(C)n(-c2ccc(OCCCCN3CCCC3)cc2)ccc1=O 10.1016/j.ejmech.2020.113096
76311111 105928 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 404 2 0 4 2.6 O=C(N1CCCN(C2CCC2)CC1)N1CCC2(CCCN(C3CCOCC3)C2)C1 10.1021/jm4014828
CHEMBL3127681 105928 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 404 2 0 4 2.6 O=C(N1CCCN(C2CCC2)CC1)N1CCC2(CCCN(C3CCOCC3)C2)C1 10.1021/jm4014828
44159640 15924 None 0 Human Functional pIC50 = 8.3 8.3 3 2
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 483 8 0 9 3.0 c1ccc(Cn2nnnc2C(c2ccc(Cn3cncn3)cc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
CHEMBL1223236 15924 None 0 Human Functional pIC50 = 8.3 8.3 3 2
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 483 8 0 9 3.0 c1ccc(Cn2nnnc2C(c2ccc(Cn3cncn3)cc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
11957573 2010 None 25 Guinea pig Functional pIC50 = 8.3 8.3 -10 5
Histamine H3 receptor agonist activity was assessed by the inhibition of the electrically evoked twitch response of the guinea-pig ileum.Histamine H3 receptor agonist activity was assessed by the inhibition of the electrically evoked twitch response of the guinea-pig ileum.
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/S0960-894X(00)80659-9
1250 2010 None 25 Guinea pig Functional pIC50 = 8.3 8.3 -10 5
Histamine H3 receptor agonist activity was assessed by the inhibition of the electrically evoked twitch response of the guinea-pig ileum.Histamine H3 receptor agonist activity was assessed by the inhibition of the electrically evoked twitch response of the guinea-pig ileum.
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/S0960-894X(00)80659-9
3692 2010 None 25 Guinea pig Functional pIC50 = 8.3 8.3 -10 5
Histamine H3 receptor agonist activity was assessed by the inhibition of the electrically evoked twitch response of the guinea-pig ileum.Histamine H3 receptor agonist activity was assessed by the inhibition of the electrically evoked twitch response of the guinea-pig ileum.
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/S0960-894X(00)80659-9
CHEMBL19439 2010 None 25 Guinea pig Functional pIC50 = 8.3 8.3 -10 5
Histamine H3 receptor agonist activity was assessed by the inhibition of the electrically evoked twitch response of the guinea-pig ileum.Histamine H3 receptor agonist activity was assessed by the inhibition of the electrically evoked twitch response of the guinea-pig ileum.
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/S0960-894X(00)80659-9
164608954 184545 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human H3 receptor by TR-FRET assayAntagonist activity at human H3 receptor by TR-FRET assay
ChEMBL 368 7 1 5 3.5 Cn1cc(O)c(=O)cc1/C=C/c1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmc.2021.116306
CHEMBL4846443 184545 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human H3 receptor by TR-FRET assayAntagonist activity at human H3 receptor by TR-FRET assay
ChEMBL 368 7 1 5 3.5 Cn1cc(O)c(=O)cc1/C=C/c1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmc.2021.116306
127035470 137516 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at recombinant human H3 receptor expressed on CHO-K1 cells assessed as cAMP level by luciferase gene reporter assayAntagonist activity at recombinant human H3 receptor expressed on CHO-K1 cells assessed as cAMP level by luciferase gene reporter assay
ChEMBL 437 5 0 4 4.1 O=C1c2ccc(OC3CCN(C4CCC4)CC3)cc2CCN1C1CCN(C2CCC2)CC1 10.1016/j.ejmech.2015.12.005
CHEMBL3753475 137516 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at recombinant human H3 receptor expressed on CHO-K1 cells assessed as cAMP level by luciferase gene reporter assayAntagonist activity at recombinant human H3 receptor expressed on CHO-K1 cells assessed as cAMP level by luciferase gene reporter assay
ChEMBL 437 5 0 4 4.1 O=C1c2ccc(OC3CCN(C4CCC4)CC3)cc2CCN1C1CCN(C2CCC2)CC1 10.1016/j.ejmech.2015.12.005
11710150 155638 None 0 Rat Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at histamine H3 receptor in rat forebrain assessed as inhibition of [3H]histamine release from synaptosomesAntagonist activity at histamine H3 receptor in rat forebrain assessed as inhibition of [3H]histamine release from synaptosomes
ChEMBL 356 6 0 6 1.8 CC1CCCN1CCN1CCN(CCN2CCCC2C)C1=C(C#N)C#N 10.1016/j.bmcl.2008.03.006
CHEMBL404288 155638 None 0 Rat Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at histamine H3 receptor in rat forebrain assessed as inhibition of [3H]histamine release from synaptosomesAntagonist activity at histamine H3 receptor in rat forebrain assessed as inhibition of [3H]histamine release from synaptosomes
ChEMBL 356 6 0 6 1.8 CC1CCCN1CCN1CCN(CCN2CCCC2C)C1=C(C#N)C#N 10.1016/j.bmcl.2008.03.006
164624277 186095 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human H3 receptor by TR-FRET assayAntagonist activity at human H3 receptor by TR-FRET assay
ChEMBL 355 7 1 5 3.7 Cc1oc(/C=C/c2ccc(OCCCN3CCCC3)cc2)cc(=O)c1O 10.1016/j.bmc.2021.116306
CHEMBL4870117 186095 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human H3 receptor by TR-FRET assayAntagonist activity at human H3 receptor by TR-FRET assay
ChEMBL 355 7 1 5 3.7 Cc1oc(/C=C/c2ccc(OCCCN3CCCC3)cc2)cc(=O)c1O 10.1016/j.bmc.2021.116306
155522219 170741 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 269 2 1 4 3.2 COc1ccc(-c2nc(N)nc3c2CCCC3C)cc1 10.1021/acs.jmedchem.9b00241
CHEMBL4451233 170741 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 269 2 1 4 3.2 COc1ccc(-c2nc(N)nc3c2CCCC3C)cc1 10.1021/acs.jmedchem.9b00241
35275893 90578 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 375 6 2 3 4.5 O=C(Nc1ccc(OCCN2CCCCC2)cc1)Nc1ccc(F)cc1F 10.1016/j.bmcl.2013.03.080
CHEMBL2387308 90578 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 375 6 2 3 4.5 O=C(Nc1ccc(OCCN2CCCCC2)cc1)Nc1ccc(F)cc1F 10.1016/j.bmcl.2013.03.080
52941061 18200 None 0 Human Functional pIC50 = 7.4 7.4 32 2
Antagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 293 0 1 2 3.3 C[C@H]1C[C@](O)(C#Cc2cccc3ccccc23)[C@H](C)CN1C 10.1016/j.bmcl.2010.08.099
CHEMBL1269950 18200 None 0 Human Functional pIC50 = 7.4 7.4 32 2
Antagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 293 0 1 2 3.3 C[C@H]1C[C@](O)(C#Cc2cccc3ccccc23)[C@H](C)CN1C 10.1016/j.bmcl.2010.08.099
44159044 15925 None 0 Human Functional pIC50 = 7.4 7.4 3 2
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 442 6 0 7 4.1 c1ccc(Cn2nnnc2C(c2ccc3occc3c2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
CHEMBL1223237 15925 None 0 Human Functional pIC50 = 7.4 7.4 3 2
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 442 6 0 7 4.1 c1ccc(Cn2nnnc2C(c2ccc3occc3c2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
24951189 189891 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 391 6 0 5 4.2 Cc1nc2ccccc2c(=O)n1-c1ccc(OCCCN2CCC[C@@H](C)C2)cc1 10.1021/jm8003834
CHEMBL516126 189891 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 391 6 0 5 4.2 Cc1nc2ccccc2c(=O)n1-c1ccc(OCCCN2CCC[C@@H](C)C2)cc1 10.1021/jm8003834
44159172 15974 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 470 6 0 6 4.4 FC(F)(F)c1ccc(C(c2nnnn2Cc2ccccc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
CHEMBL1223378 15974 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 470 6 0 6 4.4 FC(F)(F)c1ccc(C(c2nnnn2Cc2ccccc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
11779175 63186 None 0 Guinea pig Functional pIC50 = 7.4 7.4 - 1
Antagonist activity against histamine H3 receptor in guinea pig ileum assessed as inhibition of electrically-evoked twitches after 30 mins in presence of (R)-alpha-methyl-histamineAntagonist activity against histamine H3 receptor in guinea pig ileum assessed as inhibition of electrically-evoked twitches after 30 mins in presence of (R)-alpha-methyl-histamine
ChEMBL 293 8 2 3 3.4 O=C(NCCCC1CCCCC1)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
CHEMBL1774600 63186 None 0 Guinea pig Functional pIC50 = 7.4 7.4 - 1
Antagonist activity against histamine H3 receptor in guinea pig ileum assessed as inhibition of electrically-evoked twitches after 30 mins in presence of (R)-alpha-methyl-histamineAntagonist activity against histamine H3 receptor in guinea pig ileum assessed as inhibition of electrically-evoked twitches after 30 mins in presence of (R)-alpha-methyl-histamine
ChEMBL 293 8 2 3 3.4 O=C(NCCCC1CCCCC1)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
CHEMBL1789801 63186 None 0 Guinea pig Functional pIC50 = 7.4 7.4 - 1
Antagonist activity against histamine H3 receptor in guinea pig ileum assessed as inhibition of electrically-evoked twitches after 30 mins in presence of (R)-alpha-methyl-histamineAntagonist activity against histamine H3 receptor in guinea pig ileum assessed as inhibition of electrically-evoked twitches after 30 mins in presence of (R)-alpha-methyl-histamine
ChEMBL 293 8 2 3 3.4 O=C(NCCCC1CCCCC1)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
11697383 184327 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 417 4 0 5 4.9 Cc1nc2ccccc2c(=O)n1-c1ccc(OC2CCN(C3CCCCC3)CC2)cc1 10.1021/jm800569w
CHEMBL483367 184327 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 417 4 0 5 4.9 Cc1nc2ccccc2c(=O)n1-c1ccc(OC2CCN(C3CCCCC3)CC2)cc1 10.1021/jm800569w
11696359 192762 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 369 3 0 3 3.1 CN(CCN1CCCCC1)C(=O)N1CCC2(CC1)CC(=O)c1ccccc12 10.1016/j.bmcl.2008.07.125
CHEMBL521798 192762 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 369 3 0 3 3.1 CN(CCN1CCCCC1)C(=O)N1CCC2(CC1)CC(=O)c1ccccc12 10.1016/j.bmcl.2008.07.125
155522219 170741 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 269 2 1 4 3.2 COc1ccc(-c2nc(N)nc3c2CCCC3C)cc1 10.1021/acs.jmedchem.9b00241
CHEMBL4451233 170741 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 269 2 1 4 3.2 COc1ccc(-c2nc(N)nc3c2CCCC3C)cc1 10.1021/acs.jmedchem.9b00241
155542256 173187 None 0 Human Functional pIC50 = 5.4 5.4 1 2
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 257 5 1 4 3.1 CCCCc1cc(-c2ccc(OC)cc2)nc(N)n1 10.1021/acs.jmedchem.9b00241
CHEMBL4519923 173187 None 0 Human Functional pIC50 = 5.4 5.4 1 2
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 257 5 1 4 3.1 CCCCc1cc(-c2ccc(OC)cc2)nc(N)n1 10.1021/acs.jmedchem.9b00241
155542256 173187 None 0 Human Functional pIC50 = 5.4 5.4 1 2
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 257 5 1 4 3.1 CCCCc1cc(-c2ccc(OC)cc2)nc(N)n1 10.1021/acs.jmedchem.9b00241
CHEMBL4519923 173187 None 0 Human Functional pIC50 = 5.4 5.4 1 2
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 257 5 1 4 3.1 CCCCc1cc(-c2ccc(OC)cc2)nc(N)n1 10.1021/acs.jmedchem.9b00241
11531102 187239 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 384 3 0 3 2.6 CN(CCN1CCCCC1)C(=O)N1CCC2(CC1)c1ccccc1C(=O)N2C 10.1016/j.bmcl.2008.07.125
CHEMBL491806 187239 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 384 3 0 3 2.6 CN(CCN1CCCCC1)C(=O)N1CCC2(CC1)c1ccccc1C(=O)N2C 10.1016/j.bmcl.2008.07.125
155538966 172895 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 255 1 2 4 2.9 CC1CCCc2c(-c3cccc(O)c3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
CHEMBL4513478 172895 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 255 1 2 4 2.9 CC1CCCc2c(-c3cccc(O)c3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
127036362 137546 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at recombinant human H3 receptor expressed on CHO-K1 cells assessed as cAMP level by luciferase gene reporter assayAntagonist activity at recombinant human H3 receptor expressed on CHO-K1 cells assessed as cAMP level by luciferase gene reporter assay
ChEMBL 387 7 1 4 3.4 CC(C)CN1CCC(NC(=O)c2ccc(OC3CCN(C(C)C)CC3)cc2)C1 10.1016/j.ejmech.2015.12.005
CHEMBL3753703 137546 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at recombinant human H3 receptor expressed on CHO-K1 cells assessed as cAMP level by luciferase gene reporter assayAntagonist activity at recombinant human H3 receptor expressed on CHO-K1 cells assessed as cAMP level by luciferase gene reporter assay
ChEMBL 387 7 1 4 3.4 CC(C)CN1CCC(NC(=O)c2ccc(OC3CCN(C(C)C)CC3)cc2)C1 10.1016/j.ejmech.2015.12.005
72164844 92155 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assay
ChEMBL 336 7 1 3 4.2 CCN(CC)Cc1ccc(OC(=O)Cc2c[nH]c3ccccc23)cc1 10.1016/j.bmc.2013.07.051
CHEMBL2419588 92155 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assay
ChEMBL 336 7 1 3 4.2 CCN(CC)Cc1ccc(OC(=O)Cc2c[nH]c3ccccc23)cc1 10.1016/j.bmc.2013.07.051
155538966 172895 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 255 1 2 4 2.9 CC1CCCc2c(-c3cccc(O)c3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
CHEMBL4513478 172895 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 255 1 2 4 2.9 CC1CCCc2c(-c3cccc(O)c3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
155544816 175137 None 0 Human Functional pIC50 = 5.3 5.3 -2 2
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 269 2 1 4 2.9 COc1ccc(-c2nc(N)nc3c2CC(C)CC3)cc1 10.1021/acs.jmedchem.9b00241
CHEMBL4567405 175137 None 0 Human Functional pIC50 = 5.3 5.3 -2 2
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 269 2 1 4 2.9 COc1ccc(-c2nc(N)nc3c2CC(C)CC3)cc1 10.1021/acs.jmedchem.9b00241
155544816 175137 None 0 Human Functional pIC50 = 5.3 5.3 -2 2
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 269 2 1 4 2.9 COc1ccc(-c2nc(N)nc3c2CC(C)CC3)cc1 10.1021/acs.jmedchem.9b00241
CHEMBL4567405 175137 None 0 Human Functional pIC50 = 5.3 5.3 -2 2
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 269 2 1 4 2.9 COc1ccc(-c2nc(N)nc3c2CC(C)CC3)cc1 10.1021/acs.jmedchem.9b00241
44158813 15818 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 420 6 0 6 3.5 Fc1ccc(C(c2nnnn2Cc2ccccc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
CHEMBL1222873 15818 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 420 6 0 6 3.5 Fc1ccc(C(c2nnnn2Cc2ccccc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
49865395 15950 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 436 6 0 6 4.0 Clc1ccccc1C(c1nnnn1Cc1ccccc1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.07.009
CHEMBL1223308 15950 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 436 6 0 6 4.0 Clc1ccccc1C(c1nnnn1Cc1ccccc1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.07.009
46212809 105933 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 395 3 0 3 3.0 O=C(c1ccccc1)N1CCC2(CC1)CC(C(=O)N1CCN(C3CCC3)CC1)C2 10.1021/jm4014828
CHEMBL3127686 105933 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 395 3 0 3 3.0 O=C(c1ccccc1)N1CCC2(CC1)CC(C(=O)N1CCN(C3CCC3)CC1)C2 10.1021/jm4014828
52943448 18215 None 0 Mouse Functional pIC50 = 6.3 6.3 -28 2
Antagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 297 3 1 2 3.9 CC1CC(O)(CCc2cccc3ccccc23)C(C)CN1C 10.1016/j.bmcl.2010.08.099
CHEMBL1270058 18215 None 0 Mouse Functional pIC50 = 6.3 6.3 -28 2
Antagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 297 3 1 2 3.9 CC1CC(O)(CCc2cccc3ccccc23)C(C)CN1C 10.1016/j.bmcl.2010.08.099
49865172 15847 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 436 7 0 7 2.7 Fc1ccc(C(c2nnnn2Cc2ccccc2)N2CCN(CC3CCCO3)CC2)cc1 10.1016/j.bmcl.2010.07.009
CHEMBL1223011 15847 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 436 7 0 7 2.7 Fc1ccc(C(c2nnnn2Cc2ccccc2)N2CCN(CC3CCCO3)CC2)cc1 10.1016/j.bmcl.2010.07.009
11537851 184300 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 363 4 0 5 3.6 CCN1CCC(Oc2ccc(-n3c(C)nc4ccccc4c3=O)cc2)CC1 10.1021/jm800569w
CHEMBL483189 184300 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 363 4 0 5 3.6 CCN1CCC(Oc2ccc(-n3c(C)nc4ccccc4c3=O)cc2)CC1 10.1021/jm800569w
46866437 92148 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assay
ChEMBL 335 6 2 3 3.7 c1ccc2c(CCNc3ccc(CN4CCOCC4)cc3)c[nH]c2c1 10.1016/j.bmc.2013.07.051
CHEMBL2419581 92148 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assay
ChEMBL 335 6 2 3 3.7 c1ccc2c(CCNc3ccc(CN4CCOCC4)cc3)c[nH]c2c1 10.1016/j.bmc.2013.07.051
162649289 180266 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 395 4 0 5 2.9 COc1c(C)n(-c2ccc(C(=O)N3CCN(C4CCCC4)CC3)cc2)ccc1=O 10.1016/j.ejmech.2020.113096
CHEMBL4748967 180266 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 395 4 0 5 2.9 COc1c(C)n(-c2ccc(C(=O)N3CCN(C4CCCC4)CC3)cc2)ccc1=O 10.1016/j.ejmech.2020.113096
46866438 92150 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assay
ChEMBL 349 7 2 3 4.0 c1ccc2c(CCCNc3ccc(CN4CCOCC4)cc3)c[nH]c2c1 10.1016/j.bmc.2013.07.051
CHEMBL2419583 92150 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assay
ChEMBL 349 7 2 3 4.0 c1ccc2c(CCCNc3ccc(CN4CCOCC4)cc3)c[nH]c2c1 10.1016/j.bmc.2013.07.051
11507778 18234 None 0 Human Functional pIC50 = 8.3 8.3 56 2
Antagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 305 0 1 2 3.4 CC1CN2CCCC2CC1(O)C#Cc1cccc2ccccc12 10.1016/j.bmcl.2010.08.099
CHEMBL1270166 18234 None 0 Human Functional pIC50 = 8.3 8.3 56 2
Antagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 305 0 1 2 3.4 CC1CN2CCCC2CC1(O)C#Cc1cccc2ccccc12 10.1016/j.bmcl.2010.08.099
164628986 186705 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human H3 receptor by TR-FRET assayAntagonist activity at human H3 receptor by TR-FRET assay
ChEMBL 382 8 1 5 4.0 CCn1cc(O)c(=O)cc1/C=C/c1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmc.2021.116306
CHEMBL4878762 186705 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human H3 receptor by TR-FRET assayAntagonist activity at human H3 receptor by TR-FRET assay
ChEMBL 382 8 1 5 4.0 CCn1cc(O)c(=O)cc1/C=C/c1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmc.2021.116306
78324476 119163 None 0 Human Functional pIC50 = 8.3 8.3 - 1
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
ChEMBL 353 8 1 3 4.0 C[C@@H]1CCCN1CCc1ccc(-c2ccc(COCC(=O)O)cc2)cc1 nan
CHEMBL3427229 119163 None 0 Human Functional pIC50 = 8.3 8.3 - 1
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
ChEMBL 353 8 1 3 4.0 C[C@@H]1CCCN1CCc1ccc(-c2ccc(COCC(=O)O)cc2)cc1 nan
78324476 119163 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
ChEMBL 353 8 1 3 4.0 C[C@@H]1CCCN1CCc1ccc(-c2ccc(COCC(=O)O)cc2)cc1 10.1021/acsmedchemlett.5b00002
CHEMBL3427229 119163 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
ChEMBL 353 8 1 3 4.0 C[C@@H]1CCCN1CCc1ccc(-c2ccc(COCC(=O)O)cc2)cc1 10.1021/acsmedchemlett.5b00002
23151202 189811 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 377 6 0 5 3.8 Cc1nc2ccccc2c(=O)n1-c1ccc(OCCCN2CCC(C)C2)cc1 10.1021/jm8003834
CHEMBL515477 189811 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 377 6 0 5 3.8 Cc1nc2ccccc2c(=O)n1-c1ccc(OCCCN2CCC(C)C2)cc1 10.1021/jm8003834
141419105 182912 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 356 7 0 5 3.4 COc1c(C)n(-c2ccc(OCCCN3CCCCC3)cc2)ccc1=O 10.1016/j.ejmech.2020.113096
CHEMBL4790750 182912 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 356 7 0 5 3.4 COc1c(C)n(-c2ccc(OCCCN3CCCCC3)cc2)ccc1=O 10.1016/j.ejmech.2020.113096
49864869 15744 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 479 7 0 7 4.4 c1ccc(Cn2nnnc2C(c2ccc(-c3ccccn3)cc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
CHEMBL1222594 15744 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 479 7 0 7 4.4 c1ccc(Cn2nnnc2C(c2ccc(-c3ccccn3)cc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
45270855 197287 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
ChEMBL 383 7 0 4 5.6 CC[C@@H]1Sc2ccccc2O[C@@H]1c1ccc(OCCCN2CCCC2)cc1 10.1016/j.bmcl.2009.05.101
CHEMBL549433 197287 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
ChEMBL 383 7 0 4 5.6 CC[C@@H]1Sc2ccccc2O[C@@H]1c1ccc(OCCCN2CCCC2)cc1 10.1016/j.bmcl.2009.05.101
172462066 196891 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human H3 receptorAntagonist activity at human H3 receptor
ChEMBL 433 10 2 4 5.0 Cc1cc(C(N)=O)c(-c2cccc(OC(=O)NCCCCCCc3ccccc3)c2)n1C 10.1021/acs.jmedchem.2c01975
CHEMBL5434282 196891 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human H3 receptorAntagonist activity at human H3 receptor
ChEMBL 433 10 2 4 5.0 Cc1cc(C(N)=O)c(-c2cccc(OC(=O)NCCCCCCc3ccccc3)c2)n1C 10.1021/acs.jmedchem.2c01975
362025 140424 None 8 Guinea pig Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at histamine H3 receptor in guinea pig ileum assessed as inhibition of (R)-alpha-methylhistamine-induced responseAntagonist activity at histamine H3 receptor in guinea pig ileum assessed as inhibition of (R)-alpha-methylhistamine-induced response
ChEMBL 406 8 0 3 3.6 CN(C)CCCOc1c(Br)cc(CCN(C)C)cc1Br 10.1021/jm8003625
CHEMBL380697 140424 None 8 Guinea pig Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at histamine H3 receptor in guinea pig ileum assessed as inhibition of (R)-alpha-methylhistamine-induced responseAntagonist activity at histamine H3 receptor in guinea pig ileum assessed as inhibition of (R)-alpha-methylhistamine-induced response
ChEMBL 406 8 0 3 3.6 CN(C)CCCOc1c(Br)cc(CCN(C)C)cc1Br 10.1021/jm8003625
44579474 187095 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 330 4 0 3 2.3 CN(CCN1CCCCC1)C(=O)N1CCN(c2ccccc2)CC1 10.1016/j.bmcl.2008.07.125
CHEMBL490612 187095 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 330 4 0 3 2.3 CN(CCN1CCCCC1)C(=O)N1CCN(c2ccccc2)CC1 10.1016/j.bmcl.2008.07.125
52952956 63178 None 0 Guinea pig Functional pIC50 = 7.3 7.3 - 1
Antagonist activity against histamine H3 receptor in guinea pig ileum assessed as inhibition of electrically-evoked twitches after 30 mins in presence of (R)-alpha-methyl-histamineAntagonist activity against histamine H3 receptor in guinea pig ileum assessed as inhibition of electrically-evoked twitches after 30 mins in presence of (R)-alpha-methyl-histamine
ChEMBL 237 7 2 3 2.0 CC/C=C/CNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
CHEMBL1774591 63178 None 0 Guinea pig Functional pIC50 = 7.3 7.3 - 1
Antagonist activity against histamine H3 receptor in guinea pig ileum assessed as inhibition of electrically-evoked twitches after 30 mins in presence of (R)-alpha-methyl-histamineAntagonist activity against histamine H3 receptor in guinea pig ileum assessed as inhibition of electrically-evoked twitches after 30 mins in presence of (R)-alpha-methyl-histamine
ChEMBL 237 7 2 3 2.0 CC/C=C/CNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
CHEMBL1789776 63178 None 0 Guinea pig Functional pIC50 = 7.3 7.3 - 1
Antagonist activity against histamine H3 receptor in guinea pig ileum assessed as inhibition of electrically-evoked twitches after 30 mins in presence of (R)-alpha-methyl-histamineAntagonist activity against histamine H3 receptor in guinea pig ileum assessed as inhibition of electrically-evoked twitches after 30 mins in presence of (R)-alpha-methyl-histamine
ChEMBL 237 7 2 3 2.0 CC/C=C/CNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
44159046 15990 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 486 7 0 7 4.3 FC(F)(F)Oc1ccc(C(c2nnnn2Cc2ccccc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
CHEMBL1223447 15990 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 486 7 0 7 4.3 FC(F)(F)Oc1ccc(C(c2nnnn2Cc2ccccc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
54765288 69361 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assayAntagonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assay
ChEMBL 361 4 2 5 3.5 Nc1nc2ccccc2nc1NC(=O)c1ccc(CN2CCCCC2)cc1 10.1016/j.bmc.2011.09.061
CHEMBL1929400 69361 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assayAntagonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assay
ChEMBL 361 4 2 5 3.5 Nc1nc2ccccc2nc1NC(=O)c1ccc(CN2CCCCC2)cc1 10.1016/j.bmc.2011.09.061
CHEMBL1929401 69361 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assayAntagonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assay
ChEMBL 361 4 2 5 3.5 Nc1nc2ccccc2nc1NC(=O)c1ccc(CN2CCCCC2)cc1 10.1016/j.bmc.2011.09.061
49865170 15845 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 432 6 0 6 3.7 Fc1ccc(C(c2nnnn2Cc2ccccc2)N2C[C@@H]3CC[C@H](C2)N3C2CCC2)cc1 10.1016/j.bmcl.2010.07.009
CHEMBL1223009 15845 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 432 6 0 6 3.7 Fc1ccc(C(c2nnnn2Cc2ccccc2)N2C[C@@H]3CC[C@H](C2)N3C2CCC2)cc1 10.1016/j.bmcl.2010.07.009
1267 3804 None 32 Human Functional pIC50 = 6.3 6.3 -6 5
Antagonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assayAntagonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2011.09.061
3035905 3804 None 32 Human Functional pIC50 = 6.3 6.3 -6 5
Antagonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assayAntagonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2011.09.061
CHEMBL260374 3804 None 32 Human Functional pIC50 = 6.3 6.3 -6 5
Antagonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assayAntagonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2011.09.061
54584376 63188 None 0 Guinea pig Functional pIC50 = 7.3 7.3 - 1
Antagonist activity against histamine H3 receptor in guinea pig ileum assessed as inhibition of electrically-evoked twitches after 30 mins in presence of (R)-alpha-methyl-histamineAntagonist activity against histamine H3 receptor in guinea pig ileum assessed as inhibition of electrically-evoked twitches after 30 mins in presence of (R)-alpha-methyl-histamine
ChEMBL 237 7 2 3 2.0 CC/C=C\CNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
CHEMBL1774592 63188 None 0 Guinea pig Functional pIC50 = 7.3 7.3 - 1
Antagonist activity against histamine H3 receptor in guinea pig ileum assessed as inhibition of electrically-evoked twitches after 30 mins in presence of (R)-alpha-methyl-histamineAntagonist activity against histamine H3 receptor in guinea pig ileum assessed as inhibition of electrically-evoked twitches after 30 mins in presence of (R)-alpha-methyl-histamine
ChEMBL 237 7 2 3 2.0 CC/C=C\CNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
CHEMBL1789809 63188 None 0 Guinea pig Functional pIC50 = 7.3 7.3 - 1
Antagonist activity against histamine H3 receptor in guinea pig ileum assessed as inhibition of electrically-evoked twitches after 30 mins in presence of (R)-alpha-methyl-histamineAntagonist activity against histamine H3 receptor in guinea pig ileum assessed as inhibition of electrically-evoked twitches after 30 mins in presence of (R)-alpha-methyl-histamine
ChEMBL 237 7 2 3 2.0 CC/C=C\CNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
57392412 69362 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assayAntagonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assay
ChEMBL 377 7 2 6 3.7 Nc1nc2ccccc2nc1NCCOc1ccc(CN2CCCCC2)cc1 10.1016/j.bmc.2011.09.061
CHEMBL1929406 69362 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assayAntagonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assay
ChEMBL 377 7 2 6 3.7 Nc1nc2ccccc2nc1NCCOc1ccc(CN2CCCCC2)cc1 10.1016/j.bmc.2011.09.061
11595838 188800 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 370 3 1 3 2.3 CN(CCN1CCCCC1)C(=O)N1CCC2(CC1)NC(=O)c1ccccc12 10.1016/j.bmcl.2008.07.125
CHEMBL504191 188800 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 370 3 1 3 2.3 CN(CCN1CCCCC1)C(=O)N1CCC2(CC1)NC(=O)c1ccccc12 10.1016/j.bmcl.2008.07.125
44579430 187269 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 355 3 0 2 3.4 CN(CCN1CCCCC1)C(=O)N1CCC2(CC1)Cc1ccccc1C2 10.1016/j.bmcl.2008.07.125
CHEMBL492030 187269 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 355 3 0 2 3.4 CN(CCN1CCCCC1)C(=O)N1CCC2(CC1)Cc1ccccc1C2 10.1016/j.bmcl.2008.07.125
72164721 92145 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assay
ChEMBL 319 5 2 2 4.8 c1ccc2c(CNc3ccc(CN4CCCCC4)cc3)c[nH]c2c1 10.1016/j.bmc.2013.07.051
CHEMBL2419578 92145 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assay
ChEMBL 319 5 2 2 4.8 c1ccc2c(CNc3ccc(CN4CCCCC4)cc3)c[nH]c2c1 10.1016/j.bmc.2013.07.051
155525816 171157 None 0 Human Functional pIC50 = 6.3 6.3 -7 2
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 257 1 1 3 3.3 CC1CCCc2c(-c3ccc(F)cc3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
CHEMBL4456972 171157 None 0 Human Functional pIC50 = 6.3 6.3 -7 2
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 257 1 1 3 3.3 CC1CCCc2c(-c3ccc(F)cc3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
155519557 170483 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 264 1 1 4 3.0 CC1CCCc2c(-c3ccc(C#N)cc3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
CHEMBL4447843 170483 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 264 1 1 4 3.0 CC1CCCc2c(-c3ccc(C#N)cc3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
155519557 170483 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 264 1 1 4 3.0 CC1CCCc2c(-c3ccc(C#N)cc3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
CHEMBL4447843 170483 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 264 1 1 4 3.0 CC1CCCc2c(-c3ccc(C#N)cc3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
52941062 18201 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 335 1 0 3 3.9 CC(=O)OC1(C#Cc2cccc3ccccc23)CC(C)N(C)CC1C 10.1016/j.bmcl.2010.08.099
CHEMBL1269951 18201 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 335 1 0 3 3.9 CC(=O)OC1(C#Cc2cccc3ccccc23)CC(C)N(C)CC1C 10.1016/j.bmcl.2010.08.099
44159519 16011 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 487 7 0 8 3.2 c1ccc(Cn2nnnc2C(c2ccc(N3CCOCC3)cc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
CHEMBL1223516 16011 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 487 7 0 8 3.2 c1ccc(Cn2nnnc2C(c2ccc(N3CCOCC3)cc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
155525816 171157 None 0 Human Functional pIC50 = 6.3 6.3 -7 2
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 257 1 1 3 3.3 CC1CCCc2c(-c3ccc(F)cc3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
CHEMBL4456972 171157 None 0 Human Functional pIC50 = 6.3 6.3 -7 2
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 257 1 1 3 3.3 CC1CCCc2c(-c3ccc(F)cc3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
44579551 187148 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 385 3 2 4 2.2 CN(CCN1CCCCC1)C(=O)N1CCC2(CC1)NC(=O)c1ccccc1N2 10.1016/j.bmcl.2008.07.125
CHEMBL490993 187148 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 385 3 2 4 2.2 CN(CCN1CCCCC1)C(=O)N1CCC2(CC1)NC(=O)c1ccccc1N2 10.1016/j.bmcl.2008.07.125
52944686 18202 None 0 Mouse Functional pIC50 = 6.2 6.2 -28 2
Antagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 295 2 1 2 3.9 CC1CC(O)(/C=C/c2cccc3ccccc23)C(C)CN1C 10.1016/j.bmcl.2010.08.099
CHEMBL1269952 18202 None 0 Mouse Functional pIC50 = 6.2 6.2 -28 2
Antagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 295 2 1 2 3.9 CC1CC(O)(/C=C/c2cccc3ccccc23)C(C)CN1C 10.1016/j.bmcl.2010.08.099
44160009 15952 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 468 8 0 7 4.0 FC(F)Oc1cccc(C(c2nnnn2Cc2ccccc2)N2CCCN(C3CCC3)CC2)c1 10.1016/j.bmcl.2010.07.009
CHEMBL1223310 15952 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 468 8 0 7 4.0 FC(F)Oc1cccc(C(c2nnnn2Cc2ccccc2)N2CCCN(C3CCC3)CC2)c1 10.1016/j.bmcl.2010.07.009
44158485 15595 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 444 6 0 7 3.3 c1ccc(Cn2nnnc2C(c2ccc3c(c2)CCO3)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
CHEMBL1221424 15595 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 444 6 0 7 3.3 c1ccc(Cn2nnnc2C(c2ccc3c(c2)CCO3)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
76332845 105924 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 375 2 0 4 2.4 O=C(C1CC2(CCN(C3CCOCC3)CC2)C1)N1CCN2CCCCC2C1 10.1021/jm4014828
CHEMBL3127677 105924 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 375 2 0 4 2.4 O=C(C1CC2(CCN(C3CCOCC3)CC2)C1)N1CCN2CCCCC2C1 10.1021/jm4014828
72546763 102616 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 340 9 2 4 3.4 N=C(NCCCCN1CCCCC1)SCCCN1CCCCC1 10.1016/j.bmcl.2013.09.052
CHEMBL2441946 102616 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 340 9 2 4 3.4 N=C(NCCCCN1CCCCC1)SCCCN1CCCCC1 10.1016/j.bmcl.2013.09.052
CHEMBL3040721 102616 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 340 9 2 4 3.4 N=C(NCCCCN1CCCCC1)SCCCN1CCCCC1 10.1016/j.bmcl.2013.09.052
72546759 102628 None 4 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 367 9 2 3 4.8 N=C(NCCCCc1ccc(Cl)cc1)SCCCN1CCCCC1 10.1016/j.bmcl.2013.09.052
CHEMBL2441942 102628 None 4 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 367 9 2 3 4.8 N=C(NCCCCc1ccc(Cl)cc1)SCCCN1CCCCC1 10.1016/j.bmcl.2013.09.052
CHEMBL3040776 102628 None 4 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 367 9 2 3 4.8 N=C(NCCCCc1ccc(Cl)cc1)SCCCN1CCCCC1 10.1016/j.bmcl.2013.09.052
72546758 102631 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 353 8 2 3 4.4 N=C(NCCCc1ccc(Cl)cc1)SCCCN1CCCCC1 10.1016/j.bmcl.2013.09.052
CHEMBL2441941 102631 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 353 8 2 3 4.4 N=C(NCCCc1ccc(Cl)cc1)SCCCN1CCCCC1 10.1016/j.bmcl.2013.09.052
CHEMBL3040779 102631 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 353 8 2 3 4.4 N=C(NCCCc1ccc(Cl)cc1)SCCCN1CCCCC1 10.1016/j.bmcl.2013.09.052
44159045 15716 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 467 7 0 7 4.2 c1ccc(Cn2nnnc2C(c2ccc(-n3cccc3)cc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
CHEMBL1222435 15716 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 467 7 0 7 4.2 c1ccc(Cn2nnnc2C(c2ccc(-n3cccc3)cc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
73348917 90563 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 354 8 2 3 3.5 CN(C)CCc1ccc(NC(=O)Nc2ccc(CCN(C)C)cc2)cc1 10.1016/j.bmcl.2013.03.080
CHEMBL2387294 90563 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 354 8 2 3 3.5 CN(C)CCc1ccc(NC(=O)Nc2ccc(CCN(C)C)cc2)cc1 10.1016/j.bmcl.2013.03.080
76329184 105936 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 460 3 0 4 2.8 O=C(N1CCCN(C2CCC2)CC1)N1CCC2(CCCN(S(=O)(=O)c3ccccc3)C2)C1 10.1021/jm4014828
CHEMBL3127689 105936 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 460 3 0 4 2.8 O=C(N1CCCN(C2CCC2)CC1)N1CCC2(CCCN(S(=O)(=O)c3ccccc3)C2)C1 10.1021/jm4014828
141419109 180095 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 342 7 0 5 3.0 COc1c(C)n(-c2ccc(OCCCN3CCCC3)cc2)ccc1=O 10.1016/j.ejmech.2020.113096
CHEMBL4746962 180095 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 342 7 0 5 3.0 COc1c(C)n(-c2ccc(OCCCN3CCCC3)cc2)ccc1=O 10.1016/j.ejmech.2020.113096
49799508 10907 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of RAHM-induced [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAntagonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of RAHM-induced [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 283 4 1 2 4.0 CC(C)c1cccc(N2CCC(Cc3c[nH]cn3)CC2)c1 10.1016/j.bmc.2010.04.052
CHEMBL1172774 10907 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of RAHM-induced [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAntagonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of RAHM-induced [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 283 4 1 2 4.0 CC(C)c1cccc(N2CCC(Cc3c[nH]cn3)CC2)c1 10.1016/j.bmc.2010.04.052
45272576 198242 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
ChEMBL 369 6 0 4 5.2 C[C@@H]1Sc2ccccc2O[C@@H]1c1ccc(OCCCN2CCCC2)cc1 10.1016/j.bmcl.2009.05.101
CHEMBL557853 198242 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
ChEMBL 369 6 0 4 5.2 C[C@@H]1Sc2ccccc2O[C@@H]1c1ccc(OCCCN2CCCC2)cc1 10.1016/j.bmcl.2009.05.101
44159637 16010 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 509 8 0 8 2.6 CN(C)S(=O)(=O)c1ccc(C(c2nnnn2Cc2ccccc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
CHEMBL1223515 16010 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 509 8 0 8 2.6 CN(C)S(=O)(=O)c1ccc(C(c2nnnn2Cc2ccccc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
78321359 160961 None 0 Human Functional pIC50 = 8.2 8.2 - 1
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
ChEMBL 361 7 1 4 3.7 C[C@@H]1CCCN1CCc1ccc(-c2ccc(CCc3nnn[nH]3)cc2)cc1 nan
CHEMBL4114986 160961 None 0 Human Functional pIC50 = 8.2 8.2 - 1
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
ChEMBL 361 7 1 4 3.7 C[C@@H]1CCCN1CCc1ccc(-c2ccc(CCc3nnn[nH]3)cc2)cc1 nan
25139032 184420 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 377 5 0 5 3.9 CCCN1CCC(Oc2ccc(-n3c(C)nc4ccccc4c3=O)cc2)CC1 10.1021/jm800569w
CHEMBL484199 184420 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 377 5 0 5 3.9 CCCN1CCC(Oc2ccc(-n3c(C)nc4ccccc4c3=O)cc2)CC1 10.1021/jm800569w
72546518 102629 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 326 6 3 4 2.4 N=C(NCc1ccc(Cl)cc1)SCCCN1CCNCC1 10.1016/j.bmcl.2013.09.052
CHEMBL2441937 102629 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 326 6 3 4 2.4 N=C(NCc1ccc(Cl)cc1)SCCCN1CCNCC1 10.1016/j.bmcl.2013.09.052
CHEMBL3040777 102629 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 326 6 3 4 2.4 N=C(NCc1ccc(Cl)cc1)SCCCN1CCNCC1 10.1016/j.bmcl.2013.09.052
49865348 15926 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 436 6 0 6 4.0 Clc1cccc(C(c2nnnn2Cc2ccccc2)N2CCCN(C3CCC3)CC2)c1 10.1016/j.bmcl.2010.07.009
CHEMBL1223238 15926 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 436 6 0 6 4.0 Clc1cccc(C(c2nnnn2Cc2ccccc2)N2CCCN(C3CCC3)CC2)c1 10.1016/j.bmcl.2010.07.009
46212800 105932 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 367 3 0 3 3.4 O=C(C1CC2(CCN(c3ccccc3)CC2)C1)N1CCN(C2CCC2)CC1 10.1021/jm4014828
CHEMBL3127685 105932 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 367 3 0 3 3.4 O=C(C1CC2(CCN(c3ccccc3)CC2)C1)N1CCN(C2CCC2)CC1 10.1021/jm4014828
25118830 105953 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 361 3 0 4 2.0 O=C(C1CC12CCN(C1CCC1)CC2)N1CCN(C2CCOCC2)CC1 10.1021/jm4014828
CHEMBL3127706 105953 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 361 3 0 4 2.0 O=C(C1CC12CCN(C1CCC1)CC2)N1CCN(C2CCOCC2)CC1 10.1021/jm4014828
155523256 170849 None 0 Human Functional pIC50 = 7.2 7.2 3 2
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 269 2 1 4 3.2 COc1cccc(-c2nc(N)nc3c2CCCC3C)c1 10.1021/acs.jmedchem.9b00241
CHEMBL4452406 170849 None 0 Human Functional pIC50 = 7.2 7.2 3 2
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 269 2 1 4 3.2 COc1cccc(-c2nc(N)nc3c2CCCC3C)c1 10.1021/acs.jmedchem.9b00241
155548338 173846 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 240 1 1 4 2.6 CC1CCCc2c(-c3cccnc3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
CHEMBL4536532 173846 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 240 1 1 4 2.6 CC1CCCc2c(-c3cccnc3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
54584374 63144 None 0 Guinea pig Functional pIC50 = 7.2 7.2 - 1
Antagonist activity against histamine H3 receptor in guinea pig ileum assessed as inhibition of electrically-evoked twitches after 30 mins in presence of (R)-alpha-methyl-histamineAntagonist activity against histamine H3 receptor in guinea pig ileum assessed as inhibition of electrically-evoked twitches after 30 mins in presence of (R)-alpha-methyl-histamine
ChEMBL 223 7 2 3 1.6 C=CCCNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
CHEMBL1774590 63144 None 0 Guinea pig Functional pIC50 = 7.2 7.2 - 1
Antagonist activity against histamine H3 receptor in guinea pig ileum assessed as inhibition of electrically-evoked twitches after 30 mins in presence of (R)-alpha-methyl-histamineAntagonist activity against histamine H3 receptor in guinea pig ileum assessed as inhibition of electrically-evoked twitches after 30 mins in presence of (R)-alpha-methyl-histamine
ChEMBL 223 7 2 3 1.6 C=CCCNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
CHEMBL1789360 63144 None 0 Guinea pig Functional pIC50 = 7.2 7.2 - 1
Antagonist activity against histamine H3 receptor in guinea pig ileum assessed as inhibition of electrically-evoked twitches after 30 mins in presence of (R)-alpha-methyl-histamineAntagonist activity against histamine H3 receptor in guinea pig ileum assessed as inhibition of electrically-evoked twitches after 30 mins in presence of (R)-alpha-methyl-histamine
ChEMBL 223 7 2 3 1.6 C=CCCNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
44579607 187238 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 385 3 0 4 3.0 CN(CCN1CCCCC1)C(=O)N1CCC2(CC1)CC(=O)c1ccccc1O2 10.1016/j.bmcl.2008.07.125
CHEMBL491805 187238 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 385 3 0 4 3.0 CN(CCN1CCCCC1)C(=O)N1CCC2(CC1)CC(=O)c1ccccc1O2 10.1016/j.bmcl.2008.07.125
162650881 180325 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 381 4 0 5 2.5 COc1c(C)n(-c2ccc(C(=O)N3CCN(C4CCC4)CC3)cc2)ccc1=O 10.1016/j.ejmech.2020.113096
CHEMBL4749796 180325 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 381 4 0 5 2.5 COc1c(C)n(-c2ccc(C(=O)N3CCN(C4CCC4)CC3)cc2)ccc1=O 10.1016/j.ejmech.2020.113096
164623115 185620 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human H3 receptor by TR-FRET assayAntagonist activity at human H3 receptor by TR-FRET assay
ChEMBL 357 7 1 6 2.6 O=c1cc(/C=C/c2ccc(OCCCN3CCOCC3)cc2)occ1O 10.1016/j.bmc.2021.116306
CHEMBL4862604 185620 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human H3 receptor by TR-FRET assayAntagonist activity at human H3 receptor by TR-FRET assay
ChEMBL 357 7 1 6 2.6 O=c1cc(/C=C/c2ccc(OCCCN3CCOCC3)cc2)occ1O 10.1016/j.bmc.2021.116306
44579427 188508 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 301 3 0 2 2.6 CN(CCN1CCCCC1)C(=O)N1CCc2ccccc2C1 10.1016/j.bmcl.2008.07.125
CHEMBL501876 188508 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 301 3 0 2 2.6 CN(CCN1CCCCC1)C(=O)N1CCc2ccccc2C1 10.1016/j.bmcl.2008.07.125
155548338 173846 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 240 1 1 4 2.6 CC1CCCc2c(-c3cccnc3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
CHEMBL4536532 173846 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 240 1 1 4 2.6 CC1CCCc2c(-c3cccnc3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
52944521 18253 None 0 Mouse Functional pIC50 = 6.2 6.2 -57 2
Antagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 294 0 1 3 2.7 CC1CC(O)(C#Cc2cccc3ncccc23)C(C)CN1C 10.1016/j.bmcl.2010.08.099
CHEMBL1270264 18253 None 0 Mouse Functional pIC50 = 6.2 6.2 -57 2
Antagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 294 0 1 3 2.7 CC1CC(O)(C#Cc2cccc3ncccc23)C(C)CN1C 10.1016/j.bmcl.2010.08.099
23151144 191357 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 417 4 0 5 4.9 Cc1nc2ccccc2c(=O)n1-c1ccc(OC2CCCN(C3CCCC3)CC2)cc1 10.1021/jm800569w
CHEMBL519018 191357 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 417 4 0 5 4.9 Cc1nc2ccccc2c(=O)n1-c1ccc(OC2CCCN(C3CCCC3)CC2)cc1 10.1021/jm800569w
164617436 185035 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human H3 receptor by TR-FRET assayAntagonist activity at human H3 receptor by TR-FRET assay
ChEMBL 356 9 1 5 3.4 CCN(CC)CCCOc1ccc(/C=C/c2cc(=O)c(O)cn2C)cc1 10.1016/j.bmc.2021.116306
CHEMBL4853496 185035 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human H3 receptor by TR-FRET assayAntagonist activity at human H3 receptor by TR-FRET assay
ChEMBL 356 9 1 5 3.4 CCN(CC)CCCOc1ccc(/C=C/c2cc(=O)c(O)cn2C)cc1 10.1016/j.bmc.2021.116306
71625597 90571 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 377 9 2 3 4.7 CCN(CC)CCCOc1ccc(NC(=O)Nc2ccc(F)cc2F)cc1 10.1016/j.bmcl.2013.03.080
CHEMBL2387301 90571 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 377 9 2 3 4.7 CCN(CC)CCCOc1ccc(NC(=O)Nc2ccc(F)cc2F)cc1 10.1016/j.bmcl.2013.03.080
11679993 76044 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 7 2 2 2.0 CC(C)CNCCCCc1c[nH]cn1 10.1021/jm0504353
CHEMBL205559 76044 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 7 2 2 2.0 CC(C)CNCCCCc1c[nH]cn1 10.1021/jm0504353
72546757 102613 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 339 7 2 3 4.0 N=C(NCCc1ccc(Cl)cc1)SCCCN1CCCCC1 10.1016/j.bmcl.2013.09.052
CHEMBL2441940 102613 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 339 7 2 3 4.0 N=C(NCCc1ccc(Cl)cc1)SCCCN1CCCCC1 10.1016/j.bmcl.2013.09.052
CHEMBL3040715 102613 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 339 7 2 3 4.0 N=C(NCCc1ccc(Cl)cc1)SCCCN1CCCCC1 10.1016/j.bmcl.2013.09.052
141419110 179709 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 356 8 0 5 3.4 CCOc1c(C)n(-c2ccc(OCCCN3CCCC3)cc2)ccc1=O 10.1016/j.ejmech.2020.113096
CHEMBL4742309 179709 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 356 8 0 5 3.4 CCOc1c(C)n(-c2ccc(OCCCN3CCCC3)cc2)ccc1=O 10.1016/j.ejmech.2020.113096
155523256 170849 None 0 Human Functional pIC50 = 7.2 7.2 3 2
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 269 2 1 4 3.2 COc1cccc(-c2nc(N)nc3c2CCCC3C)c1 10.1021/acs.jmedchem.9b00241
CHEMBL4452406 170849 None 0 Human Functional pIC50 = 7.2 7.2 3 2
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 269 2 1 4 3.2 COc1cccc(-c2nc(N)nc3c2CCCC3C)c1 10.1021/acs.jmedchem.9b00241
52943330 18254 None 0 Human Functional pIC50 = 6.2 6.2 13 2
Antagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 294 0 1 3 2.7 CC1CC(O)(C#Cc2cccc3cccnc23)C(C)CN1C 10.1016/j.bmcl.2010.08.099
CHEMBL1270265 18254 None 0 Human Functional pIC50 = 6.2 6.2 13 2
Antagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 294 0 1 3 2.7 CC1CC(O)(C#Cc2cccc3cccnc23)C(C)CN1C 10.1016/j.bmcl.2010.08.099
71625480 90564 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 327 6 2 3 3.9 Cc1cccc(NC(=O)Nc2ccc(OCCN(C)C)cc2)c1C 10.1016/j.bmcl.2013.03.080
CHEMBL2387295 90564 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 327 6 2 3 3.9 Cc1cccc(NC(=O)Nc2ccc(OCCN(C)C)cc2)c1C 10.1016/j.bmcl.2013.03.080
49865047 15816 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 380 5 0 6 2.6 CN1CCCN(C(c2ccc(F)cc2)c2nnnn2Cc2ccccc2)CC1 10.1016/j.bmcl.2010.07.009
CHEMBL1222871 15816 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 380 5 0 6 2.6 CN1CCCN(C(c2ccc(F)cc2)c2nnnn2Cc2ccccc2)CC1 10.1016/j.bmcl.2010.07.009
25118126 105950 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 403 3 0 4 3.1 O=C(C1CC12CCN(C1CCOCC1)CC2)N1CCN(C2CCCCCC2)CC1 10.1021/jm4014828
CHEMBL3127703 105950 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 403 3 0 4 3.1 O=C(C1CC12CCN(C1CCOCC1)CC2)N1CCN(C2CCCCCC2)CC1 10.1021/jm4014828
25139031 192518 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 349 3 0 5 3.2 Cc1nc2ccccc2c(=O)n1-c1ccc(OC2CCN(C)CC2)cc1 10.1021/jm800569w
CHEMBL520800 192518 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 349 3 0 5 3.2 Cc1nc2ccccc2c(=O)n1-c1ccc(OC2CCN(C)CC2)cc1 10.1021/jm800569w
44579549 192870 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 384 3 1 3 2.2 CN(CCN1CCCCC1)C(=O)N1CCC2(CC1)NC(=O)Cc1ccccc12 10.1016/j.bmcl.2008.07.125
CHEMBL522117 192870 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 384 3 1 3 2.2 CN(CCN1CCCCC1)C(=O)N1CCC2(CC1)NC(=O)Cc1ccccc12 10.1016/j.bmcl.2008.07.125
10314270 102595 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 325 6 2 3 4.0 N=C(NCc1ccc(Cl)cc1)SCCCN1CCCCC1 10.1016/j.bmcl.2013.09.052
CHEMBL2441935 102595 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 325 6 2 3 4.0 N=C(NCc1ccc(Cl)cc1)SCCCN1CCCCC1 10.1016/j.bmcl.2013.09.052
CHEMBL3040654 102595 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 325 6 2 3 4.0 N=C(NCc1ccc(Cl)cc1)SCCCN1CCCCC1 10.1016/j.bmcl.2013.09.052
46866439 92154 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assay
ChEMBL 350 5 1 4 3.1 O=C(Cc1c[nH]c2ccccc12)Oc1ccc(CN2CCOCC2)cc1 10.1016/j.bmc.2013.07.051
CHEMBL2419587 92154 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assay
ChEMBL 350 5 1 4 3.1 O=C(Cc1c[nH]c2ccccc12)Oc1ccc(CN2CCOCC2)cc1 10.1016/j.bmc.2013.07.051
78324474 119160 None 0 Human Functional pIC50 = 8.1 8.1 - 1
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
ChEMBL 323 6 1 2 4.0 C[C@@H]1CCCN1CCc1ccc(-c2ccc(CC(=O)O)cc2)cc1 nan
CHEMBL3427226 119160 None 0 Human Functional pIC50 = 8.1 8.1 - 1
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
ChEMBL 323 6 1 2 4.0 C[C@@H]1CCCN1CCc1ccc(-c2ccc(CC(=O)O)cc2)cc1 nan
78324474 119160 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
ChEMBL 323 6 1 2 4.0 C[C@@H]1CCCN1CCc1ccc(-c2ccc(CC(=O)O)cc2)cc1 10.1021/acsmedchemlett.5b00002
CHEMBL3427226 119160 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
ChEMBL 323 6 1 2 4.0 C[C@@H]1CCCN1CCc1ccc(-c2ccc(CC(=O)O)cc2)cc1 10.1021/acsmedchemlett.5b00002
164618887 186010 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human H3 receptor by TR-FRET assayAntagonist activity at human H3 receptor by TR-FRET assay
ChEMBL 341 7 1 5 3.4 O=c1cc(/C=C/c2ccc(OCCCN3CCCC3)cc2)occ1O 10.1016/j.bmc.2021.116306
CHEMBL4868743 186010 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human H3 receptor by TR-FRET assayAntagonist activity at human H3 receptor by TR-FRET assay
ChEMBL 341 7 1 5 3.4 O=c1cc(/C=C/c2ccc(OCCCN3CCCC3)cc2)occ1O 10.1016/j.bmc.2021.116306
76314722 105700 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 349 3 0 4 1.8 CC(C)N1CCN(C(=O)[C@H]2CC23CCN(C2CCOCC2)CC3)CC1 10.1021/jm4014828
CHEMBL3124968 105700 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 349 3 0 4 1.8 CC(C)N1CCN(C(=O)[C@H]2CC23CCN(C2CCOCC2)CC3)CC1 10.1021/jm4014828
16082831 80377 None 0 Human Functional pIC50 = 8.1 8.1 100 3
Antagonist activity at human H3 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assayAntagonist activity at human H3 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assay
ChEMBL 275 6 2 2 3.3 Clc1ccc(CNCC[C@H]2C[C@@H]2c2c[nH]cn2)cc1 10.1021/jm0603318
CHEMBL214311 80377 None 0 Human Functional pIC50 = 8.1 8.1 100 3
Antagonist activity at human H3 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assayAntagonist activity at human H3 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assay
ChEMBL 275 6 2 2 3.3 Clc1ccc(CNCC[C@H]2C[C@@H]2c2c[nH]cn2)cc1 10.1021/jm0603318
23151223 184608 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 389 4 0 5 4.1 Cc1nc2ccccc2c(=O)n1-c1ccc(OC2CCC(N3CCCC3)C2)cc1 10.1021/jm800569w
CHEMBL484740 184608 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 389 4 0 5 4.1 Cc1nc2ccccc2c(=O)n1-c1ccc(OC2CCC(N3CCCC3)C2)cc1 10.1021/jm800569w
45268290 198565 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
ChEMBL 367 6 0 4 5.4 CC1=C(c2ccc(OCCCN3CCCC3)cc2)Oc2ccccc2S1 10.1016/j.bmcl.2009.05.101
CHEMBL560923 198565 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
ChEMBL 367 6 0 4 5.4 CC1=C(c2ccc(OCCCN3CCCC3)cc2)Oc2ccccc2S1 10.1016/j.bmcl.2009.05.101
25118127 105948 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 375 3 0 4 2.4 O=C(C1CC12CCN(C1CCOCC1)CC2)N1CCN(C2CCCC2)CC1 10.1021/jm4014828
CHEMBL3127701 105948 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 375 3 0 4 2.4 O=C(C1CC12CCN(C1CCOCC1)CC2)N1CCN(C2CCCC2)CC1 10.1021/jm4014828
141351664 182793 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 356 5 0 5 3.4 COc1c(C)n(-c2ccc(OC3CCN(C(C)C)CC3)cc2)ccc1=O 10.1016/j.ejmech.2020.113096
CHEMBL4789311 182793 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
ChEMBL 356 5 0 5 3.4 COc1c(C)n(-c2ccc(OC3CCN(C(C)C)CC3)cc2)ccc1=O 10.1016/j.ejmech.2020.113096
72164838 92146 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assay
ChEMBL 333 6 2 2 4.8 c1ccc2c(CCNc3ccc(CN4CCCCC4)cc3)c[nH]c2c1 10.1016/j.bmc.2013.07.051
CHEMBL2419579 92146 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assay
ChEMBL 333 6 2 2 4.8 c1ccc2c(CCNc3ccc(CN4CCCCC4)cc3)c[nH]c2c1 10.1016/j.bmc.2013.07.051
52943449 18218 None 0 Mouse Functional pIC50 = 6.1 6.1 -9 2
Antagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 293 0 1 2 3.3 CC1CC(O)(C#Cc2ccc3ccccc3c2)C(C)CN1C 10.1016/j.bmcl.2010.08.099
CHEMBL1270060 18218 None 0 Mouse Functional pIC50 = 6.1 6.1 -9 2
Antagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 293 0 1 2 3.3 CC1CC(O)(C#Cc2ccc3ccccc3c2)C(C)CN1C 10.1016/j.bmcl.2010.08.099
23151329 185200 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 403 4 0 5 4.5 Cc1nc2ccccc2c(=O)n1-c1ccc(O[C@H]2CC[C@H](N3CCCC3)CC2)cc1 10.1021/jm800569w
CHEMBL485604 185200 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 403 4 0 5 4.5 Cc1nc2ccccc2c(=O)n1-c1ccc(O[C@H]2CC[C@H](N3CCCC3)CC2)cc1 10.1021/jm800569w
25119191 105919 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 382 3 0 4 3.2 O=C(C1CC12CCN(c1ccncc1)CC2)N1CCN(C2CCCCC2)CC1 10.1021/jm4014828
CHEMBL3127671 105919 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 382 3 0 4 3.2 O=C(C1CC12CCN(c1ccncc1)CC2)N1CCN(C2CCCCC2)CC1 10.1021/jm4014828
172457780 196310 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Inhibition of recombinant human histamine H3 receptor stably expressed in HEK293 cells assessed as increase in cAMP accumulation in presence of forskolin incubated for 30 mins by TR-FRET LANCE assayInhibition of recombinant human histamine H3 receptor stably expressed in HEK293 cells assessed as increase in cAMP accumulation in presence of forskolin incubated for 30 mins by TR-FRET LANCE assay
ChEMBL 309 6 0 2 5.0 c1ccc(-c2ccc(OCCCN3CCCCCC3)cc2)cc1 10.1021/acs.jmedchem.3c00430
CHEMBL5421122 196310 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Inhibition of recombinant human histamine H3 receptor stably expressed in HEK293 cells assessed as increase in cAMP accumulation in presence of forskolin incubated for 30 mins by TR-FRET LANCE assayInhibition of recombinant human histamine H3 receptor stably expressed in HEK293 cells assessed as increase in cAMP accumulation in presence of forskolin incubated for 30 mins by TR-FRET LANCE assay
ChEMBL 309 6 0 2 5.0 c1ccc(-c2ccc(OCCCN3CCCCCC3)cc2)cc1 10.1021/acs.jmedchem.3c00430
172447536 195938 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Inhibition of recombinant human histamine H3 receptor stably expressed in HEK293 cells assessed as increase in cAMP accumulation in presence of forskolin incubated for 30 mins by TR-FRET LANCE assayInhibition of recombinant human histamine H3 receptor stably expressed in HEK293 cells assessed as increase in cAMP accumulation in presence of forskolin incubated for 30 mins by TR-FRET LANCE assay
ChEMBL 310 7 1 3 4.7 c1ccc(Nc2ccc(OCCCN3CCCCC3)cc2)cc1 10.1021/acs.jmedchem.3c00430
CHEMBL5413694 195938 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Inhibition of recombinant human histamine H3 receptor stably expressed in HEK293 cells assessed as increase in cAMP accumulation in presence of forskolin incubated for 30 mins by TR-FRET LANCE assayInhibition of recombinant human histamine H3 receptor stably expressed in HEK293 cells assessed as increase in cAMP accumulation in presence of forskolin incubated for 30 mins by TR-FRET LANCE assay
ChEMBL 310 7 1 3 4.7 c1ccc(Nc2ccc(OCCCN3CCCCC3)cc2)cc1 10.1021/acs.jmedchem.3c00430
9578063 43403 None 6 Guinea pig Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at histamine H3 receptor in guinea pig ileum assessed as inhibition of (R)-alpha-methylhistamine-induced responseAntagonist activity at histamine H3 receptor in guinea pig ileum assessed as inhibition of (R)-alpha-methylhistamine-induced response
ChEMBL 380 7 3 5 1.9 COc1ccc(C/C(=N\O)C(=O)NCCc2c[nH]cn2)cc1Br 10.1021/jm8003625
CHEMBL15075 43403 None 6 Guinea pig Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at histamine H3 receptor in guinea pig ileum assessed as inhibition of (R)-alpha-methylhistamine-induced responseAntagonist activity at histamine H3 receptor in guinea pig ileum assessed as inhibition of (R)-alpha-methylhistamine-induced response
ChEMBL 380 7 3 5 1.9 COc1ccc(C/C(=N\O)C(=O)NCCc2c[nH]cn2)cc1Br 10.1021/jm8003625
52943449 18218 None 0 Human Functional pIC50 = 7.1 7.1 9 2
Antagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 293 0 1 2 3.3 CC1CC(O)(C#Cc2ccc3ccccc3c2)C(C)CN1C 10.1016/j.bmcl.2010.08.099
CHEMBL1270060 18218 None 0 Human Functional pIC50 = 7.1 7.1 9 2
Antagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 293 0 1 2 3.3 CC1CC(O)(C#Cc2ccc3ccccc3c2)C(C)CN1C 10.1016/j.bmcl.2010.08.099
52941024 18216 None 0 Mouse Functional pIC50 = 7.1 7.1 -42 2
Antagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 297 3 1 2 3.9 C[C@H]1CN(C)[C@H](C)C[C@@]1(O)CCc1cccc2ccccc12 10.1016/j.bmcl.2010.08.099
CHEMBL1270059 18216 None 0 Mouse Functional pIC50 = 7.1 7.1 -42 2
Antagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 297 3 1 2 3.9 C[C@H]1CN(C)[C@H](C)C[C@@]1(O)CCc1cccc2ccccc12 10.1016/j.bmcl.2010.08.099
155565842 175720 None 0 Human Functional pIC50 = 7.1 7.1 5 2
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 317 1 1 3 3.9 CC1CCCc2c(-c3cccc(Br)c3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
CHEMBL4580450 175720 None 0 Human Functional pIC50 = 7.1 7.1 5 2
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 317 1 1 3 3.9 CC1CCCc2c(-c3cccc(Br)c3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
164610106 184982 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human H3 receptor by TR-FRET assayAntagonist activity at human H3 receptor by TR-FRET assay
ChEMBL 328 7 1 5 2.6 CN(C)CCCOc1ccc(/C=C/c2cc(=O)c(O)cn2C)cc1 10.1016/j.bmc.2021.116306
CHEMBL4852674 184982 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human H3 receptor by TR-FRET assayAntagonist activity at human H3 receptor by TR-FRET assay
ChEMBL 328 7 1 5 2.6 CN(C)CCCOc1ccc(/C=C/c2cc(=O)c(O)cn2C)cc1 10.1016/j.bmc.2021.116306
76318296 105920 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 349 3 0 4 1.8 CC(C)N1CCN(C(=O)[C@@H]2CC23CCN(C2CCOCC2)CC3)CC1 10.1021/jm4014828
CHEMBL3127672 105920 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 349 3 0 4 1.8 CC(C)N1CCN(C(=O)[C@@H]2CC23CCN(C2CCOCC2)CC3)CC1 10.1021/jm4014828
44579389 187068 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 329 4 0 2 3.4 CN(CCN1CCCCC1)C(=O)N1CCC(c2ccccc2)CC1 10.1016/j.bmcl.2008.07.125
CHEMBL490400 187068 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 329 4 0 2 3.4 CN(CCN1CCCCC1)C(=O)N1CCC(c2ccccc2)CC1 10.1016/j.bmcl.2008.07.125
52941057 18191 None 0 Human Functional pIC50 = 8.1 8.1 13 2
Antagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 293 0 1 2 3.3 C[C@H]1CN(C)[C@H](C)C[C@@]1(O)C#Cc1cccc2ccccc12 10.1016/j.bmcl.2010.08.099
CHEMBL1269844 18191 None 0 Human Functional pIC50 = 8.1 8.1 13 2
Antagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 293 0 1 2 3.3 C[C@H]1CN(C)[C@H](C)C[C@@]1(O)C#Cc1cccc2ccccc12 10.1016/j.bmcl.2010.08.099
155567030 176522 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human H3R expressed in HEK293 cells assessed as reduction in R)(-)-alpha methylhistamine-induced inhibition of forskolin-induced cAMP accumulation by TR-FRET based LANCE ultra cAMP immunoassayAntagonist activity at human H3R expressed in HEK293 cells assessed as reduction in R)(-)-alpha methylhistamine-induced inhibition of forskolin-induced cAMP accumulation by TR-FRET based LANCE ultra cAMP immunoassay
ChEMBL 337 8 0 2 5.8 c1ccc(-c2ccc(OCCCCCN3CCCCCC3)cc2)cc1 10.1016/j.bmc.2017.07.058
CHEMBL4586133 176522 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human H3R expressed in HEK293 cells assessed as reduction in R)(-)-alpha methylhistamine-induced inhibition of forskolin-induced cAMP accumulation by TR-FRET based LANCE ultra cAMP immunoassayAntagonist activity at human H3R expressed in HEK293 cells assessed as reduction in R)(-)-alpha methylhistamine-induced inhibition of forskolin-induced cAMP accumulation by TR-FRET based LANCE ultra cAMP immunoassay
ChEMBL 337 8 0 2 5.8 c1ccc(-c2ccc(OCCCCCN3CCCCCC3)cc2)cc1 10.1016/j.bmc.2017.07.058
CHEMBL4596108 176522 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human H3R expressed in HEK293 cells assessed as reduction in R)(-)-alpha methylhistamine-induced inhibition of forskolin-induced cAMP accumulation by TR-FRET based LANCE ultra cAMP immunoassayAntagonist activity at human H3R expressed in HEK293 cells assessed as reduction in R)(-)-alpha methylhistamine-induced inhibition of forskolin-induced cAMP accumulation by TR-FRET based LANCE ultra cAMP immunoassay
ChEMBL 337 8 0 2 5.8 c1ccc(-c2ccc(OCCCCCN3CCCCCC3)cc2)cc1 10.1016/j.bmc.2017.07.058
71625598 90572 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 385 10 2 4 4.8 CCOc1ccc(C)cc1NC(=O)Nc1ccc(OCCN(CC)CC)cc1 10.1016/j.bmcl.2013.03.080
CHEMBL2387302 90572 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 385 10 2 4 4.8 CCOc1ccc(C)cc1NC(=O)Nc1ccc(OCCN(CC)CC)cc1 10.1016/j.bmcl.2013.03.080
49864802 15730 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 484 7 0 9 3.7 Cc1nonc1-c1ccc(C(c2nnnn2Cc2ccccc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
CHEMBL1222500 15730 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 484 7 0 9 3.7 Cc1nonc1-c1ccc(C(c2nnnn2Cc2ccccc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
44159759 15923 None 0 Rat Functional pIC50 = 8.0 8.0 -5 2
Antagonist activity at rat histamine H3 receptorAntagonist activity at rat histamine H3 receptor
ChEMBL 469 7 0 9 3.0 c1ccc(Cn2nnnc2C(c2ccc(-n3cncn3)cc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
CHEMBL1223235 15923 None 0 Rat Functional pIC50 = 8.0 8.0 -5 2
Antagonist activity at rat histamine H3 receptorAntagonist activity at rat histamine H3 receptor
ChEMBL 469 7 0 9 3.0 c1ccc(Cn2nnnc2C(c2ccc(-n3cncn3)cc2)N2CCCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2010.07.009
155565842 175720 None 0 Human Functional pIC50 = 7.1 7.1 5 2
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 317 1 1 3 3.9 CC1CCCc2c(-c3cccc(Br)c3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
CHEMBL4580450 175720 None 0 Human Functional pIC50 = 7.1 7.1 5 2
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 317 1 1 3 3.9 CC1CCCc2c(-c3cccc(Br)c3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
3201696 15776 None 2 Human Functional pIC50 = 6.1 6.1 22 2
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 348 5 0 6 2.1 CN1CCN(C(c2ccccc2)c2nnnn2Cc2ccccc2)CC1 10.1016/j.bmcl.2010.07.009
CHEMBL1222728 15776 None 2 Human Functional pIC50 = 6.1 6.1 22 2
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 348 5 0 6 2.1 CN1CCN(C(c2ccccc2)c2nnnn2Cc2ccccc2)CC1 10.1016/j.bmcl.2010.07.009
76318297 105927 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 364 2 0 4 1.7 CC(C)N1CCN(C(=O)N2CC3(CCN(C4CCOCC4)CC3)C2)CC1 10.1021/jm4014828
CHEMBL3127680 105927 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
ChEMBL 364 2 0 4 1.7 CC(C)N1CCN(C(=O)N2CC3(CCN(C4CCOCC4)CC3)C2)CC1 10.1021/jm4014828
155553964 175561 None 0 Human Functional pIC50 = 6.1 6.1 -11 2
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 273 1 1 3 3.8 CC1CCCc2c(-c3ccc(Cl)cc3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
CHEMBL4576986 175561 None 0 Human Functional pIC50 = 6.1 6.1 -11 2
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 273 1 1 3 3.8 CC1CCCc2c(-c3ccc(Cl)cc3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
11545613 184422 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 391 6 0 5 4.3 CCCCN1CCC(Oc2ccc(-n3c(C)nc4ccccc4c3=O)cc2)CC1 10.1021/jm800569w
CHEMBL484200 184422 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 391 6 0 5 4.3 CCCCN1CCC(Oc2ccc(-n3c(C)nc4ccccc4c3=O)cc2)CC1 10.1021/jm800569w
155553964 175561 None 0 Human Functional pIC50 = 6.0 6.0 -11 2
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 273 1 1 3 3.8 CC1CCCc2c(-c3ccc(Cl)cc3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
CHEMBL4576986 175561 None 0 Human Functional pIC50 = 6.0 6.0 -11 2
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
ChEMBL 273 1 1 3 3.8 CC1CCCc2c(-c3ccc(Cl)cc3)nc(N)nc21 10.1021/acs.jmedchem.9b00241
49865048 15817 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 394 6 0 6 3.0 CCN1CCCN(C(c2ccc(F)cc2)c2nnnn2Cc2ccccc2)CC1 10.1016/j.bmcl.2010.07.009
CHEMBL1222872 15817 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 394 6 0 6 3.0 CCN1CCCN(C(c2ccc(F)cc2)c2nnnn2Cc2ccccc2)CC1 10.1016/j.bmcl.2010.07.009
52943330 18254 None 0 Mouse Functional pIC50 = 5.0 5.0 -13 2
Antagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 294 0 1 3 2.7 CC1CC(O)(C#Cc2cccc3cccnc23)C(C)CN1C 10.1016/j.bmcl.2010.08.099
CHEMBL1270265 18254 None 0 Mouse Functional pIC50 = 5.0 5.0 -13 2
Antagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 294 0 1 3 2.7 CC1CC(O)(C#Cc2cccc3cccnc23)C(C)CN1C 10.1016/j.bmcl.2010.08.099
44159887 15759 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 455 6 0 7 3.9 Cn1ccc2cc(C(c3nnnn3Cc3ccccc3)N3CCCN(C4CCC4)CC3)ccc21 10.1016/j.bmcl.2010.07.009
CHEMBL1222663 15759 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 455 6 0 7 3.9 Cn1ccc2cc(C(c3nnnn3Cc3ccccc3)N3CCCN(C4CCC4)CC3)ccc21 10.1016/j.bmcl.2010.07.009
44579431 193392 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 405 5 0 2 4.6 CN(CCN1CCCCC1)C(=O)N1CCC(c2ccccc2)(c2ccccc2)CC1 10.1016/j.bmcl.2008.07.125
CHEMBL523992 193392 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 405 5 0 2 4.6 CN(CCN1CCCCC1)C(=O)N1CCC(c2ccccc2)(c2ccccc2)CC1 10.1016/j.bmcl.2008.07.125
44455850 97885 None 0 Human Functional pKd = 10.7 10.7 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 415 6 1 4 4.4 CNCc1cc(C(=O)N2CCCN(C(C)C)CC2)ccc1Oc1ccc(Cl)cc1 10.1016/j.bmcl.2007.11.016
CHEMBL272077 97885 None 0 Human Functional pKd = 10.7 10.7 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 415 6 1 4 4.4 CNCc1cc(C(=O)N2CCCN(C(C)C)CC2)ccc1Oc1ccc(Cl)cc1 10.1016/j.bmcl.2007.11.016
24855949 155144 None 0 Human Functional pKd = 10.7 10.7 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 379 6 1 4 3.5 CNCc1cc(C(=O)N2CCCN(C3CC3)CC2)ccc1Oc1ccccc1 10.1016/j.bmcl.2007.11.016
CHEMBL401683 155144 None 0 Human Functional pKd = 10.7 10.7 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 379 6 1 4 3.5 CNCc1cc(C(=O)N2CCCN(C3CC3)CC2)ccc1Oc1ccccc1 10.1016/j.bmcl.2007.11.016
24856012 95784 None 0 Human Functional pKd = 10.7 10.7 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 397 6 1 4 3.6 CNCc1cc(C(=O)N2CCCN(C3CC3)CC2)ccc1Oc1ccc(F)cc1 10.1016/j.bmcl.2007.11.016
CHEMBL258349 95784 None 0 Human Functional pKd = 10.7 10.7 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 397 6 1 4 3.6 CNCc1cc(C(=O)N2CCCN(C3CC3)CC2)ccc1Oc1ccc(F)cc1 10.1016/j.bmcl.2007.11.016
24856010 95525 None 0 Human Functional pKd = 10.4 10.4 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 404 6 1 5 3.4 CNCc1cc(C(=O)N2CCCN(C3CC3)CC2)ccc1Oc1cccc(C#N)c1 10.1016/j.bmcl.2007.11.016
CHEMBL257208 95525 None 0 Human Functional pKd = 10.4 10.4 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 404 6 1 5 3.4 CNCc1cc(C(=O)N2CCCN(C3CC3)CC2)ccc1Oc1cccc(C#N)c1 10.1016/j.bmcl.2007.11.016
44455822 98026 None 0 Human Functional pKd = 10.4 10.4 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 413 6 1 4 4.2 CNCc1cc(C(=O)N2CCCN(C3CC3)CC2)ccc1Oc1cccc(Cl)c1 10.1016/j.bmcl.2007.11.016
CHEMBL272699 98026 None 0 Human Functional pKd = 10.4 10.4 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 413 6 1 4 4.2 CNCc1cc(C(=O)N2CCCN(C3CC3)CC2)ccc1Oc1cccc(Cl)c1 10.1016/j.bmcl.2007.11.016
24856047 95475 None 0 Human Functional pKd = 10.4 10.4 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 404 6 1 5 3.4 CNCc1cc(C(=O)N2CCCN(C3CC3)CC2)ccc1Oc1ccccc1C#N 10.1016/j.bmcl.2007.11.016
CHEMBL257009 95475 None 0 Human Functional pKd = 10.4 10.4 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 404 6 1 5 3.4 CNCc1cc(C(=O)N2CCCN(C3CC3)CC2)ccc1Oc1ccccc1C#N 10.1016/j.bmcl.2007.11.016
24856014 98105 None 0 Human Functional pKd = 10.4 10.4 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 409 7 1 5 3.5 CNCc1cc(C(=O)N2CCCN(C3CC3)CC2)ccc1Oc1cccc(OC)c1 10.1016/j.bmcl.2007.11.016
CHEMBL273136 98105 None 0 Human Functional pKd = 10.4 10.4 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 409 7 1 5 3.5 CNCc1cc(C(=O)N2CCCN(C3CC3)CC2)ccc1Oc1cccc(OC)c1 10.1016/j.bmcl.2007.11.016
24855980 98025 None 0 Human Functional pKd = 10.3 10.3 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 431 6 1 4 4.3 CNCc1cc(C(=O)N2CCCN(C3CC3)CC2)ccc1Oc1ccc(Cl)cc1F 10.1016/j.bmcl.2007.11.016
CHEMBL272698 98025 None 0 Human Functional pKd = 10.3 10.3 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 431 6 1 4 4.3 CNCc1cc(C(=O)N2CCCN(C3CC3)CC2)ccc1Oc1ccc(Cl)cc1F 10.1016/j.bmcl.2007.11.016
24855979 98068 None 0 Human Functional pKd = 10.3 10.3 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 431 6 1 4 4.3 CNCc1cc(C(=O)N2CCCN(C3CC3)CC2)ccc1Oc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2007.11.016
CHEMBL272917 98068 None 0 Human Functional pKd = 10.3 10.3 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 431 6 1 4 4.3 CNCc1cc(C(=O)N2CCCN(C3CC3)CC2)ccc1Oc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2007.11.016
24855981 155702 None 0 Human Functional pKd = 10.3 10.3 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 404 6 1 5 3.4 CNCc1cc(C(=O)N2CCCN(C3CC3)CC2)ccc1Oc1ccc(C#N)cc1 10.1016/j.bmcl.2007.11.016
CHEMBL404572 155702 None 0 Human Functional pKd = 10.3 10.3 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 404 6 1 5 3.4 CNCc1cc(C(=O)N2CCCN(C3CC3)CC2)ccc1Oc1ccc(C#N)cc1 10.1016/j.bmcl.2007.11.016
44455512 95685 None 0 Human Functional pKd = 10.1 10.1 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 413 6 1 4 4.2 CNCc1cc(C(=O)N2CCCN(C3CC3)CC2)ccc1Oc1ccc(Cl)cc1 10.1016/j.bmcl.2007.11.016
CHEMBL257909 95685 None 0 Human Functional pKd = 10.1 10.1 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 413 6 1 4 4.2 CNCc1cc(C(=O)N2CCCN(C3CC3)CC2)ccc1Oc1ccc(Cl)cc1 10.1016/j.bmcl.2007.11.016
9928224 134426 None 0 Guinea pig Functional pKd = 10.1 10.1 - 0
Antagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileumAntagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileum
ChEMBL 346 6 2 3 3.3 O=C(CCN1CCC(Cc2c[nH]cn2)CC1)Nc1ccc(Cl)cc1 10.1016/j.bmcl.2005.09.076
CHEMBL371730 134426 None 0 Guinea pig Functional pKd = 10.1 10.1 - 0
Antagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileumAntagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileum
ChEMBL 346 6 2 3 3.3 O=C(CCN1CCC(Cc2c[nH]cn2)CC1)Nc1ccc(Cl)cc1 10.1016/j.bmcl.2005.09.076
10286408 200475 None 0 Human Functional pKd = 10.1 10.1 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation treated 10 min before histamine challengeAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation treated 10 min before histamine challenge
ChEMBL 310 4 0 2 3.9 C(#Cc1cccc(CN2CCCCC2)c1)CCN1CCCCC1 10.1016/j.ejmech.2009.04.049
CHEMBL573817 200475 None 0 Human Functional pKd = 10.1 10.1 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation treated 10 min before histamine challengeAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation treated 10 min before histamine challenge
ChEMBL 310 4 0 2 3.9 C(#Cc1cccc(CN2CCCCC2)c1)CCN1CCCCC1 10.1016/j.ejmech.2009.04.049
24855918 155175 None 0 Human Functional pKd = 10 10.0 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 397 6 1 4 3.6 CNCc1cc(C(=O)N2CCCN(C3CC3)CC2)ccc1Oc1cccc(F)c1 10.1016/j.bmcl.2007.11.016
CHEMBL401867 155175 None 0 Human Functional pKd = 10 10.0 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 397 6 1 4 3.6 CNCc1cc(C(=O)N2CCCN(C3CC3)CC2)ccc1Oc1cccc(F)c1 10.1016/j.bmcl.2007.11.016
1223 953 None 33 Human Functional pKd = 10 10.0 1 4
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1016/j.bmcl.2013.09.052
2790 953 None 33 Human Functional pKd = 10 10.0 1 4
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1016/j.bmcl.2013.09.052
CHEMBL14690 953 None 33 Human Functional pKd = 10 10.0 1 4
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1016/j.bmcl.2013.09.052
24855952 95529 None 0 Human Functional pKd = 10.0 10.0 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 439 7 1 5 4.5 CNCc1cc(C(=O)N2CCCN(C3CC3)CC2)ccc1Oc1ccc(SC)c(C)c1 10.1016/j.bmcl.2007.11.016
CHEMBL257221 95529 None 0 Human Functional pKd = 10.0 10.0 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 439 7 1 5 4.5 CNCc1cc(C(=O)N2CCCN(C3CC3)CC2)ccc1Oc1ccc(SC)c(C)c1 10.1016/j.bmcl.2007.11.016
44455851 97926 None 0 Human Functional pKd = 10.0 10.0 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 415 6 1 4 4.4 CNCc1cc(C(=O)N2CCCN(C(C)C)CC2)ccc1Oc1cccc(Cl)c1 10.1016/j.bmcl.2007.11.016
CHEMBL272289 97926 None 0 Human Functional pKd = 10.0 10.0 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 415 6 1 4 4.4 CNCc1cc(C(=O)N2CCCN(C(C)C)CC2)ccc1Oc1cccc(Cl)c1 10.1016/j.bmcl.2007.11.016
24856107 97128 None 0 Human Functional pKd = 10.0 10.0 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 427 7 1 5 4.5 CNCc1cc(C(=O)N2CCCN(C(C)C)CC2)ccc1Oc1ccc(SC)cc1 10.1016/j.bmcl.2007.11.016
CHEMBL267267 97128 None 0 Human Functional pKd = 10.0 10.0 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 427 7 1 5 4.5 CNCc1cc(C(=O)N2CCCN(C(C)C)CC2)ccc1Oc1ccc(SC)cc1 10.1016/j.bmcl.2007.11.016
9862335 72921 None 0 Guinea pig Functional pKd = 9.9 9.9 - 0
Antagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileumAntagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileum
ChEMBL 330 6 2 3 2.8 O=C(CCN1CCC(Cc2c[nH]cn2)CC1)Nc1cccc(F)c1 10.1016/j.bmcl.2005.09.076
CHEMBL200382 72921 None 0 Guinea pig Functional pKd = 9.9 9.9 - 0
Antagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileumAntagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileum
ChEMBL 330 6 2 3 2.8 O=C(CCN1CCC(Cc2c[nH]cn2)CC1)Nc1cccc(F)c1 10.1016/j.bmcl.2005.09.076
46861756 8574 None 0 Human Functional pKd = 9.9 9.9 - 0
Antagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 403 4 0 4 2.3 CC(=O)N1C[C@@H](Oc2ccc(F)cc2)C[C@@H]1C(=O)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.03.071
CHEMBL1094562 8574 None 0 Human Functional pKd = 9.9 9.9 - 0
Antagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 403 4 0 4 2.3 CC(=O)N1C[C@@H](Oc2ccc(F)cc2)C[C@@H]1C(=O)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.03.071
1256 2148 None 46 Human Functional pKd = 9.8 9.8 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 316 7 0 3 3.9 C1CCN(CC1)CCCOc1ccc(cc1)CN1CCCCC1 10.1016/j.bmcl.2007.04.056
2766326 2148 None 46 Human Functional pKd = 9.8 9.8 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 316 7 0 3 3.9 C1CCN(CC1)CCCOc1ccc(cc1)CN1CCCCC1 10.1016/j.bmcl.2007.04.056
CHEMBL129542 2148 None 46 Human Functional pKd = 9.8 9.8 - 1
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 316 7 0 3 3.9 C1CCN(CC1)CCCOc1ccc(cc1)CN1CCCCC1 10.1016/j.bmcl.2007.04.056
1256 2148 None 46 Human Functional pKd = 9.8 9.8 - 1
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrs
ChEMBL 316 7 0 3 3.9 C1CCN(CC1)CCCOc1ccc(cc1)CN1CCCCC1 10.1016/j.ejmech.2009.06.007
2766326 2148 None 46 Human Functional pKd = 9.8 9.8 - 1
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrs
ChEMBL 316 7 0 3 3.9 C1CCN(CC1)CCCOc1ccc(cc1)CN1CCCCC1 10.1016/j.ejmech.2009.06.007
CHEMBL129542 2148 None 46 Human Functional pKd = 9.8 9.8 - 1
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrs
ChEMBL 316 7 0 3 3.9 C1CCN(CC1)CCCOc1ccc(cc1)CN1CCCCC1 10.1016/j.ejmech.2009.06.007
1256 2148 None 46 Human Functional pKd = 9.8 9.8 - 1
Histamine-induced inhibition of forskolin- stimulated cAMP accumulation in SK-N-MC cells overexpressing the human Histamine H3 receptorHistamine-induced inhibition of forskolin- stimulated cAMP accumulation in SK-N-MC cells overexpressing the human Histamine H3 receptor
ChEMBL 316 7 0 3 3.9 C1CCN(CC1)CCCOc1ccc(cc1)CN1CCCCC1 10.1021/jm030185v
2766326 2148 None 46 Human Functional pKd = 9.8 9.8 - 1
Histamine-induced inhibition of forskolin- stimulated cAMP accumulation in SK-N-MC cells overexpressing the human Histamine H3 receptorHistamine-induced inhibition of forskolin- stimulated cAMP accumulation in SK-N-MC cells overexpressing the human Histamine H3 receptor
ChEMBL 316 7 0 3 3.9 C1CCN(CC1)CCCOc1ccc(cc1)CN1CCCCC1 10.1021/jm030185v
CHEMBL129542 2148 None 46 Human Functional pKd = 9.8 9.8 - 1
Histamine-induced inhibition of forskolin- stimulated cAMP accumulation in SK-N-MC cells overexpressing the human Histamine H3 receptorHistamine-induced inhibition of forskolin- stimulated cAMP accumulation in SK-N-MC cells overexpressing the human Histamine H3 receptor
ChEMBL 316 7 0 3 3.9 C1CCN(CC1)CCCOc1ccc(cc1)CN1CCCCC1 10.1021/jm030185v
10193212 145184 None 0 Human Functional pKd = 9.8 9.8 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation treated 10 min before histamine challengeAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation treated 10 min before histamine challenge
ChEMBL 310 4 0 2 3.9 C(#Cc1ccc(CN2CCCCC2)cc1)CCN1CCCCC1 10.1016/j.ejmech.2009.04.049
CHEMBL391168 145184 None 0 Human Functional pKd = 9.8 9.8 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation treated 10 min before histamine challengeAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation treated 10 min before histamine challenge
ChEMBL 310 4 0 2 3.9 C(#Cc1ccc(CN2CCCCC2)cc1)CCN1CCCCC1 10.1016/j.ejmech.2009.04.049
44581099 187971 None 0 Human Functional pKd = 9.8 9.8 - 0
Antagonist activity at human recombinant histamine H3 receptor expressed in human SK-N-MC cellsAntagonist activity at human recombinant histamine H3 receptor expressed in human SK-N-MC cells
ChEMBL 358 6 0 4 3.7 c1cc(OCC2CN(C3CCCC3)CCO2)ccc1CN1CCCCC1 10.1016/j.bmcl.2008.09.077
CHEMBL496366 187971 None 0 Human Functional pKd = 9.8 9.8 - 0
Antagonist activity at human recombinant histamine H3 receptor expressed in human SK-N-MC cellsAntagonist activity at human recombinant histamine H3 receptor expressed in human SK-N-MC cells
ChEMBL 358 6 0 4 3.7 c1cc(OCC2CN(C3CCCC3)CCO2)ccc1CN1CCCCC1 10.1016/j.bmcl.2008.09.077
25061410 18389 None 0 Human Functional pKd = 9.8 9.8 - 0
Antagonist activity against human histamine H3 receptorAntagonist activity against human histamine H3 receptor
ChEMBL 382 4 1 4 2.3 O=C(c1ccc2c(CN3CCOCC3)c[nH]c2c1)N1CCN(C2CCC2)CC1 10.1016/j.bmcl.2010.08.103
CHEMBL1271277 18389 None 0 Human Functional pKd = 9.8 9.8 - 0
Antagonist activity against human histamine H3 receptorAntagonist activity against human histamine H3 receptor
ChEMBL 382 4 1 4 2.3 O=C(c1ccc2c(CN3CCOCC3)c[nH]c2c1)N1CCN(C2CCC2)CC1 10.1016/j.bmcl.2010.08.103
9884637 135800 None 0 Guinea pig Functional pKd = 9.8 9.8 - 0
Antagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileumAntagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileum
ChEMBL 346 6 2 3 3.3 O=C(CCN1CCC(Cc2c[nH]cn2)CC1)Nc1cccc(Cl)c1 10.1016/j.bmcl.2005.09.076
CHEMBL373000 135800 None 0 Guinea pig Functional pKd = 9.8 9.8 - 0
Antagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileumAntagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileum
ChEMBL 346 6 2 3 3.3 O=C(CCN1CCC(Cc2c[nH]cn2)CC1)Nc1cccc(Cl)c1 10.1016/j.bmcl.2005.09.076
24855953 95575 None 0 Human Functional pKd = 9.8 9.8 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 425 7 1 5 4.2 CNCc1cc(C(=O)N2CCCN(C3CC3)CC2)ccc1Oc1ccc(SC)cc1 10.1016/j.bmcl.2007.11.016
CHEMBL257434 95575 None 0 Human Functional pKd = 9.8 9.8 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 425 7 1 5 4.2 CNCc1cc(C(=O)N2CCCN(C3CC3)CC2)ccc1Oc1ccc(SC)cc1 10.1016/j.bmcl.2007.11.016
24855884 95644 None 0 Human Functional pKd = 9.8 9.8 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 447 6 1 4 4.8 CNCc1cc(C(=O)N2CCCN(C3CC3)CC2)ccc1Oc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2007.11.016
CHEMBL257738 95644 None 0 Human Functional pKd = 9.8 9.8 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 447 6 1 4 4.8 CNCc1cc(C(=O)N2CCCN(C3CC3)CC2)ccc1Oc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2007.11.016
9880608 19423 None 0 Human Functional pKd = 9.7 9.7 - 0
Histamine-induced inhibition of forskolin- stimulated cAMP accumulation in SK-N-MC cells overexpressing the human Histamine H3 receptorHistamine-induced inhibition of forskolin- stimulated cAMP accumulation in SK-N-MC cells overexpressing the human Histamine H3 receptor
ChEMBL 330 8 1 3 4.4 c1cc(OCCCN2CCCCC2)ccc1CNC1CCCCC1 10.1021/jm030185v
CHEMBL129411 19423 None 0 Human Functional pKd = 9.7 9.7 - 0
Histamine-induced inhibition of forskolin- stimulated cAMP accumulation in SK-N-MC cells overexpressing the human Histamine H3 receptorHistamine-induced inhibition of forskolin- stimulated cAMP accumulation in SK-N-MC cells overexpressing the human Histamine H3 receptor
ChEMBL 330 8 1 3 4.4 c1cc(OCCCN2CCCCC2)ccc1CNC1CCCCC1 10.1021/jm030185v
49865043 15814 None 0 Guinea pig Functional pKd = 9.7 9.7 - 0
Antagonist activity at histamine H3 receptor in electrically-stimulated guinea pig ileumAntagonist activity at histamine H3 receptor in electrically-stimulated guinea pig ileum
ChEMBL 504 8 0 7 3.2 CN(C)CCCn1c(=O)n(C2CCN(C(=O)C3CCN(Cc4ccncc4)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2010.07.052
CHEMBL1222865 15814 None 0 Guinea pig Functional pKd = 9.7 9.7 - 0
Antagonist activity at histamine H3 receptor in electrically-stimulated guinea pig ileumAntagonist activity at histamine H3 receptor in electrically-stimulated guinea pig ileum
ChEMBL 504 8 0 7 3.2 CN(C)CCCn1c(=O)n(C2CCN(C(=O)C3CCN(Cc4ccncc4)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2010.07.052
10292893 183965 None 0 Human Functional pKd = 9.7 9.7 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 375 6 0 5 3.8 CC(C)N1CCC(COc2ncc(C(=O)c3cccc(Cl)c3)n2C)CC1 10.1016/j.bmcl.2008.11.114
CHEMBL480829 183965 None 0 Human Functional pKd = 9.7 9.7 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 375 6 0 5 3.8 CC(C)N1CCC(COc2ncc(C(=O)c3cccc(Cl)c3)n2C)CC1 10.1016/j.bmcl.2008.11.114
24855886 155454 None 0 Human Functional pKd = 9.7 9.7 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 447 6 1 4 4.5 CNCc1cc(C(=O)N2CCCN(C3CC3)CC2)ccc1Oc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2007.11.016
CHEMBL403377 155454 None 0 Human Functional pKd = 9.7 9.7 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 447 6 1 4 4.5 CNCc1cc(C(=O)N2CCCN(C3CC3)CC2)ccc1Oc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2007.11.016
10131681 19405 None 1 Human Functional pKd = 9.6 9.6 - 1
Histamine-induced inhibition of forskolin- stimulated cAMP accumulation in SK-N-MC cells overexpressing the human Histamine H3 receptorHistamine-induced inhibition of forskolin- stimulated cAMP accumulation in SK-N-MC cells overexpressing the human Histamine H3 receptor
ChEMBL 332 7 1 4 2.9 OC1CCN(Cc2ccc(OCCCN3CCCCC3)cc2)CC1 10.1021/jm030185v
CHEMBL129306 19405 None 1 Human Functional pKd = 9.6 9.6 - 1
Histamine-induced inhibition of forskolin- stimulated cAMP accumulation in SK-N-MC cells overexpressing the human Histamine H3 receptorHistamine-induced inhibition of forskolin- stimulated cAMP accumulation in SK-N-MC cells overexpressing the human Histamine H3 receptor
ChEMBL 332 7 1 4 2.9 OC1CCN(Cc2ccc(OCCCN3CCCCC3)cc2)CC1 10.1021/jm030185v
10359235 62693 None 0 Human Functional pKd = 9.6 9.6 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrs
ChEMBL 329 4 0 3 2.8 CC(C)N1CCN(C(=O)c2ccc(CN3CCCCC3)cc2)CC1 10.1016/j.ejmech.2009.06.007
CHEMBL1783889 62693 None 0 Human Functional pKd = 9.6 9.6 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrs
ChEMBL 329 4 0 3 2.8 CC(C)N1CCN(C(=O)c2ccc(CN3CCCCC3)cc2)CC1 10.1016/j.ejmech.2009.06.007
24783527 18355 None 0 Human Functional pKd = 9.6 9.6 - 0
Antagonist activity against human histamine H3 receptorAntagonist activity against human histamine H3 receptor
ChEMBL 370 4 1 4 2.2 CC(C)N1CCN(C(=O)c2ccc3c(CN4CCOCC4)c[nH]c3c2)CC1 10.1016/j.bmcl.2010.08.103
CHEMBL1270966 18355 None 0 Human Functional pKd = 9.6 9.6 - 0
Antagonist activity against human histamine H3 receptorAntagonist activity against human histamine H3 receptor
ChEMBL 370 4 1 4 2.2 CC(C)N1CCN(C(=O)c2ccc3c(CN4CCOCC4)c[nH]c3c2)CC1 10.1016/j.bmcl.2010.08.103
24856046 95099 None 0 Human Functional pKd = 9.6 9.6 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 463 7 1 5 4.4 CNCc1cc(C(=O)N2CCCN(C3CC3)CC2)ccc1Oc1ccccc1OC(F)(F)F 10.1016/j.bmcl.2007.11.016
CHEMBL255127 95099 None 0 Human Functional pKd = 9.6 9.6 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 463 7 1 5 4.4 CNCc1cc(C(=O)N2CCCN(C3CC3)CC2)ccc1Oc1ccccc1OC(F)(F)F 10.1016/j.bmcl.2007.11.016
72546759 102628 None 4 Human Functional pKd = 9.6 9.6 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 367 9 2 3 4.8 N=C(NCCCCc1ccc(Cl)cc1)SCCCN1CCCCC1 10.1016/j.bmcl.2013.09.052
CHEMBL2441942 102628 None 4 Human Functional pKd = 9.6 9.6 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 367 9 2 3 4.8 N=C(NCCCCc1ccc(Cl)cc1)SCCCN1CCCCC1 10.1016/j.bmcl.2013.09.052
CHEMBL3040776 102628 None 4 Human Functional pKd = 9.6 9.6 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 367 9 2 3 4.8 N=C(NCCCCc1ccc(Cl)cc1)SCCCN1CCCCC1 10.1016/j.bmcl.2013.09.052
24771416 10727 None 0 Human Functional pKd = 9.6 9.6 - 0
Antagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 351 4 0 4 3.6 O=C(c1ccc(Oc2ccccc2)nc1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.05.041
CHEMBL1170999 10727 None 0 Human Functional pKd = 9.6 9.6 - 0
Antagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 351 4 0 4 3.6 O=C(c1ccc(Oc2ccccc2)nc1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.05.041
24771627 10836 None 0 Human Functional pKd = 9.5 9.5 - 0
Antagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 407 4 0 4 4.7 CC(C)N1CCCN(C(=O)c2ccc(Oc3ccc(Cl)c(Cl)c3)cn2)CC1 10.1016/j.bmcl.2010.05.041
CHEMBL1172074 10836 None 0 Human Functional pKd = 9.5 9.5 - 0
Antagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 407 4 0 4 4.7 CC(C)N1CCCN(C(=O)c2ccc(Oc3ccc(Cl)c(Cl)c3)cn2)CC1 10.1016/j.bmcl.2010.05.041
52941660 18397 None 0 Human Functional pKd = 9.5 9.5 - 0
Antagonist activity against human histamine H3 receptorAntagonist activity against human histamine H3 receptor
ChEMBL 398 4 0 5 2.6 CC(C)N1CCCN(C(=O)c2ccc3c(CN4CCOCC4)cn(C)c3c2)CC1 10.1016/j.bmcl.2010.08.103
CHEMBL1271381 18397 None 0 Human Functional pKd = 9.5 9.5 - 0
Antagonist activity against human histamine H3 receptorAntagonist activity against human histamine H3 receptor
ChEMBL 398 4 0 5 2.6 CC(C)N1CCCN(C(=O)c2ccc3c(CN4CCOCC4)cn(C)c3c2)CC1 10.1016/j.bmcl.2010.08.103
44598902 8823 None 0 Human Functional pKd = 9.5 9.5 - 0
Antagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 403 4 0 4 2.3 CC(=O)N1C[C@@H](Oc2cccc(F)c2)C[C@@H]1C(=O)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.03.071
CHEMBL1096827 8823 None 0 Human Functional pKd = 9.5 9.5 - 0
Antagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 403 4 0 4 2.3 CC(=O)N1C[C@@H](Oc2cccc(F)c2)C[C@@H]1C(=O)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.03.071
10155386 183964 None 0 Human Functional pKd = 9.5 9.5 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 359 6 0 5 3.3 CC(C)N1CCC(COc2ncc(C(=O)c3ccc(F)cc3)n2C)CC1 10.1016/j.bmcl.2008.11.114
CHEMBL480828 183964 None 0 Human Functional pKd = 9.5 9.5 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 359 6 0 5 3.3 CC(C)N1CCC(COc2ncc(C(=O)c3ccc(F)cc3)n2C)CC1 10.1016/j.bmcl.2008.11.114
44571277 184121 None 0 Human Functional pKd = 9.5 9.5 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 341 6 0 5 3.2 CC(C)N1CCC(COc2ncc(C(=O)c3ccccc3)n2C)CC1 10.1016/j.bmcl.2008.11.114
CHEMBL482008 184121 None 0 Human Functional pKd = 9.5 9.5 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 341 6 0 5 3.2 CC(C)N1CCC(COc2ncc(C(=O)c3ccccc3)n2C)CC1 10.1016/j.bmcl.2008.11.114
24771013 10618 None 0 Human Functional pKd = 9.5 9.5 - 0
Antagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 385 4 0 4 4.1 O=C(c1ccc(Sc2ccc(F)cc2)nc1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.05.041
CHEMBL1170110 10618 None 0 Human Functional pKd = 9.5 9.5 - 0
Antagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 385 4 0 4 4.1 O=C(c1ccc(Sc2ccc(F)cc2)nc1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.05.041
24771071 10756 None 0 Human Functional pKd = 9.5 9.5 - 0
Antagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 367 4 0 4 3.9 O=C(c1ccc(Sc2ccccc2)nc1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.05.041
CHEMBL1171343 10756 None 0 Human Functional pKd = 9.5 9.5 - 0
Antagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 367 4 0 4 3.9 O=C(c1ccc(Sc2ccccc2)nc1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.05.041
44581098 187941 None 0 Human Functional pKd = 9.5 9.5 - 0
Antagonist activity at human recombinant histamine H3 receptor expressed in human SK-N-MC cellsAntagonist activity at human recombinant histamine H3 receptor expressed in human SK-N-MC cells
ChEMBL 344 6 0 4 3.3 c1cc(OCC2CN(C3CCCC3)CCO2)ccc1CN1CCCC1 10.1016/j.bmcl.2008.09.077
CHEMBL496167 187941 None 0 Human Functional pKd = 9.5 9.5 - 0
Antagonist activity at human recombinant histamine H3 receptor expressed in human SK-N-MC cellsAntagonist activity at human recombinant histamine H3 receptor expressed in human SK-N-MC cells
ChEMBL 344 6 0 4 3.3 c1cc(OCC2CN(C3CCCC3)CCO2)ccc1CN1CCCC1 10.1016/j.bmcl.2008.09.077
11666852 62714 None 0 Human Functional pKd = 9.5 9.5 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrs
ChEMBL 317 7 0 4 3.3 c1cc(OCCCN2CCCCC2)ncc1CN1CCCCC1 10.1016/j.ejmech.2009.06.007
CHEMBL1783910 62714 None 0 Human Functional pKd = 9.5 9.5 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrs
ChEMBL 317 7 0 4 3.3 c1cc(OCCCN2CCCCC2)ncc1CN1CCCCC1 10.1016/j.ejmech.2009.06.007
24771368 10787 None 12 Human Functional pKd = 9.4 9.4 - 0
Antagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 369 4 0 4 3.7 O=C(c1ccc(Oc2ccc(F)cc2)nc1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.05.041
CHEMBL1171754 10787 None 12 Human Functional pKd = 9.4 9.4 - 0
Antagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 369 4 0 4 3.7 O=C(c1ccc(Oc2ccc(F)cc2)nc1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.05.041
25211254 188081 None 0 Human Functional pKd = 9.4 9.4 - 0
Antagonist activity at human recombinant histamine H3 receptor expressed in human SK-N-MC cellsAntagonist activity at human recombinant histamine H3 receptor expressed in human SK-N-MC cells
ChEMBL 360 6 0 5 2.5 c1cc(OC[C@@H]2CN(C3CCCC3)CCO2)ccc1CN1CCOCC1 10.1016/j.bmcl.2008.09.077
CHEMBL497192 188081 None 0 Human Functional pKd = 9.4 9.4 - 0
Antagonist activity at human recombinant histamine H3 receptor expressed in human SK-N-MC cellsAntagonist activity at human recombinant histamine H3 receptor expressed in human SK-N-MC cells
ChEMBL 360 6 0 5 2.5 c1cc(OC[C@@H]2CN(C3CCCC3)CCO2)ccc1CN1CCOCC1 10.1016/j.bmcl.2008.09.077
24856048 169107 None 3 Human Functional pKd = 9.4 9.4 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 447 6 1 4 4.5 CNCc1cc(C(=O)N2CCCN(C3CC3)CC2)ccc1Oc1ccccc1C(F)(F)F 10.1016/j.bmcl.2007.11.016
CHEMBL439246 169107 None 3 Human Functional pKd = 9.4 9.4 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 447 6 1 4 4.5 CNCc1cc(C(=O)N2CCCN(C3CC3)CC2)ccc1Oc1ccccc1C(F)(F)F 10.1016/j.bmcl.2007.11.016
24771524 10701 None 0 Human Functional pKd = 9.4 9.4 - 0
Antagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 369 4 0 4 3.7 O=C(c1ccc(Oc2cccc(F)c2)nc1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.05.041
CHEMBL1170790 10701 None 0 Human Functional pKd = 9.4 9.4 - 0
Antagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 369 4 0 4 3.7 O=C(c1ccc(Oc2cccc(F)c2)nc1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.05.041
23624312 10789 None 1 Human Functional pKd = 9.4 9.4 - 0
Antagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 376 4 0 5 3.4 N#Cc1cccc(Oc2ccc(C(=O)N3CCCN(C4CCC4)CC3)cn2)c1 10.1016/j.bmcl.2010.05.041
CHEMBL1171756 10789 None 1 Human Functional pKd = 9.4 9.4 - 0
Antagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 376 4 0 5 3.4 N#Cc1cccc(Oc2ccc(C(=O)N3CCCN(C4CCC4)CC3)cn2)c1 10.1016/j.bmcl.2010.05.041
11174563 62699 None 0 Human Functional pKd = 9.4 9.4 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrs
ChEMBL 317 7 0 4 3.3 c1cc(CN2CCCCC2)ncc1OCCCN1CCCCC1 10.1016/j.ejmech.2009.06.007
CHEMBL1783895 62699 None 0 Human Functional pKd = 9.4 9.4 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrs
ChEMBL 317 7 0 4 3.3 c1cc(CN2CCCCC2)ncc1OCCCN1CCCCC1 10.1016/j.ejmech.2009.06.007
9858195 70263 None 4 Human Functional pKd = 9.3 9.3 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrs
ChEMBL 318 5 0 4 2.8 CC(C)N1CCC(Oc2ccc(CN3CCOCC3)cc2)CC1 10.1016/j.ejmech.2009.06.007
CHEMBL194092 70263 None 4 Human Functional pKd = 9.3 9.3 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrs
ChEMBL 318 5 0 4 2.8 CC(C)N1CCC(Oc2ccc(CN3CCOCC3)cc2)CC1 10.1016/j.ejmech.2009.06.007
25126154 62709 None 0 Human Functional pKd = 9.3 9.3 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrs
ChEMBL 330 4 0 4 2.2 CC(C)N1CCN(C(=O)c2ccc(CN3CCCCC3)cn2)CC1 10.1016/j.ejmech.2009.06.007
CHEMBL1783905 62709 None 0 Human Functional pKd = 9.3 9.3 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrs
ChEMBL 330 4 0 4 2.2 CC(C)N1CCN(C(=O)c2ccc(CN3CCCCC3)cn2)CC1 10.1016/j.ejmech.2009.06.007
9944610 89470 None 20 Human Functional pKd = 9.3 9.3 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation treated 10 min before histamine challengeAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation treated 10 min before histamine challenge
ChEMBL 312 4 0 3 2.7 C(#Cc1cccc(CN2CCOCC2)c1)CCN1CCCCC1 10.1016/j.ejmech.2009.04.049
CHEMBL237087 89470 None 20 Human Functional pKd = 9.3 9.3 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation treated 10 min before histamine challengeAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation treated 10 min before histamine challenge
ChEMBL 312 4 0 3 2.7 C(#Cc1cccc(CN2CCOCC2)c1)CCN1CCCCC1 10.1016/j.ejmech.2009.04.049
11694965 75863 None 0 Human Functional pKd = 9.3 9.3 - 0
Activity against human histamine H3 receptor by histamine induced inhibition of forskolin stimulated cAMP accumulation in SK-N-MC cellsActivity against human histamine H3 receptor by histamine induced inhibition of forskolin stimulated cAMP accumulation in SK-N-MC cells
ChEMBL 290 8 0 3 3.0 CN(C)CCc1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2005.11.003
CHEMBL204872 75863 None 0 Human Functional pKd = 9.3 9.3 - 0
Activity against human histamine H3 receptor by histamine induced inhibition of forskolin stimulated cAMP accumulation in SK-N-MC cellsActivity against human histamine H3 receptor by histamine induced inhibition of forskolin stimulated cAMP accumulation in SK-N-MC cells
ChEMBL 290 8 0 3 3.0 CN(C)CCc1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2005.11.003
25061924 18342 None 0 Human Functional pKd = 9.3 9.3 - 0
Antagonist activity against human histamine H3 receptorAntagonist activity against human histamine H3 receptor
ChEMBL 368 4 1 3 3.3 CC(C)N1CCN(C(=O)c2ccc3c(CN4CCCCC4)c[nH]c3c2)CC1 10.1016/j.bmcl.2010.08.103
CHEMBL1270864 18342 None 0 Human Functional pKd = 9.3 9.3 - 0
Antagonist activity against human histamine H3 receptorAntagonist activity against human histamine H3 receptor
ChEMBL 368 4 1 3 3.3 CC(C)N1CCN(C(=O)c2ccc3c(CN4CCCCC4)c[nH]c3c2)CC1 10.1016/j.bmcl.2010.08.103
25061409 18388 None 0 Human Functional pKd = 9.3 9.3 - 0
Antagonist activity against human histamine H3 receptorAntagonist activity against human histamine H3 receptor
ChEMBL 368 4 1 4 1.9 O=C(c1ccc2c(CN3CCOCC3)c[nH]c2c1)N1CCN(C2CC2)CC1 10.1016/j.bmcl.2010.08.103
CHEMBL1271276 18388 None 0 Human Functional pKd = 9.3 9.3 - 0
Antagonist activity against human histamine H3 receptorAntagonist activity against human histamine H3 receptor
ChEMBL 368 4 1 4 1.9 O=C(c1ccc2c(CN3CCOCC3)c[nH]c2c1)N1CCN(C2CC2)CC1 10.1016/j.bmcl.2010.08.103
49864938 15775 None 0 Guinea pig Functional pKd = 9.3 9.3 - 0
Antagonist activity at histamine H3 receptor in electrically-stimulated guinea pig ileumAntagonist activity at histamine H3 receptor in electrically-stimulated guinea pig ileum
ChEMBL 505 8 0 7 3.7 CC(C)OCCn1c(=O)n(C2CCN(C(=O)C3CCN(Cc4ccncc4)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2010.07.052
CHEMBL1222719 15775 None 0 Guinea pig Functional pKd = 9.3 9.3 - 0
Antagonist activity at histamine H3 receptor in electrically-stimulated guinea pig ileumAntagonist activity at histamine H3 receptor in electrically-stimulated guinea pig ileum
ChEMBL 505 8 0 7 3.7 CC(C)OCCn1c(=O)n(C2CCN(C(=O)C3CCN(Cc4ccncc4)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2010.07.052
46933385 15802 None 0 Guinea pig Functional pKd = 9.3 9.3 - 0
Antagonist activity at histamine H3 receptor in electrically-stimulated guinea pig ileumAntagonist activity at histamine H3 receptor in electrically-stimulated guinea pig ileum
ChEMBL 490 7 0 7 2.8 CN(C)CCn1c(=O)n(C2CCN(C(=O)C3CCN(Cc4ccncc4)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2010.07.052
CHEMBL1222800 15802 None 0 Guinea pig Functional pKd = 9.3 9.3 - 0
Antagonist activity at histamine H3 receptor in electrically-stimulated guinea pig ileumAntagonist activity at histamine H3 receptor in electrically-stimulated guinea pig ileum
ChEMBL 490 7 0 7 2.8 CN(C)CCn1c(=O)n(C2CCN(C(=O)C3CCN(Cc4ccncc4)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2010.07.052
16747689 169004 None 0 Human Functional pKd = 9.3 9.3 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 396 11 0 4 5.0 CN(C)CCC(Oc1ccccc1)c1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2007.03.034
CHEMBL438490 169004 None 0 Human Functional pKd = 9.3 9.3 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 396 11 0 4 5.0 CN(C)CCC(Oc1ccccc1)c1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2007.03.034
10156476 179868 None 0 Human Functional pKd = 9.3 9.3 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 377 5 0 5 4.3 CC(C)N1CCC(Sc2ncc(C(=O)c3ccc(Cl)cc3)n2C)CC1 10.1016/j.bmcl.2008.11.114
CHEMBL474440 179868 None 0 Human Functional pKd = 9.3 9.3 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 377 5 0 5 4.3 CC(C)N1CCC(Sc2ncc(C(=O)c3ccc(Cl)cc3)n2C)CC1 10.1016/j.bmcl.2008.11.114
10201558 183201 None 0 Human Functional pKd = 9.3 9.3 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 409 6 0 5 4.2 CC(C)N1CCC(COc2ncc(C(=O)c3ccc(C(F)(F)F)cc3)n2C)CC1 10.1016/j.bmcl.2008.11.114
CHEMBL479452 183201 None 0 Human Functional pKd = 9.3 9.3 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 409 6 0 5 4.2 CC(C)N1CCC(COc2ncc(C(=O)c3ccc(C(F)(F)F)cc3)n2C)CC1 10.1016/j.bmcl.2008.11.114
10134089 184077 None 0 Human Functional pKd = 9.3 9.3 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 375 6 0 5 3.8 CC(C)N1CCC(COc2ncc(C(=O)c3ccc(Cl)cc3)n2C)CC1 10.1016/j.bmcl.2008.11.114
CHEMBL481745 184077 None 0 Human Functional pKd = 9.3 9.3 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 375 6 0 5 3.8 CC(C)N1CCC(COc2ncc(C(=O)c3ccc(Cl)cc3)n2C)CC1 10.1016/j.bmcl.2008.11.114
46887993 8724 None 0 Human Functional pKd = 9.3 9.3 - 0
Antagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 377 4 1 4 2.5 O=C([C@H]1C[C@H](Oc2cccc(Cl)c2)CN1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.03.071
CHEMBL1095877 8724 None 0 Human Functional pKd = 9.3 9.3 - 0
Antagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 377 4 1 4 2.5 O=C([C@H]1C[C@H](Oc2cccc(Cl)c2)CN1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.03.071
44598905 9059 None 0 Human Functional pKd = 9.3 9.3 - 0
Antagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 391 4 0 5 2.2 CC(=O)N1C[C@@H](Oc2ccsc2)C[C@@H]1C(=O)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.03.071
CHEMBL1098781 9059 None 0 Human Functional pKd = 9.3 9.3 - 0
Antagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 391 4 0 5 2.2 CC(=O)N1C[C@@H](Oc2ccsc2)C[C@@H]1C(=O)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.03.071
11669791 150798 None 0 Human Functional pKd = 9.3 9.3 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 460 7 0 5 3.9 CN1Cc2cc(OCCCN3CCC(F)CC3)ccc2C(c2ccc(S(C)(=O)=O)cc2)C1 10.1016/j.bmcl.2006.11.036
CHEMBL395608 150798 None 0 Human Functional pKd = 9.3 9.3 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 460 7 0 5 3.9 CN1Cc2cc(OCCCN3CCC(F)CC3)ccc2C(c2ccc(S(C)(=O)=O)cc2)C1 10.1016/j.bmcl.2006.11.036
24770908 10744 None 0 Human Functional pKd = 9.3 9.3 - 0
Antagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 369 4 0 4 3.7 O=C(c1ccc(Oc2ccccc2F)cn1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.05.041
CHEMBL1171155 10744 None 0 Human Functional pKd = 9.3 9.3 - 0
Antagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 369 4 0 4 3.7 O=C(c1ccc(Oc2ccccc2F)cn1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.05.041
9880039 117521 None 0 Human Functional pKd = 9.3 9.3 - 0
Histamine-induced inhibition of forskolin- stimulated cAMP accumulation in SK-N-MC cells overexpressing the human Histamine H3 receptorHistamine-induced inhibition of forskolin- stimulated cAMP accumulation in SK-N-MC cells overexpressing the human Histamine H3 receptor
ChEMBL 318 7 0 4 2.8 c1cc(OCCCN2CCCCC2)ccc1CN1CCOCC1 10.1021/jm030185v
CHEMBL339867 117521 None 0 Human Functional pKd = 9.3 9.3 - 0
Histamine-induced inhibition of forskolin- stimulated cAMP accumulation in SK-N-MC cells overexpressing the human Histamine H3 receptorHistamine-induced inhibition of forskolin- stimulated cAMP accumulation in SK-N-MC cells overexpressing the human Histamine H3 receptor
ChEMBL 318 7 0 4 2.8 c1cc(OCCCN2CCCCC2)ccc1CN1CCOCC1 10.1021/jm030185v
10473209 62694 None 3 Human Functional pKd = 9.3 9.3 - 1
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrs
ChEMBL 352 4 1 5 2.6 CNC(=O)c1cnc(Oc2ccc3c(c2)CCN(C2CCC2)CC3)cn1 10.1016/j.ejmech.2009.06.007
CHEMBL1783890 62694 None 3 Human Functional pKd = 9.3 9.3 - 1
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrs
ChEMBL 352 4 1 5 2.6 CNC(=O)c1cnc(Oc2ccc3c(c2)CCN(C2CCC2)CC3)cn1 10.1016/j.ejmech.2009.06.007
24771363 10809 None 0 Human Functional pKd = 9.3 9.3 - 0
Antagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 419 4 0 4 4.9 O=C(c1ccc(Oc2ccc(Cl)c(Cl)c2)nc1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.05.041
CHEMBL1171936 10809 None 0 Human Functional pKd = 9.3 9.3 - 0
Antagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 419 4 0 4 4.9 O=C(c1ccc(Oc2ccc(Cl)c(Cl)c2)nc1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.05.041
11544498 62695 None 0 Human Functional pKd = 9.3 9.3 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrs
ChEMBL 331 4 0 5 1.6 CC(C)N1CCN(C(=O)c2cnc(CN3CCCCC3)cn2)CC1 10.1016/j.ejmech.2009.06.007
CHEMBL1783891 62695 None 0 Human Functional pKd = 9.3 9.3 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrs
ChEMBL 331 4 0 5 1.6 CC(C)N1CCN(C(=O)c2cnc(CN3CCCCC3)cn2)CC1 10.1016/j.ejmech.2009.06.007
11244101 62701 None 0 Human Functional pKd = 9.2 9.2 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrs
ChEMBL 319 4 0 4 2.4 CC(C)N1CCN(C(=O)c2ccc(CN3CCCCC3)o2)CC1 10.1016/j.ejmech.2009.06.007
CHEMBL1783897 62701 None 0 Human Functional pKd = 9.2 9.2 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrs
ChEMBL 319 4 0 4 2.4 CC(C)N1CCN(C(=O)c2ccc(CN3CCCCC3)o2)CC1 10.1016/j.ejmech.2009.06.007
24856015 155258 None 0 Human Functional pKd = 9.2 9.2 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 479 7 1 5 5.1 CNCc1cc(C(=O)N2CCCN(C3CC3)CC2)ccc1Oc1ccc(SC(F)(F)F)cc1 10.1016/j.bmcl.2007.11.016
CHEMBL402286 155258 None 0 Human Functional pKd = 9.2 9.2 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 479 7 1 5 5.1 CNCc1cc(C(=O)N2CCCN(C3CC3)CC2)ccc1Oc1ccc(SC(F)(F)F)cc1 10.1016/j.bmcl.2007.11.016
11668368 149894 None 0 Human Functional pKd = 9.2 9.2 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 394 7 0 4 4.5 COc1ccc(C2CN(C)Cc3cc(OCCCN4CCCCC4)ccc32)cc1 10.1016/j.bmcl.2006.11.036
CHEMBL394861 149894 None 0 Human Functional pKd = 9.2 9.2 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 394 7 0 4 4.5 COc1ccc(C2CN(C)Cc3cc(OCCCN4CCCCC4)ccc32)cc1 10.1016/j.bmcl.2006.11.036
9944610 89470 None 20 Human Functional pKd = 9.2 9.2 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrs
ChEMBL 312 4 0 3 2.7 C(#Cc1cccc(CN2CCOCC2)c1)CCN1CCCCC1 10.1016/j.ejmech.2009.06.007
CHEMBL237087 89470 None 20 Human Functional pKd = 9.2 9.2 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrs
ChEMBL 312 4 0 3 2.7 C(#Cc1cccc(CN2CCOCC2)c1)CCN1CCCCC1 10.1016/j.ejmech.2009.06.007
24771420 10804 None 0 Human Functional pKd = 9.2 9.2 - 0
Antagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 385 4 0 4 4.2 O=C(c1ccc(Oc2ccc(Cl)cc2)nc1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.05.041
CHEMBL1171886 10804 None 0 Human Functional pKd = 9.2 9.2 - 0
Antagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 385 4 0 4 4.2 O=C(c1ccc(Oc2ccc(Cl)cc2)nc1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.05.041
11697697 2547 None 25 Human Functional pKd = 9.2 9.2 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced binding of [35S]GTPgammaS bindingAntagonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced binding of [35S]GTPgammaS binding
ChEMBL 431 6 0 5 4.6 Cc1nc2cccc(c2c(=O)n1c1ccc(cc1)OCCCN1CCCC1)C(F)(F)F 10.1021/jm8003834
7346 2547 None 25 Human Functional pKd = 9.2 9.2 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced binding of [35S]GTPgammaS bindingAntagonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced binding of [35S]GTPgammaS binding
ChEMBL 431 6 0 5 4.6 Cc1nc2cccc(c2c(=O)n1c1ccc(cc1)OCCCN1CCCC1)C(F)(F)F 10.1021/jm8003834
CHEMBL476323 2547 None 25 Human Functional pKd = 9.2 9.2 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced binding of [35S]GTPgammaS bindingAntagonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced binding of [35S]GTPgammaS binding
ChEMBL 431 6 0 5 4.6 Cc1nc2cccc(c2c(=O)n1c1ccc(cc1)OCCCN1CCCC1)C(F)(F)F 10.1021/jm8003834
DB11910 2547 None 25 Human Functional pKd = 9.2 9.2 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced binding of [35S]GTPgammaS bindingAntagonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced binding of [35S]GTPgammaS binding
ChEMBL 431 6 0 5 4.6 Cc1nc2cccc(c2c(=O)n1c1ccc(cc1)OCCCN1CCCC1)C(F)(F)F 10.1021/jm8003834
15983457 93798 None 0 Human Functional pKd = 9.2 9.2 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulationAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulation
ChEMBL 353 8 0 4 3.8 CCN(CC)CCCOc1cc2c(cn1)C(c1ccccc1)CN(C)C2 10.1016/j.bmcl.2007.02.006
CHEMBL247268 93798 None 0 Human Functional pKd = 9.2 9.2 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulationAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulation
ChEMBL 353 8 0 4 3.8 CCN(CC)CCCOc1cc2c(cn1)C(c1ccccc1)CN(C)C2 10.1016/j.bmcl.2007.02.006
46887995 8942 None 0 Human Functional pKd = 9.2 9.2 - 0
Antagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 382 4 1 5 2.1 N#Cc1ccc(O[C@@H]2CN[C@@H](C(=O)N3CCCN(C4CCCC4)CC3)C2)cc1 10.1016/j.bmcl.2010.03.071
CHEMBL1097883 8942 None 0 Human Functional pKd = 9.2 9.2 - 0
Antagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 382 4 1 5 2.1 N#Cc1ccc(O[C@@H]2CN[C@@H](C(=O)N3CCCN(C4CCCC4)CC3)C2)cc1 10.1016/j.bmcl.2010.03.071
44439856 152510 None 0 Human Functional pKd = 9.1 9.1 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 382 6 0 3 4.5 CN1Cc2cc(OCCCN3CCC(F)CC3)ccc2C(c2ccccc2)C1 10.1016/j.bmcl.2006.11.036
CHEMBL397065 152510 None 0 Human Functional pKd = 9.1 9.1 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 382 6 0 3 4.5 CN1Cc2cc(OCCCN3CCC(F)CC3)ccc2C(c2ccccc2)C1 10.1016/j.bmcl.2006.11.036
15983456 93755 None 0 Human Functional pKd = 9.1 9.1 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulationAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulation
ChEMBL 351 6 1 4 3.6 c1ccc(C2CNCc3cc(OCCCN4CCCCC4)ncc32)cc1 10.1016/j.bmcl.2007.02.006
CHEMBL247062 93755 None 0 Human Functional pKd = 9.1 9.1 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulationAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulation
ChEMBL 351 6 1 4 3.6 c1ccc(C2CNCc3cc(OCCCN4CCCCC4)ncc32)cc1 10.1016/j.bmcl.2007.02.006
46861747 9021 None 0 Human Functional pKd = 9.1 9.1 - 0
Antagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 375 4 0 4 2.4 CN1C[C@@H](Oc2ccc(F)cc2)C[C@@H]1C(=O)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.03.071
CHEMBL1098485 9021 None 0 Human Functional pKd = 9.1 9.1 - 0
Antagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 375 4 0 4 2.4 CN1C[C@@H](Oc2ccc(F)cc2)C[C@@H]1C(=O)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.03.071
49864988 15799 None 0 Guinea pig Functional pKd = 9.1 9.1 - 0
Antagonist activity at histamine H3 receptor in electrically-stimulated guinea pig ileumAntagonist activity at histamine H3 receptor in electrically-stimulated guinea pig ileum
ChEMBL 539 8 0 7 4.4 O=C(C1CCN(Cc2ccncc2)CC1)N1CCC(n2c(=O)n(CCOc3ccccc3)c3ccccc32)CC1 10.1016/j.bmcl.2010.07.052
CHEMBL1222798 15799 None 0 Guinea pig Functional pKd = 9.1 9.1 - 0
Antagonist activity at histamine H3 receptor in electrically-stimulated guinea pig ileumAntagonist activity at histamine H3 receptor in electrically-stimulated guinea pig ileum
ChEMBL 539 8 0 7 4.4 O=C(C1CCN(Cc2ccncc2)CC1)N1CCC(n2c(=O)n(CCOc3ccccc3)c3ccccc32)CC1 10.1016/j.bmcl.2010.07.052
46933530 15813 None 0 Guinea pig Functional pKd = 9.1 9.1 - 0
Antagonist activity at histamine H3 receptor in electrically-stimulated guinea pig ileumAntagonist activity at histamine H3 receptor in electrically-stimulated guinea pig ileum
ChEMBL 532 7 0 8 2.6 O=C(C1CCN(Cc2ccncc2)CC1)N1CCC(n2c(=O)n(CCN3CCOCC3)c3ccccc32)CC1 10.1016/j.bmcl.2010.07.052
CHEMBL1222864 15813 None 0 Guinea pig Functional pKd = 9.1 9.1 - 0
Antagonist activity at histamine H3 receptor in electrically-stimulated guinea pig ileumAntagonist activity at histamine H3 receptor in electrically-stimulated guinea pig ileum
ChEMBL 532 7 0 8 2.6 O=C(C1CCN(Cc2ccncc2)CC1)N1CCC(n2c(=O)n(CCN3CCOCC3)c3ccccc32)CC1 10.1016/j.bmcl.2010.07.052
44434165 89635 None 0 Human Functional pKd = 9.1 9.1 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 380 8 1 4 4.8 CNCc1cc(C#CCCN(C)C2CC2)ccc1Oc1ccc(SC)cc1 10.1016/j.bmcl.2007.06.061
CHEMBL237512 89635 None 0 Human Functional pKd = 9.1 9.1 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 380 8 1 4 4.8 CNCc1cc(C#CCCN(C)C2CC2)ccc1Oc1ccc(SC)cc1 10.1016/j.bmcl.2007.06.061
10295613 183681 None 0 Human Functional pKd = 9.1 9.1 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 419 6 0 5 3.9 CC(C)N1CCC(COc2ncc(C(=O)c3ccc(Br)cc3)n2C)CC1 10.1016/j.bmcl.2008.11.114
CHEMBL480048 183681 None 0 Human Functional pKd = 9.1 9.1 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 419 6 0 5 3.9 CC(C)N1CCC(COc2ncc(C(=O)c3ccc(Br)cc3)n2C)CC1 10.1016/j.bmcl.2008.11.114
11522780 62697 None 0 Human Functional pKd = 9.1 9.1 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrs
ChEMBL 330 4 0 4 2.2 CC(C)N1CCN(C(=O)c2ccc(CN3CCCCC3)nc2)CC1 10.1016/j.ejmech.2009.06.007
CHEMBL1783893 62697 None 0 Human Functional pKd = 9.1 9.1 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrs
ChEMBL 330 4 0 4 2.2 CC(C)N1CCN(C(=O)c2ccc(CN3CCCCC3)nc2)CC1 10.1016/j.ejmech.2009.06.007
1256 2148 None 46 Human Functional pKd = 9.1 9.1 - 1
Activity against human histamine H3 receptor by histamine induced inhibition of forskolin stimulated cAMP accumulation in SK-N-MC cellsActivity against human histamine H3 receptor by histamine induced inhibition of forskolin stimulated cAMP accumulation in SK-N-MC cells
ChEMBL 316 7 0 3 3.9 C1CCN(CC1)CCCOc1ccc(cc1)CN1CCCCC1 10.1016/j.bmcl.2005.11.003
2766326 2148 None 46 Human Functional pKd = 9.1 9.1 - 1
Activity against human histamine H3 receptor by histamine induced inhibition of forskolin stimulated cAMP accumulation in SK-N-MC cellsActivity against human histamine H3 receptor by histamine induced inhibition of forskolin stimulated cAMP accumulation in SK-N-MC cells
ChEMBL 316 7 0 3 3.9 C1CCN(CC1)CCCOc1ccc(cc1)CN1CCCCC1 10.1016/j.bmcl.2005.11.003
CHEMBL129542 2148 None 46 Human Functional pKd = 9.1 9.1 - 1
Activity against human histamine H3 receptor by histamine induced inhibition of forskolin stimulated cAMP accumulation in SK-N-MC cellsActivity against human histamine H3 receptor by histamine induced inhibition of forskolin stimulated cAMP accumulation in SK-N-MC cells
ChEMBL 316 7 0 3 3.9 C1CCN(CC1)CCCOc1ccc(cc1)CN1CCCCC1 10.1016/j.bmcl.2005.11.003
11517190 152796 None 0 Human Functional pKd = 9.1 9.1 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 412 7 0 4 4.5 COc1cccc(C2CN(C)Cc3cc(OCCCN4CCC(F)CC4)ccc32)c1 10.1016/j.bmcl.2006.11.036
CHEMBL397299 152796 None 0 Human Functional pKd = 9.1 9.1 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 412 7 0 4 4.5 COc1cccc(C2CN(C)Cc3cc(OCCCN4CCC(F)CC4)ccc32)c1 10.1016/j.bmcl.2006.11.036
1267 3804 None 32 Guinea pig Functional pKd = 9.1 9.1 - 5
Antagonist activity at histamine H3 receptor in guinea pig jejunum assessed as electrically evoked contractionsAntagonist activity at histamine H3 receptor in guinea pig jejunum assessed as electrically evoked contractions
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.ejmech.2008.09.019
3035905 3804 None 32 Guinea pig Functional pKd = 9.1 9.1 - 5
Antagonist activity at histamine H3 receptor in guinea pig jejunum assessed as electrically evoked contractionsAntagonist activity at histamine H3 receptor in guinea pig jejunum assessed as electrically evoked contractions
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.ejmech.2008.09.019
CHEMBL260374 3804 None 32 Guinea pig Functional pKd = 9.1 9.1 - 5
Antagonist activity at histamine H3 receptor in guinea pig jejunum assessed as electrically evoked contractionsAntagonist activity at histamine H3 receptor in guinea pig jejunum assessed as electrically evoked contractions
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.ejmech.2008.09.019
24771419 10730 None 0 Human Functional pKd = 9.1 9.1 - 0
Antagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 385 4 0 4 4.2 O=C(c1ccc(Oc2cccc(Cl)c2)nc1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.05.041
CHEMBL1171002 10730 None 0 Human Functional pKd = 9.1 9.1 - 0
Antagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 385 4 0 4 4.2 O=C(c1ccc(Oc2cccc(Cl)c2)nc1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.05.041
44439863 150799 None 0 Human Functional pKd = 9.1 9.1 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 410 7 0 5 3.8 COc1ccc([C@@H]2CN(C)Cc3cc(OCCCN4CCOC[C@@H]4C)ccc32)cc1 10.1016/j.bmcl.2006.11.036
CHEMBL395609 150799 None 0 Human Functional pKd = 9.1 9.1 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 410 7 0 5 3.8 COc1ccc([C@@H]2CN(C)Cc3cc(OCCCN4CCOC[C@@H]4C)ccc32)cc1 10.1016/j.bmcl.2006.11.036
46887963 8722 None 0 Human Functional pKd = 9.0 9.0 - 0
Antagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 377 4 1 4 2.5 O=C([C@H]1C[C@H](Oc2ccc(Cl)cc2)CN1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.03.071
CHEMBL1095847 8722 None 0 Human Functional pKd = 9.0 9.0 - 0
Antagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 377 4 1 4 2.5 O=C([C@H]1C[C@H](Oc2ccc(Cl)cc2)CN1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.03.071
44581060 172680 None 0 Human Functional pKd = 9.0 9.0 - 0
Antagonist activity at human recombinant histamine H3 receptor expressed in human SK-N-MC cellsAntagonist activity at human recombinant histamine H3 receptor expressed in human SK-N-MC cells
ChEMBL 360 6 0 5 2.5 c1cc(OCC2CN(C3CCCC3)CCO2)ccc1CN1CCOCC1 10.1016/j.bmcl.2008.09.077
CHEMBL448825 172680 None 0 Human Functional pKd = 9.0 9.0 - 0
Antagonist activity at human recombinant histamine H3 receptor expressed in human SK-N-MC cellsAntagonist activity at human recombinant histamine H3 receptor expressed in human SK-N-MC cells
ChEMBL 360 6 0 5 2.5 c1cc(OCC2CN(C3CCCC3)CCO2)ccc1CN1CCOCC1 10.1016/j.bmcl.2008.09.077
10200160 183940 None 0 Human Functional pKd = 9 9.0 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 386 7 0 7 3.1 CC(C)N1CCC(COc2ncc(C(=O)c3ccc([N+](=O)[O-])cc3)n2C)CC1 10.1016/j.bmcl.2008.11.114
CHEMBL480633 183940 None 0 Human Functional pKd = 9 9.0 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 386 7 0 7 3.1 CC(C)N1CCC(COc2ncc(C(=O)c3ccc([N+](=O)[O-])cc3)n2C)CC1 10.1016/j.bmcl.2008.11.114
10179744 192691 None 0 Human Functional pKd = 9 9.0 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 409 6 0 5 4.5 CC(C)N1CCC(COc2ncc(C(=O)c3cc(Cl)cc(Cl)c3)n2C)CC1 10.1016/j.bmcl.2008.11.114
CHEMBL521415 192691 None 0 Human Functional pKd = 9 9.0 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 409 6 0 5 4.5 CC(C)N1CCC(COc2ncc(C(=O)c3cc(Cl)cc(Cl)c3)n2C)CC1 10.1016/j.bmcl.2008.11.114
15983454 93756 None 0 Human Functional pKd = 9.0 9.0 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulationAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulation
ChEMBL 383 6 0 4 4.1 CN1Cc2cc(OCCCN3CCCCC3)ncc2C(c2ccccc2F)C1 10.1016/j.bmcl.2007.02.006
CHEMBL247063 93756 None 0 Human Functional pKd = 9.0 9.0 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulationAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulation
ChEMBL 383 6 0 4 4.1 CN1Cc2cc(OCCCN3CCCCC3)ncc2C(c2ccccc2F)C1 10.1016/j.bmcl.2007.02.006
15983836 93758 None 0 Human Functional pKd = 9.0 9.0 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulationAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulation
ChEMBL 385 6 1 4 4.2 Clc1ccccc1C1CNCc2cc(OCCCN3CCCCC3)ncc21 10.1016/j.bmcl.2007.02.006
CHEMBL247076 93758 None 0 Human Functional pKd = 9.0 9.0 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulationAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulation
ChEMBL 385 6 1 4 4.2 Clc1ccccc1C1CNCc2cc(OCCCN3CCCCC3)ncc21 10.1016/j.bmcl.2007.02.006
44600844 8860 None 0 Human Functional pKd = 8.9 8.9 - 0
Antagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 411 4 1 4 2.9 O=C([C@H]1C[C@H](Oc2ccc(C(F)(F)F)cc2)CN1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.03.071
CHEMBL1097143 8860 None 0 Human Functional pKd = 8.9 8.9 - 0
Antagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 411 4 1 4 2.9 O=C([C@H]1C[C@H](Oc2ccc(C(F)(F)F)cc2)CN1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.03.071
44600841 9100 None 0 Human Functional pKd = 8.9 8.9 - 0
Antagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 391 4 1 4 2.8 Cc1cc(O[C@@H]2CN[C@@H](C(=O)N3CCCN(C4CCC4)CC3)C2)ccc1Cl 10.1016/j.bmcl.2010.03.071
CHEMBL1099147 9100 None 0 Human Functional pKd = 8.9 8.9 - 0
Antagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 391 4 1 4 2.8 Cc1cc(O[C@@H]2CN[C@@H](C(=O)N3CCCN(C4CCC4)CC3)C2)ccc1Cl 10.1016/j.bmcl.2010.03.071
44215838 15812 None 0 Guinea pig Functional pKd = 8.9 8.9 - 0
Antagonist activity at histamine H3 receptor in electrically-stimulated guinea pig ileumAntagonist activity at histamine H3 receptor in electrically-stimulated guinea pig ileum
ChEMBL 530 7 0 7 3.8 O=C(C1CCN(Cc2ccncc2)CC1)N1CCC(n2c(=O)n(CCN3CCCCC3)c3ccccc32)CC1 10.1016/j.bmcl.2010.07.052
CHEMBL1222863 15812 None 0 Guinea pig Functional pKd = 8.9 8.9 - 0
Antagonist activity at histamine H3 receptor in electrically-stimulated guinea pig ileumAntagonist activity at histamine H3 receptor in electrically-stimulated guinea pig ileum
ChEMBL 530 7 0 7 3.8 O=C(C1CCN(Cc2ccncc2)CC1)N1CCC(n2c(=O)n(CCN3CCCCC3)c3ccccc32)CC1 10.1016/j.bmcl.2010.07.052
49865104 15823 None 0 Guinea pig Functional pKd = 8.9 8.9 - 0
Antagonist activity at histamine H3 receptor in electrically-stimulated guinea pig ileumAntagonist activity at histamine H3 receptor in electrically-stimulated guinea pig ileum
ChEMBL 509 6 0 6 4.3 O=C(C1CCN(Cc2ccncc2)CC1)N1CCC(n2c(=O)n(Cc3ccccc3)c3ccccc32)CC1 10.1016/j.bmcl.2010.07.052
CHEMBL1222938 15823 None 0 Guinea pig Functional pKd = 8.9 8.9 - 0
Antagonist activity at histamine H3 receptor in electrically-stimulated guinea pig ileumAntagonist activity at histamine H3 receptor in electrically-stimulated guinea pig ileum
ChEMBL 509 6 0 6 4.3 O=C(C1CCN(Cc2ccncc2)CC1)N1CCC(n2c(=O)n(Cc3ccccc3)c3ccccc32)CC1 10.1016/j.bmcl.2010.07.052
15987008 12401 None 0 Guinea pig Functional pKd = 8.9 8.9 - 0
Antagonist activity at histamine H3 receptor in guinea pig ileum assessed as inhibition of (R)-methyl histamine induced longitudinal smooth muscle contractionAntagonist activity at histamine H3 receptor in guinea pig ileum assessed as inhibition of (R)-methyl histamine induced longitudinal smooth muscle contraction
ChEMBL 425 7 0 4 3.2 O=C(c1ccc(F)cc1)N1CCN(c2ccc(OCCCN3CCCC3)cc2)C(=O)C1 10.1021/jm0708228
CHEMBL1185719 12401 None 0 Guinea pig Functional pKd = 8.9 8.9 - 0
Antagonist activity at histamine H3 receptor in guinea pig ileum assessed as inhibition of (R)-methyl histamine induced longitudinal smooth muscle contractionAntagonist activity at histamine H3 receptor in guinea pig ileum assessed as inhibition of (R)-methyl histamine induced longitudinal smooth muscle contraction
ChEMBL 425 7 0 4 3.2 O=C(c1ccc(F)cc1)N1CCN(c2ccc(OCCCN3CCCC3)cc2)C(=O)C1 10.1021/jm0708228
CHEMBL429458 12401 None 0 Guinea pig Functional pKd = 8.9 8.9 - 0
Antagonist activity at histamine H3 receptor in guinea pig ileum assessed as inhibition of (R)-methyl histamine induced longitudinal smooth muscle contractionAntagonist activity at histamine H3 receptor in guinea pig ileum assessed as inhibition of (R)-methyl histamine induced longitudinal smooth muscle contraction
ChEMBL 425 7 0 4 3.2 O=C(c1ccc(F)cc1)N1CCN(c2ccc(OCCCN3CCCC3)cc2)C(=O)C1 10.1021/jm0708228
46887962 8721 None 0 Human Functional pKd = 8.9 8.9 - 0
Antagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 361 4 1 4 2.0 O=C([C@H]1C[C@H](Oc2ccc(F)cc2)CN1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.03.071
CHEMBL1095846 8721 None 0 Human Functional pKd = 8.9 8.9 - 0
Antagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 361 4 1 4 2.0 O=C([C@H]1C[C@H](Oc2ccc(F)cc2)CN1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.03.071
11653860 192061 None 0 Human Functional pKd = 8.9 8.9 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 383 7 0 5 4.3 CC(C)c1ccc(C(=O)c2cnc(OCC3CCN(C(C)C)CC3)n2C)cc1 10.1016/j.bmcl.2008.11.114
CHEMBL520085 192061 None 0 Human Functional pKd = 8.9 8.9 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 383 7 0 5 4.3 CC(C)c1ccc(C(=O)c2cnc(OCC3CCN(C(C)C)CC3)n2C)cc1 10.1016/j.bmcl.2008.11.114
44406535 141464 None 0 Guinea pig Functional pKd = 8.9 8.9 - 0
Antagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileumAntagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileum
ChEMBL 312 6 2 3 2.7 O=C(CCN1CCC(Cc2c[nH]cn2)CC1)Nc1ccccc1 10.1016/j.bmcl.2005.09.076
CHEMBL383825 141464 None 0 Guinea pig Functional pKd = 8.9 8.9 - 0
Antagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileumAntagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileum
ChEMBL 312 6 2 3 2.7 O=C(CCN1CCC(Cc2c[nH]cn2)CC1)Nc1ccccc1 10.1016/j.bmcl.2005.09.076
11582342 87296 None 0 Human Functional pKd = 8.9 8.9 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 412 7 0 4 4.5 COc1ccc(C2CN(C)Cc3cc(OCCCN4CCC(F)CC4)ccc32)cc1 10.1016/j.bmcl.2006.11.036
CHEMBL233054 87296 None 0 Human Functional pKd = 8.9 8.9 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 412 7 0 4 4.5 COc1ccc(C2CN(C)Cc3cc(OCCCN4CCC(F)CC4)ccc32)cc1 10.1016/j.bmcl.2006.11.036
49797822 10573 None 0 Human Functional pKd = 8.9 8.9 - 0
Antagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 369 4 0 4 3.7 O=C(c1cncc(Oc2ccc(F)cc2)c1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.05.041
CHEMBL1169741 10573 None 0 Human Functional pKd = 8.9 8.9 - 0
Antagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 369 4 0 4 3.7 O=C(c1cncc(Oc2ccc(F)cc2)c1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.05.041
10402802 106958 None 0 Guinea pig Functional pKd = 8.9 8.9 - 0
Histamine H3-antagonist potency on electrically stimulated guinea pig ileumHistamine H3-antagonist potency on electrically stimulated guinea pig ileum
ChEMBL 304 5 2 3 3.8 Clc1ccc(-c2c[nH]c(SCCc3c[nH]cn3)n2)cc1 10.1021/jm970070p
CHEMBL314614 106958 None 0 Guinea pig Functional pKd = 8.9 8.9 - 0
Histamine H3-antagonist potency on electrically stimulated guinea pig ileumHistamine H3-antagonist potency on electrically stimulated guinea pig ileum
ChEMBL 304 5 2 3 3.8 Clc1ccc(-c2c[nH]c(SCCc3c[nH]cn3)n2)cc1 10.1021/jm970070p
24855977 97967 None 0 Human Functional pKd = 8.9 8.9 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 449 6 1 4 5.1 CNCc1cc(C(=O)N2CCCN(C(C)C)CC2)ccc1Oc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2007.11.016
CHEMBL272503 97967 None 0 Human Functional pKd = 8.9 8.9 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 449 6 1 4 5.1 CNCc1cc(C(=O)N2CCCN(C(C)C)CC2)ccc1Oc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2007.11.016
11668849 152799 None 0 Human Functional pKd = 8.9 8.9 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 416 6 0 3 5.1 CN1Cc2cc(OCCCN3CCC(F)CC3)ccc2C(c2cccc(Cl)c2)C1 10.1016/j.bmcl.2006.11.036
CHEMBL397300 152799 None 0 Human Functional pKd = 8.9 8.9 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 416 6 0 3 5.1 CN1Cc2cc(OCCCN3CCC(F)CC3)ccc2C(c2cccc(Cl)c2)C1 10.1016/j.bmcl.2006.11.036
44439859 93693 None 0 Human Functional pKd = 8.9 8.9 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 407 6 0 4 4.3 CN1Cc2cc(OCCCN3CCC(F)CC3)ccc2C(c2ccc(C#N)cc2)C1 10.1016/j.bmcl.2006.11.036
CHEMBL246748 93693 None 0 Human Functional pKd = 8.9 8.9 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 407 6 0 4 4.3 CN1Cc2cc(OCCCN3CCC(F)CC3)ccc2C(c2ccc(C#N)cc2)C1 10.1016/j.bmcl.2006.11.036
24771741 10725 None 0 Human Functional pKd = 8.9 8.9 - 0
Antagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 369 4 0 4 3.7 O=C(c1ccc(Oc2ccc(F)cc2)cn1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.05.041
CHEMBL1170953 10725 None 0 Human Functional pKd = 8.9 8.9 - 0
Antagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 369 4 0 4 3.7 O=C(c1ccc(Oc2ccc(F)cc2)cn1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.05.041
44581099 187971 None 0 Rat Functional pKd = 8.8 8.8 - 0
Antagonist activity rat recombinant histamine H3 receptor expressed in human SK-N-MC cellsAntagonist activity rat recombinant histamine H3 receptor expressed in human SK-N-MC cells
ChEMBL 358 6 0 4 3.7 c1cc(OCC2CN(C3CCCC3)CCO2)ccc1CN1CCCCC1 10.1016/j.bmcl.2008.09.077
CHEMBL496366 187971 None 0 Rat Functional pKd = 8.8 8.8 - 0
Antagonist activity rat recombinant histamine H3 receptor expressed in human SK-N-MC cellsAntagonist activity rat recombinant histamine H3 receptor expressed in human SK-N-MC cells
ChEMBL 358 6 0 4 3.7 c1cc(OCC2CN(C3CCCC3)CCO2)ccc1CN1CCCCC1 10.1016/j.bmcl.2008.09.077
49864936 15773 None 0 Guinea pig Functional pKd = 8.8 8.8 - 0
Antagonist activity at histamine H3 receptor in electrically-stimulated guinea pig ileumAntagonist activity at histamine H3 receptor in electrically-stimulated guinea pig ileum
ChEMBL 477 7 0 7 2.9 COCCn1c(=O)n(C2CCN(C(=O)C3CCN(Cc4ccncc4)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2010.07.052
CHEMBL1222717 15773 None 0 Guinea pig Functional pKd = 8.8 8.8 - 0
Antagonist activity at histamine H3 receptor in electrically-stimulated guinea pig ileumAntagonist activity at histamine H3 receptor in electrically-stimulated guinea pig ileum
ChEMBL 477 7 0 7 2.9 COCCn1c(=O)n(C2CCN(C(=O)C3CCN(Cc4ccncc4)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2010.07.052
44600846 8941 None 0 Human Functional pKd = 8.8 8.8 - 0
Antagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 375 4 1 4 2.4 O=C([C@H]1C[C@H](Oc2ccc(F)cc2)CN1)N1CCCN(C2CCCC2)CC1 10.1016/j.bmcl.2010.03.071
CHEMBL1097882 8941 None 0 Human Functional pKd = 8.8 8.8 - 0
Antagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 375 4 1 4 2.4 O=C([C@H]1C[C@H](Oc2ccc(F)cc2)CN1)N1CCCN(C2CCCC2)CC1 10.1016/j.bmcl.2010.03.071
24771367 10699 None 0 Human Functional pKd = 8.8 8.8 - 0
Antagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 355 4 0 4 3.3 O=C(c1ccc(Oc2ccc(F)cc2)nc1)N1CCCN(C2CC2)CC1 10.1016/j.bmcl.2010.05.041
CHEMBL1170788 10699 None 0 Human Functional pKd = 8.8 8.8 - 0
Antagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 355 4 0 4 3.3 O=C(c1ccc(Oc2ccc(F)cc2)nc1)N1CCCN(C2CC2)CC1 10.1016/j.bmcl.2010.05.041
44581098 187941 None 0 Rat Functional pKd = 8.8 8.8 - 0
Antagonist activity rat recombinant histamine H3 receptor expressed in human SK-N-MC cellsAntagonist activity rat recombinant histamine H3 receptor expressed in human SK-N-MC cells
ChEMBL 344 6 0 4 3.3 c1cc(OCC2CN(C3CCCC3)CCO2)ccc1CN1CCCC1 10.1016/j.bmcl.2008.09.077
CHEMBL496167 187941 None 0 Rat Functional pKd = 8.8 8.8 - 0
Antagonist activity rat recombinant histamine H3 receptor expressed in human SK-N-MC cellsAntagonist activity rat recombinant histamine H3 receptor expressed in human SK-N-MC cells
ChEMBL 344 6 0 4 3.3 c1cc(OCC2CN(C3CCCC3)CCO2)ccc1CN1CCCC1 10.1016/j.bmcl.2008.09.077
44406536 73045 None 0 Guinea pig Functional pKd = 8.8 8.8 - 0
Antagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileumAntagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileum
ChEMBL 342 7 2 4 2.7 COc1ccc(NC(=O)CCN2CCC(Cc3c[nH]cn3)CC2)cc1 10.1016/j.bmcl.2005.09.076
CHEMBL200941 73045 None 0 Guinea pig Functional pKd = 8.8 8.8 - 0
Antagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileumAntagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileum
ChEMBL 342 7 2 4 2.7 COc1ccc(NC(=O)CCN2CCC(Cc3c[nH]cn3)CC2)cc1 10.1016/j.bmcl.2005.09.076
44406483 135820 None 0 Guinea pig Functional pKd = 8.8 8.8 - 0
Antagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileumAntagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileum
ChEMBL 331 7 1 2 4.3 Clc1ccc(CCCCN2CCC(Cc3c[nH]cn3)CC2)cc1 10.1016/j.bmcl.2005.09.076
CHEMBL373010 135820 None 0 Guinea pig Functional pKd = 8.8 8.8 - 0
Antagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileumAntagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileum
ChEMBL 331 7 1 2 4.3 Clc1ccc(CCCCN2CCC(Cc3c[nH]cn3)CC2)cc1 10.1016/j.bmcl.2005.09.076
44406444 136250 None 0 Guinea pig Functional pKd = 8.8 8.8 - 0
Antagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileumAntagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileum
ChEMBL 370 7 2 5 2.5 COC(=O)c1ccc(NC(=O)CCN2CCC(Cc3c[nH]cn3)CC2)cc1 10.1016/j.bmcl.2005.09.076
CHEMBL373263 136250 None 0 Guinea pig Functional pKd = 8.8 8.8 - 0
Antagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileumAntagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileum
ChEMBL 370 7 2 5 2.5 COC(=O)c1ccc(NC(=O)CCN2CCC(Cc3c[nH]cn3)CC2)cc1 10.1016/j.bmcl.2005.09.076
44408116 139575 None 0 Guinea pig Functional pKd = 8.8 8.8 - 0
Antagonistic activity against histamine H3 receptor in guinea pig ileumAntagonistic activity against histamine H3 receptor in guinea pig ileum
ChEMBL 384 11 1 4 4.0 CCN(CC)Cc1ccc(OCCCN2CCC(Cc3c[nH]cn3)CC2)cc1 10.1016/j.bmcl.2005.10.087
CHEMBL379445 139575 None 0 Guinea pig Functional pKd = 8.8 8.8 - 0
Antagonistic activity against histamine H3 receptor in guinea pig ileumAntagonistic activity against histamine H3 receptor in guinea pig ileum
ChEMBL 384 11 1 4 4.0 CCN(CC)Cc1ccc(OCCCN2CCC(Cc3c[nH]cn3)CC2)cc1 10.1016/j.bmcl.2005.10.087
24965237 153127 None 0 Human Functional pKd = 8.8 8.8 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 402 6 1 4 4.1 CNCc1cc(C#CCCN2CCOCC2)ccc1Oc1ccc(F)cc1Cl 10.1016/j.bmcl.2007.06.061
CHEMBL397577 153127 None 0 Human Functional pKd = 8.8 8.8 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 402 6 1 4 4.1 CNCc1cc(C#CCCN2CCOCC2)ccc1Oc1ccc(F)cc1Cl 10.1016/j.bmcl.2007.06.061
10359235 62693 None 0 Rat Functional pKd = 8.7 8.7 - 0
Antagonist activity at histamine H3 receptor in rat cortical hemispheres assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrsAntagonist activity at histamine H3 receptor in rat cortical hemispheres assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrs
ChEMBL 329 4 0 3 2.8 CC(C)N1CCN(C(=O)c2ccc(CN3CCCCC3)cc2)CC1 10.1016/j.ejmech.2009.06.007
CHEMBL1783889 62693 None 0 Rat Functional pKd = 8.7 8.7 - 0
Antagonist activity at histamine H3 receptor in rat cortical hemispheres assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrsAntagonist activity at histamine H3 receptor in rat cortical hemispheres assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrs
ChEMBL 329 4 0 3 2.8 CC(C)N1CCN(C(=O)c2ccc(CN3CCCCC3)cc2)CC1 10.1016/j.ejmech.2009.06.007
24770906 10724 None 0 Human Functional pKd = 8.7 8.7 - 0
Antagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 385 4 0 4 4.2 O=C(c1ccc(Oc2cccc(Cl)c2)cn1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.05.041
CHEMBL1170952 10724 None 0 Human Functional pKd = 8.7 8.7 - 0
Antagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 385 4 0 4 4.2 O=C(c1ccc(Oc2cccc(Cl)c2)cn1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.05.041
49864937 15774 None 0 Guinea pig Functional pKd = 8.7 8.7 - 0
Antagonist activity at histamine H3 receptor in electrically-stimulated guinea pig ileumAntagonist activity at histamine H3 receptor in electrically-stimulated guinea pig ileum
ChEMBL 491 8 0 7 3.3 CCOCCn1c(=O)n(C2CCN(C(=O)C3CCN(Cc4ccncc4)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2010.07.052
CHEMBL1222718 15774 None 0 Guinea pig Functional pKd = 8.7 8.7 - 0
Antagonist activity at histamine H3 receptor in electrically-stimulated guinea pig ileumAntagonist activity at histamine H3 receptor in electrically-stimulated guinea pig ileum
ChEMBL 491 8 0 7 3.3 CCOCCn1c(=O)n(C2CCN(C(=O)C3CCN(Cc4ccncc4)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2010.07.052
24748992 12329 None 0 Guinea pig Functional pKd = 8.7 8.7 - 0
Antagonist activity at histamine H3 receptor in guinea pig ileum assessed as inhibition of (R)-methyl histamine induced longitudinal smooth muscle contractionAntagonist activity at histamine H3 receptor in guinea pig ileum assessed as inhibition of (R)-methyl histamine induced longitudinal smooth muscle contraction
ChEMBL 439 7 0 4 3.6 C[C@@H]1CCCN1CCCOc1ccc(N2CCN(C(=O)c3ccc(F)cc3)CC2=O)cc1 10.1021/jm0708228
CHEMBL1185158 12329 None 0 Guinea pig Functional pKd = 8.7 8.7 - 0
Antagonist activity at histamine H3 receptor in guinea pig ileum assessed as inhibition of (R)-methyl histamine induced longitudinal smooth muscle contractionAntagonist activity at histamine H3 receptor in guinea pig ileum assessed as inhibition of (R)-methyl histamine induced longitudinal smooth muscle contraction
ChEMBL 439 7 0 4 3.6 C[C@@H]1CCCN1CCCOc1ccc(N2CCN(C(=O)c3ccc(F)cc3)CC2=O)cc1 10.1021/jm0708228
CHEMBL394144 12329 None 0 Guinea pig Functional pKd = 8.7 8.7 - 0
Antagonist activity at histamine H3 receptor in guinea pig ileum assessed as inhibition of (R)-methyl histamine induced longitudinal smooth muscle contractionAntagonist activity at histamine H3 receptor in guinea pig ileum assessed as inhibition of (R)-methyl histamine induced longitudinal smooth muscle contraction
ChEMBL 439 7 0 4 3.6 C[C@@H]1CCCN1CCCOc1ccc(N2CCN(C(=O)c3ccc(F)cc3)CC2=O)cc1 10.1021/jm0708228
11551796 192658 None 0 Human Functional pKd = 8.7 8.7 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 337 7 0 5 3.3 CN(C)CCCSc1ncc(C(=O)c2ccc(Cl)cc2)n1C 10.1016/j.bmcl.2008.11.114
CHEMBL521118 192658 None 0 Human Functional pKd = 8.7 8.7 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 337 7 0 5 3.3 CN(C)CCCSc1ncc(C(=O)c2ccc(Cl)cc2)n1C 10.1016/j.bmcl.2008.11.114
72546763 102616 None 0 Human Functional pKd = 8.7 8.7 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 340 9 2 4 3.4 N=C(NCCCCN1CCCCC1)SCCCN1CCCCC1 10.1016/j.bmcl.2013.09.052
CHEMBL2441946 102616 None 0 Human Functional pKd = 8.7 8.7 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 340 9 2 4 3.4 N=C(NCCCCN1CCCCC1)SCCCN1CCCCC1 10.1016/j.bmcl.2013.09.052
CHEMBL3040721 102616 None 0 Human Functional pKd = 8.7 8.7 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 340 9 2 4 3.4 N=C(NCCCCN1CCCCC1)SCCCN1CCCCC1 10.1016/j.bmcl.2013.09.052
72546762 102619 None 0 Human Functional pKd = 8.7 8.7 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 358 9 2 4 4.0 N#Cc1ccc(CCCCNC(=N)SCCCN2CCCCC2)cc1 10.1016/j.bmcl.2013.09.052
CHEMBL2441945 102619 None 0 Human Functional pKd = 8.7 8.7 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 358 9 2 4 4.0 N#Cc1ccc(CCCCNC(=N)SCCCN2CCCCC2)cc1 10.1016/j.bmcl.2013.09.052
CHEMBL3040738 102619 None 0 Human Functional pKd = 8.7 8.7 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 358 9 2 4 4.0 N#Cc1ccc(CCCCNC(=N)SCCCN2CCCCC2)cc1 10.1016/j.bmcl.2013.09.052
72546758 102631 None 0 Human Functional pKd = 8.7 8.7 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 353 8 2 3 4.4 N=C(NCCCc1ccc(Cl)cc1)SCCCN1CCCCC1 10.1016/j.bmcl.2013.09.052
CHEMBL2441941 102631 None 0 Human Functional pKd = 8.7 8.7 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 353 8 2 3 4.4 N=C(NCCCc1ccc(Cl)cc1)SCCCN1CCCCC1 10.1016/j.bmcl.2013.09.052
CHEMBL3040779 102631 None 0 Human Functional pKd = 8.7 8.7 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 353 8 2 3 4.4 N=C(NCCCc1ccc(Cl)cc1)SCCCN1CCCCC1 10.1016/j.bmcl.2013.09.052
10466840 206939 None 0 Guinea pig Functional pKd = 8 8.0 - 0
Agonist activity at histamine H3 receptor in guinea pig ileumAgonist activity at histamine H3 receptor in guinea pig ileum
ChEMBL 240 7 3 2 2.0 CC/N=C(\S)NCCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL72424 206939 None 0 Guinea pig Functional pKd = 8 8.0 - 0
Agonist activity at histamine H3 receptor in guinea pig ileumAgonist activity at histamine H3 receptor in guinea pig ileum
ChEMBL 240 7 3 2 2.0 CC/N=C(\S)NCCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
44571278 192671 None 0 Human Functional pKd = 8 8.0 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 359 7 0 4 4.1 Cn1c(C(=O)c2ccc(Cl)cc2)cnc1CCCCN1CCCCC1 10.1016/j.bmcl.2008.11.114
CHEMBL521256 192671 None 0 Human Functional pKd = 8 8.0 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 359 7 0 4 4.1 Cn1c(C(=O)c2ccc(Cl)cc2)cnc1CCCCN1CCCCC1 10.1016/j.bmcl.2008.11.114
73354133 102615 None 0 Human Functional pKd = 8 8.0 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 347 10 2 3 4.5 N=C(NCCCCCc1ccccc1)SCCCN1CCCCC1 10.1016/j.bmcl.2013.09.052
CHEMBL2441943 102615 None 0 Human Functional pKd = 8 8.0 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 347 10 2 3 4.5 N=C(NCCCCCc1ccccc1)SCCCN1CCCCC1 10.1016/j.bmcl.2013.09.052
CHEMBL3040720 102615 None 0 Human Functional pKd = 8 8.0 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 347 10 2 3 4.5 N=C(NCCCCCc1ccccc1)SCCCN1CCCCC1 10.1016/j.bmcl.2013.09.052
10134089 184077 None 0 Rat Functional pKd = 8 8.0 - 0
Antagonist activity at rat histamine H3 receptorAntagonist activity at rat histamine H3 receptor
ChEMBL 375 6 0 5 3.8 CC(C)N1CCC(COc2ncc(C(=O)c3ccc(Cl)cc3)n2C)CC1 10.1016/j.bmcl.2008.11.114
CHEMBL481745 184077 None 0 Rat Functional pKd = 8 8.0 - 0
Antagonist activity at rat histamine H3 receptorAntagonist activity at rat histamine H3 receptor
ChEMBL 375 6 0 5 3.8 CC(C)N1CCC(COc2ncc(C(=O)c3ccc(Cl)cc3)n2C)CC1 10.1016/j.bmcl.2008.11.114
44308792 206284 None 0 Guinea pig Functional pKd = 8 8.0 - 0
H3 -antagonist potency determined in electrically stimulated guinea-pig ileumH3 -antagonist potency determined in electrically stimulated guinea-pig ileum
ChEMBL 363 8 2 4 2.6 O=S(=O)(NCCCCc1c[nH]cn1)c1ccc(OC(F)(F)F)cc1 10.1016/s0960-894x(98)00379-5
CHEMBL68475 206284 None 0 Guinea pig Functional pKd = 8 8.0 - 0
H3 -antagonist potency determined in electrically stimulated guinea-pig ileumH3 -antagonist potency determined in electrically stimulated guinea-pig ileum
ChEMBL 363 8 2 4 2.6 O=S(=O)(NCCCCc1c[nH]cn1)c1ccc(OC(F)(F)F)cc1 10.1016/s0960-894x(98)00379-5
44308663 206324 None 0 Guinea pig Functional pKd = 8 8.0 - 0
H3 -antagonist potency determined in electrically stimulated guinea-pig ileumH3 -antagonist potency determined in electrically stimulated guinea-pig ileum
ChEMBL 349 8 2 3 3.4 CC(C)(C)c1ccc(S(=O)(=O)NCCCCCc2c[nH]cn2)cc1 10.1016/s0960-894x(98)00379-5
CHEMBL68718 206324 None 0 Guinea pig Functional pKd = 8 8.0 - 0
H3 -antagonist potency determined in electrically stimulated guinea-pig ileumH3 -antagonist potency determined in electrically stimulated guinea-pig ileum
ChEMBL 349 8 2 3 3.4 CC(C)(C)c1ccc(S(=O)(=O)NCCCCCc2c[nH]cn2)cc1 10.1016/s0960-894x(98)00379-5
44308995 206854 None 0 Guinea pig Functional pKd = 8 8.0 - 0
H3 -antagonist potency determined in electrically stimulated guinea-pig ileumH3 -antagonist potency determined in electrically stimulated guinea-pig ileum
ChEMBL 377 9 2 4 3.0 O=S(=O)(NCCCCCc1c[nH]cn1)c1ccc(OC(F)(F)F)cc1 10.1016/s0960-894x(98)00379-5
CHEMBL71941 206854 None 0 Guinea pig Functional pKd = 8 8.0 - 0
H3 -antagonist potency determined in electrically stimulated guinea-pig ileumH3 -antagonist potency determined in electrically stimulated guinea-pig ileum
ChEMBL 377 9 2 4 3.0 O=S(=O)(NCCCCCc1c[nH]cn1)c1ccc(OC(F)(F)F)cc1 10.1016/s0960-894x(98)00379-5
11779710 104407 None 0 Guinea pig Functional pKd = 8 8.0 - 0
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 302 8 3 2 3.5 S=C(NCCCCCCc1c[nH]cn1)Nc1ccccc1 10.1021/jm00012a025
CHEMBL310028 104407 None 0 Guinea pig Functional pKd = 8 8.0 - 0
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 302 8 3 2 3.5 S=C(NCCCCCCc1c[nH]cn1)Nc1ccccc1 10.1021/jm00012a025
5250783 169490 None 0 Guinea pig Functional pKd = 8 8.0 - 0
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 226 6 3 2 1.6 C/N=C(\S)NCCCCCc1c[nH]cn1 10.1021/jm00012a025
CHEMBL44220 169490 None 0 Guinea pig Functional pKd = 8 8.0 - 0
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 226 6 3 2 1.6 C/N=C(\S)NCCCCCc1c[nH]cn1 10.1021/jm00012a025
10466840 206939 None 0 Guinea pig Functional pKd = 8 8.0 - 0
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 240 7 3 2 2.0 CC/N=C(\S)NCCCCCc1c[nH]cn1 10.1021/jm00012a025
CHEMBL72424 206939 None 0 Guinea pig Functional pKd = 8 8.0 - 0
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 240 7 3 2 2.0 CC/N=C(\S)NCCCCCc1c[nH]cn1 10.1021/jm00012a025
11235688 119916 None 0 Guinea pig Functional pKd = 8.0 8.0 - 1
Tested for Antagonistic activity at histamine H3 receptor in guinea pig ileal longitudinal muscle in the presence of mepyramine at a concentration of 1-3 micro MTested for Antagonistic activity at histamine H3 receptor in guinea pig ileal longitudinal muscle in the presence of mepyramine at a concentration of 1-3 micro M
ChEMBL 427 13 3 3 5.1 c1ccc(C(CCc2nc(CCNCCCCc3c[nH]cn3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
CHEMBL348656 119916 None 0 Guinea pig Functional pKd = 8.0 8.0 - 1
Tested for Antagonistic activity at histamine H3 receptor in guinea pig ileal longitudinal muscle in the presence of mepyramine at a concentration of 1-3 micro MTested for Antagonistic activity at histamine H3 receptor in guinea pig ileal longitudinal muscle in the presence of mepyramine at a concentration of 1-3 micro M
ChEMBL 427 13 3 3 5.1 c1ccc(C(CCc2nc(CCNCCCCc3c[nH]cn3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
44351678 116888 None 0 Human Functional pKd = 8.0 8.0 - 0
Histamine-induced inhibition of forskolin- stimulated cAMP accumulation in SK-N-MC cells overexpressing the human Histamine H3 receptorHistamine-induced inhibition of forskolin- stimulated cAMP accumulation in SK-N-MC cells overexpressing the human Histamine H3 receptor
ChEMBL 262 6 0 3 2.6 CN(C)CCOc1ccc(CN2CCCCC2)cc1 10.1021/jm030185v
CHEMBL337942 116888 None 0 Human Functional pKd = 8.0 8.0 - 0
Histamine-induced inhibition of forskolin- stimulated cAMP accumulation in SK-N-MC cells overexpressing the human Histamine H3 receptorHistamine-induced inhibition of forskolin- stimulated cAMP accumulation in SK-N-MC cells overexpressing the human Histamine H3 receptor
ChEMBL 262 6 0 3 2.6 CN(C)CCOc1ccc(CN2CCCCC2)cc1 10.1021/jm030185v
24964160 89086 None 0 Human Functional pKd = 8.0 8.0 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 384 6 1 4 3.9 CNCc1cc(C#CCCN2CCOCC2)ccc1Oc1ccc(Cl)cc1 10.1016/j.bmcl.2007.06.061
CHEMBL236475 89086 None 0 Human Functional pKd = 8.0 8.0 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 384 6 1 4 3.9 CNCc1cc(C#CCCN2CCOCC2)ccc1Oc1ccc(Cl)cc1 10.1016/j.bmcl.2007.06.061
3032915 15502 None 19 Guinea pig Functional pKd = 7 7.0 - 1
Agonist activity at histamine H3 receptor in guinea pig ileumAgonist activity at histamine H3 receptor in guinea pig ileum
ChEMBL 212 5 3 2 1.2 C/N=C(\S)NCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL12160 15502 None 19 Guinea pig Functional pKd = 7 7.0 - 1
Agonist activity at histamine H3 receptor in guinea pig ileumAgonist activity at histamine H3 receptor in guinea pig ileum
ChEMBL 212 5 3 2 1.2 C/N=C(\S)NCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
10017821 103841 None 0 Guinea pig Functional pKd = 7 7.0 - 1
Agonist activity at histamine H3 receptor in guinea pig ileumAgonist activity at histamine H3 receptor in guinea pig ileum
ChEMBL 302 8 3 2 2.4 S=C(NCCCCc1c[nH]cn1)NCCc1ccccc1 10.1016/j.bmcl.2010.10.041
CHEMBL308913 103841 None 0 Guinea pig Functional pKd = 7 7.0 - 1
Agonist activity at histamine H3 receptor in guinea pig ileumAgonist activity at histamine H3 receptor in guinea pig ileum
ChEMBL 302 8 3 2 2.4 S=C(NCCCCc1c[nH]cn1)NCCc1ccccc1 10.1016/j.bmcl.2010.10.041
11459067 11352 None 0 Guinea pig Functional pKd = 7 7.0 - 0
Functional Histamine H3 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H3 receptor antagonistic activity in vitro assay on guinea pig ileum
ChEMBL 238 11 1 2 3.7 CCCCCCCCOCCCc1c[nH]cn1 10.1021/jm031065q
CHEMBL1179647 11352 None 0 Guinea pig Functional pKd = 7 7.0 - 0
Functional Histamine H3 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H3 receptor antagonistic activity in vitro assay on guinea pig ileum
ChEMBL 238 11 1 2 3.7 CCCCCCCCOCCCc1c[nH]cn1 10.1021/jm031065q
CHEMBL91523 11352 None 0 Guinea pig Functional pKd = 7 7.0 - 0
Functional Histamine H3 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H3 receptor antagonistic activity in vitro assay on guinea pig ileum
ChEMBL 238 11 1 2 3.7 CCCCCCCCOCCCc1c[nH]cn1 10.1021/jm031065q
44308790 206539 None 0 Guinea pig Functional pKd = 7 7.0 - 0
H3 -antagonist potency determined in electrically stimulated guinea-pig ileumH3 -antagonist potency determined in electrically stimulated guinea-pig ileum
ChEMBL 327 8 2 3 2.8 O=S(=O)(NCCCCCc1c[nH]cn1)c1ccc(Cl)cc1 10.1016/s0960-894x(98)00379-5
CHEMBL70148 206539 None 0 Guinea pig Functional pKd = 7 7.0 - 0
H3 -antagonist potency determined in electrically stimulated guinea-pig ileumH3 -antagonist potency determined in electrically stimulated guinea-pig ileum
ChEMBL 327 8 2 3 2.8 O=S(=O)(NCCCCCc1c[nH]cn1)c1ccc(Cl)cc1 10.1016/s0960-894x(98)00379-5
3032915 15502 None 19 Guinea pig Functional pKd = 7 7.0 - 1
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 212 5 3 2 1.2 C/N=C(\S)NCCCCc1c[nH]cn1 10.1021/jm00012a025
CHEMBL12160 15502 None 19 Guinea pig Functional pKd = 7 7.0 - 1
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 212 5 3 2 1.2 C/N=C(\S)NCCCCc1c[nH]cn1 10.1021/jm00012a025
10017821 103841 None 0 Guinea pig Functional pKd = 7 7.0 - 1
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 302 8 3 2 2.4 S=C(NCCCCc1c[nH]cn1)NCCc1ccccc1 10.1021/jm00012a025
CHEMBL308913 103841 None 0 Guinea pig Functional pKd = 7 7.0 - 1
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 302 8 3 2 2.4 S=C(NCCCCc1c[nH]cn1)NCCc1ccccc1 10.1021/jm00012a025
10398801 169182 None 0 Guinea pig Functional pKd = 7 7.0 - 0
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 226 6 3 2 1.6 CCC/N=C(\S)NCCCc1c[nH]cn1 10.1021/jm00012a025
CHEMBL439758 169182 None 0 Guinea pig Functional pKd = 7 7.0 - 0
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 226 6 3 2 1.6 CCC/N=C(\S)NCCCc1c[nH]cn1 10.1021/jm00012a025
10420190 209218 None 0 Guinea pig Functional pKd = 6 6.0 - 1
Tested in vitro for antagonist activity against H3 receptor of guinea pig jejunum.Tested in vitro for antagonist activity against H3 receptor of guinea pig jejunum.
ChEMBL 195 8 2 2 2.3 NCCCCCCCCc1c[nH]cn1 10.1021/jm00002a008
CHEMBL90063 209218 None 0 Guinea pig Functional pKd = 6 6.0 - 1
Tested in vitro for antagonist activity against H3 receptor of guinea pig jejunum.Tested in vitro for antagonist activity against H3 receptor of guinea pig jejunum.
ChEMBL 195 8 2 2 2.3 NCCCCCCCCc1c[nH]cn1 10.1021/jm00002a008
10263017 209921 None 0 Guinea pig Functional pKd = 6 6.0 - 1
Tested in vitro for antagonist activity against H3 receptor of guinea pig jejunum.Tested in vitro for antagonist activity against H3 receptor of guinea pig jejunum.
ChEMBL 223 10 2 2 3.0 NCCCCCCCCCCc1c[nH]cn1 10.1021/jm00002a008
CHEMBL94249 209921 None 0 Guinea pig Functional pKd = 6 6.0 - 1
Tested in vitro for antagonist activity against H3 receptor of guinea pig jejunum.Tested in vitro for antagonist activity against H3 receptor of guinea pig jejunum.
ChEMBL 223 10 2 2 3.0 NCCCCCCCCCCc1c[nH]cn1 10.1021/jm00002a008
11645731 188982 None 0 Human Functional pKd = 5 5.0 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 336 7 0 4 4.8 CC(C)CCCSc1ncc(C(=O)c2ccc(Cl)cc2)n1C 10.1016/j.bmcl.2008.11.114
CHEMBL507084 188982 None 0 Human Functional pKd = 5 5.0 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 336 7 0 4 4.8 CC(C)CCCSc1ncc(C(=O)c2ccc(Cl)cc2)n1C 10.1016/j.bmcl.2008.11.114
1258 196 None 15 Guinea pig Functional pKd = 7.0 7.0 - 0
Tested in vitro for histamine H3 receptor mediate inhibition of neurogenic contractions in guinea pig isolated ileum assayTested in vitro for histamine H3 receptor mediate inhibition of neurogenic contractions in guinea pig isolated ileum assay
ChEMBL 359 8 1 5 1.5 C[C@H](C(=O)N1CCN(CC1)CCCOc1ccc(cc1)C(=O)C1CC1)N 10.1016/s0960-894x(02)00310-4
9906860 196 None 15 Guinea pig Functional pKd = 7.0 7.0 - 0
Tested in vitro for histamine H3 receptor mediate inhibition of neurogenic contractions in guinea pig isolated ileum assayTested in vitro for histamine H3 receptor mediate inhibition of neurogenic contractions in guinea pig isolated ileum assay
ChEMBL 359 8 1 5 1.5 C[C@H](C(=O)N1CCN(CC1)CCCOc1ccc(cc1)C(=O)C1CC1)N 10.1016/s0960-894x(02)00310-4
CHEMBL302196 196 None 15 Guinea pig Functional pKd = 7.0 7.0 - 0
Tested in vitro for histamine H3 receptor mediate inhibition of neurogenic contractions in guinea pig isolated ileum assayTested in vitro for histamine H3 receptor mediate inhibition of neurogenic contractions in guinea pig isolated ileum assay
ChEMBL 359 8 1 5 1.5 C[C@H](C(=O)N1CCN(CC1)CCCOc1ccc(cc1)C(=O)C1CC1)N 10.1016/s0960-894x(02)00310-4
24964158 88746 None 0 Human Functional pKd = 8.0 8.0 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 396 7 1 5 4.0 CNCc1cc(C#CCCN2CCOCC2)ccc1Oc1ccc(SC)cc1 10.1016/j.bmcl.2007.06.061
CHEMBL236046 88746 None 0 Human Functional pKd = 8.0 8.0 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 396 7 1 5 4.0 CNCc1cc(C#CCCN2CCOCC2)ccc1Oc1ccc(SC)cc1 10.1016/j.bmcl.2007.06.061
15983579 149731 None 0 Human Functional pKd = 8.0 8.0 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulationAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulation
ChEMBL 419 6 1 4 4.9 Clc1ccc(C2CNCc3cc(OCCCN4CCCCC4)ncc32)cc1Cl 10.1016/j.bmcl.2007.02.006
CHEMBL394732 149731 None 0 Human Functional pKd = 8.0 8.0 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulationAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulation
ChEMBL 419 6 1 4 4.9 Clc1ccc(C2CNCc3cc(OCCCN4CCCCC4)ncc32)cc1Cl 10.1016/j.bmcl.2007.02.006
24771418 10729 None 0 Rat Functional pKd = 7.9 7.9 - 0
Antagonist activity at rat histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at rat histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 371 4 0 4 3.8 O=C(c1ccc(Oc2cccc(Cl)c2)nc1)N1CCCN(C2CC2)CC1 10.1016/j.bmcl.2010.05.041
CHEMBL1171001 10729 None 0 Rat Functional pKd = 7.9 7.9 - 0
Antagonist activity at rat histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at rat histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 371 4 0 4 3.8 O=C(c1ccc(Oc2cccc(Cl)c2)nc1)N1CCCN(C2CC2)CC1 10.1016/j.bmcl.2010.05.041
15983576 93828 None 0 Human Functional pKd = 7.9 7.9 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulationAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulation
ChEMBL 397 7 0 6 2.8 COc1ccc(C2CN(C)Cc3cc(OCCCN4CCOCC4)ncc32)cc1 10.1016/j.bmcl.2007.02.006
CHEMBL247472 93828 None 0 Human Functional pKd = 7.9 7.9 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulationAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulation
ChEMBL 397 7 0 6 2.8 COc1ccc(C2CN(C)Cc3cc(OCCCN4CCOCC4)ncc32)cc1 10.1016/j.bmcl.2007.02.006
46887962 8721 None 0 Rat Functional pKd = 7.9 7.9 - 0
Antagonist activity at rat H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at rat H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 361 4 1 4 2.0 O=C([C@H]1C[C@H](Oc2ccc(F)cc2)CN1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.03.071
CHEMBL1095846 8721 None 0 Rat Functional pKd = 7.9 7.9 - 0
Antagonist activity at rat H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at rat H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 361 4 1 4 2.0 O=C([C@H]1C[C@H](Oc2ccc(F)cc2)CN1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.03.071
10407870 106817 None 0 Guinea pig Functional pKd = 6.0 6.0 - 0
Compound was tested for the agonist activity against histamine H3 receptor of guinea pig ileumCompound was tested for the agonist activity against histamine H3 receptor of guinea pig ileum
ChEMBL 283 4 1 2 3.2 CN(C)CCc1c[nH]c(-c2cccc(C(F)(F)F)c2)n1 10.1016/s0960-894x(98)00461-2
CHEMBL314438 106817 None 0 Guinea pig Functional pKd = 6.0 6.0 - 0
Compound was tested for the agonist activity against histamine H3 receptor of guinea pig ileumCompound was tested for the agonist activity against histamine H3 receptor of guinea pig ileum
ChEMBL 283 4 1 2 3.2 CN(C)CCc1c[nH]c(-c2cccc(C(F)(F)F)c2)n1 10.1016/s0960-894x(98)00461-2
42604368 12545 None 0 Guinea pig Functional pKd = 6.9 6.9 - 0
Antagonist activity at histamine H3 receptor in guinea pig jejunum assessed as electrically evoked contractionsAntagonist activity at histamine H3 receptor in guinea pig jejunum assessed as electrically evoked contractions
ChEMBL 282 7 1 5 1.0 CCCN1CCN(c2ncc(CCNC=O)s2)CC1 10.1016/j.ejmech.2008.09.019
CHEMBL1186667 12545 None 0 Guinea pig Functional pKd = 6.9 6.9 - 0
Antagonist activity at histamine H3 receptor in guinea pig jejunum assessed as electrically evoked contractionsAntagonist activity at histamine H3 receptor in guinea pig jejunum assessed as electrically evoked contractions
ChEMBL 282 7 1 5 1.0 CCCN1CCN(c2ncc(CCNC=O)s2)CC1 10.1016/j.ejmech.2008.09.019
CHEMBL474109 12545 None 0 Guinea pig Functional pKd = 6.9 6.9 - 0
Antagonist activity at histamine H3 receptor in guinea pig jejunum assessed as electrically evoked contractionsAntagonist activity at histamine H3 receptor in guinea pig jejunum assessed as electrically evoked contractions
ChEMBL 282 7 1 5 1.0 CCCN1CCN(c2ncc(CCNC=O)s2)CC1 10.1016/j.ejmech.2008.09.019
10018468 164509 None 0 Guinea pig Functional pKd = 6.9 6.9 - 0
Histamine H3-antagonist potency on electrically stimulated guinea pig ileumHistamine H3-antagonist potency on electrically stimulated guinea pig ileum
ChEMBL 313 6 3 4 2.2 NC(=O)c1ccc(-c2c[nH]c(SCCc3c[nH]cn3)n2)cc1 10.1021/jm970070p
CHEMBL421350 164509 None 0 Guinea pig Functional pKd = 6.9 6.9 - 0
Histamine H3-antagonist potency on electrically stimulated guinea pig ileumHistamine H3-antagonist potency on electrically stimulated guinea pig ileum
ChEMBL 313 6 3 4 2.2 NC(=O)c1ccc(-c2c[nH]c(SCCc3c[nH]cn3)n2)cc1 10.1021/jm970070p
44320686 208911 None 0 Guinea pig Functional pKd = 4.9 4.9 - 0
Compound was tested for the agonist activity against histamine H3 receptor of guinea pig ileumCompound was tested for the agonist activity against histamine H3 receptor of guinea pig ileum
ChEMBL 279 4 2 2 2.6 CNCCc1c[nH]c(-c2cccc(Br)c2)n1 10.1016/s0960-894x(98)00461-2
CHEMBL88075 208911 None 0 Guinea pig Functional pKd = 4.9 4.9 - 0
Compound was tested for the agonist activity against histamine H3 receptor of guinea pig ileumCompound was tested for the agonist activity against histamine H3 receptor of guinea pig ileum
ChEMBL 279 4 2 2 2.6 CNCCc1c[nH]c(-c2cccc(Br)c2)n1 10.1016/s0960-894x(98)00461-2
46888210 8975 None 0 Human Functional pKd = 7.9 7.9 - 0
Antagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 368 4 1 5 1.8 N#Cc1ccc(O[C@H]2CN[C@H](C(=O)N3CCCN(C4CCC4)CC3)C2)cc1 10.1016/j.bmcl.2010.03.071
CHEMBL1098195 8975 None 0 Human Functional pKd = 7.9 7.9 - 0
Antagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 368 4 1 5 1.8 N#Cc1ccc(O[C@H]2CN[C@H](C(=O)N3CCCN(C4CCC4)CC3)C2)cc1 10.1016/j.bmcl.2010.03.071
24964162 89219 None 0 Human Functional pKd = 7.9 7.9 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 418 6 1 4 4.3 CNCc1cc(C#CCCN2CCOCC2)ccc1Oc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2007.06.061
CHEMBL236675 89219 None 0 Human Functional pKd = 7.9 7.9 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 418 6 1 4 4.3 CNCc1cc(C#CCCN2CCOCC2)ccc1Oc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2007.06.061
11574091 179857 None 0 Human Functional pKd = 7.9 7.9 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 361 7 0 5 3.6 Cn1c(C(=O)c2ccc(Cl)cc2)cnc1OCCCN1CCCCC1 10.1016/j.bmcl.2008.11.114
CHEMBL474429 179857 None 0 Human Functional pKd = 7.9 7.9 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 361 7 0 5 3.6 Cn1c(C(=O)c2ccc(Cl)cc2)cnc1OCCCN1CCCCC1 10.1016/j.bmcl.2008.11.114
72546761 102599 None 0 Human Functional pKd = 7.9 7.9 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 401 9 2 3 5.2 N=C(NCCCCc1ccc(C(F)(F)F)cc1)SCCCN1CCCCC1 10.1016/j.bmcl.2013.09.052
CHEMBL2441944 102599 None 0 Human Functional pKd = 7.9 7.9 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 401 9 2 3 5.2 N=C(NCCCCc1ccc(C(F)(F)F)cc1)SCCCN1CCCCC1 10.1016/j.bmcl.2013.09.052
CHEMBL3040666 102599 None 0 Human Functional pKd = 7.9 7.9 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 401 9 2 3 5.2 N=C(NCCCCc1ccc(C(F)(F)F)cc1)SCCCN1CCCCC1 10.1016/j.bmcl.2013.09.052
46887994 8940 None 0 Rat Functional pKd = 7.9 7.9 - 0
Antagonist activity at rat H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at rat H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 368 4 1 5 1.8 N#Cc1ccc(O[C@@H]2CN[C@@H](C(=O)N3CCCN(C4CCC4)CC3)C2)cc1 10.1016/j.bmcl.2010.03.071
CHEMBL1097881 8940 None 0 Rat Functional pKd = 7.9 7.9 - 0
Antagonist activity at rat H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at rat H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 368 4 1 5 1.8 N#Cc1ccc(O[C@@H]2CN[C@@H](C(=O)N3CCCN(C4CCC4)CC3)C2)cc1 10.1016/j.bmcl.2010.03.071
44406392 72884 None 0 Guinea pig Functional pKd = 7.9 7.9 - 0
Antagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileumAntagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileum
ChEMBL 333 7 1 3 3.8 Clc1cccc(OCCCN2CCC(Cc3c[nH]cn3)CC2)c1 10.1016/j.bmcl.2005.09.076
CHEMBL200268 72884 None 0 Guinea pig Functional pKd = 7.9 7.9 - 0
Antagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileumAntagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileum
ChEMBL 333 7 1 3 3.8 Clc1cccc(OCCCN2CCC(Cc3c[nH]cn3)CC2)c1 10.1016/j.bmcl.2005.09.076
44406390 72958 None 0 Guinea pig Functional pKd = 7.9 7.9 - 0
Antagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileumAntagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileum
ChEMBL 346 6 2 3 2.7 O=C(NCCN1CCC(Cc2c[nH]cn2)CC1)c1ccc(Cl)cc1 10.1016/j.bmcl.2005.09.076
CHEMBL200519 72958 None 0 Guinea pig Functional pKd = 7.9 7.9 - 0
Antagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileumAntagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileum
ChEMBL 346 6 2 3 2.7 O=C(NCCN1CCC(Cc2c[nH]cn2)CC1)c1ccc(Cl)cc1 10.1016/j.bmcl.2005.09.076
44308838 206504 None 0 Guinea pig Functional pKd = 7.9 7.9 - 0
H3 -antagonist potency determined in electrically stimulated guinea-pig ileumH3 -antagonist potency determined in electrically stimulated guinea-pig ileum
ChEMBL 313 7 2 3 2.4 O=S(=O)(NCCCCc1c[nH]cn1)c1ccc(Cl)cc1 10.1016/s0960-894x(98)00379-5
CHEMBL69901 206504 None 0 Guinea pig Functional pKd = 7.9 7.9 - 0
H3 -antagonist potency determined in electrically stimulated guinea-pig ileumH3 -antagonist potency determined in electrically stimulated guinea-pig ileum
ChEMBL 313 7 2 3 2.4 O=S(=O)(NCCCCc1c[nH]cn1)c1ccc(Cl)cc1 10.1016/s0960-894x(98)00379-5
10014535 207075 None 0 Guinea pig Functional pKd = 7.9 7.9 - 0
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 240 7 3 2 2.0 C/N=C(\S)NCCCCCCc1c[nH]cn1 10.1021/jm00012a025
CHEMBL73370 207075 None 0 Guinea pig Functional pKd = 7.9 7.9 - 0
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 240 7 3 2 2.0 C/N=C(\S)NCCCCCCc1c[nH]cn1 10.1021/jm00012a025
24965236 89220 None 0 Human Functional pKd = 7.9 7.9 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 452 6 1 4 4.9 CNCc1cc(C#CCCN2CCOCC2)ccc1Oc1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2007.06.061
CHEMBL236676 89220 None 0 Human Functional pKd = 7.9 7.9 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 452 6 1 4 4.9 CNCc1cc(C#CCCN2CCOCC2)ccc1Oc1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2007.06.061
1218 229 None 35 Human Functional pKd = 7.9 7.9 19 2
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrs
ChEMBL 330 4 0 3 5.0 N#Cc1ccc(cc1)c1ccc2c(c1)cc(o2)CCN1CCC[C@H]1C 10.1016/j.ejmech.2009.06.007
9818903 229 None 35 Human Functional pKd = 7.9 7.9 19 2
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrs
ChEMBL 330 4 0 3 5.0 N#Cc1ccc(cc1)c1ccc2c(c1)cc(o2)CCN1CCC[C@H]1C 10.1016/j.ejmech.2009.06.007
CHEMBL351231 229 None 35 Human Functional pKd = 7.9 7.9 19 2
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrs
ChEMBL 330 4 0 3 5.0 N#Cc1ccc(cc1)c1ccc2c(c1)cc(o2)CCN1CCC[C@H]1C 10.1016/j.ejmech.2009.06.007
11269940 46545 None 1 Guinea pig Functional pKd = 6.9 6.9 - 1
Tested for Antagonistic activity at histamine H3 receptor in guinea pig ileal longitudinal muscle in the presence of mepyramine at a concentration of 1-3 micro MTested for Antagonistic activity at histamine H3 receptor in guinea pig ileal longitudinal muscle in the presence of mepyramine at a concentration of 1-3 micro M
ChEMBL 413 12 3 3 4.7 c1ccc(C(CCc2nc(CCNCCCc3c[nH]cn3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
CHEMBL153776 46545 None 1 Guinea pig Functional pKd = 6.9 6.9 - 1
Tested for Antagonistic activity at histamine H3 receptor in guinea pig ileal longitudinal muscle in the presence of mepyramine at a concentration of 1-3 micro MTested for Antagonistic activity at histamine H3 receptor in guinea pig ileal longitudinal muscle in the presence of mepyramine at a concentration of 1-3 micro M
ChEMBL 413 12 3 3 4.7 c1ccc(C(CCc2nc(CCNCCCc3c[nH]cn3)c[nH]2)c2ccccc2)cc1 10.1021/jm0309147
11154035 179760 None 0 Guinea pig Functional pKd = 6.9 6.9 - 0
Antagonist activity at histamine H3 receptor in guinea pig jejunum assessed as electrically evoked contractionsAntagonist activity at histamine H3 receptor in guinea pig jejunum assessed as electrically evoked contractions
ChEMBL 246 3 0 5 1.8 CCCN1CCN(c2nc3cnccc3o2)CC1 10.1016/j.ejmech.2008.09.019
CHEMBL474314 179760 None 0 Guinea pig Functional pKd = 6.9 6.9 - 0
Antagonist activity at histamine H3 receptor in guinea pig jejunum assessed as electrically evoked contractionsAntagonist activity at histamine H3 receptor in guinea pig jejunum assessed as electrically evoked contractions
ChEMBL 246 3 0 5 1.8 CCCN1CCN(c2nc3cnccc3o2)CC1 10.1016/j.ejmech.2008.09.019
11777401 206900 None 0 Guinea pig Functional pKd = 6.9 6.9 - 0
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 260 5 3 2 2.3 S=C(NCCCc1c[nH]cn1)Nc1ccccc1 10.1021/jm00012a025
CHEMBL72174 206900 None 0 Guinea pig Functional pKd = 6.9 6.9 - 0
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 260 5 3 2 2.3 S=C(NCCCc1c[nH]cn1)Nc1ccccc1 10.1021/jm00012a025
10107003 207186 None 0 Guinea pig Functional pKd = 6.9 6.9 - 0
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 266 5 3 2 2.1 S=C(NCCCc1c[nH]cn1)NC1CCCCC1 10.1021/jm00012a025
CHEMBL74293 207186 None 0 Guinea pig Functional pKd = 6.9 6.9 - 0
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 266 5 3 2 2.1 S=C(NCCCc1c[nH]cn1)NC1CCCCC1 10.1021/jm00012a025
1858147 103878 None 7 Guinea pig Functional pKd = 5.9 5.9 - 0
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 274 6 3 2 1.7 S=C(NCCc1ccccc1)NCCc1c[nH]cn1 10.1021/jm00012a025
CHEMBL309164 103878 None 7 Guinea pig Functional pKd = 5.9 5.9 - 0
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 274 6 3 2 1.7 S=C(NCCc1ccccc1)NCCc1c[nH]cn1 10.1021/jm00012a025
5112720 207004 None 2 Guinea pig Functional pKd = 5.9 5.9 - 0
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 252 4 3 2 1.7 S=C(NCCc1c[nH]cn1)NC1CCCCC1 10.1021/jm00012a025
CHEMBL72881 207004 None 2 Guinea pig Functional pKd = 5.9 5.9 - 0
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 252 4 3 2 1.7 S=C(NCCc1c[nH]cn1)NC1CCCCC1 10.1021/jm00012a025
170389 209439 None 25 Guinea pig Functional pKd = 5.9 5.9 - 2
Tested in vitro for antagonist activity against H3 receptor of guinea pig jejunum.Tested in vitro for antagonist activity against H3 receptor of guinea pig jejunum.
ChEMBL 125 3 2 2 0.3 NCCCc1c[nH]cn1 10.1021/jm00002a008
CHEMBL4634086 209439 None 25 Guinea pig Functional pKd = 5.9 5.9 - 2
Tested in vitro for antagonist activity against H3 receptor of guinea pig jejunum.Tested in vitro for antagonist activity against H3 receptor of guinea pig jejunum.
ChEMBL 125 3 2 2 0.3 NCCCc1c[nH]cn1 10.1021/jm00002a008
CHEMBL91353 209439 None 25 Guinea pig Functional pKd = 5.9 5.9 - 2
Tested in vitro for antagonist activity against H3 receptor of guinea pig jejunum.Tested in vitro for antagonist activity against H3 receptor of guinea pig jejunum.
ChEMBL 125 3 2 2 0.3 NCCCc1c[nH]cn1 10.1021/jm00002a008
15983706 93795 None 0 Human Functional pKd = 7.9 7.9 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulationAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulation
ChEMBL 407 8 1 4 4.7 CCN(CC)CCCOc1cc2c(cn1)C(c1ccc(Cl)c(Cl)c1)CNC2 10.1016/j.bmcl.2007.02.006
CHEMBL247265 93795 None 0 Human Functional pKd = 7.9 7.9 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulationAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulation
ChEMBL 407 8 1 4 4.7 CCN(CC)CCCOc1cc2c(cn1)C(c1ccc(Cl)c(Cl)c1)CNC2 10.1016/j.bmcl.2007.02.006
44581078 187881 None 0 Human Functional pKd = 7.9 7.9 - 0
Antagonist activity at human recombinant histamine H3 receptor expressed in human SK-N-MC cellsAntagonist activity at human recombinant histamine H3 receptor expressed in human SK-N-MC cells
ChEMBL 346 6 0 5 2.2 c1cc(CN2CCOCC2)cc(OCC2CN(C3CCC3)CCO2)c1 10.1016/j.bmcl.2008.09.077
CHEMBL495744 187881 None 0 Human Functional pKd = 7.9 7.9 - 0
Antagonist activity at human recombinant histamine H3 receptor expressed in human SK-N-MC cellsAntagonist activity at human recombinant histamine H3 receptor expressed in human SK-N-MC cells
ChEMBL 346 6 0 5 2.2 c1cc(CN2CCOCC2)cc(OCC2CN(C3CCC3)CCO2)c1 10.1016/j.bmcl.2008.09.077
10571747 189514 None 0 Guinea pig Functional pKd = 7.8 7.8 - 0
In vitro histamine H3 receptor antagonist activity was determined on guinea pig jejunumIn vitro histamine H3 receptor antagonist activity was determined on guinea pig jejunum
ChEMBL 378 3 2 2 3.4 S=C(NCc1ccccc1Br)N1CCC(c2c[nH]cn2)CC1 10.1021/jm981106w
CHEMBL51309 189514 None 0 Guinea pig Functional pKd = 7.8 7.8 - 0
In vitro histamine H3 receptor antagonist activity was determined on guinea pig jejunumIn vitro histamine H3 receptor antagonist activity was determined on guinea pig jejunum
ChEMBL 378 3 2 2 3.4 S=C(NCc1ccccc1Br)N1CCC(c2c[nH]cn2)CC1 10.1021/jm981106w
11723102 106503 None 0 Guinea pig Functional pKd = 6.8 6.8 - 0
Histamine H3-antagonist potency on electrically stimulated guinea pig ileumHistamine H3-antagonist potency on electrically stimulated guinea pig ileum
ChEMBL 313 6 3 4 2.2 NC(=O)c1cccc(-c2c[nH]c(SCCc3c[nH]cn3)n2)c1 10.1021/jm970070p
CHEMBL313987 106503 None 0 Guinea pig Functional pKd = 6.8 6.8 - 0
Histamine H3-antagonist potency on electrically stimulated guinea pig ileumHistamine H3-antagonist potency on electrically stimulated guinea pig ileum
ChEMBL 313 6 3 4 2.2 NC(=O)c1cccc(-c2c[nH]c(SCCc3c[nH]cn3)n2)c1 10.1021/jm970070p
44320707 106086 None 0 Guinea pig Functional pKd = 5.8 5.8 - 0
Compound was tested for the agonist activity against histamine H3 receptor of guinea pig ileumCompound was tested for the agonist activity against histamine H3 receptor of guinea pig ileum
ChEMBL 293 4 1 2 2.9 CN(C)CCc1c[nH]c(-c2cccc(Br)c2)n1 10.1016/s0960-894x(98)00461-2
CHEMBL313301 106086 None 0 Guinea pig Functional pKd = 5.8 5.8 - 0
Compound was tested for the agonist activity against histamine H3 receptor of guinea pig ileumCompound was tested for the agonist activity against histamine H3 receptor of guinea pig ileum
ChEMBL 293 4 1 2 2.9 CN(C)CCc1c[nH]c(-c2cccc(Br)c2)n1 10.1016/s0960-894x(98)00461-2
23276430 208550 None 0 Guinea pig Functional pKd = 6.8 6.8 - 0
Histamine H3-antagonist potency on electrically stimulated guinea pig ileumHistamine H3-antagonist potency on electrically stimulated guinea pig ileum
ChEMBL 342 9 2 4 4.3 CCCCOc1ccc(-c2c[nH]c(SCCc3c[nH]cn3)n2)cc1 10.1021/jm970070p
CHEMBL85635 208550 None 0 Guinea pig Functional pKd = 6.8 6.8 - 0
Histamine H3-antagonist potency on electrically stimulated guinea pig ileumHistamine H3-antagonist potency on electrically stimulated guinea pig ileum
ChEMBL 342 9 2 4 4.3 CCCCOc1ccc(-c2c[nH]c(SCCc3c[nH]cn3)n2)cc1 10.1021/jm970070p
9796764 73029 None 0 Guinea pig Functional pKd = 7.8 7.8 - 0
Antagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileumAntagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileum
ChEMBL 311 6 1 2 3.2 O=C(CCCc1ccccc1)N1CCC(Cc2c[nH]cn2)CC1 10.1016/j.bmcl.2005.09.076
CHEMBL200853 73029 None 0 Guinea pig Functional pKd = 7.8 7.8 - 0
Antagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileumAntagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileum
ChEMBL 311 6 1 2 3.2 O=C(CCCc1ccccc1)N1CCC(Cc2c[nH]cn2)CC1 10.1016/j.bmcl.2005.09.076
9861608 140368 None 0 Guinea pig Functional pKd = 7.8 7.8 - 0
Antagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileumAntagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileum
ChEMBL 313 6 1 3 2.7 O=C(CCOc1ccccc1)N1CCC(Cc2c[nH]cn2)CC1 10.1016/j.bmcl.2005.09.076
CHEMBL380584 140368 None 0 Guinea pig Functional pKd = 7.8 7.8 - 0
Antagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileumAntagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileum
ChEMBL 313 6 1 3 2.7 O=C(CCOc1ccccc1)N1CCC(Cc2c[nH]cn2)CC1 10.1016/j.bmcl.2005.09.076
44408029 75532 None 0 Guinea pig Functional pKd = 7.8 7.8 - 0
Antagonistic activity against histamine H3 receptor in guinea pig ileumAntagonistic activity against histamine H3 receptor in guinea pig ileum
ChEMBL 410 10 1 4 4.5 c1nc(CC2CCN(CCCCOc3ccc(CN4CCCCC4)cc3)CC2)c[nH]1 10.1016/j.bmcl.2005.10.087
CHEMBL204301 75532 None 0 Guinea pig Functional pKd = 7.8 7.8 - 0
Antagonistic activity against histamine H3 receptor in guinea pig ileumAntagonistic activity against histamine H3 receptor in guinea pig ileum
ChEMBL 410 10 1 4 4.5 c1nc(CC2CCN(CCCCOc3ccc(CN4CCCCC4)cc3)CC2)c[nH]1 10.1016/j.bmcl.2005.10.087
44407899 166161 None 0 Guinea pig Functional pKd = 7.8 7.8 - 0
Antagonistic activity against histamine H3 receptor in guinea pig ileumAntagonistic activity against histamine H3 receptor in guinea pig ileum
ChEMBL 411 8 2 5 2.2 O=C(c1ccc(OCCCN2CCC(Cc3c[nH]cn3)CC2)cc1)N1CCNCC1 10.1016/j.bmcl.2005.10.087
CHEMBL425765 166161 None 0 Guinea pig Functional pKd = 7.8 7.8 - 0
Antagonistic activity against histamine H3 receptor in guinea pig ileumAntagonistic activity against histamine H3 receptor in guinea pig ileum
ChEMBL 411 8 2 5 2.2 O=C(c1ccc(OCCCN2CCC(Cc3c[nH]cn3)CC2)cc1)N1CCNCC1 10.1016/j.bmcl.2005.10.087
11436304 11341 None 0 Guinea pig Functional pKd = 7.8 7.8 - 0
Functional Histamine H3 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H3 receptor antagonistic activity in vitro assay on guinea pig ileum
ChEMBL 236 8 1 2 3.3 c1nc(CCCOCCCC2CCCC2)c[nH]1 10.1021/jm031065q
CHEMBL1179594 11341 None 0 Guinea pig Functional pKd = 7.8 7.8 - 0
Functional Histamine H3 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H3 receptor antagonistic activity in vitro assay on guinea pig ileum
ChEMBL 236 8 1 2 3.3 c1nc(CCCOCCCC2CCCC2)c[nH]1 10.1021/jm031065q
CHEMBL88306 11341 None 0 Guinea pig Functional pKd = 7.8 7.8 - 0
Functional Histamine H3 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H3 receptor antagonistic activity in vitro assay on guinea pig ileum
ChEMBL 236 8 1 2 3.3 c1nc(CCCOCCCC2CCCC2)c[nH]1 10.1021/jm031065q
11276413 12075 None 0 Guinea pig Functional pKd = 7.8 7.8 - 0
Functional Histamine H3 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H3 receptor antagonistic activity in vitro assay on guinea pig ileum
ChEMBL 236 7 1 2 3.3 c1nc(CCCOCCC2CCCCC2)c[nH]1 10.1021/jm031065q
CHEMBL1183700 12075 None 0 Guinea pig Functional pKd = 7.8 7.8 - 0
Functional Histamine H3 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H3 receptor antagonistic activity in vitro assay on guinea pig ileum
ChEMBL 236 7 1 2 3.3 c1nc(CCCOCCC2CCCCC2)c[nH]1 10.1021/jm031065q
CHEMBL313803 12075 None 0 Guinea pig Functional pKd = 7.8 7.8 - 0
Functional Histamine H3 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H3 receptor antagonistic activity in vitro assay on guinea pig ileum
ChEMBL 236 7 1 2 3.3 c1nc(CCCOCCC2CCCCC2)c[nH]1 10.1021/jm031065q
11218373 12112 None 0 Guinea pig Functional pKd = 7.8 7.8 - 0
Functional Histamine H3 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H3 receptor antagonistic activity in vitro assay on guinea pig ileum
ChEMBL 224 10 1 2 3.3 CCCCCCCOCCCc1c[nH]cn1 10.1021/jm031065q
CHEMBL1184028 12112 None 0 Guinea pig Functional pKd = 7.8 7.8 - 0
Functional Histamine H3 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H3 receptor antagonistic activity in vitro assay on guinea pig ileum
ChEMBL 224 10 1 2 3.3 CCCCCCCOCCCc1c[nH]cn1 10.1021/jm031065q
CHEMBL329116 12112 None 0 Guinea pig Functional pKd = 7.8 7.8 - 0
Functional Histamine H3 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H3 receptor antagonistic activity in vitro assay on guinea pig ileum
ChEMBL 224 10 1 2 3.3 CCCCCCCOCCCc1c[nH]cn1 10.1021/jm031065q
44308603 206064 None 0 Guinea pig Functional pKd = 7.8 7.8 - 0
H3 -antagonist potency determined in electrically stimulated guinea-pig ileumH3 -antagonist potency determined in electrically stimulated guinea-pig ileum
ChEMBL 437 9 1 3 4.9 O=S(=O)(c1ccc(Cl)cc1)N(CCCCc1c[nH]cn1)Cc1ccc(Cl)cc1 10.1016/s0960-894x(98)00379-5
CHEMBL66994 206064 None 0 Guinea pig Functional pKd = 7.8 7.8 - 0
H3 -antagonist potency determined in electrically stimulated guinea-pig ileumH3 -antagonist potency determined in electrically stimulated guinea-pig ileum
ChEMBL 437 9 1 3 4.9 O=S(=O)(c1ccc(Cl)cc1)N(CCCCc1c[nH]cn1)Cc1ccc(Cl)cc1 10.1016/s0960-894x(98)00379-5
10359599 206335 None 0 Guinea pig Functional pKd = 7.8 7.8 - 0
H3 -antagonist potency determined in electrically stimulated guinea-pig ileumH3 -antagonist potency determined in electrically stimulated guinea-pig ileum
ChEMBL 335 7 2 3 3.0 CC(C)(C)c1ccc(S(=O)(=O)NCCCCc2c[nH]cn2)cc1 10.1016/s0960-894x(98)00379-5
CHEMBL68764 206335 None 0 Guinea pig Functional pKd = 7.8 7.8 - 0
H3 -antagonist potency determined in electrically stimulated guinea-pig ileumH3 -antagonist potency determined in electrically stimulated guinea-pig ileum
ChEMBL 335 7 2 3 3.0 CC(C)(C)c1ccc(S(=O)(=O)NCCCCc2c[nH]cn2)cc1 10.1016/s0960-894x(98)00379-5
10002564 101837 None 0 Guinea pig Functional pKd = 7.8 7.8 - 0
In vitro histamine H3 receptor antagonist activity was determined on guinea pig jejunumIn vitro histamine H3 receptor antagonist activity was determined on guinea pig jejunum
ChEMBL 426 3 2 2 3.3 S=C(NCc1cccc(I)c1)N1CCC(c2c[nH]cn2)CC1 10.1021/jm981106w
CHEMBL300012 101837 None 0 Guinea pig Functional pKd = 7.8 7.8 - 0
In vitro histamine H3 receptor antagonist activity was determined on guinea pig jejunumIn vitro histamine H3 receptor antagonist activity was determined on guinea pig jejunum
ChEMBL 426 3 2 2 3.3 S=C(NCc1cccc(I)c1)N1CCC(c2c[nH]cn2)CC1 10.1021/jm981106w
10261471 197980 None 0 Guinea pig Functional pKd = 7.8 7.8 - 1
Tested in vitro for antagonist activity against H3 receptor of guinea pig jejunum.Tested in vitro for antagonist activity against H3 receptor of guinea pig jejunum.
ChEMBL 167 6 2 2 1.5 NCCCCCCc1c[nH]cn1 10.1021/jm00002a008
CHEMBL554031 197980 None 0 Guinea pig Functional pKd = 7.8 7.8 - 1
Tested in vitro for antagonist activity against H3 receptor of guinea pig jejunum.Tested in vitro for antagonist activity against H3 receptor of guinea pig jejunum.
ChEMBL 167 6 2 2 1.5 NCCCCCCc1c[nH]cn1 10.1021/jm00002a008
44308807 206783 None 0 Guinea pig Functional pKd = 6.8 6.8 - 0
H3 -antagonist potency determined in electrically stimulated guinea-pig ileumH3 -antagonist potency determined in electrically stimulated guinea-pig ileum
ChEMBL 297 7 2 3 1.9 O=S(=O)(NCCCCc1c[nH]cn1)c1ccc(F)cc1 10.1016/s0960-894x(98)00379-5
CHEMBL71487 206783 None 0 Guinea pig Functional pKd = 6.8 6.8 - 0
H3 -antagonist potency determined in electrically stimulated guinea-pig ileumH3 -antagonist potency determined in electrically stimulated guinea-pig ileum
ChEMBL 297 7 2 3 1.9 O=S(=O)(NCCCCc1c[nH]cn1)c1ccc(F)cc1 10.1016/s0960-894x(98)00379-5
10400394 206577 None 0 Guinea pig Functional pKd = 5.8 5.8 - 0
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 260 5 3 2 1.6 S=C(NCCc1c[nH]cn1)NCc1ccccc1 10.1021/jm00012a025
CHEMBL70349 206577 None 0 Guinea pig Functional pKd = 5.8 5.8 - 0
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 260 5 3 2 1.6 S=C(NCCc1c[nH]cn1)NCc1ccccc1 10.1021/jm00012a025
10420729 207111 None 0 Guinea pig Functional pKd = 4.8 4.8 - 0
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 212 4 3 2 1.2 CC(C)/N=C(\S)NCCc1c[nH]cn1 10.1021/jm00012a025
CHEMBL73629 207111 None 0 Guinea pig Functional pKd = 4.8 4.8 - 0
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 212 4 3 2 1.2 CC(C)/N=C(\S)NCCc1c[nH]cn1 10.1021/jm00012a025
23275969 208905 None 0 Guinea pig Functional pKd = 7.8 7.8 - 0
Histamine H3-antagonist potency on electrically stimulated guinea pig ileumHistamine H3-antagonist potency on electrically stimulated guinea pig ileum
ChEMBL 315 6 2 5 3.0 O=[N+]([O-])c1ccc(-c2c[nH]c(SCCc3c[nH]cn3)n2)cc1 10.1021/jm970070p
CHEMBL88051 208905 None 0 Guinea pig Functional pKd = 7.8 7.8 - 0
Histamine H3-antagonist potency on electrically stimulated guinea pig ileumHistamine H3-antagonist potency on electrically stimulated guinea pig ileum
ChEMBL 315 6 2 5 3.0 O=[N+]([O-])c1ccc(-c2c[nH]c(SCCc3c[nH]cn3)n2)cc1 10.1021/jm970070p
42604375 12560 None 0 Guinea pig Functional pKd = 7.8 7.8 - 0
Antagonist activity at histamine H3 receptor in guinea pig jejunum assessed as electrically evoked contractionsAntagonist activity at histamine H3 receptor in guinea pig jejunum assessed as electrically evoked contractions
ChEMBL 282 6 0 5 1.8 CCCN1CCN(c2ncc(CCN(C)C)s2)CC1 10.1016/j.ejmech.2008.09.019
CHEMBL1186717 12560 None 0 Guinea pig Functional pKd = 7.8 7.8 - 0
Antagonist activity at histamine H3 receptor in guinea pig jejunum assessed as electrically evoked contractionsAntagonist activity at histamine H3 receptor in guinea pig jejunum assessed as electrically evoked contractions
ChEMBL 282 6 0 5 1.8 CCCN1CCN(c2ncc(CCN(C)C)s2)CC1 10.1016/j.ejmech.2008.09.019
CHEMBL475323 12560 None 0 Guinea pig Functional pKd = 7.8 7.8 - 0
Antagonist activity at histamine H3 receptor in guinea pig jejunum assessed as electrically evoked contractionsAntagonist activity at histamine H3 receptor in guinea pig jejunum assessed as electrically evoked contractions
ChEMBL 282 6 0 5 1.8 CCCN1CCN(c2ncc(CCN(C)C)s2)CC1 10.1016/j.ejmech.2008.09.019
44438666 93761 None 0 Human Functional pKd = 7.8 7.8 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulationAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulation
ChEMBL 417 6 0 4 4.7 CN1Cc2cc(OCCCN3CCCCC3)ncc2C(c2ccc(Cl)c(F)c2)C1 10.1016/j.bmcl.2007.02.006
CHEMBL247094 93761 None 0 Human Functional pKd = 7.8 7.8 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulationAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulation
ChEMBL 417 6 0 4 4.7 CN1Cc2cc(OCCCN3CCCCC3)ncc2C(c2ccc(Cl)c(F)c2)C1 10.1016/j.bmcl.2007.02.006
44407803 75561 None 8 Human Functional pKd = 7.8 7.8 - 0
Activity against human histamine H3 receptor by histamine induced inhibition of forskolin stimulated cAMP accumulation in SK-N-MC cellsActivity against human histamine H3 receptor by histamine induced inhibition of forskolin stimulated cAMP accumulation in SK-N-MC cells
ChEMBL 250 8 0 3 2.1 CN(C)CCCOc1ccc(CCN(C)C)cc1 10.1016/j.bmcl.2005.11.003
CHEMBL204377 75561 None 8 Human Functional pKd = 7.8 7.8 - 0
Activity against human histamine H3 receptor by histamine induced inhibition of forskolin stimulated cAMP accumulation in SK-N-MC cellsActivity against human histamine H3 receptor by histamine induced inhibition of forskolin stimulated cAMP accumulation in SK-N-MC cells
ChEMBL 250 8 0 3 2.1 CN(C)CCCOc1ccc(CCN(C)C)cc1 10.1016/j.bmcl.2005.11.003
10002565 169572 None 0 Guinea pig Functional pKd = 6.8 6.8 - 0
In vitro histamine H3 receptor antagonist activity was determined on guinea pig jejunumIn vitro histamine H3 receptor antagonist activity was determined on guinea pig jejunum
ChEMBL 426 3 2 2 3.3 S=C(NCc1ccc(I)cc1)N1CCC(c2c[nH]cn2)CC1 10.1021/jm981106w
CHEMBL442958 169572 None 0 Guinea pig Functional pKd = 6.8 6.8 - 0
In vitro histamine H3 receptor antagonist activity was determined on guinea pig jejunumIn vitro histamine H3 receptor antagonist activity was determined on guinea pig jejunum
ChEMBL 426 3 2 2 3.3 S=C(NCc1ccc(I)cc1)N1CCC(c2c[nH]cn2)CC1 10.1021/jm981106w
42604651 12532 None 0 Guinea pig Functional pKd = 7.8 7.8 - 0
Antagonist activity at histamine H3 receptor in guinea pig jejunum assessed as electrically evoked contractionsAntagonist activity at histamine H3 receptor in guinea pig jejunum assessed as electrically evoked contractions
ChEMBL 358 8 0 5 3.4 CCCN1CCN(c2ncc(CCN(C)Cc3ccccc3)s2)CC1 10.1016/j.ejmech.2008.09.019
CHEMBL1186609 12532 None 0 Guinea pig Functional pKd = 7.8 7.8 - 0
Antagonist activity at histamine H3 receptor in guinea pig jejunum assessed as electrically evoked contractionsAntagonist activity at histamine H3 receptor in guinea pig jejunum assessed as electrically evoked contractions
ChEMBL 358 8 0 5 3.4 CCCN1CCN(c2ncc(CCN(C)Cc3ccccc3)s2)CC1 10.1016/j.ejmech.2008.09.019
CHEMBL472690 12532 None 0 Guinea pig Functional pKd = 7.8 7.8 - 0
Antagonist activity at histamine H3 receptor in guinea pig jejunum assessed as electrically evoked contractionsAntagonist activity at histamine H3 receptor in guinea pig jejunum assessed as electrically evoked contractions
ChEMBL 358 8 0 5 3.4 CCCN1CCN(c2ncc(CCN(C)Cc3ccccc3)s2)CC1 10.1016/j.ejmech.2008.09.019
15983580 93876 None 0 Human Functional pKd = 7.7 7.7 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulationAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulation
ChEMBL 433 6 0 4 5.2 CN1Cc2cc(OCCCN3CCCCC3)ncc2C(c2ccc(Cl)c(Cl)c2)C1 10.1016/j.bmcl.2007.02.006
CHEMBL247683 93876 None 0 Human Functional pKd = 7.7 7.7 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulationAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulation
ChEMBL 433 6 0 4 5.2 CN1Cc2cc(OCCCN3CCCCC3)ncc2C(c2ccc(Cl)c(Cl)c2)C1 10.1016/j.bmcl.2007.02.006
44581059 187999 None 0 Rat Functional pKd = 7.7 7.7 - 0
Antagonist activity rat recombinant histamine H3 receptor expressed in human SK-N-MC cellsAntagonist activity rat recombinant histamine H3 receptor expressed in human SK-N-MC cells
ChEMBL 346 6 0 5 2.2 c1cc(OCC2CN(C3CCC3)CCO2)ccc1CN1CCOCC1 10.1016/j.bmcl.2008.09.077
CHEMBL496554 187999 None 0 Rat Functional pKd = 7.7 7.7 - 0
Antagonist activity rat recombinant histamine H3 receptor expressed in human SK-N-MC cellsAntagonist activity rat recombinant histamine H3 receptor expressed in human SK-N-MC cells
ChEMBL 346 6 0 5 2.2 c1cc(OCC2CN(C3CCC3)CCO2)ccc1CN1CCOCC1 10.1016/j.bmcl.2008.09.077
9923762 192723 None 0 Rat Functional pKd = 7.7 7.7 - 0
Antagonist activity at rat histamine H3 receptor expressed in SK-NM-C cellsAntagonist activity at rat histamine H3 receptor expressed in SK-NM-C cells
ChEMBL 334 6 0 3 4.9 c1ccn2cc(-c3ccc(OCCCN4CCCCC4)cc3)cc2c1 10.1016/j.ejmech.2011.08.042
CHEMBL52160 192723 None 0 Rat Functional pKd = 7.7 7.7 - 0
Antagonist activity at rat histamine H3 receptor expressed in SK-NM-C cellsAntagonist activity at rat histamine H3 receptor expressed in SK-NM-C cells
ChEMBL 334 6 0 3 4.9 c1ccn2cc(-c3ccc(OCCCN4CCCCC4)cc3)cc2c1 10.1016/j.ejmech.2011.08.042
10177656 180007 None 0 Human Functional pKd = 7.7 7.7 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 377 7 0 5 4.3 Cn1c(C(=O)c2ccc(Cl)cc2)cnc1SCCCN1CCCCC1 10.1016/j.bmcl.2008.11.114
CHEMBL474597 180007 None 0 Human Functional pKd = 7.7 7.7 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 377 7 0 5 4.3 Cn1c(C(=O)c2ccc(Cl)cc2)cnc1SCCCN1CCCCC1 10.1016/j.bmcl.2008.11.114
44408015 75401 None 0 Guinea pig Functional pKd = 7.7 7.7 - 0
Antagonistic activity against histamine H3 receptor in guinea pig ileumAntagonistic activity against histamine H3 receptor in guinea pig ileum
ChEMBL 410 8 1 4 3.8 O=C(c1ccc(OCCCN2CCC(Cc3c[nH]cn3)CC2)cc1)N1CCCCC1 10.1016/j.bmcl.2005.10.087
CHEMBL203805 75401 None 0 Guinea pig Functional pKd = 7.7 7.7 - 0
Antagonistic activity against histamine H3 receptor in guinea pig ileumAntagonistic activity against histamine H3 receptor in guinea pig ileum
ChEMBL 410 8 1 4 3.8 O=C(c1ccc(OCCCN2CCC(Cc3c[nH]cn3)CC2)cc1)N1CCCCC1 10.1016/j.bmcl.2005.10.087
44408011 75428 None 0 Guinea pig Functional pKd = 7.7 7.7 - 0
Antagonistic activity against histamine H3 receptor in guinea pig ileumAntagonistic activity against histamine H3 receptor in guinea pig ileum
ChEMBL 392 8 2 6 3.2 Nc1ncc(-c2ccc(OCCCN3CCC(Cc4c[nH]cn4)CC3)cc2)cn1 10.1016/j.bmcl.2005.10.087
CHEMBL203983 75428 None 0 Guinea pig Functional pKd = 7.7 7.7 - 0
Antagonistic activity against histamine H3 receptor in guinea pig ileumAntagonistic activity against histamine H3 receptor in guinea pig ileum
ChEMBL 392 8 2 6 3.2 Nc1ncc(-c2ccc(OCCCN3CCC(Cc4c[nH]cn4)CC3)cc2)cn1 10.1016/j.bmcl.2005.10.087
44407955 75683 None 0 Guinea pig Functional pKd = 7.7 7.7 - 0
Antagonistic activity against histamine H3 receptor in guinea pig ileumAntagonistic activity against histamine H3 receptor in guinea pig ileum
ChEMBL 411 8 1 5 3.2 O=C(c1ccc(OCCCN2CCC(Cc3c[nH]cn3)CC2)nc1)N1CCCCC1 10.1016/j.bmcl.2005.10.087
CHEMBL204742 75683 None 0 Guinea pig Functional pKd = 7.7 7.7 - 0
Antagonistic activity against histamine H3 receptor in guinea pig ileumAntagonistic activity against histamine H3 receptor in guinea pig ileum
ChEMBL 411 8 1 5 3.2 O=C(c1ccc(OCCCN2CCC(Cc3c[nH]cn3)CC2)nc1)N1CCCCC1 10.1016/j.bmcl.2005.10.087
24180451 89922 None 0 Human Functional pKd = 7.7 7.7 - 0
Antagonistic activity at H3 receptor expressed in SK-NM-C cells assessed as forskolin stimulated cyclic AMP accumulation by functional assayAntagonistic activity at H3 receptor expressed in SK-NM-C cells assessed as forskolin stimulated cyclic AMP accumulation by functional assay
ChEMBL 459 6 0 5 6.2 CSc1ccc(C2CN(C)Cc3cc(Oc4ccc(CN5CCCCC5)cn4)ccc32)cc1 10.1016/j.bmcl.2007.08.017
CHEMBL237862 89922 None 0 Human Functional pKd = 7.7 7.7 - 0
Antagonistic activity at H3 receptor expressed in SK-NM-C cells assessed as forskolin stimulated cyclic AMP accumulation by functional assayAntagonistic activity at H3 receptor expressed in SK-NM-C cells assessed as forskolin stimulated cyclic AMP accumulation by functional assay
ChEMBL 459 6 0 5 6.2 CSc1ccc(C2CN(C)Cc3cc(Oc4ccc(CN5CCCCC5)cn4)ccc32)cc1 10.1016/j.bmcl.2007.08.017
25119061 89984 None 0 Human Functional pKd = 7.7 7.7 - 0
Antagonistic activity at H3 receptor expressed in SK-NM-C cells assessed as forskolin stimulated cyclic AMP accumulation by functional assayAntagonistic activity at H3 receptor expressed in SK-NM-C cells assessed as forskolin stimulated cyclic AMP accumulation by functional assay
ChEMBL 465 6 0 6 6.2 CSc1ccc(C2CN(C)Cc3cc(Oc4nc(CN5CCCCC5)cs4)ccc32)cc1 10.1016/j.bmcl.2007.08.017
CHEMBL238054 89984 None 0 Human Functional pKd = 7.7 7.7 - 0
Antagonistic activity at H3 receptor expressed in SK-NM-C cells assessed as forskolin stimulated cyclic AMP accumulation by functional assayAntagonistic activity at H3 receptor expressed in SK-NM-C cells assessed as forskolin stimulated cyclic AMP accumulation by functional assay
ChEMBL 465 6 0 6 6.2 CSc1ccc(C2CN(C)Cc3cc(Oc4nc(CN5CCCCC5)cs4)ccc32)cc1 10.1016/j.bmcl.2007.08.017
44308916 206459 None 0 Guinea pig Functional pKd = 7.7 7.7 - 0
H3 -antagonist potency determined in electrically stimulated guinea-pig ileumH3 -antagonist potency determined in electrically stimulated guinea-pig ileum
ChEMBL 324 8 2 5 1.6 O=[N+]([O-])c1ccc(S(=O)(=O)NCCCCc2c[nH]cn2)cc1 10.1016/s0960-894x(98)00379-5
CHEMBL69607 206459 None 0 Guinea pig Functional pKd = 7.7 7.7 - 0
H3 -antagonist potency determined in electrically stimulated guinea-pig ileumH3 -antagonist potency determined in electrically stimulated guinea-pig ileum
ChEMBL 324 8 2 5 1.6 O=[N+]([O-])c1ccc(S(=O)(=O)NCCCCc2c[nH]cn2)cc1 10.1016/s0960-894x(98)00379-5
10015196 103675 None 0 Guinea pig Functional pKd = 7.7 7.7 - 0
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 254 8 3 2 2.4 CCC/N=C(\S)NCCCCCc1c[nH]cn1 10.1021/jm00012a025
CHEMBL308717 103675 None 0 Guinea pig Functional pKd = 7.7 7.7 - 0
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 254 8 3 2 2.4 CCC/N=C(\S)NCCCCCc1c[nH]cn1 10.1021/jm00012a025
10422468 206616 None 0 Guinea pig Functional pKd = 7.7 7.7 - 0
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 254 7 3 2 2.4 CC(C)/N=C(\S)NCCCCCc1c[nH]cn1 10.1021/jm00012a025
CHEMBL70603 206616 None 0 Guinea pig Functional pKd = 7.7 7.7 - 0
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 254 7 3 2 2.4 CC(C)/N=C(\S)NCCCCCc1c[nH]cn1 10.1021/jm00012a025
10017820 206653 None 0 Guinea pig Functional pKd = 7.7 7.7 - 0
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 302 8 3 2 2.8 S=C(NCCCCCc1c[nH]cn1)NCc1ccccc1 10.1021/jm00012a025
CHEMBL70811 206653 None 0 Guinea pig Functional pKd = 7.7 7.7 - 0
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 302 8 3 2 2.8 S=C(NCCCCCc1c[nH]cn1)NCc1ccccc1 10.1021/jm00012a025
1249 2009 None 10 Guinea pig Functional pKd = 7.7 7.7 - 2
Tested in vitro for antagonist activity against H3 receptor of guinea pig jejunum.Tested in vitro for antagonist activity against H3 receptor of guinea pig jejunum.
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1021/jm00002a008
13499360 2009 None 10 Guinea pig Functional pKd = 7.7 7.7 - 2
Tested in vitro for antagonist activity against H3 receptor of guinea pig jejunum.Tested in vitro for antagonist activity against H3 receptor of guinea pig jejunum.
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1021/jm00002a008
CHEMBL90019 2009 None 10 Guinea pig Functional pKd = 7.7 7.7 - 2
Tested in vitro for antagonist activity against H3 receptor of guinea pig jejunum.Tested in vitro for antagonist activity against H3 receptor of guinea pig jejunum.
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1021/jm00002a008
10084747 102974 None 0 Guinea pig Functional pKd = 6.7 6.7 - 0
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 274 6 3 2 2.0 S=C(NCCCc1c[nH]cn1)NCc1ccccc1 10.1021/jm00012a025
CHEMBL306130 102974 None 0 Guinea pig Functional pKd = 6.7 6.7 - 0
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 274 6 3 2 2.0 S=C(NCCCc1c[nH]cn1)NCc1ccccc1 10.1021/jm00012a025
10424221 102997 None 0 Guinea pig Functional pKd = 6.7 6.7 - 0
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 288 7 3 2 2.0 S=C(NCCCc1c[nH]cn1)NCCc1ccccc1 10.1021/jm00012a025
CHEMBL306317 102997 None 0 Guinea pig Functional pKd = 6.7 6.7 - 0
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 288 7 3 2 2.0 S=C(NCCCc1c[nH]cn1)NCCc1ccccc1 10.1021/jm00012a025
10291489 187815 None 10 Human Functional pKd = 8.7 8.7 - 0
Antagonist activity for human histamine H3 receptor was determinedAntagonist activity for human histamine H3 receptor was determined
ChEMBL 349 6 0 4 4.6 Cc1ccn2cc(-c3ccc(OCCCN4CCCCC4)cc3)nc2c1 10.1016/s0960-894x(02)00738-2
CHEMBL49532 187815 None 10 Human Functional pKd = 8.7 8.7 - 0
Antagonist activity for human histamine H3 receptor was determinedAntagonist activity for human histamine H3 receptor was determined
ChEMBL 349 6 0 4 4.6 Cc1ccn2cc(-c3ccc(OCCCN4CCCCC4)cc3)nc2c1 10.1016/s0960-894x(02)00738-2
46887961 8720 None 0 Human Functional pKd = 8.7 8.7 - 0
Antagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 361 4 1 4 2.0 O=C([C@H]1C[C@H](Oc2cccc(F)c2)CN1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.03.071
CHEMBL1095845 8720 None 0 Human Functional pKd = 8.7 8.7 - 0
Antagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 361 4 1 4 2.0 O=C([C@H]1C[C@H](Oc2cccc(F)c2)CN1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.03.071
46887994 8940 None 0 Human Functional pKd = 8.7 8.7 - 0
Antagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 368 4 1 5 1.8 N#Cc1ccc(O[C@@H]2CN[C@@H](C(=O)N3CCCN(C4CCC4)CC3)C2)cc1 10.1016/j.bmcl.2010.03.071
CHEMBL1097881 8940 None 0 Human Functional pKd = 8.7 8.7 - 0
Antagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 368 4 1 5 1.8 N#Cc1ccc(O[C@@H]2CN[C@@H](C(=O)N3CCCN(C4CCC4)CC3)C2)cc1 10.1016/j.bmcl.2010.03.071
25211254 188081 None 0 Rat Functional pKd = 8.7 8.7 - 0
Antagonist activity rat recombinant histamine H3 receptor expressed in human SK-N-MC cellsAntagonist activity rat recombinant histamine H3 receptor expressed in human SK-N-MC cells
ChEMBL 360 6 0 5 2.5 c1cc(OC[C@@H]2CN(C3CCCC3)CCO2)ccc1CN1CCOCC1 10.1016/j.bmcl.2008.09.077
CHEMBL497192 188081 None 0 Rat Functional pKd = 8.7 8.7 - 0
Antagonist activity rat recombinant histamine H3 receptor expressed in human SK-N-MC cellsAntagonist activity rat recombinant histamine H3 receptor expressed in human SK-N-MC cells
ChEMBL 360 6 0 5 2.5 c1cc(OC[C@@H]2CN(C3CCCC3)CCO2)ccc1CN1CCOCC1 10.1016/j.bmcl.2008.09.077
46888327 8656 None 0 Human Functional pKd = 8.7 8.7 - 0
Antagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 349 4 1 5 1.9 O=C([C@H]1C[C@H](Oc2ccsc2)CN1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.03.071
CHEMBL1095355 8656 None 0 Human Functional pKd = 8.7 8.7 - 0
Antagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 349 4 1 5 1.9 O=C([C@H]1C[C@H](Oc2ccsc2)CN1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.03.071
44600840 8681 None 0 Human Functional pKd = 8.7 8.7 - 0
Antagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 389 5 1 5 2.6 CSc1ccc(O[C@@H]2CN[C@@H](C(=O)N3CCCN(C4CCC4)CC3)C2)cc1 10.1016/j.bmcl.2010.03.071
CHEMBL1095547 8681 None 0 Human Functional pKd = 8.7 8.7 - 0
Antagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 389 5 1 5 2.6 CSc1ccc(O[C@@H]2CN[C@@H](C(=O)N3CCCN(C4CCC4)CC3)C2)cc1 10.1016/j.bmcl.2010.03.071
11509486 87295 None 0 Human Functional pKd = 8.6 8.6 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 396 7 0 5 3.4 COc1ccc(C2CN(C)Cc3cc(OCCCN4CCOCC4)ccc32)cc1 10.1016/j.bmcl.2006.11.036
CHEMBL233053 87295 None 0 Human Functional pKd = 8.6 8.6 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 396 7 0 5 3.4 COc1ccc(C2CN(C)Cc3cc(OCCCN4CCOCC4)ccc32)cc1 10.1016/j.bmcl.2006.11.036
46861756 8574 None 0 Rat Functional pKd = 8.6 8.6 - 0
Antagonist activity at rat H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at rat H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 403 4 0 4 2.3 CC(=O)N1C[C@@H](Oc2ccc(F)cc2)C[C@@H]1C(=O)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.03.071
CHEMBL1094562 8574 None 0 Rat Functional pKd = 8.6 8.6 - 0
Antagonist activity at rat H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at rat H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 403 4 0 4 2.3 CC(=O)N1C[C@@H](Oc2ccc(F)cc2)C[C@@H]1C(=O)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.03.071
24947753 95276 None 0 Human Functional pKd = 8.6 8.6 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 401 6 1 4 4.0 CNCc1cc(C(=O)N2CCN(C(C)C)CC2)ccc1Oc1ccc(Cl)cc1 10.1016/j.bmcl.2007.11.016
CHEMBL256044 95276 None 0 Human Functional pKd = 8.6 8.6 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 401 6 1 4 4.0 CNCc1cc(C(=O)N2CCN(C(C)C)CC2)ccc1Oc1ccc(Cl)cc1 10.1016/j.bmcl.2007.11.016
24964157 147565 None 0 Human Functional pKd = 8.6 8.6 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 394 7 1 4 5.1 CNCc1cc(C#CCCN2CCCCC2)ccc1Oc1ccc(SC)cc1 10.1016/j.bmcl.2007.06.061
CHEMBL393036 147565 None 0 Human Functional pKd = 8.6 8.6 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 394 7 1 4 5.1 CNCc1cc(C#CCCN2CCCCC2)ccc1Oc1ccc(SC)cc1 10.1016/j.bmcl.2007.06.061
24771740 10592 None 0 Human Functional pKd = 8.6 8.6 - 0
Antagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 385 4 0 4 4.2 O=C(c1ccc(Oc2ccc(Cl)cc2)cn1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.05.041
CHEMBL1169939 10592 None 0 Human Functional pKd = 8.6 8.6 - 0
Antagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 385 4 0 4 4.2 O=C(c1ccc(Oc2ccc(Cl)cc2)cn1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.05.041
44406484 165912 None 0 Guinea pig Functional pKd = 8.6 8.6 - 0
Antagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileumAntagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileum
ChEMBL 263 8 1 2 3.6 CCCCCCCN1CCC(Cc2c[nH]cn2)CC1 10.1016/j.bmcl.2005.09.076
CHEMBL424847 165912 None 0 Guinea pig Functional pKd = 8.6 8.6 - 0
Antagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileumAntagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileum
ChEMBL 263 8 1 2 3.6 CCCCCCCN1CCC(Cc2c[nH]cn2)CC1 10.1016/j.bmcl.2005.09.076
10475883 165850 None 0 Guinea pig Functional pKd = 8.6 8.6 - 0
Antagonistic activity against histamine H3 receptor in guinea pig ileumAntagonistic activity against histamine H3 receptor in guinea pig ileum
ChEMBL 396 9 1 4 4.1 c1nc(CC2CCN(CCCOc3ccc(CN4CCCCC4)cc3)CC2)c[nH]1 10.1016/j.bmcl.2005.10.087
CHEMBL424675 165850 None 0 Guinea pig Functional pKd = 8.6 8.6 - 0
Antagonistic activity against histamine H3 receptor in guinea pig ileumAntagonistic activity against histamine H3 receptor in guinea pig ileum
ChEMBL 396 9 1 4 4.1 c1nc(CC2CCN(CCCOc3ccc(CN4CCCCC4)cc3)CC2)c[nH]1 10.1016/j.bmcl.2005.10.087
46887993 8724 None 0 Rat Functional pKd = 8.6 8.6 - 0
Antagonist activity at rat H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at rat H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 377 4 1 4 2.5 O=C([C@H]1C[C@H](Oc2cccc(Cl)c2)CN1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.03.071
CHEMBL1095877 8724 None 0 Rat Functional pKd = 8.6 8.6 - 0
Antagonist activity at rat H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at rat H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 377 4 1 4 2.5 O=C([C@H]1C[C@H](Oc2cccc(Cl)c2)CN1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.03.071
11582342 87296 None 0 Human Functional pKd = 8.6 8.6 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 412 7 0 4 4.5 COc1ccc(C2CN(C)Cc3cc(OCCCN4CCC(F)CC4)ccc32)cc1 10.1016/j.bmcl.2006.11.036
CHEMBL233054 87296 None 0 Human Functional pKd = 8.6 8.6 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 412 7 0 4 4.5 COc1ccc(C2CN(C)Cc3cc(OCCCN4CCC(F)CC4)ccc32)cc1 10.1016/j.bmcl.2006.11.036
24964522 153123 None 0 Human Functional pKd = 8.6 8.6 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 384 6 1 4 3.9 CNCc1cc(C#CCCN2CCOCC2)ccc1Oc1cccc(Cl)c1 10.1016/j.bmcl.2007.06.061
CHEMBL397575 153123 None 0 Human Functional pKd = 8.6 8.6 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 384 6 1 4 3.9 CNCc1cc(C#CCCN2CCOCC2)ccc1Oc1cccc(Cl)c1 10.1016/j.bmcl.2007.06.061
24947750 97610 None 0 Human Functional pKd = 8.6 8.6 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 413 7 1 5 4.1 CNCc1cc(C(=O)N2CCN(C(C)C)CC2)ccc1Oc1ccc(SC)cc1 10.1016/j.bmcl.2007.11.016
CHEMBL270625 97610 None 0 Human Functional pKd = 8.6 8.6 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 413 7 1 5 4.1 CNCc1cc(C(=O)N2CCN(C(C)C)CC2)ccc1Oc1ccc(SC)cc1 10.1016/j.bmcl.2007.11.016
11624178 62691 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrs
ChEMBL 335 4 0 4 2.9 CC(C)N1CCN(C(=O)c2csc(CN3CCCCC3)c2)CC1 10.1016/j.ejmech.2009.06.007
CHEMBL1783877 62691 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrs
ChEMBL 335 4 0 4 2.9 CC(C)N1CCN(C(=O)c2csc(CN3CCCCC3)c2)CC1 10.1016/j.ejmech.2009.06.007
44439862 93777 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 410 7 0 5 3.8 COc1ccc([C@H]2CN(C)Cc3cc(OCCCN4CCOC[C@@H]4C)ccc32)cc1 10.1016/j.bmcl.2006.11.036
CHEMBL247161 93777 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 410 7 0 5 3.8 COc1ccc([C@H]2CN(C)Cc3cc(OCCCN4CCOC[C@@H]4C)ccc32)cc1 10.1016/j.bmcl.2006.11.036
24947752 155418 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 397 7 1 5 3.4 CNCc1cc(C(=O)N2CCN(C(C)C)CC2)ccc1Oc1cccc(OC)c1 10.1016/j.bmcl.2007.11.016
CHEMBL403148 155418 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 397 7 1 5 3.4 CNCc1cc(C(=O)N2CCN(C(C)C)CC2)ccc1Oc1cccc(OC)c1 10.1016/j.bmcl.2007.11.016
24771308 10788 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 362 4 0 5 3.1 N#Cc1cccc(Oc2ccc(C(=O)N3CCCN(C4CC4)CC3)cn2)c1 10.1016/j.bmcl.2010.05.041
CHEMBL1171755 10788 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 362 4 0 5 3.1 N#Cc1cccc(Oc2ccc(C(=O)N3CCCN(C4CC4)CC3)cn2)c1 10.1016/j.bmcl.2010.05.041
46888207 8678 None 0 Human Functional pKd = 7.7 7.7 - 0
Antagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 431 5 0 5 2.9 CSc1ccc(O[C@H]2C[C@@H](C(=O)N3CCCN(C4CCC4)CC3)N(C(C)=O)C2)cc1 10.1016/j.bmcl.2010.03.071
CHEMBL1095533 8678 None 0 Human Functional pKd = 7.7 7.7 - 0
Antagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at human H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 431 5 0 5 2.9 CSc1ccc(O[C@H]2C[C@@H](C(=O)N3CCCN(C4CCC4)CC3)N(C(C)=O)C2)cc1 10.1016/j.bmcl.2010.03.071
15983453 93754 None 0 Human Functional pKd = 7.7 7.7 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulationAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulation
ChEMBL 365 6 0 4 3.9 CN1Cc2cc(OCCCN3CCCCC3)ncc2C(c2ccccc2)C1 10.1016/j.bmcl.2007.02.006
CHEMBL247061 93754 None 0 Human Functional pKd = 7.7 7.7 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulationAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulation
ChEMBL 365 6 0 4 3.9 CN1Cc2cc(OCCCN3CCCCC3)ncc2C(c2ccccc2)C1 10.1016/j.bmcl.2007.02.006
44315771 207892 None 0 Guinea pig Functional pKd = 7.7 7.7 - 0
Compound was tested in vitro against histamine H3 receptor mediated inhibition of cholinergic neurogenic contractions in isolated guinea pig ileumCompound was tested in vitro against histamine H3 receptor mediated inhibition of cholinergic neurogenic contractions in isolated guinea pig ileum
ChEMBL 412 8 1 7 4.6 O=[N+]([O-])c1ccc(OCCCN2CCC(Nc3nc4ccccc4s3)CC2)cc1 10.1021/jm990952j
CHEMBL80253 207892 None 0 Guinea pig Functional pKd = 7.7 7.7 - 0
Compound was tested in vitro against histamine H3 receptor mediated inhibition of cholinergic neurogenic contractions in isolated guinea pig ileumCompound was tested in vitro against histamine H3 receptor mediated inhibition of cholinergic neurogenic contractions in isolated guinea pig ileum
ChEMBL 412 8 1 7 4.6 O=[N+]([O-])c1ccc(OCCCN2CCC(Nc3nc4ccccc4s3)CC2)cc1 10.1021/jm990952j
24825526 174514 None 0 Guinea pig Functional pKd = 5.7 5.7 - 1
Antagonist activity at guinea pig histamine H3 receptor assessed as inhibition of electrically induced twitch contractionAntagonist activity at guinea pig histamine H3 receptor assessed as inhibition of electrically induced twitch contraction
ChEMBL 317 5 1 3 3.4 c1ccc(C[C@@H]2COC(c3cccc(Cc4c[nH]cn4)c3)=N2)cc1 10.1021/jm7014149
CHEMBL455266 174514 None 0 Guinea pig Functional pKd = 5.7 5.7 - 1
Antagonist activity at guinea pig histamine H3 receptor assessed as inhibition of electrically induced twitch contractionAntagonist activity at guinea pig histamine H3 receptor assessed as inhibition of electrically induced twitch contraction
ChEMBL 317 5 1 3 3.4 c1ccc(C[C@@H]2COC(c3cccc(Cc4c[nH]cn4)c3)=N2)cc1 10.1021/jm7014149
44320685 208910 None 0 Guinea pig Functional pKd = 5.6 5.6 - 0
Compound was tested for the agonist activity against histamine H3 receptor of guinea pig ileumCompound was tested for the agonist activity against histamine H3 receptor of guinea pig ileum
ChEMBL 283 5 2 2 3.2 CCNCCc1c[nH]c(-c2cccc(C(F)(F)F)c2)n1 10.1016/s0960-894x(98)00461-2
CHEMBL88074 208910 None 0 Guinea pig Functional pKd = 5.6 5.6 - 0
Compound was tested for the agonist activity against histamine H3 receptor of guinea pig ileumCompound was tested for the agonist activity against histamine H3 receptor of guinea pig ileum
ChEMBL 283 5 2 2 3.2 CCNCCc1c[nH]c(-c2cccc(C(F)(F)F)c2)n1 10.1016/s0960-894x(98)00461-2
44408034 75141 None 0 Guinea pig Functional pKd = 7.6 7.6 - 0
Antagonistic activity against histamine H3 receptor in guinea pig ileumAntagonistic activity against histamine H3 receptor in guinea pig ileum
ChEMBL 439 10 2 5 2.8 NC(=O)C1CCN(Cc2ccc(OCCCN3CCC(Cc4c[nH]cn4)CC3)cc2)CC1 10.1016/j.bmcl.2005.10.087
CHEMBL203604 75141 None 0 Guinea pig Functional pKd = 7.6 7.6 - 0
Antagonistic activity against histamine H3 receptor in guinea pig ileumAntagonistic activity against histamine H3 receptor in guinea pig ileum
ChEMBL 439 10 2 5 2.8 NC(=O)C1CCN(Cc2ccc(OCCCN3CCC(Cc4c[nH]cn4)CC3)cc2)CC1 10.1016/j.bmcl.2005.10.087
44408055 138599 None 0 Guinea pig Functional pKd = 7.6 7.6 - 0
Antagonistic activity against histamine H3 receptor in guinea pig ileumAntagonistic activity against histamine H3 receptor in guinea pig ileum
ChEMBL 291 3 2 4 2.4 O=C(Nc1nccs1)N1CCC(Cc2c[nH]cn2)CC1 10.1016/j.bmcl.2005.10.087
CHEMBL377500 138599 None 0 Guinea pig Functional pKd = 7.6 7.6 - 0
Antagonistic activity against histamine H3 receptor in guinea pig ileumAntagonistic activity against histamine H3 receptor in guinea pig ileum
ChEMBL 291 3 2 4 2.4 O=C(Nc1nccs1)N1CCC(Cc2c[nH]cn2)CC1 10.1016/j.bmcl.2005.10.087
44408110 139311 None 0 Guinea pig Functional pKd = 7.6 7.6 - 0
Antagonistic activity against histamine H3 receptor in guinea pig ileumAntagonistic activity against histamine H3 receptor in guinea pig ileum
ChEMBL 286 3 2 4 1.7 O=C(Nc1ncccn1)N1CCC(Cc2c[nH]cn2)CC1 10.1016/j.bmcl.2005.10.087
CHEMBL378821 139311 None 0 Guinea pig Functional pKd = 7.6 7.6 - 0
Antagonistic activity against histamine H3 receptor in guinea pig ileumAntagonistic activity against histamine H3 receptor in guinea pig ileum
ChEMBL 286 3 2 4 1.7 O=C(Nc1ncccn1)N1CCC(Cc2c[nH]cn2)CC1 10.1016/j.bmcl.2005.10.087
44308676 206433 None 0 Guinea pig Functional pKd = 7.6 7.6 - 0
H3 -antagonist potency determined in electrically stimulated guinea-pig ileumH3 -antagonist potency determined in electrically stimulated guinea-pig ileum
ChEMBL 293 7 2 3 2.0 Cc1ccc(S(=O)(=O)NCCCCc2c[nH]cn2)cc1 10.1016/s0960-894x(98)00379-5
CHEMBL69456 206433 None 0 Guinea pig Functional pKd = 7.6 7.6 - 0
H3 -antagonist potency determined in electrically stimulated guinea-pig ileumH3 -antagonist potency determined in electrically stimulated guinea-pig ileum
ChEMBL 293 7 2 3 2.0 Cc1ccc(S(=O)(=O)NCCCCc2c[nH]cn2)cc1 10.1016/s0960-894x(98)00379-5
10039772 104416 None 0 Guinea pig Functional pKd = 7.6 7.6 - 0
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 288 7 3 2 3.1 S=C(NCCCCCc1c[nH]cn1)Nc1ccccc1 10.1021/jm00012a025
CHEMBL310087 104416 None 0 Guinea pig Functional pKd = 7.6 7.6 - 0
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 288 7 3 2 3.1 S=C(NCCCCCc1c[nH]cn1)Nc1ccccc1 10.1021/jm00012a025
10221184 206677 None 0 Guinea pig Functional pKd = 7.6 7.6 - 0
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 274 6 3 2 2.7 S=C(NCCCCc1c[nH]cn1)Nc1ccccc1 10.1021/jm00012a025
CHEMBL70897 206677 None 0 Guinea pig Functional pKd = 7.6 7.6 - 0
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 274 6 3 2 2.7 S=C(NCCCCc1c[nH]cn1)Nc1ccccc1 10.1021/jm00012a025
15983578 92042 None 0 Human Functional pKd = 7.6 7.6 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulationAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulation
ChEMBL 395 7 0 5 3.9 COc1cccc(C2CN(C)Cc3cc(OCCCN4CCCCC4)ncc32)c1 10.1016/j.bmcl.2007.02.006
CHEMBL241705 92042 None 0 Human Functional pKd = 7.6 7.6 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulationAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulation
ChEMBL 395 7 0 5 3.9 COc1cccc(C2CN(C)Cc3cc(OCCCN4CCCCC4)ncc32)c1 10.1016/j.bmcl.2007.02.006
44581077 193494 None 0 Rat Functional pKd = 6.6 6.6 - 0
Antagonist activity rat recombinant histamine H3 receptor expressed in human SK-N-MC cellsAntagonist activity rat recombinant histamine H3 receptor expressed in human SK-N-MC cells
ChEMBL 334 6 0 5 2.0 CC(C)N1CCOC(COc2cccc(CN3CCOCC3)c2)C1 10.1016/j.bmcl.2008.09.077
CHEMBL525376 193494 None 0 Rat Functional pKd = 6.6 6.6 - 0
Antagonist activity rat recombinant histamine H3 receptor expressed in human SK-N-MC cellsAntagonist activity rat recombinant histamine H3 receptor expressed in human SK-N-MC cells
ChEMBL 334 6 0 5 2.0 CC(C)N1CCOC(COc2cccc(CN3CCOCC3)c2)C1 10.1016/j.bmcl.2008.09.077
24771741 10725 None 0 Rat Functional pKd = 7.6 7.6 - 0
Antagonist activity at rat histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at rat histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 369 4 0 4 3.7 O=C(c1ccc(Oc2ccc(F)cc2)cn1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.05.041
CHEMBL1170953 10725 None 0 Rat Functional pKd = 7.6 7.6 - 0
Antagonist activity at rat histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at rat histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 369 4 0 4 3.7 O=C(c1ccc(Oc2ccc(F)cc2)cn1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.05.041
10546206 186265 None 0 Guinea pig Functional pKd = 7.5 7.5 - 0
In vitro histamine H3 receptor antagonist activity was determined on guinea pig jejunumIn vitro histamine H3 receptor antagonist activity was determined on guinea pig jejunum
ChEMBL 356 3 2 2 4.4 CC(C)(C)c1ccccc1C/N=C(\S)N1CCC(c2c[nH]cn2)CC1 10.1021/jm981106w
CHEMBL48724 186265 None 0 Guinea pig Functional pKd = 7.5 7.5 - 0
In vitro histamine H3 receptor antagonist activity was determined on guinea pig jejunumIn vitro histamine H3 receptor antagonist activity was determined on guinea pig jejunum
ChEMBL 356 3 2 2 4.4 CC(C)(C)c1ccccc1C/N=C(\S)N1CCC(c2c[nH]cn2)CC1 10.1021/jm981106w
441082 1163 None 35 Guinea pig Functional pKd = 6.6 6.6 - 1
Antagonist activity at histamine H3 receptor in guinea pig ileum assessed as inhibition of (R)-alpha-methylhistamine-induced responseAntagonist activity at histamine H3 receptor in guinea pig ileum assessed as inhibition of (R)-alpha-methylhistamine-induced response
ChEMBL 356 1 0 2 4.8 CN([C@H]1CC[C@]2(C(=CC[C@@H]3[C@@H]2CC[C@]24[C@H]3CC[C@@H]4[C@@H](N(C2)C)C)C1)C)C 10.1021/jm8003625
8981 1163 None 35 Guinea pig Functional pKd = 6.6 6.6 - 1
Antagonist activity at histamine H3 receptor in guinea pig ileum assessed as inhibition of (R)-alpha-methylhistamine-induced responseAntagonist activity at histamine H3 receptor in guinea pig ileum assessed as inhibition of (R)-alpha-methylhistamine-induced response
ChEMBL 356 1 0 2 4.8 CN([C@H]1CC[C@]2(C(=CC[C@@H]3[C@@H]2CC[C@]24[C@H]3CC[C@@H]4[C@@H](N(C2)C)C)C1)C)C 10.1021/jm8003625
CHEMBL191703 1163 None 35 Guinea pig Functional pKd = 6.6 6.6 - 1
Antagonist activity at histamine H3 receptor in guinea pig ileum assessed as inhibition of (R)-alpha-methylhistamine-induced responseAntagonist activity at histamine H3 receptor in guinea pig ileum assessed as inhibition of (R)-alpha-methylhistamine-induced response
ChEMBL 356 1 0 2 4.8 CN([C@H]1CC[C@]2(C(=CC[C@@H]3[C@@H]2CC[C@]24[C@H]3CC[C@@H]4[C@@H](N(C2)C)C)C1)C)C 10.1021/jm8003625
42604650 12727 None 0 Guinea pig Functional pKd = 7.5 7.5 - 0
Antagonist activity at histamine H3 receptor in guinea pig jejunum assessed as electrically evoked contractionsAntagonist activity at histamine H3 receptor in guinea pig jejunum assessed as electrically evoked contractions
ChEMBL 310 8 0 5 2.6 CCCN(C)CCc1cnc(N2CCN(CCC)CC2)s1 10.1016/j.ejmech.2008.09.019
CHEMBL1187678 12727 None 0 Guinea pig Functional pKd = 7.5 7.5 - 0
Antagonist activity at histamine H3 receptor in guinea pig jejunum assessed as electrically evoked contractionsAntagonist activity at histamine H3 receptor in guinea pig jejunum assessed as electrically evoked contractions
ChEMBL 310 8 0 5 2.6 CCCN(C)CCc1cnc(N2CCN(CCC)CC2)s1 10.1016/j.ejmech.2008.09.019
CHEMBL514976 12727 None 0 Guinea pig Functional pKd = 7.5 7.5 - 0
Antagonist activity at histamine H3 receptor in guinea pig jejunum assessed as electrically evoked contractionsAntagonist activity at histamine H3 receptor in guinea pig jejunum assessed as electrically evoked contractions
ChEMBL 310 8 0 5 2.6 CCCN(C)CCc1cnc(N2CCN(CCC)CC2)s1 10.1016/j.ejmech.2008.09.019
44581059 187999 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human recombinant histamine H3 receptor expressed in human SK-N-MC cellsAntagonist activity at human recombinant histamine H3 receptor expressed in human SK-N-MC cells
ChEMBL 346 6 0 5 2.2 c1cc(OCC2CN(C3CCC3)CCO2)ccc1CN1CCOCC1 10.1016/j.bmcl.2008.09.077
CHEMBL496554 187999 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human recombinant histamine H3 receptor expressed in human SK-N-MC cellsAntagonist activity at human recombinant histamine H3 receptor expressed in human SK-N-MC cells
ChEMBL 346 6 0 5 2.2 c1cc(OCC2CN(C3CCC3)CCO2)ccc1CN1CCOCC1 10.1016/j.bmcl.2008.09.077
46887995 8942 None 0 Rat Functional pKd = 8.5 8.5 - 0
Antagonist activity at rat H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at rat H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 382 4 1 5 2.1 N#Cc1ccc(O[C@@H]2CN[C@@H](C(=O)N3CCCN(C4CCCC4)CC3)C2)cc1 10.1016/j.bmcl.2010.03.071
CHEMBL1097883 8942 None 0 Rat Functional pKd = 8.5 8.5 - 0
Antagonist activity at rat H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at rat H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 382 4 1 5 2.1 N#Cc1ccc(O[C@@H]2CN[C@@H](C(=O)N3CCCN(C4CCCC4)CC3)C2)cc1 10.1016/j.bmcl.2010.03.071
25062200 18367 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity against human histamine H3 receptorAntagonist activity against human histamine H3 receptor
ChEMBL 446 5 0 6 2.6 CC(C)N1CCN(C(=O)c2ccc3c(CN4CCCCC4)cn(S(C)(=O)=O)c3c2)CC1 10.1016/j.bmcl.2010.08.103
CHEMBL1271072 18367 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity against human histamine H3 receptorAntagonist activity against human histamine H3 receptor
ChEMBL 446 5 0 6 2.6 CC(C)N1CCN(C(=O)c2ccc3c(CN4CCCCC4)cn(S(C)(=O)=O)c3c2)CC1 10.1016/j.bmcl.2010.08.103
49864989 15800 None 0 Guinea pig Functional pKd = 8.5 8.5 - 0
Antagonist activity at histamine H3 receptor in electrically-stimulated guinea pig ileumAntagonist activity at histamine H3 receptor in electrically-stimulated guinea pig ileum
ChEMBL 505 9 0 7 3.7 CCOCCCn1c(=O)n(C2CCN(C(=O)C3CCN(Cc4ccncc4)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2010.07.052
CHEMBL1222799 15800 None 0 Guinea pig Functional pKd = 8.5 8.5 - 0
Antagonist activity at histamine H3 receptor in electrically-stimulated guinea pig ileumAntagonist activity at histamine H3 receptor in electrically-stimulated guinea pig ileum
ChEMBL 505 9 0 7 3.7 CCOCCCn1c(=O)n(C2CCN(C(=O)C3CCN(Cc4ccncc4)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2010.07.052
44441089 93379 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 432 6 0 6 3.7 c1ccn2c([C@@H]3CN4CCC[C@@H]4c4cc(OCCCN5CCOCC5)ccc43)cnc2c1 10.1016/j.bmcl.2007.03.043
CHEMBL245294 93379 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 432 6 0 6 3.7 c1ccn2c([C@@H]3CN4CCC[C@@H]4c4cc(OCCCN5CCOCC5)ccc43)cnc2c1 10.1016/j.bmcl.2007.03.043
44441077 93679 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 396 6 0 4 5.3 c1csc([C@@H]2CN3CCC[C@@H]3c3cc(OCCCN4CCCCC4)ccc32)c1 10.1016/j.bmcl.2007.03.043
CHEMBL246716 93679 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 396 6 0 4 5.3 c1csc([C@@H]2CN3CCC[C@@H]3c3cc(OCCCN4CCCCC4)ccc32)c1 10.1016/j.bmcl.2007.03.043
16005497 93722 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 458 7 0 6 4.3 c1cn(-c2ccc([C@@H]3CN4CCC[C@@H]4c4cc(OCCCN5CCOCC5)ccc43)cc2)cn1 10.1016/j.bmcl.2007.03.043
CHEMBL246913 93722 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 458 7 0 6 4.3 c1cn(-c2ccc([C@@H]3CN4CCC[C@@H]4c4cc(OCCCN5CCOCC5)ccc43)cc2)cn1 10.1016/j.bmcl.2007.03.043
44441079 93728 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 398 6 0 5 4.1 c1csc([C@@H]2CN3CCC[C@@H]3c3cc(OCCCN4CCOCC4)ccc32)c1 10.1016/j.bmcl.2007.03.043
CHEMBL246927 93728 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 398 6 0 5 4.1 c1csc([C@@H]2CN3CCC[C@@H]3c3cc(OCCCN4CCOCC4)ccc32)c1 10.1016/j.bmcl.2007.03.043
44441084 93770 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 399 6 0 6 3.5 c1ncc([C@@H]2CN3CCC[C@@H]3c3cc(OCCCN4CCOCC4)ccc32)s1 10.1016/j.bmcl.2007.03.043
CHEMBL247136 93770 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 399 6 0 6 3.5 c1ncc([C@@H]2CN3CCC[C@@H]3c3cc(OCCCN4CCOCC4)ccc32)s1 10.1016/j.bmcl.2007.03.043
44441073 93809 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 393 6 0 5 3.5 c1ccc([C@@H]2CN3CCC[C@@H]3c3cc(OCCCN4CCOCC4)ccc32)nc1 10.1016/j.bmcl.2007.03.043
CHEMBL247335 93809 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 393 6 0 5 3.5 c1ccc([C@@H]2CN3CCC[C@@H]3c3cc(OCCCN4CCOCC4)ccc32)nc1 10.1016/j.bmcl.2007.03.043
44441067 93918 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 391 6 0 4 4.6 c1cncc([C@@H]2CN3CCC[C@@H]3c3cc(OCCCN4CCCCC4)ccc32)c1 10.1016/j.bmcl.2007.03.043
CHEMBL247933 93918 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 391 6 0 4 4.6 c1cncc([C@@H]2CN3CCC[C@@H]3c3cc(OCCCN4CCCCC4)ccc32)c1 10.1016/j.bmcl.2007.03.043
44441071 93919 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 391 6 0 4 4.6 c1ccc([C@@H]2CN3CCC[C@@H]3c3cc(OCCCN4CCCCC4)ccc32)nc1 10.1016/j.bmcl.2007.03.043
CHEMBL247935 93919 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 391 6 0 4 4.6 c1ccc([C@@H]2CN3CCC[C@@H]3c3cc(OCCCN4CCCCC4)ccc32)nc1 10.1016/j.bmcl.2007.03.043
44441085 146060 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 399 6 0 6 3.5 c1csc([C@@H]2CN3CCC[C@@H]3c3cc(OCCCN4CCOCC4)ccc32)n1 10.1016/j.bmcl.2007.03.043
CHEMBL391829 146060 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 399 6 0 6 3.5 c1csc([C@@H]2CN3CCC[C@@H]3c3cc(OCCCN4CCOCC4)ccc32)n1 10.1016/j.bmcl.2007.03.043
44441058 146521 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 458 7 0 6 4.3 c1cnn(-c2ccc([C@@H]3CN4CCC[C@@H]4c4cc(OCCCN5CCOCC5)ccc43)cc2)c1 10.1016/j.bmcl.2007.03.043
CHEMBL392196 146521 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 458 7 0 6 4.3 c1cnn(-c2ccc([C@@H]3CN4CCC[C@@H]4c4cc(OCCCN5CCOCC5)ccc43)cc2)c1 10.1016/j.bmcl.2007.03.043
16006719 148374 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 391 6 0 4 4.6 c1cc([C@@H]2CN3CCC[C@@H]3c3cc(OCCCN4CCCCC4)ccc32)ccn1 10.1016/j.bmcl.2007.03.043
CHEMBL393669 148374 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 391 6 0 4 4.6 c1cc([C@@H]2CN3CCC[C@@H]3c3cc(OCCCN4CCCCC4)ccc32)ccn1 10.1016/j.bmcl.2007.03.043
16006612 149984 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 396 6 0 4 5.3 c1cc([C@@H]2CN3CCC[C@@H]3c3cc(OCCCN4CCCCC4)ccc32)cs1 10.1016/j.bmcl.2007.03.043
CHEMBL394928 149984 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 396 6 0 4 5.3 c1cc([C@@H]2CN3CCC[C@@H]3c3cc(OCCCN4CCCCC4)ccc32)cs1 10.1016/j.bmcl.2007.03.043
44441088 153149 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 382 6 1 5 2.8 c1cc([C@@H]2CN3CCC[C@@H]3c3cc(OCCCN4CCOCC4)ccc32)[nH]n1 10.1016/j.bmcl.2007.03.043
CHEMBL397597 153149 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 382 6 1 5 2.8 c1cc([C@@H]2CN3CCC[C@@H]3c3cc(OCCCN4CCOCC4)ccc32)[nH]n1 10.1016/j.bmcl.2007.03.043
16005500 153212 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 394 6 0 6 2.9 c1cnc([C@@H]2CN3CCC[C@@H]3c3cc(OCCCN4CCOCC4)ccc32)cn1 10.1016/j.bmcl.2007.03.043
CHEMBL397643 153212 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 394 6 0 6 2.9 c1cnc([C@@H]2CN3CCC[C@@H]3c3cc(OCCCN4CCOCC4)ccc32)cn1 10.1016/j.bmcl.2007.03.043
44441083 169129 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 398 6 0 5 4.1 c1cc([C@@H]2CN3CCC[C@@H]3c3cc(OCCCN4CCOCC4)ccc32)cs1 10.1016/j.bmcl.2007.03.043
CHEMBL439389 169129 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 398 6 0 5 4.1 c1cc([C@@H]2CN3CCC[C@@H]3c3cc(OCCCN4CCOCC4)ccc32)cs1 10.1016/j.bmcl.2007.03.043
44441070 169148 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 393 6 0 5 3.5 c1cncc([C@@H]2CN3CCC[C@@H]3c3cc(OCCCN4CCOCC4)ccc32)c1 10.1016/j.bmcl.2007.03.043
CHEMBL439561 169148 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 393 6 0 5 3.5 c1cncc([C@@H]2CN3CCC[C@@H]3c3cc(OCCCN4CCOCC4)ccc32)c1 10.1016/j.bmcl.2007.03.043
9923762 192723 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-NM-C cellsAntagonist activity at human histamine H3 receptor expressed in SK-NM-C cells
ChEMBL 334 6 0 3 4.9 c1ccn2cc(-c3ccc(OCCCN4CCCCC4)cc3)cc2c1 10.1016/j.ejmech.2011.08.042
CHEMBL52160 192723 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-NM-C cellsAntagonist activity at human histamine H3 receptor expressed in SK-NM-C cells
ChEMBL 334 6 0 3 4.9 c1ccn2cc(-c3ccc(OCCCN4CCCCC4)cc3)cc2c1 10.1016/j.ejmech.2011.08.042
44408036 75960 None 0 Guinea pig Functional pKd = 8.5 8.5 - 0
Antagonistic activity against histamine H3 receptor in guinea pig ileumAntagonistic activity against histamine H3 receptor in guinea pig ileum
ChEMBL 410 10 1 4 4.2 c1nc(CC2CCN(CCCOc3ccc(CCN4CCCCC4)cc3)CC2)c[nH]1 10.1016/j.bmcl.2005.10.087
CHEMBL205129 75960 None 0 Guinea pig Functional pKd = 8.5 8.5 - 0
Antagonistic activity against histamine H3 receptor in guinea pig ileumAntagonistic activity against histamine H3 receptor in guinea pig ileum
ChEMBL 410 10 1 4 4.2 c1nc(CC2CCN(CCCOc3ccc(CCN4CCCCC4)cc3)CC2)c[nH]1 10.1016/j.bmcl.2005.10.087
10193234 200387 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation treated 10 min before histamine challengeAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation treated 10 min before histamine challenge
ChEMBL 312 4 0 3 2.7 C(#Cc1ccc(CN2CCOCC2)cc1)CCN1CCCCC1 10.1016/j.ejmech.2009.04.049
CHEMBL573090 200387 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation treated 10 min before histamine challengeAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation treated 10 min before histamine challenge
ChEMBL 312 4 0 3 2.7 C(#Cc1ccc(CN2CCOCC2)cc1)CCN1CCCCC1 10.1016/j.ejmech.2009.04.049
23275970 208885 None 0 Guinea pig Functional pKd = 8.5 8.5 - 0
Histamine H3-antagonist potency on electrically stimulated guinea pig ileumHistamine H3-antagonist potency on electrically stimulated guinea pig ileum
ChEMBL 315 6 2 5 3.0 O=[N+]([O-])c1cccc(-c2c[nH]c(SCCc3c[nH]cn3)n2)c1 10.1021/jm970070p
CHEMBL87911 208885 None 0 Guinea pig Functional pKd = 8.5 8.5 - 0
Histamine H3-antagonist potency on electrically stimulated guinea pig ileumHistamine H3-antagonist potency on electrically stimulated guinea pig ileum
ChEMBL 315 6 2 5 3.0 O=[N+]([O-])c1cccc(-c2c[nH]c(SCCc3c[nH]cn3)n2)c1 10.1021/jm970070p
24964163 89218 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 368 6 1 4 3.4 CNCc1cc(C#CCCN2CCOCC2)ccc1Oc1cccc(F)c1 10.1016/j.bmcl.2007.06.061
CHEMBL236674 89218 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 368 6 1 4 3.4 CNCc1cc(C#CCCN2CCOCC2)ccc1Oc1cccc(F)c1 10.1016/j.bmcl.2007.06.061
15983703 92044 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulationAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulation
ChEMBL 383 6 0 4 4.1 CN1Cc2cc(OCCCN3CCCCC3)ncc2C(c2ccc(F)cc2)C1 10.1016/j.bmcl.2007.02.006
CHEMBL241712 92044 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulationAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulation
ChEMBL 383 6 0 4 4.1 CN1Cc2cc(OCCCN3CCCCC3)ncc2C(c2ccc(F)cc2)C1 10.1016/j.bmcl.2007.02.006
15981911 93873 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulationAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulation
ChEMBL 395 6 1 5 3.8 COc1ccc(C2CNCc3cc(OCC4CCN(C(C)C)CC4)ncc32)cc1 10.1016/j.bmcl.2007.02.006
CHEMBL247670 93873 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulationAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulation
ChEMBL 395 6 1 5 3.8 COc1ccc(C2CNCc3cc(OCC4CCN(C(C)C)CC4)ncc32)cc1 10.1016/j.bmcl.2007.02.006
24771368 10787 None 12 Rat Functional pKd = 8.5 8.5 - 0
Antagonist activity at rat histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at rat histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 369 4 0 4 3.7 O=C(c1ccc(Oc2ccc(F)cc2)nc1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.05.041
CHEMBL1171754 10787 None 12 Rat Functional pKd = 8.5 8.5 - 0
Antagonist activity at rat histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at rat histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 369 4 0 4 3.7 O=C(c1ccc(Oc2ccc(F)cc2)nc1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.05.041
1267 3804 None 32 Guinea pig Functional pKd = 8.4 8.4 - 5
Antagonist activity at histamine H3 receptor in guinea pig ileum assessed as inhibition of (R)-alpha-methylhistamine-induced responseAntagonist activity at histamine H3 receptor in guinea pig ileum assessed as inhibition of (R)-alpha-methylhistamine-induced response
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm8003625
3035905 3804 None 32 Guinea pig Functional pKd = 8.4 8.4 - 5
Antagonist activity at histamine H3 receptor in guinea pig ileum assessed as inhibition of (R)-alpha-methylhistamine-induced responseAntagonist activity at histamine H3 receptor in guinea pig ileum assessed as inhibition of (R)-alpha-methylhistamine-induced response
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm8003625
CHEMBL260374 3804 None 32 Guinea pig Functional pKd = 8.4 8.4 - 5
Antagonist activity at histamine H3 receptor in guinea pig ileum assessed as inhibition of (R)-alpha-methylhistamine-induced responseAntagonist activity at histamine H3 receptor in guinea pig ileum assessed as inhibition of (R)-alpha-methylhistamine-induced response
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm8003625
11582342 87296 None 0 Human Functional pKd = 8.4 8.4 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 412 7 0 4 4.5 COc1ccc(C2CN(C)Cc3cc(OCCCN4CCC(F)CC4)ccc32)cc1 10.1016/j.bmcl.2006.11.036
CHEMBL233054 87296 None 0 Human Functional pKd = 8.4 8.4 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 412 7 0 4 4.5 COc1ccc(C2CN(C)Cc3cc(OCCCN4CCC(F)CC4)ccc32)cc1 10.1016/j.bmcl.2006.11.036
24771416 10727 None 0 Rat Functional pKd = 8.4 8.4 - 0
Antagonist activity at rat histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at rat histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 351 4 0 4 3.6 O=C(c1ccc(Oc2ccccc2)nc1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.05.041
CHEMBL1170999 10727 None 0 Rat Functional pKd = 8.4 8.4 - 0
Antagonist activity at rat histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at rat histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 351 4 0 4 3.6 O=C(c1ccc(Oc2ccccc2)nc1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.05.041
15983708 93713 None 0 Human Functional pKd = 8.4 8.4 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulationAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulation
ChEMBL 385 6 1 4 4.2 Clc1ccc(C2CNCc3cc(OCCCN4CCCCC4)ncc32)cc1 10.1016/j.bmcl.2007.02.006
CHEMBL246873 93713 None 0 Human Functional pKd = 8.4 8.4 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulationAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as effect on cAMP accumulation
ChEMBL 385 6 1 4 4.2 Clc1ccc(C2CNCc3cc(OCCCN4CCCCC4)ncc32)cc1 10.1016/j.bmcl.2007.02.006
24825522 187749 None 0 Guinea pig Functional pKd = 8.4 8.4 - 1
Antagonist activity at guinea pig histamine H3 receptor assessed as inhibition of electrically induced twitch contractionAntagonist activity at guinea pig histamine H3 receptor assessed as inhibition of electrically induced twitch contraction
ChEMBL 283 3 1 3 3.3 CC1CC(C)(C)N=C(c2cccc(Cc3c[nH]cn3)c2)O1 10.1021/jm7014149
CHEMBL494982 187749 None 0 Guinea pig Functional pKd = 8.4 8.4 - 1
Antagonist activity at guinea pig histamine H3 receptor assessed as inhibition of electrically induced twitch contractionAntagonist activity at guinea pig histamine H3 receptor assessed as inhibition of electrically induced twitch contraction
ChEMBL 283 3 1 3 3.3 CC1CC(C)(C)N=C(c2cccc(Cc3c[nH]cn3)c2)O1 10.1021/jm7014149
15986917 91240 None 0 Guinea pig Functional pKd = 8.4 8.4 - 0
Antagonist activity at histamine H3 receptor in guinea pig ileum assessed as inhibition of (R)-methyl histamine induced longitudinal smooth muscle contractionAntagonist activity at histamine H3 receptor in guinea pig ileum assessed as inhibition of (R)-methyl histamine induced longitudinal smooth muscle contraction
ChEMBL 439 7 0 4 3.6 O=C(c1ccc(F)cc1)N1CCN(c2ccc(OCCCN3CCCCC3)cc2)C(=O)C1 10.1021/jm0708228
CHEMBL239975 91240 None 0 Guinea pig Functional pKd = 8.4 8.4 - 0
Antagonist activity at histamine H3 receptor in guinea pig ileum assessed as inhibition of (R)-methyl histamine induced longitudinal smooth muscle contractionAntagonist activity at histamine H3 receptor in guinea pig ileum assessed as inhibition of (R)-methyl histamine induced longitudinal smooth muscle contraction
ChEMBL 439 7 0 4 3.6 O=C(c1ccc(F)cc1)N1CCN(c2ccc(OCCCN3CCCCC3)cc2)C(=O)C1 10.1021/jm0708228
CHEMBL240185 91240 None 0 Guinea pig Functional pKd = 8.4 8.4 - 0
Antagonist activity at histamine H3 receptor in guinea pig ileum assessed as inhibition of (R)-methyl histamine induced longitudinal smooth muscle contractionAntagonist activity at histamine H3 receptor in guinea pig ileum assessed as inhibition of (R)-methyl histamine induced longitudinal smooth muscle contraction
ChEMBL 439 7 0 4 3.6 O=C(c1ccc(F)cc1)N1CCN(c2ccc(OCCCN3CCCCC3)cc2)C(=O)C1 10.1021/jm0708228
44570656 183736 None 0 Human Functional pKd = 8.4 8.4 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 339 7 1 5 3.2 CN(C)CCCSc1ncc(C(O)c2ccc(Cl)cc2)n1C 10.1016/j.bmcl.2008.11.114
CHEMBL480245 183736 None 0 Human Functional pKd = 8.4 8.4 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 339 7 1 5 3.2 CN(C)CCCSc1ncc(C(O)c2ccc(Cl)cc2)n1C 10.1016/j.bmcl.2008.11.114
10291633 184166 None 0 Human Functional pKd = 8.4 8.4 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 352 7 1 6 3.3 CN(C)CCCSc1ncc(/C(=N\O)c2ccc(Cl)cc2)n1C 10.1016/j.bmcl.2008.11.114
CHEMBL482306 184166 None 0 Human Functional pKd = 8.4 8.4 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 352 7 1 6 3.3 CN(C)CCCSc1ncc(/C(=N\O)c2ccc(Cl)cc2)n1C 10.1016/j.bmcl.2008.11.114
24771420 10804 None 0 Rat Functional pKd = 8.4 8.4 - 0
Antagonist activity at rat histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at rat histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 385 4 0 4 4.2 O=C(c1ccc(Oc2ccc(Cl)cc2)nc1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.05.041
CHEMBL1171886 10804 None 0 Rat Functional pKd = 8.4 8.4 - 0
Antagonist activity at rat histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at rat histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 385 4 0 4 4.2 O=C(c1ccc(Oc2ccc(Cl)cc2)nc1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.05.041
44406394 72986 None 0 Guinea pig Functional pKd = 8.4 8.4 - 0
Antagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileumAntagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileum
ChEMBL 332 7 2 3 3.8 Clc1cccc(NCCCN2CCC(Cc3c[nH]cn3)CC2)c1 10.1016/j.bmcl.2005.09.076
CHEMBL200643 72986 None 0 Guinea pig Functional pKd = 8.4 8.4 - 0
Antagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileumAntagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileum
ChEMBL 332 7 2 3 3.8 Clc1cccc(NCCCN2CCC(Cc3c[nH]cn3)CC2)c1 10.1016/j.bmcl.2005.09.076
44408021 140317 None 0 Guinea pig Functional pKd = 8.4 8.4 - 0
Antagonistic activity against histamine H3 receptor in guinea pig ileumAntagonistic activity against histamine H3 receptor in guinea pig ileum
ChEMBL 396 9 1 4 4.1 c1cc(CN2CCCCC2)cc(OCCCN2CCC(Cc3c[nH]cn3)CC2)c1 10.1016/j.bmcl.2005.10.087
CHEMBL380525 140317 None 0 Guinea pig Functional pKd = 8.4 8.4 - 0
Antagonistic activity against histamine H3 receptor in guinea pig ileumAntagonistic activity against histamine H3 receptor in guinea pig ileum
ChEMBL 396 9 1 4 4.1 c1cc(CN2CCCCC2)cc(OCCCN2CCC(Cc3c[nH]cn3)CC2)c1 10.1016/j.bmcl.2005.10.087
44308793 206799 None 0 Guinea pig Functional pKd = 8.4 8.4 - 0
H3 -antagonist potency determined in electrically stimulated guinea-pig ileumH3 -antagonist potency determined in electrically stimulated guinea-pig ileum
ChEMBL 347 7 2 3 2.7 O=S(=O)(NCCCCc1c[nH]cn1)c1ccc(C(F)(F)F)cc1 10.1016/s0960-894x(98)00379-5
CHEMBL71592 206799 None 0 Guinea pig Functional pKd = 8.4 8.4 - 0
H3 -antagonist potency determined in electrically stimulated guinea-pig ileumH3 -antagonist potency determined in electrically stimulated guinea-pig ileum
ChEMBL 347 7 2 3 2.7 O=S(=O)(NCCCCc1c[nH]cn1)c1ccc(C(F)(F)F)cc1 10.1016/s0960-894x(98)00379-5
1252 2017 None 16 Guinea pig Functional pKd = 8.4 8.4 - 1
Tested in vitro for antagonist activity against H3 receptor of guinea pig jejunum.Tested in vitro for antagonist activity against H3 receptor of guinea pig jejunum.
ChEMBL 153 5 2 2 1.1 NCCCCCc1cnc[nH]1 10.1021/jm00002a008
9793868 2017 None 16 Guinea pig Functional pKd = 8.4 8.4 - 1
Tested in vitro for antagonist activity against H3 receptor of guinea pig jejunum.Tested in vitro for antagonist activity against H3 receptor of guinea pig jejunum.
ChEMBL 153 5 2 2 1.1 NCCCCCc1cnc[nH]1 10.1021/jm00002a008
CHEMBL417096 2017 None 16 Guinea pig Functional pKd = 8.4 8.4 - 1
Tested in vitro for antagonist activity against H3 receptor of guinea pig jejunum.Tested in vitro for antagonist activity against H3 receptor of guinea pig jejunum.
ChEMBL 153 5 2 2 1.1 NCCCCCc1cnc[nH]1 10.1021/jm00002a008
10060213 102966 None 0 Guinea pig Functional pKd = 7.5 7.5 - 1
Agonist activity at histamine H3 receptor in guinea pig ileumAgonist activity at histamine H3 receptor in guinea pig ileum
ChEMBL 240 6 3 2 2.0 CC(C)/N=C(\S)NCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL306077 102966 None 0 Guinea pig Functional pKd = 7.5 7.5 - 1
Agonist activity at histamine H3 receptor in guinea pig ileumAgonist activity at histamine H3 receptor in guinea pig ileum
ChEMBL 240 6 3 2 2.0 CC(C)/N=C(\S)NCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
9835305 140796 None 0 Guinea pig Functional pKd = 7.5 7.5 - 0
Antagonistic activity against histamine H3 receptor in guinea pig ileumAntagonistic activity against histamine H3 receptor in guinea pig ileum
ChEMBL 276 7 0 3 3.0 CN(C)CCCOc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2005.10.087
CHEMBL381717 140796 None 0 Guinea pig Functional pKd = 7.5 7.5 - 0
Antagonistic activity against histamine H3 receptor in guinea pig ileumAntagonistic activity against histamine H3 receptor in guinea pig ileum
ChEMBL 276 7 0 3 3.0 CN(C)CCCOc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2005.10.087
44308914 206445 None 1 Guinea pig Functional pKd = 7.5 7.5 - 0
H3 -antagonist potency determined in electrically stimulated guinea-pig ileumH3 -antagonist potency determined in electrically stimulated guinea-pig ileum
ChEMBL 279 7 2 3 1.7 O=S(=O)(NCCCCc1c[nH]cn1)c1ccccc1 10.1016/s0960-894x(98)00379-5
CHEMBL69551 206445 None 1 Guinea pig Functional pKd = 7.5 7.5 - 0
H3 -antagonist potency determined in electrically stimulated guinea-pig ileumH3 -antagonist potency determined in electrically stimulated guinea-pig ileum
ChEMBL 279 7 2 3 1.7 O=S(=O)(NCCCCc1c[nH]cn1)c1ccccc1 10.1016/s0960-894x(98)00379-5
44308825 206456 None 0 Guinea pig Functional pKd = 7.5 7.5 - 0
H3 -antagonist potency determined in electrically stimulated guinea-pig ileumH3 -antagonist potency determined in electrically stimulated guinea-pig ileum
ChEMBL 293 8 2 3 1.9 O=S(=O)(Cc1ccccc1)NCCCCc1c[nH]cn1 10.1016/s0960-894x(98)00379-5
CHEMBL69594 206456 None 0 Guinea pig Functional pKd = 7.5 7.5 - 0
H3 -antagonist potency determined in electrically stimulated guinea-pig ileumH3 -antagonist potency determined in electrically stimulated guinea-pig ileum
ChEMBL 293 8 2 3 1.9 O=S(=O)(Cc1ccccc1)NCCCCc1c[nH]cn1 10.1016/s0960-894x(98)00379-5
11723317 102949 None 0 Guinea pig Functional pKd = 7.5 7.5 - 0
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 316 9 3 2 2.8 S=C(NCCCCCc1c[nH]cn1)NCCc1ccccc1 10.1021/jm00012a025
CHEMBL305929 102949 None 0 Guinea pig Functional pKd = 7.5 7.5 - 0
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 316 9 3 2 2.8 S=C(NCCCCCc1c[nH]cn1)NCCc1ccccc1 10.1021/jm00012a025
10060213 102966 None 0 Guinea pig Functional pKd = 7.5 7.5 - 1
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 240 6 3 2 2.0 CC(C)/N=C(\S)NCCCCc1c[nH]cn1 10.1021/jm00012a025
CHEMBL306077 102966 None 0 Guinea pig Functional pKd = 7.5 7.5 - 1
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 240 6 3 2 2.0 CC(C)/N=C(\S)NCCCCc1c[nH]cn1 10.1021/jm00012a025
10085839 206960 None 0 Guinea pig Functional pKd = 7.5 7.5 - 0
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 294 7 3 2 2.9 S=C(NCCCCCc1c[nH]cn1)NC1CCCCC1 10.1021/jm00012a025
CHEMBL72571 206960 None 0 Guinea pig Functional pKd = 7.5 7.5 - 0
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 294 7 3 2 2.9 S=C(NCCCCCc1c[nH]cn1)NC1CCCCC1 10.1021/jm00012a025
11183143 11340 None 0 Guinea pig Functional pKd = 6.5 6.5 - 0
Functional Histamine H3 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H3 receptor antagonistic activity in vitro assay on guinea pig ileum
ChEMBL 192 7 1 2 1.8 C#CCCCOCCCc1c[nH]cn1 10.1021/jm031065q
CHEMBL1179592 11340 None 0 Guinea pig Functional pKd = 6.5 6.5 - 0
Functional Histamine H3 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H3 receptor antagonistic activity in vitro assay on guinea pig ileum
ChEMBL 192 7 1 2 1.8 C#CCCCOCCCc1c[nH]cn1 10.1021/jm031065q
CHEMBL88256 11340 None 0 Guinea pig Functional pKd = 6.5 6.5 - 0
Functional Histamine H3 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H3 receptor antagonistic activity in vitro assay on guinea pig ileum
ChEMBL 192 7 1 2 1.8 C#CCCCOCCCc1c[nH]cn1 10.1021/jm031065q
10397487 103706 None 8 Guinea pig Functional pKd = 5.5 5.5 - 0
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 184 3 3 2 0.5 C/N=C(\S)NCCc1c[nH]cn1 10.1021/jm00012a025
CHEMBL308729 103706 None 8 Guinea pig Functional pKd = 5.5 5.5 - 0
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 184 3 3 2 0.5 C/N=C(\S)NCCc1c[nH]cn1 10.1021/jm00012a025
11690966 93638 None 0 Human Functional pKd = 7.5 7.5 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 450 6 0 3 5.8 CN1Cc2cc(OCCCN3CCC(F)CC3)ccc2C(c2ccc(Cl)c(Cl)c2)C1 10.1016/j.bmcl.2006.11.036
CHEMBL246540 93638 None 0 Human Functional pKd = 7.5 7.5 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 450 6 0 3 5.8 CN1Cc2cc(OCCCN3CCC(F)CC3)ccc2C(c2ccc(Cl)c(Cl)c2)C1 10.1016/j.bmcl.2006.11.036
10667411 100306 None 0 Guinea pig Functional pKd = 7.5 7.5 - 0
In vitro histamine H3 receptor antagonist activity was determined on guinea pig jejunumIn vitro histamine H3 receptor antagonist activity was determined on guinea pig jejunum
ChEMBL 378 3 2 2 3.4 S=C(NCc1cccc(Br)c1)N1CCC(c2c[nH]cn2)CC1 10.1021/jm981106w
CHEMBL288757 100306 None 0 Guinea pig Functional pKd = 7.5 7.5 - 0
In vitro histamine H3 receptor antagonist activity was determined on guinea pig jejunumIn vitro histamine H3 receptor antagonist activity was determined on guinea pig jejunum
ChEMBL 378 3 2 2 3.4 S=C(NCc1cccc(Br)c1)N1CCC(c2c[nH]cn2)CC1 10.1021/jm981106w
10714725 102072 None 0 Guinea pig Functional pKd = 6.5 6.5 - 0
In vitro histamine H3 receptor antagonist activity was determined on guinea pig jejunumIn vitro histamine H3 receptor antagonist activity was determined on guinea pig jejunum
ChEMBL 378 3 2 2 3.4 S=C(NCc1ccc(Br)cc1)N1CCC(c2c[nH]cn2)CC1 10.1021/jm981106w
CHEMBL301712 102072 None 0 Guinea pig Functional pKd = 6.5 6.5 - 0
In vitro histamine H3 receptor antagonist activity was determined on guinea pig jejunumIn vitro histamine H3 receptor antagonist activity was determined on guinea pig jejunum
ChEMBL 378 3 2 2 3.4 S=C(NCc1ccc(Br)cc1)N1CCC(c2c[nH]cn2)CC1 10.1021/jm981106w
10495797 187845 None 0 Guinea pig Functional pKd = 6.4 6.4 - 0
In vitro histamine H3 receptor antagonist activity was determined on guinea pig jejunumIn vitro histamine H3 receptor antagonist activity was determined on guinea pig jejunum
ChEMBL 318 3 2 2 3.2 Fc1cccc(C/N=C(\S)N2CCC(c3c[nH]cn3)CC2)c1 10.1021/jm981106w
CHEMBL49554 187845 None 0 Guinea pig Functional pKd = 6.4 6.4 - 0
In vitro histamine H3 receptor antagonist activity was determined on guinea pig jejunumIn vitro histamine H3 receptor antagonist activity was determined on guinea pig jejunum
ChEMBL 318 3 2 2 3.2 Fc1cccc(C/N=C(\S)N2CCC(c3c[nH]cn3)CC2)c1 10.1021/jm981106w
10806686 184989 None 0 Guinea pig Functional pKd = 7.4 7.4 - 0
In vitro histamine H3 receptor antagonist activity was determined on guinea pig jejunumIn vitro histamine H3 receptor antagonist activity was determined on guinea pig jejunum
ChEMBL 334 3 2 2 3.3 S=C(NCc1cccc(Cl)c1)N1CCC(c2c[nH]cn2)CC1 10.1021/jm981106w
CHEMBL48528 184989 None 0 Guinea pig Functional pKd = 7.4 7.4 - 0
In vitro histamine H3 receptor antagonist activity was determined on guinea pig jejunumIn vitro histamine H3 receptor antagonist activity was determined on guinea pig jejunum
ChEMBL 334 3 2 2 3.3 S=C(NCc1cccc(Cl)c1)N1CCC(c2c[nH]cn2)CC1 10.1021/jm981106w
10105117 104250 None 0 Guinea pig Functional pKd = 7.4 7.4 - 1
Agonist activity at histamine H3 receptor in guinea pig ileumAgonist activity at histamine H3 receptor in guinea pig ileum
ChEMBL 226 6 3 2 1.6 CC/N=C(\S)NCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL309819 104250 None 0 Guinea pig Functional pKd = 7.4 7.4 - 1
Agonist activity at histamine H3 receptor in guinea pig ileumAgonist activity at histamine H3 receptor in guinea pig ileum
ChEMBL 226 6 3 2 1.6 CC/N=C(\S)NCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
11602952 179859 None 0 Human Functional pKd = 7.4 7.4 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 360 7 1 5 3.6 Cn1c(C(=O)c2ccc(Cl)cc2)cnc1NCCCN1CCCCC1 10.1016/j.bmcl.2008.11.114
CHEMBL474430 179859 None 0 Human Functional pKd = 7.4 7.4 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 360 7 1 5 3.6 Cn1c(C(=O)c2ccc(Cl)cc2)cnc1NCCCN1CCCCC1 10.1016/j.bmcl.2008.11.114
10314270 102595 None 0 Human Functional pKd = 7.4 7.4 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 325 6 2 3 4.0 N=C(NCc1ccc(Cl)cc1)SCCCN1CCCCC1 10.1016/j.bmcl.2013.09.052
CHEMBL2441935 102595 None 0 Human Functional pKd = 7.4 7.4 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 325 6 2 3 4.0 N=C(NCc1ccc(Cl)cc1)SCCCN1CCCCC1 10.1016/j.bmcl.2013.09.052
CHEMBL3040654 102595 None 0 Human Functional pKd = 7.4 7.4 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 325 6 2 3 4.0 N=C(NCc1ccc(Cl)cc1)SCCCN1CCCCC1 10.1016/j.bmcl.2013.09.052
72546757 102613 None 0 Human Functional pKd = 7.4 7.4 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 339 7 2 3 4.0 N=C(NCCc1ccc(Cl)cc1)SCCCN1CCCCC1 10.1016/j.bmcl.2013.09.052
CHEMBL2441940 102613 None 0 Human Functional pKd = 7.4 7.4 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 339 7 2 3 4.0 N=C(NCCc1ccc(Cl)cc1)SCCCN1CCCCC1 10.1016/j.bmcl.2013.09.052
CHEMBL3040715 102613 None 0 Human Functional pKd = 7.4 7.4 - 1
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
ChEMBL 339 7 2 3 4.0 N=C(NCCc1ccc(Cl)cc1)SCCCN1CCCCC1 10.1016/j.bmcl.2013.09.052
44406488 72879 None 0 Guinea pig Functional pKd = 7.4 7.4 - 0
Antagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileumAntagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileum
ChEMBL 277 7 1 2 3.2 CCCCCCC(=O)N1CCC(Cc2c[nH]cn2)CC1 10.1016/j.bmcl.2005.09.076
CHEMBL200244 72879 None 0 Guinea pig Functional pKd = 7.4 7.4 - 0
Antagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileumAntagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileum
ChEMBL 277 7 1 2 3.2 CCCCCCC(=O)N1CCC(Cc2c[nH]cn2)CC1 10.1016/j.bmcl.2005.09.076
11413171 12114 None 0 Guinea pig Functional pKd = 7.4 7.4 - 1
Functional Histamine H3 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H3 receptor antagonistic activity in vitro assay on guinea pig ileum
ChEMBL 210 9 1 2 2.9 CCCCCCOCCCc1c[nH]cn1 10.1021/jm031065q
CHEMBL1184057 12114 None 0 Guinea pig Functional pKd = 7.4 7.4 - 1
Functional Histamine H3 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H3 receptor antagonistic activity in vitro assay on guinea pig ileum
ChEMBL 210 9 1 2 2.9 CCCCCCOCCCc1c[nH]cn1 10.1021/jm031065q
CHEMBL330688 12114 None 0 Guinea pig Functional pKd = 7.4 7.4 - 1
Functional Histamine H3 receptor antagonistic activity in vitro assay on guinea pig ileumFunctional Histamine H3 receptor antagonistic activity in vitro assay on guinea pig ileum
ChEMBL 210 9 1 2 2.9 CCCCCCOCCCc1c[nH]cn1 10.1021/jm031065q
10105117 104250 None 0 Guinea pig Functional pKd = 7.4 7.4 - 1
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 226 6 3 2 1.6 CC/N=C(\S)NCCCCc1c[nH]cn1 10.1021/jm00012a025
CHEMBL309819 104250 None 0 Guinea pig Functional pKd = 7.4 7.4 - 1
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 226 6 3 2 1.6 CC/N=C(\S)NCCCCc1c[nH]cn1 10.1021/jm00012a025
3082406 206941 None 13 Guinea pig Functional pKd = 6.4 6.4 - 0
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 198 4 3 2 0.8 C/N=C(\S)NCCCc1c[nH]cn1 10.1021/jm00012a025
CHEMBL72427 206941 None 13 Guinea pig Functional pKd = 6.4 6.4 - 0
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 198 4 3 2 0.8 C/N=C(\S)NCCCc1c[nH]cn1 10.1021/jm00012a025
10465786 207067 None 0 Guinea pig Functional pKd = 5.4 5.4 - 0
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 212 5 3 2 1.2 CCC/N=C(\S)NCCc1c[nH]cn1 10.1021/jm00012a025
CHEMBL73274 207067 None 0 Guinea pig Functional pKd = 5.4 5.4 - 0
In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.In vitro inhibitory effect of histamine H3 antagonist on the electrically evoked contractile response of isolated guinea pig jejunum segments.
ChEMBL 212 5 3 2 1.2 CCC/N=C(\S)NCCc1c[nH]cn1 10.1021/jm00012a025
24771524 10701 None 0 Rat Functional pKd = 8.4 8.4 - 0
Antagonist activity at rat histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at rat histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 369 4 0 4 3.7 O=C(c1ccc(Oc2cccc(F)c2)nc1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.05.041
CHEMBL1170790 10701 None 0 Rat Functional pKd = 8.4 8.4 - 0
Antagonist activity at rat histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at rat histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 369 4 0 4 3.7 O=C(c1ccc(Oc2cccc(F)c2)nc1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.05.041
11690910 93743 None 0 Human Functional pKd = 8.4 8.4 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 448 8 0 4 5.1 CN1Cc2cc(OCCCN3CCC(F)CC3)ccc2C(c2ccc(OC(F)F)cc2)C1 10.1016/j.bmcl.2006.11.036
CHEMBL246954 93743 None 0 Human Functional pKd = 8.4 8.4 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 448 8 0 4 5.1 CN1Cc2cc(OCCCN3CCC(F)CC3)ccc2C(c2ccc(OC(F)F)cc2)C1 10.1016/j.bmcl.2006.11.036
24946664 95737 None 0 Human Functional pKd = 8.4 8.4 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 447 6 1 4 4.8 CNCc1cc(C(=O)N2CCN(C3CCC3)CC2)ccc1Oc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2007.11.016
CHEMBL258153 95737 None 0 Human Functional pKd = 8.4 8.4 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 447 6 1 4 4.8 CNCc1cc(C(=O)N2CCN(C3CCC3)CC2)ccc1Oc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2007.11.016
11518064 93639 None 0 Human Functional pKd = 8.3 8.3 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 450 6 0 3 5.8 CN1Cc2cc(OCCCN3CCC(F)CC3)ccc2C(c2cc(Cl)ccc2Cl)C1 10.1016/j.bmcl.2006.11.036
CHEMBL246541 93639 None 0 Human Functional pKd = 8.3 8.3 - 0
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
ChEMBL 450 6 0 3 5.8 CN1Cc2cc(OCCCN3CCC(F)CC3)ccc2C(c2cc(Cl)ccc2Cl)C1 10.1016/j.bmcl.2006.11.036
9944610 89470 None 20 Rat Functional pKd = 8.3 8.3 - 0
Antagonist activity at rat H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation treated 10 min before histamine challengeAntagonist activity at rat H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation treated 10 min before histamine challenge
ChEMBL 312 4 0 3 2.7 C(#Cc1cccc(CN2CCOCC2)c1)CCN1CCCCC1 10.1016/j.ejmech.2009.04.049
CHEMBL237087 89470 None 20 Rat Functional pKd = 8.3 8.3 - 0
Antagonist activity at rat H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation treated 10 min before histamine challengeAntagonist activity at rat H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation treated 10 min before histamine challenge
ChEMBL 312 4 0 3 2.7 C(#Cc1cccc(CN2CCOCC2)c1)CCN1CCCCC1 10.1016/j.ejmech.2009.04.049
10291489 187815 None 10 Rat Functional pKd = 8.3 8.3 - 0
Antagonist activity for rat histamine H3 receptor was determinedAntagonist activity for rat histamine H3 receptor was determined
ChEMBL 349 6 0 4 4.6 Cc1ccn2cc(-c3ccc(OCCCN4CCCCC4)cc3)nc2c1 10.1016/s0960-894x(02)00738-2
CHEMBL49532 187815 None 10 Rat Functional pKd = 8.3 8.3 - 0
Antagonist activity for rat histamine H3 receptor was determinedAntagonist activity for rat histamine H3 receptor was determined
ChEMBL 349 6 0 4 4.6 Cc1ccn2cc(-c3ccc(OCCCN4CCCCC4)cc3)nc2c1 10.1016/s0960-894x(02)00738-2
44581060 172680 None 0 Rat Functional pKd = 8.3 8.3 - 0
Antagonist activity rat recombinant histamine H3 receptor expressed in human SK-N-MC cellsAntagonist activity rat recombinant histamine H3 receptor expressed in human SK-N-MC cells
ChEMBL 360 6 0 5 2.5 c1cc(OCC2CN(C3CCCC3)CCO2)ccc1CN1CCOCC1 10.1016/j.bmcl.2008.09.077
CHEMBL448825 172680 None 0 Rat Functional pKd = 8.3 8.3 - 0
Antagonist activity rat recombinant histamine H3 receptor expressed in human SK-N-MC cellsAntagonist activity rat recombinant histamine H3 receptor expressed in human SK-N-MC cells
ChEMBL 360 6 0 5 2.5 c1cc(OCC2CN(C3CCCC3)CCO2)ccc1CN1CCOCC1 10.1016/j.bmcl.2008.09.077
11630921 62713 None 0 Human Functional pKd = 8.3 8.3 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrs
ChEMBL 307 7 0 5 2.9 c1c(OCCCN2CCCCC2)noc1CN1CCCCC1 10.1016/j.ejmech.2009.06.007
CHEMBL1783909 62713 None 0 Human Functional pKd = 8.3 8.3 - 0
Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrs
ChEMBL 307 7 0 5 2.9 c1c(OCCCN2CCCCC2)noc1CN1CCCCC1 10.1016/j.ejmech.2009.06.007
42604373 12729 None 0 Guinea pig Functional pKd = 7.4 7.4 - 0
Antagonist activity at histamine H3 receptor in guinea pig jejunum assessed as electrically evoked contractionsAntagonist activity at histamine H3 receptor in guinea pig jejunum assessed as electrically evoked contractions
ChEMBL 324 7 0 5 2.1 CCCN1CCN(c2ncc(CCN(C)C(=O)CC)s2)CC1 10.1016/j.ejmech.2008.09.019
CHEMBL1187681 12729 None 0 Guinea pig Functional pKd = 7.4 7.4 - 0
Antagonist activity at histamine H3 receptor in guinea pig jejunum assessed as electrically evoked contractionsAntagonist activity at histamine H3 receptor in guinea pig jejunum assessed as electrically evoked contractions
ChEMBL 324 7 0 5 2.1 CCCN1CCN(c2ncc(CCN(C)C(=O)CC)s2)CC1 10.1016/j.ejmech.2008.09.019
CHEMBL515121 12729 None 0 Guinea pig Functional pKd = 7.4 7.4 - 0
Antagonist activity at histamine H3 receptor in guinea pig jejunum assessed as electrically evoked contractionsAntagonist activity at histamine H3 receptor in guinea pig jejunum assessed as electrically evoked contractions
ChEMBL 324 7 0 5 2.1 CCCN1CCN(c2ncc(CCN(C)C(=O)CC)s2)CC1 10.1016/j.ejmech.2008.09.019
44581100 193412 None 0 Rat Functional pKd = 7.4 7.4 - 0
Antagonist activity rat recombinant histamine H3 receptor expressed in human SK-N-MC cellsAntagonist activity rat recombinant histamine H3 receptor expressed in human SK-N-MC cells
ChEMBL 360 6 0 5 2.5 c1cc(OC[C@H]2CN(C3CCCC3)CCO2)ccc1CN1CCOCC1 10.1016/j.bmcl.2008.09.077
CHEMBL524088 193412 None 0 Rat Functional pKd = 7.4 7.4 - 0
Antagonist activity rat recombinant histamine H3 receptor expressed in human SK-N-MC cellsAntagonist activity rat recombinant histamine H3 receptor expressed in human SK-N-MC cells
ChEMBL 360 6 0 5 2.5 c1cc(OC[C@H]2CN(C3CCCC3)CCO2)ccc1CN1CCOCC1 10.1016/j.bmcl.2008.09.077
9993212 208665 None 0 Guinea pig Functional pKd = 5.4 5.4 - 0
Compound was tested for the agonist activity against histamine H3 receptor of guinea pig ileumCompound was tested for the agonist activity against histamine H3 receptor of guinea pig ileum
ChEMBL 269 4 2 2 2.9 CNCCc1c[nH]c(-c2cccc(C(F)(F)F)c2)n1 10.1016/s0960-894x(98)00461-2
CHEMBL86522 208665 None 0 Guinea pig Functional pKd = 5.4 5.4 - 0
Compound was tested for the agonist activity against histamine H3 receptor of guinea pig ileumCompound was tested for the agonist activity against histamine H3 receptor of guinea pig ileum
ChEMBL 269 4 2 2 2.9 CNCCc1c[nH]c(-c2cccc(C(F)(F)F)c2)n1 10.1016/s0960-894x(98)00461-2
44581077 193494 None 0 Human Functional pKd = 7.4 7.4 - 0
Antagonist activity at human recombinant histamine H3 receptor expressed in human SK-N-MC cellsAntagonist activity at human recombinant histamine H3 receptor expressed in human SK-N-MC cells
ChEMBL 334 6 0 5 2.0 CC(C)N1CCOC(COc2cccc(CN3CCOCC3)c2)C1 10.1016/j.bmcl.2008.09.077
CHEMBL525376 193494 None 0 Human Functional pKd = 7.4 7.4 - 0
Antagonist activity at human recombinant histamine H3 receptor expressed in human SK-N-MC cellsAntagonist activity at human recombinant histamine H3 receptor expressed in human SK-N-MC cells
ChEMBL 334 6 0 5 2.0 CC(C)N1CCOC(COc2cccc(CN3CCOCC3)c2)C1 10.1016/j.bmcl.2008.09.077
10685638 189103 None 0 Guinea pig Functional pKd = 7.3 7.3 - 0
In vitro histamine H3 receptor antagonist activity was determined on guinea pig jejunumIn vitro histamine H3 receptor antagonist activity was determined on guinea pig jejunum
ChEMBL 300 3 2 2 2.7 S=C(NCc1ccccc1)N1CCC(c2c[nH]cn2)CC1 10.1021/jm981106w
CHEMBL50868 189103 None 0 Guinea pig Functional pKd = 7.3 7.3 - 0
In vitro histamine H3 receptor antagonist activity was determined on guinea pig jejunumIn vitro histamine H3 receptor antagonist activity was determined on guinea pig jejunum
ChEMBL 300 3 2 2 2.7 S=C(NCc1ccccc1)N1CCC(c2c[nH]cn2)CC1 10.1021/jm981106w
49864901 15755 None 0 Guinea pig Functional pKd = 8.3 8.3 - 0
Antagonist activity at histamine H3 receptor in electrically-stimulated guinea pig ileumAntagonist activity at histamine H3 receptor in electrically-stimulated guinea pig ileum
ChEMBL 433 4 0 6 2.8 Cn1c(=O)n(C2CCN(C(=O)C3CCN(Cc4ccncc4)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2010.07.052
CHEMBL1222649 15755 None 0 Guinea pig Functional pKd = 8.3 8.3 - 0
Antagonist activity at histamine H3 receptor in electrically-stimulated guinea pig ileumAntagonist activity at histamine H3 receptor in electrically-stimulated guinea pig ileum
ChEMBL 433 4 0 6 2.8 Cn1c(=O)n(C2CCN(C(=O)C3CCN(Cc4ccncc4)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2010.07.052
46887963 8722 None 0 Rat Functional pKd = 8.3 8.3 - 0
Antagonist activity at rat H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at rat H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 377 4 1 4 2.5 O=C([C@H]1C[C@H](Oc2ccc(Cl)cc2)CN1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.03.071
CHEMBL1095847 8722 None 0 Rat Functional pKd = 8.3 8.3 - 0
Antagonist activity at rat H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at rat H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 377 4 1 4 2.5 O=C([C@H]1C[C@H](Oc2ccc(Cl)cc2)CN1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.03.071
24771419 10730 None 0 Rat Functional pKd = 8.3 8.3 - 0
Antagonist activity at rat histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at rat histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 385 4 0 4 4.2 O=C(c1ccc(Oc2cccc(Cl)c2)nc1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.05.041
CHEMBL1171002 10730 None 0 Rat Functional pKd = 8.3 8.3 - 0
Antagonist activity at rat histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrsAntagonist activity at rat histamine H3 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 385 4 0 4 4.2 O=C(c1ccc(Oc2cccc(Cl)c2)nc1)N1CCCN(C2CCC2)CC1 10.1016/j.bmcl.2010.05.041
9948238 72883 None 0 Guinea pig Functional pKd = 8.3 8.3 - 0
Antagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileumAntagonist potency against histamine H3 receptor in an electrically stimulated guinea pig ileum
ChEMBL 299 7 1 3 3.1 c1ccc(OCCCN2CCC(Cc3c[nH]cn3)CC2)cc1 10.1016/j.bmcl.2005.09.076