Ligand source activities (1 row/activity)



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ligand		 Fold
selectivity		 # Tested
GPCRs		 Species

 p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 AssayType

 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

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 DOI
1251 8795 39 None 204 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmcl.2010.10.041
3035842 8795 39 None 204 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmcl.2010.10.041
CHEMBL18661 8795 39 None 204 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmcl.2010.10.041
1253 8839 7 None 251 2 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 342 6 1 2 3.2 Ic1ccc(cc1)COCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
132937 8839 7 None 251 2 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 342 6 1 2 3.2 Ic1ccc(cc1)COCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL19010 8839 7 None 251 2 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 342 6 1 2 3.2 Ic1ccc(cc1)COCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
11957573 8791 34 None 3 5 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.ejmech.2018.04.020
1250 8791 34 None 3 5 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.ejmech.2018.04.020
3692 8791 34 None 3 5 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.ejmech.2018.04.020
CHEMBL19439 8791 34 None 3 5 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.ejmech.2018.04.020
11957573 8791 34 None 3 5 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.ejmech.2018.04.020
1250 8791 34 None 3 5 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.ejmech.2018.04.020
3692 8791 34 None 3 5 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.ejmech.2018.04.020
CHEMBL19439 8791 34 None 3 5 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.ejmech.2018.04.020
145956362 168791 0 None - 1 Human 10.0 pEC50 = 10 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 500 7 1 5 5.0 COc1cc(N2C(=O)/C(=C\c3ccccc3)C2(C(=O)NC(C)(C)C)c2ccccc2)cc(OC)c1OC 10.1016/j.ejmech.2018.04.020
CHEMBL4159570 168791 0 None - 1 Human 10.0 pEC50 = 10 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 500 7 1 5 5.0 COc1cc(N2C(=O)/C(=C\c3ccccc3)C2(C(=O)NC(C)(C)C)c2ccccc2)cc(OC)c1OC 10.1016/j.ejmech.2018.04.020
145949589 169495 0 None - 1 Human 10.0 pEC50 = 10 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 520 6 1 3 5.9 COc1ccc(N2C(=O)/C(=C\c3ccccc3)C2(C(=O)NC2CCCCC2)c2cc(F)c(F)c(F)c2)cc1 10.1016/j.ejmech.2018.04.020
CHEMBL4170869 169495 0 None - 1 Human 10.0 pEC50 = 10 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 520 6 1 3 5.9 COc1ccc(N2C(=O)/C(=C\c3ccccc3)C2(C(=O)NC2CCCCC2)c2cc(F)c(F)c(F)c2)cc1 10.1016/j.ejmech.2018.04.020
155491015 183274 4 None 10 4 Mouse 10.0 pEC50 = 10 Functional
Agonist activity at mouse H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by luciferase reporter gene assayAgonist activity at mouse H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by luciferase reporter gene assay
ChEMBL 207 4 2 5 0.2 CCCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4441731 183274 4 None 10 4 Mouse 10.0 pEC50 = 10 Functional
Agonist activity at mouse H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by luciferase reporter gene assayAgonist activity at mouse H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by luciferase reporter gene assay
ChEMBL 207 4 2 5 0.2 CCCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4596734 183274 4 None 10 4 Mouse 10.0 pEC50 = 10 Functional
Agonist activity at mouse H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by luciferase reporter gene assayAgonist activity at mouse H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by luciferase reporter gene assay
ChEMBL 207 4 2 5 0.2 CCCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
145956362 168791 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 500 7 1 5 5.0 COc1cc(N2C(=O)/C(=C\c3ccccc3)C2(C(=O)NC(C)(C)C)c2ccccc2)cc(OC)c1OC 10.1016/j.ejmech.2018.04.020
CHEMBL4159570 168791 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 500 7 1 5 5.0 COc1cc(N2C(=O)/C(=C\c3ccccc3)C2(C(=O)NC(C)(C)C)c2ccccc2)cc(OC)c1OC 10.1016/j.ejmech.2018.04.020
565544 116520 11 None 4466 2 Human 9.9 pEC50 = 9.9 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptor
ChEMBL 125 2 2 2 0.5 CC(CN)c1cnc[nH]1 10.1021/jm0300025
CHEMBL322988 116520 11 None 4466 2 Human 9.9 pEC50 = 9.9 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptor
ChEMBL 125 2 2 2 0.5 CC(CN)c1cnc[nH]1 10.1021/jm0300025
11957573 8791 34 None 3 5 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1250 8791 34 None 3 5 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
3692 8791 34 None 3 5 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL19439 8791 34 None 3 5 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1251 8795 39 None 204 2 Human 9.9 pEC50 = 9.9 Functional
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm049475h
3035842 8795 39 None 204 2 Human 9.9 pEC50 = 9.9 Functional
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm049475h
CHEMBL18661 8795 39 None 204 2 Human 9.9 pEC50 = 9.9 Functional
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm049475h
145949589 169495 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 520 6 1 3 5.9 COc1ccc(N2C(=O)/C(=C\c3ccccc3)C2(C(=O)NC2CCCCC2)c2cc(F)c(F)c(F)c2)cc1 10.1016/j.ejmech.2018.04.020
CHEMBL4170869 169495 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 520 6 1 3 5.9 COc1ccc(N2C(=O)/C(=C\c3ccccc3)C2(C(=O)NC2CCCCC2)c2cc(F)c(F)c(F)c2)cc1 10.1016/j.ejmech.2018.04.020
4024 8796 20 None 3388 2 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
9989505 8796 20 None 3388 2 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL82298 8796 20 None 3388 2 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
4024 8796 20 None 3388 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human histamine H3 receptor assessed as beta galactosidase activityAgonist activity at human histamine H3 receptor assessed as beta galactosidase activity
ChEMBL 159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1 10.1021/jm7014149
9989505 8796 20 None 3388 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human histamine H3 receptor assessed as beta galactosidase activityAgonist activity at human histamine H3 receptor assessed as beta galactosidase activity
ChEMBL 159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1 10.1021/jm7014149
CHEMBL82298 8796 20 None 3388 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human histamine H3 receptor assessed as beta galactosidase activityAgonist activity at human histamine H3 receptor assessed as beta galactosidase activity
ChEMBL 159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1 10.1021/jm7014149
23628252 172890 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Inverse agonist activity at human histamine H3 receptor by GTP gammaS assayInverse agonist activity at human histamine H3 receptor by GTP gammaS assay
ChEMBL 419 9 1 6 4.7 CN(C)Cc1cc(OCCCN2CCCCC2)ccc1Nc1ncnc2ccccc12 10.1016/j.bmcl.2007.04.056
CHEMBL425994 172890 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Inverse agonist activity at human histamine H3 receptor by GTP gammaS assayInverse agonist activity at human histamine H3 receptor by GTP gammaS assay
ChEMBL 419 9 1 6 4.7 CN(C)Cc1cc(OCCCN2CCCCC2)ccc1Nc1ncnc2ccccc12 10.1016/j.bmcl.2007.04.056
49799506 17651 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 309 3 1 2 3.9 FC(F)(F)c1cccc(N2CCC(Cc3c[nH]cn3)CC2)c1 10.1016/j.bmc.2010.04.052
CHEMBL1172579 17651 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 309 3 1 2 3.9 FC(F)(F)c1cccc(N2CCC(Cc3c[nH]cn3)CC2)c1 10.1016/j.bmc.2010.04.052
145956355 168782 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 415 3 1 5 2.3 O=C1C=C[C@]23C(c4ccccc4)=CC(=O)N2[C@H](c2ccc([N+](=O)[O-])cc2)C(=O)N[C@@H]3C1 10.1016/j.ejmech.2018.04.020
CHEMBL4159472 168782 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 415 3 1 5 2.3 O=C1C=C[C@]23C(c4ccccc4)=CC(=O)N2[C@H](c2ccc([N+](=O)[O-])cc2)C(=O)N[C@@H]3C1 10.1016/j.ejmech.2018.04.020
145971293 169902 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 536 7 1 5 5.2 COc1cc(N2C(=O)/C(=C\c3ccccc3)C2(C(=O)NC(C)(C)C)c2cc(F)cc(F)c2)cc(OC)c1OC 10.1016/j.ejmech.2018.04.020
CHEMBL4177416 169902 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 536 7 1 5 5.2 COc1cc(N2C(=O)/C(=C\c3ccccc3)C2(C(=O)NC(C)(C)C)c2cc(F)cc(F)c2)cc(OC)c1OC 10.1016/j.ejmech.2018.04.020
145956355 168782 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 415 3 1 5 2.3 O=C1C=C[C@]23C(c4ccccc4)=CC(=O)N2[C@H](c2ccc([N+](=O)[O-])cc2)C(=O)N[C@@H]3C1 10.1016/j.ejmech.2018.04.020
CHEMBL4159472 168782 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 415 3 1 5 2.3 O=C1C=C[C@]23C(c4ccccc4)=CC(=O)N2[C@H](c2ccc([N+](=O)[O-])cc2)C(=O)N[C@@H]3C1 10.1016/j.ejmech.2018.04.020
145971293 169902 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 536 7 1 5 5.2 COc1cc(N2C(=O)/C(=C\c3ccccc3)C2(C(=O)NC(C)(C)C)c2cc(F)cc(F)c2)cc(OC)c1OC 10.1016/j.ejmech.2018.04.020
CHEMBL4177416 169902 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 536 7 1 5 5.2 COc1cc(N2C(=O)/C(=C\c3ccccc3)C2(C(=O)NC(C)(C)C)c2cc(F)cc(F)c2)cc(OC)c1OC 10.1016/j.ejmech.2018.04.020
155491015 183274 4 None -11 4 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 207 4 2 5 0.2 CCCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4441731 183274 4 None -11 4 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 207 4 2 5 0.2 CCCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4596734 183274 4 None -11 4 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 207 4 2 5 0.2 CCCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
11313837 9278 8 None 15848 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human histamine H3 receptor assessed as beta galactosidase activityAgonist activity at human histamine H3 receptor assessed as beta galactosidase activity
ChEMBL 179 2 1 2 1.3 CN1CCC(CC1)Cc1[nH]cnc1 10.1021/jm7014149
1254 9278 8 None 15848 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human histamine H3 receptor assessed as beta galactosidase activityAgonist activity at human histamine H3 receptor assessed as beta galactosidase activity
ChEMBL 179 2 1 2 1.3 CN1CCC(CC1)Cc1[nH]cnc1 10.1021/jm7014149
CHEMBL175782 9278 8 None 15848 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human histamine H3 receptor assessed as beta galactosidase activityAgonist activity at human histamine H3 receptor assessed as beta galactosidase activity
ChEMBL 179 2 1 2 1.3 CN1CCC(CC1)Cc1[nH]cnc1 10.1021/jm7014149
1236 8848 25 None -1 3 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1016/j.bmcl.2010.10.041
1237 8848 25 None -1 3 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1016/j.bmcl.2010.10.041
156615 8848 25 None -1 3 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1016/j.bmcl.2010.10.041
CHEMBL268229 8848 25 None -1 3 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1016/j.bmcl.2010.10.041
11313837 9278 8 None 15848 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 179 2 1 2 1.3 CN1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmcl.2010.10.041
1254 9278 8 None 15848 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 179 2 1 2 1.3 CN1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmcl.2010.10.041
CHEMBL175782 9278 8 None 15848 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 179 2 1 2 1.3 CN1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmcl.2010.10.041
11313837 9278 8 None 15848 2 Human 9.5 pEC50 = 9.5 Functional
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
ChEMBL 179 2 1 2 1.3 CN1CCC(CC1)Cc1[nH]cnc1 10.1021/jm049475h
1254 9278 8 None 15848 2 Human 9.5 pEC50 = 9.5 Functional
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
ChEMBL 179 2 1 2 1.3 CN1CCC(CC1)Cc1[nH]cnc1 10.1021/jm049475h
CHEMBL175782 9278 8 None 15848 2 Human 9.5 pEC50 = 9.5 Functional
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
ChEMBL 179 2 1 2 1.3 CN1CCC(CC1)Cc1[nH]cnc1 10.1021/jm049475h
1239 8814 24 None 1995 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 3 2 2 0.2 CNCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1240 8814 24 None 1995 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 3 2 2 0.2 CNCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
912 8814 24 None 1995 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 3 2 2 0.2 CNCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL268490 8814 24 None 1995 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 3 2 2 0.2 CNCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
53321919 63252 0 None 50 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 322 7 3 3 3.8 N=C(NCc1ccc(Cl)cc1)SCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL1632409 63252 0 None 50 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 322 7 3 3 3.8 N=C(NCc1ccc(Cl)cc1)SCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
76328873 112272 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Inverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assay
ChEMBL 339 4 1 4 2.6 O=C1NN=C(c2ccc(OC3CCN(C4CCC4)CC3)cc2)[C@H]2C[C@@H]12 10.1016/j.bmcl.2014.01.061
CHEMBL3121095 112272 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Inverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assay
ChEMBL 339 4 1 4 2.6 O=C1NN=C(c2ccc(OC3CCN(C4CCC4)CC3)cc2)[C@H]2C[C@@H]12 10.1016/j.bmcl.2014.01.061
76321713 112273 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Inverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assay
ChEMBL 339 4 1 4 2.6 O=C1NN=C(c2ccc(OC3CCN(C4CCC4)CC3)cc2)[C@@H]2C[C@H]12 10.1016/j.bmcl.2014.01.061
CHEMBL3121096 112273 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Inverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assay
ChEMBL 339 4 1 4 2.6 O=C1NN=C(c2ccc(OC3CCN(C4CCC4)CC3)cc2)[C@@H]2C[C@H]12 10.1016/j.bmcl.2014.01.061
10176414 10835 16 None 25 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 184 4 3 3 1.0 NC(=N)SCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1246 10835 16 None 25 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 184 4 3 3 1.0 NC(=N)SCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL281576 10835 16 None 25 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 184 4 3 3 1.0 NC(=N)SCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
11554040 96317 0 None 1 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 442 7 0 7 4.6 CCOc1ccc(-n2ncc(-c3ccc4cc(CCN5CCC[C@H]5C)ccc4n3)c2C)nn1 10.1021/jm0705051
CHEMBL237394 96317 0 None 1 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 442 7 0 7 4.6 CCOc1ccc(-n2ncc(-c3ccc4cc(CCN5CCC[C@H]5C)ccc4n3)c2C)nn1 10.1021/jm0705051
11554040 96317 0 None 1 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 442 7 0 7 4.6 CCOc1ccc(-n2ncc(-c3ccc4cc(CCN5CCC[C@H]5C)ccc4n3)c2C)nn1 10.1021/jm0705051
CHEMBL237394 96317 0 None 1 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 442 7 0 7 4.6 CCOc1ccc(-n2ncc(-c3ccc4cc(CCN5CCC[C@H]5C)ccc4n3)c2C)nn1 10.1021/jm0705051
118734876 125516 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Inverse agonist activity at human H3R expressed in CHO cells assessed as inhibition of RAMH-induced [35S]GTPgammaS binding relative to controlInverse agonist activity at human H3R expressed in CHO cells assessed as inhibition of RAMH-induced [35S]GTPgammaS binding relative to control
ChEMBL 327 6 1 4 2.4 C[C@@H]1CCCN1CCCOc1ccc(C2=NNC(=O)[C@H]3C[C@@H]23)cc1 10.1016/j.ejmech.2015.03.054
CHEMBL3417586 125516 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Inverse agonist activity at human H3R expressed in CHO cells assessed as inhibition of RAMH-induced [35S]GTPgammaS binding relative to controlInverse agonist activity at human H3R expressed in CHO cells assessed as inhibition of RAMH-induced [35S]GTPgammaS binding relative to control
ChEMBL 327 6 1 4 2.4 C[C@@H]1CCCN1CCCOc1ccc(C2=NNC(=O)[C@H]3C[C@@H]23)cc1 10.1016/j.ejmech.2015.03.054
155547602 183472 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 193 3 2 5 -0.1 CCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4535316 183472 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 193 3 2 5 -0.1 CCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4598409 183472 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 193 3 2 5 -0.1 CCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
1249 8790 16 None 18 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
13499360 8790 16 None 18 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL90019 8790 16 None 18 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
90666843 116211 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation countingInverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation counting
ChEMBL 328 4 0 4 3.6 CC1(C)COC(c2ccc(O[C@H]3C[C@H](N4CCCCC4)C3)cc2)=N1 10.1039/C0MD00056F
CHEMBL3220120 116211 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation countingInverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation counting
ChEMBL 328 4 0 4 3.6 CC1(C)COC(c2ccc(O[C@H]3C[C@H](N4CCCCC4)C3)cc2)=N1 10.1039/C0MD00056F
1251 8795 39 None 204 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm100643t
3035842 8795 39 None 204 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm100643t
CHEMBL18661 8795 39 None 204 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm100643t
1251 8795 39 None 204 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmc.2010.04.052
3035842 8795 39 None 204 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmc.2010.04.052
CHEMBL18661 8795 39 None 204 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmc.2010.04.052
54764158 75852 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Inhibition of basal activity of human histamine H3 receptor expressed in CHO cells assessed as inhibition of RAHM-induced [35S]GTPgammaS binding after 4 hrs by beta liquid scintillation countingInhibition of basal activity of human histamine H3 receptor expressed in CHO cells assessed as inhibition of RAHM-induced [35S]GTPgammaS binding after 4 hrs by beta liquid scintillation counting
ChEMBL 326 6 0 4 3.3 C[C@@H]1CCCN1CCCOc1ccc(-c2ccc(=O)n(C)c2)cc1 10.1016/j.bmcl.2011.09.091
CHEMBL1923729 75852 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Inhibition of basal activity of human histamine H3 receptor expressed in CHO cells assessed as inhibition of RAHM-induced [35S]GTPgammaS binding after 4 hrs by beta liquid scintillation countingInhibition of basal activity of human histamine H3 receptor expressed in CHO cells assessed as inhibition of RAHM-induced [35S]GTPgammaS binding after 4 hrs by beta liquid scintillation counting
ChEMBL 326 6 0 4 3.3 C[C@@H]1CCCN1CCCOc1ccc(-c2ccc(=O)n(C)c2)cc1 10.1016/j.bmcl.2011.09.091
118734875 125515 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Inverse agonist activity at human H3R expressed in CHO cells assessed as inhibition of RAMH-induced [35S]GTPgammaS binding relative to controlInverse agonist activity at human H3R expressed in CHO cells assessed as inhibition of RAMH-induced [35S]GTPgammaS binding relative to control
ChEMBL 327 6 1 4 2.4 C[C@@H]1CCCN1CCCOc1ccc(C2=NNC(=O)[C@@H]3C[C@H]23)cc1 10.1016/j.ejmech.2015.03.054
CHEMBL3417585 125515 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Inverse agonist activity at human H3R expressed in CHO cells assessed as inhibition of RAMH-induced [35S]GTPgammaS binding relative to controlInverse agonist activity at human H3R expressed in CHO cells assessed as inhibition of RAMH-induced [35S]GTPgammaS binding relative to control
ChEMBL 327 6 1 4 2.4 C[C@@H]1CCCN1CCCOc1ccc(C2=NNC(=O)[C@@H]3C[C@H]23)cc1 10.1016/j.ejmech.2015.03.054
25265089 110468 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Inverse agonist activity at human histamine H3 receptor (445 amino acid residues) expressed in CHO cells by CRE-luciferase reporter gene assayInverse agonist activity at human histamine H3 receptor (445 amino acid residues) expressed in CHO cells by CRE-luciferase reporter gene assay
ChEMBL 382 4 1 5 3.9 Cc1cc(N2CC[C@H](N3CCC[C@@H]3C)C2)ccc1NC(=O)c1c(C)noc1C 10.1016/j.bmcl.2013.09.081
CHEMBL3087669 110468 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Inverse agonist activity at human histamine H3 receptor (445 amino acid residues) expressed in CHO cells by CRE-luciferase reporter gene assayInverse agonist activity at human histamine H3 receptor (445 amino acid residues) expressed in CHO cells by CRE-luciferase reporter gene assay
ChEMBL 382 4 1 5 3.9 Cc1cc(N2CC[C@H](N3CCC[C@@H]3C)C2)ccc1NC(=O)c1c(C)noc1C 10.1016/j.bmcl.2013.09.081
24994127 76431 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Inverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assay
ChEMBL 315 6 1 4 2.6 C[C@@H]1CCCN1CCCOc1ccc(C2=NNC(=O)CC2)cc1 10.1016/j.bmcl.2011.11.037
CHEMBL1935100 76431 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Inverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assay
ChEMBL 315 6 1 4 2.6 C[C@@H]1CCCN1CCCOc1ccc(C2=NNC(=O)CC2)cc1 10.1016/j.bmcl.2011.11.037
56835090 76445 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Inverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assay
ChEMBL 343 6 1 4 3.2 C[C@@H]1CCCN1CCCOc1ccc(C2=NNC(=O)C(C)(C)C2)cc1 10.1016/j.bmcl.2011.11.037
CHEMBL1935114 76445 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Inverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assay
ChEMBL 343 6 1 4 3.2 C[C@@H]1CCCN1CCCOc1ccc(C2=NNC(=O)C(C)(C)C2)cc1 10.1016/j.bmcl.2011.11.037
11554040 96317 0 None -1 2 Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 442 7 0 7 4.6 CCOc1ccc(-n2ncc(-c3ccc4cc(CCN5CCC[C@H]5C)ccc4n3)c2C)nn1 10.1021/jm0705051
CHEMBL237394 96317 0 None -1 2 Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 442 7 0 7 4.6 CCOc1ccc(-n2ncc(-c3ccc4cc(CCN5CCC[C@H]5C)ccc4n3)c2C)nn1 10.1021/jm0705051
11554040 96317 0 None -1 2 Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 442 7 0 7 4.6 CCOc1ccc(-n2ncc(-c3ccc4cc(CCN5CCC[C@H]5C)ccc4n3)c2C)nn1 10.1021/jm0705051
CHEMBL237394 96317 0 None -1 2 Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 442 7 0 7 4.6 CCOc1ccc(-n2ncc(-c3ccc4cc(CCN5CCC[C@H]5C)ccc4n3)c2C)nn1 10.1021/jm0705051
46222048 15756 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 260 4 1 2 4.0 CC(C)(C)c1ccc(SCCc2c[nH]cn2)cc1 10.1021/jm100643t
CHEMBL1098230 15756 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 260 4 1 2 4.0 CC(C)(C)c1ccc(SCCc2c[nH]cn2)cc1 10.1021/jm100643t
46222048 15756 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 260 4 1 2 4.0 CC(C)(C)c1ccc(SCCc2c[nH]cn2)cc1 10.1021/jm901890s
CHEMBL1098230 15756 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 260 4 1 2 4.0 CC(C)(C)c1ccc(SCCc2c[nH]cn2)cc1 10.1021/jm901890s
46222048 15756 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 260 4 1 2 4.0 CC(C)(C)c1ccc(SCCc2c[nH]cn2)cc1 10.1016/j.bmc.2010.04.052
CHEMBL1098230 15756 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 260 4 1 2 4.0 CC(C)(C)c1ccc(SCCc2c[nH]cn2)cc1 10.1016/j.bmc.2010.04.052
11647025 96248 0 None 3 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 401 5 0 5 4.6 Cc1nc(N2CCCC2)ncc1-c1ccc2cc(CCN3CCC[C@H]3C)ccc2n1 10.1021/jm0705051
CHEMBL237191 96248 0 None 3 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 401 5 0 5 4.6 Cc1nc(N2CCCC2)ncc1-c1ccc2cc(CCN3CCC[C@H]3C)ccc2n1 10.1021/jm0705051
11647025 96248 0 None 3 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 401 5 0 5 4.6 Cc1nc(N2CCCC2)ncc1-c1ccc2cc(CCN3CCC[C@H]3C)ccc2n1 10.1021/jm0705051
CHEMBL237191 96248 0 None 3 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 401 5 0 5 4.6 Cc1nc(N2CCCC2)ncc1-c1ccc2cc(CCN3CCC[C@H]3C)ccc2n1 10.1021/jm0705051
155558361 183028 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 221 5 2 5 0.6 CCCCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4560428 183028 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 221 5 2 5 0.6 CCCCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4594866 183028 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 221 5 2 5 0.6 CCCCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
54753626 72676 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Inverse agonist activity at human histamine H3 receptor assessed as decrease of basal activity of [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as decrease of basal activity of [35S]GTPgammaS binding
ChEMBL 367 6 0 5 3.2 C[C@@H]1CCCN1CCCOc1ccc(-c2nn(C)c(=O)c3c2CCC3)cc1 10.1016/j.bmcl.2011.08.045
CHEMBL1835782 72676 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Inverse agonist activity at human histamine H3 receptor assessed as decrease of basal activity of [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as decrease of basal activity of [35S]GTPgammaS binding
ChEMBL 367 6 0 5 3.2 C[C@@H]1CCCN1CCCOc1ccc(-c2nn(C)c(=O)c3c2CCC3)cc1 10.1016/j.bmcl.2011.08.045
54753627 72677 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Inverse agonist activity at human histamine H3 receptor assessed as decrease of basal activity of [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as decrease of basal activity of [35S]GTPgammaS binding
ChEMBL 367 6 0 5 3.2 Cn1nc(-c2ccc(OCCCN3CCCCC3)cc2)c2c(c1=O)CCC2 10.1016/j.bmcl.2011.08.045
CHEMBL1835783 72677 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Inverse agonist activity at human histamine H3 receptor assessed as decrease of basal activity of [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as decrease of basal activity of [35S]GTPgammaS binding
ChEMBL 367 6 0 5 3.2 Cn1nc(-c2ccc(OCCCN3CCCCC3)cc2)c2c(c1=O)CCC2 10.1016/j.bmcl.2011.08.045
24993178 77517 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 355 4 1 4 3.3 CC1(C)CC(c2ccc(OC3CCN(C4CCC4)CC3)cc2)=NNC1=O 10.1016/j.bmcl.2012.01.026
CHEMBL1950743 77517 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 355 4 1 4 3.3 CC1(C)CC(c2ccc(OC3CCN(C4CCC4)CC3)cc2)=NNC1=O 10.1016/j.bmcl.2012.01.026
25265516 99792 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity at human histamine H3 receptor expressed in CHO cells co-expressing CRE-LucAntagonist activity at human histamine H3 receptor expressed in CHO cells co-expressing CRE-Luc
ChEMBL 371 4 1 4 3.4 Cc1cc(N2CC[C@H](N3CCC[C@@H]3C)C2)ccc1NC(=O)C1CCOCC1 10.1016/j.bmcl.2013.09.006
CHEMBL2441636 99792 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity at human histamine H3 receptor expressed in CHO cells co-expressing CRE-LucAntagonist activity at human histamine H3 receptor expressed in CHO cells co-expressing CRE-Luc
ChEMBL 371 4 1 4 3.4 Cc1cc(N2CC[C@H](N3CCC[C@@H]3C)C2)ccc1NC(=O)C1CCOCC1 10.1016/j.bmcl.2013.09.006
49856084 81964 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Inverse agonist activity at human histamine H3 receptor by [35S]-GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor by [35S]-GTPgammaS binding assay
ChEMBL 403 8 0 6 2.5 COC(=O)N1CCN(CC(=O)c2ccc(OCCCN3CCC[C@H]3C)cc2)CC1 10.1016/j.bmcl.2012.02.081
CHEMBL2036653 81964 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Inverse agonist activity at human histamine H3 receptor by [35S]-GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor by [35S]-GTPgammaS binding assay
ChEMBL 403 8 0 6 2.5 COC(=O)N1CCN(CC(=O)c2ccc(OCCCN3CCC[C@H]3C)cc2)CC1 10.1016/j.bmcl.2012.02.081
23725172 71155 0 None 2 2 Human 9.0 pEC50 = 9 Functional
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS binding
ChEMBL 327 6 0 5 2.7 C[C@@H]1CCCN1CCCOc1ccc(-c2ccc(=O)n(C)n2)cc1 10.1021/jm200401v
CHEMBL1813057 71155 0 None 2 2 Human 9.0 pEC50 = 9 Functional
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS binding
ChEMBL 327 6 0 5 2.7 C[C@@H]1CCCN1CCCOc1ccc(-c2ccc(=O)n(C)n2)cc1 10.1021/jm200401v
49855513 81951 0 None - 1 Human 9.0 pEC50 = 9 Functional
Inverse agonist activity at human histamine H3 receptor by [35S]-GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor by [35S]-GTPgammaS binding assay
ChEMBL 449 9 0 5 3.6 C[C@@H]1CCCN1CCCOc1ccc(C(=O)CN2CCN(C(=O)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2012.02.081
CHEMBL2036635 81951 0 None - 1 Human 9.0 pEC50 = 9 Functional
Inverse agonist activity at human histamine H3 receptor by [35S]-GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor by [35S]-GTPgammaS binding assay
ChEMBL 449 9 0 5 3.6 C[C@@H]1CCCN1CCCOc1ccc(C(=O)CN2CCN(C(=O)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2012.02.081
11957573 8791 34 None -3 5 Rat 9.0 pEC50 = 9 Functional
The compound was evaluated for agonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uMThe compound was evaluated for agonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uM
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/S0960-894X(00)80219-X
1250 8791 34 None -3 5 Rat 9.0 pEC50 = 9 Functional
The compound was evaluated for agonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uMThe compound was evaluated for agonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uM
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/S0960-894X(00)80219-X
3692 8791 34 None -3 5 Rat 9.0 pEC50 = 9 Functional
The compound was evaluated for agonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uMThe compound was evaluated for agonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uM
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/S0960-894X(00)80219-X
CHEMBL19439 8791 34 None -3 5 Rat 9.0 pEC50 = 9 Functional
The compound was evaluated for agonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uMThe compound was evaluated for agonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uM
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/S0960-894X(00)80219-X
145956781 168985 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 552 7 1 5 5.7 COc1cc(N2C(=O)/C(=C\c3ccccc3)C2(C(=O)NC(C)(C)C)c2ccc(Cl)c(F)c2)cc(OC)c1OC 10.1016/j.ejmech.2018.04.020
CHEMBL4162793 168985 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 552 7 1 5 5.7 COc1cc(N2C(=O)/C(=C\c3ccccc3)C2(C(=O)NC(C)(C)C)c2ccc(Cl)c(F)c2)cc(OC)c1OC 10.1016/j.ejmech.2018.04.020
4024 8796 20 None 3388 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1 10.1021/jm100643t
9989505 8796 20 None 3388 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1 10.1021/jm100643t
CHEMBL82298 8796 20 None 3388 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1 10.1021/jm100643t
46912441 17674 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 309 3 1 2 3.9 FC(F)(F)c1ccc(N2CCC(Cc3c[nH]cn3)CC2)cc1 10.1016/j.bmc.2010.04.052
CHEMBL1172754 17674 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 309 3 1 2 3.9 FC(F)(F)c1ccc(N2CCC(Cc3c[nH]cn3)CC2)cc1 10.1016/j.bmc.2010.04.052
49799253 17777 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 259 3 1 2 3.0 Fc1ccc(N2CCC(Cc3c[nH]cn3)CC2)cc1 10.1016/j.bmc.2010.04.052
CHEMBL1173809 17777 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 259 3 1 2 3.0 Fc1ccc(N2CCC(Cc3c[nH]cn3)CC2)cc1 10.1016/j.bmc.2010.04.052
24996644 77198 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Inverse agonist activity at human histamine H3 histamine receptor by [35S]GTPgammaS binding assayInverse agonist activity at human histamine H3 histamine receptor by [35S]GTPgammaS binding assay
ChEMBL 339 4 1 4 3.1 Cc1n[nH]c(=O)cc1-c1ccc(OC2CCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2011.11.118
CHEMBL1945845 77198 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Inverse agonist activity at human histamine H3 histamine receptor by [35S]GTPgammaS binding assayInverse agonist activity at human histamine H3 histamine receptor by [35S]GTPgammaS binding assay
ChEMBL 339 4 1 4 3.1 Cc1n[nH]c(=O)cc1-c1ccc(OC2CCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2011.11.118
53363442 71162 0 None 1 2 Human 9.0 pEC50 = 9.0 Functional
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS binding
ChEMBL 313 6 1 4 2.7 C[C@@H]1CCCN1CCCOc1ccc(-c2cn[nH]c(=O)c2)cc1 10.1021/jm200401v
CHEMBL1813065 71162 0 None 1 2 Human 9.0 pEC50 = 9.0 Functional
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS binding
ChEMBL 313 6 1 4 2.7 C[C@@H]1CCCN1CCCOc1ccc(-c2cn[nH]c(=O)c2)cc1 10.1021/jm200401v
25070031 72159 18 None 1 2 Human 9.0 pEC50 = 9.0 Functional
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS binding
ChEMBL 313 6 1 4 2.7 C[C@@H]1CCCN1CCCOc1ccc(-c2ccc(=O)[nH]n2)cc1 10.1021/jm200401v
CHEMBL1829335 72159 18 None 1 2 Human 9.0 pEC50 = 9.0 Functional
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS binding
ChEMBL 313 6 1 4 2.7 C[C@@H]1CCCN1CCCOc1ccc(-c2ccc(=O)[nH]n2)cc1 10.1021/jm200401v
24993500 77483 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 325 4 1 4 2.8 O=c1ccc(-c2ccc(OC3CCN(C4CCC4)CC3)cc2)n[nH]1 10.1016/j.bmcl.2012.01.026
CHEMBL1950643 77483 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 325 4 1 4 2.8 O=c1ccc(-c2ccc(OC3CCN(C4CCC4)CC3)cc2)n[nH]1 10.1016/j.bmcl.2012.01.026
11538251 153696 0 None 4 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 385 4 0 5 4.6 Cc1cc2ncc(-c3ccc4cc(CCN5CCC[C@H]5C)ccc4n3)c(C)n2n1 10.1021/jm0705051
CHEMBL392573 153696 0 None 4 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 385 4 0 5 4.6 Cc1cc2ncc(-c3ccc4cc(CCN5CCC[C@H]5C)ccc4n3)c(C)n2n1 10.1021/jm0705051
145956781 168985 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 552 7 1 5 5.7 COc1cc(N2C(=O)/C(=C\c3ccccc3)C2(C(=O)NC(C)(C)C)c2ccc(Cl)c(F)c2)cc(OC)c1OC 10.1016/j.ejmech.2018.04.020
CHEMBL4162793 168985 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 552 7 1 5 5.7 COc1cc(N2C(=O)/C(=C\c3ccccc3)C2(C(=O)NC(C)(C)C)c2ccc(Cl)c(F)c2)cc(OC)c1OC 10.1016/j.ejmech.2018.04.020
11538251 153696 0 None 4 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 385 4 0 5 4.6 Cc1cc2ncc(-c3ccc4cc(CCN5CCC[C@H]5C)ccc4n3)c(C)n2n1 10.1021/jm0705051
CHEMBL392573 153696 0 None 4 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 385 4 0 5 4.6 Cc1cc2ncc(-c3ccc4cc(CCN5CCC[C@H]5C)ccc4n3)c(C)n2n1 10.1021/jm0705051
145954498 169188 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 458 5 1 4 5.4 COc1ccc(NC2(c3ccc(F)cc3)C(=O)N(C(C)(C)C)C(=O)/C2=C/c2ccccc2)cc1 10.1016/j.ejmech.2018.04.020
CHEMBL4165989 169188 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 458 5 1 4 5.4 COc1ccc(NC2(c3ccc(F)cc3)C(=O)N(C(C)(C)C)C(=O)/C2=C/c2ccccc2)cc1 10.1016/j.ejmech.2018.04.020
11708125 83294 3 None - 1 Human 8.9 pEC50 = 8.9 Functional
Activity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cellsActivity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cells
ChEMBL 167 5 1 2 1.3 CN(C)CCCCc1c[nH]cn1 10.1021/jm0504353
CHEMBL206000 83294 3 None - 1 Human 8.9 pEC50 = 8.9 Functional
Activity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cellsActivity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cells
ChEMBL 167 5 1 2 1.3 CN(C)CCCCc1c[nH]cn1 10.1021/jm0504353
89104074 183027 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 179 2 2 5 -0.5 CNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4466700 183027 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 179 2 2 5 -0.5 CNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4594865 183027 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 179 2 2 5 -0.5 CNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
145959298 169086 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 548 6 1 5 6.0 COc1ccc(NC2(c3ccc(Br)cc3)C(=O)N(C(C)(C)C)C(=O)/C2=C/c2ccccc2)cc1OC 10.1016/j.ejmech.2018.04.020
CHEMBL4164467 169086 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 548 6 1 5 6.0 COc1ccc(NC2(c3ccc(Br)cc3)C(=O)N(C(C)(C)C)C(=O)/C2=C/c2ccccc2)cc1OC 10.1016/j.ejmech.2018.04.020
1218 7017 52 None 19 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 330 4 0 3 5.0 N#Cc1ccc(cc1)c1ccc2c(c1)cc(o2)CCN1CCC[C@H]1C 10.1021/jm0705051
9818903 7017 52 None 19 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 330 4 0 3 5.0 N#Cc1ccc(cc1)c1ccc2c(c1)cc(o2)CCN1CCC[C@H]1C 10.1021/jm0705051
CHEMBL351231 7017 52 None 19 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 330 4 0 3 5.0 N#Cc1ccc(cc1)c1ccc2c(c1)cc(o2)CCN1CCC[C@H]1C 10.1021/jm0705051
1218 7017 52 None 19 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 330 4 0 3 5.0 N#Cc1ccc(cc1)c1ccc2c(c1)cc(o2)CCN1CCC[C@H]1C 10.1021/jm0705051
9818903 7017 52 None 19 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 330 4 0 3 5.0 N#Cc1ccc(cc1)c1ccc2c(c1)cc(o2)CCN1CCC[C@H]1C 10.1021/jm0705051
CHEMBL351231 7017 52 None 19 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 330 4 0 3 5.0 N#Cc1ccc(cc1)c1ccc2c(c1)cc(o2)CCN1CCC[C@H]1C 10.1021/jm0705051
145959298 169086 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 548 6 1 5 6.0 COc1ccc(NC2(c3ccc(Br)cc3)C(=O)N(C(C)(C)C)C(=O)/C2=C/c2ccccc2)cc1OC 10.1016/j.ejmech.2018.04.020
CHEMBL4164467 169086 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 548 6 1 5 6.0 COc1ccc(NC2(c3ccc(Br)cc3)C(=O)N(C(C)(C)C)C(=O)/C2=C/c2ccccc2)cc1OC 10.1016/j.ejmech.2018.04.020
145954498 169188 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 458 5 1 4 5.4 COc1ccc(NC2(c3ccc(F)cc3)C(=O)N(C(C)(C)C)C(=O)/C2=C/c2ccccc2)cc1 10.1016/j.ejmech.2018.04.020
CHEMBL4165989 169188 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 458 5 1 4 5.4 COc1ccc(NC2(c3ccc(F)cc3)C(=O)N(C(C)(C)C)C(=O)/C2=C/c2ccccc2)cc1 10.1016/j.ejmech.2018.04.020
53483937 72175 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity at human histamine 3 receptor by [35S]GTPgammaS binding assayAntagonist activity at human histamine 3 receptor by [35S]GTPgammaS binding assay
ChEMBL 345 6 0 5 2.8 C[C@@H]1CCCN1CCCOc1ccc(-c2ccc(=O)n(C)n2)cc1F 10.1016/j.bmcl.2011.06.108
CHEMBL1829477 72175 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity at human histamine 3 receptor by [35S]GTPgammaS binding assayAntagonist activity at human histamine 3 receptor by [35S]GTPgammaS binding assay
ChEMBL 345 6 0 5 2.8 C[C@@H]1CCCN1CCCOc1ccc(-c2ccc(=O)n(C)n2)cc1F 10.1016/j.bmcl.2011.06.108
57396087 77520 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 341 4 1 4 2.9 C[C@@H]1CC(=O)NN=C1c1ccc(OC2CCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2012.01.026
CHEMBL1950746 77520 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 341 4 1 4 2.9 C[C@@H]1CC(=O)NN=C1c1ccc(OC2CCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2012.01.026
57397654 76442 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Inverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assay
ChEMBL 329 6 1 4 2.8 CC1CC(=O)NN=C1c1ccc(OCCCN2CCC[C@H]2C)cc1 10.1016/j.bmcl.2011.11.037
CHEMBL1935111 76442 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Inverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assay
ChEMBL 329 6 1 4 2.8 CC1CC(=O)NN=C1c1ccc(OCCCN2CCC[C@H]2C)cc1 10.1016/j.bmcl.2011.11.037
57397654 76442 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Inverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assay
ChEMBL 329 6 1 4 2.8 CC1CC(=O)NN=C1c1ccc(OCCCN2CCC[C@H]2C)cc1 10.1016/j.bmcl.2011.11.037
CHEMBL1935111 76442 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Inverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assay
ChEMBL 329 6 1 4 2.8 CC1CC(=O)NN=C1c1ccc(OCCCN2CCC[C@H]2C)cc1 10.1016/j.bmcl.2011.11.037
11603648 154966 0 None 2 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 397 5 0 5 4.8 Cc1c(-c2ccc3cc(CCN4CCC[C@H]4C)ccc3n2)cnn1-c1ccccn1 10.1021/jm0705051
CHEMBL393581 154966 0 None 2 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 397 5 0 5 4.8 Cc1c(-c2ccc3cc(CCN4CCC[C@H]4C)ccc3n2)cnn1-c1ccccn1 10.1021/jm0705051
11603648 154966 0 None 2 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 397 5 0 5 4.8 Cc1c(-c2ccc3cc(CCN4CCC[C@H]4C)ccc3n2)cnn1-c1ccccn1 10.1021/jm0705051
CHEMBL393581 154966 0 None 2 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 397 5 0 5 4.8 Cc1c(-c2ccc3cc(CCN4CCC[C@H]4C)ccc3n2)cnn1-c1ccccn1 10.1021/jm0705051
5048 9907 64 None 10 5 Guinea pig 8.8 pEC50 = 8.8 Functional
Antagonist activity at human histamine H3 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAntagonist activity at human histamine H3 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.1016/j.bmc.2009.03.014
8924 9907 64 None 10 5 Guinea pig 8.8 pEC50 = 8.8 Functional
Antagonist activity at human histamine H3 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAntagonist activity at human histamine H3 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.1016/j.bmc.2009.03.014
9948102 9907 64 None 10 5 Guinea pig 8.8 pEC50 = 8.8 Functional
Antagonist activity at human histamine H3 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAntagonist activity at human histamine H3 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.1016/j.bmc.2009.03.014
CHEMBL462605 9907 64 None 10 5 Guinea pig 8.8 pEC50 = 8.8 Functional
Antagonist activity at human histamine H3 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAntagonist activity at human histamine H3 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.1016/j.bmc.2009.03.014
DB11642 9907 64 None 10 5 Guinea pig 8.8 pEC50 = 8.8 Functional
Antagonist activity at human histamine H3 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAntagonist activity at human histamine H3 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 10.1016/j.bmc.2009.03.014
11710694 103354 0 None 4 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 382 4 0 4 5.2 Cc1nc2ncccc2cc1-c1ccc2cc(CCN3CCC[C@H]3C)ccc2n1 10.1021/jm0705051
CHEMBL263101 103354 0 None 4 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 382 4 0 4 5.2 Cc1nc2ncccc2cc1-c1ccc2cc(CCN3CCC[C@H]3C)ccc2n1 10.1021/jm0705051
11710694 103354 0 None 4 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 382 4 0 4 5.2 Cc1nc2ncccc2cc1-c1ccc2cc(CCN3CCC[C@H]3C)ccc2n1 10.1021/jm0705051
CHEMBL263101 103354 0 None 4 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 382 4 0 4 5.2 Cc1nc2ncccc2cc1-c1ccc2cc(CCN3CCC[C@H]3C)ccc2n1 10.1021/jm0705051
11689509 116215 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation countingInverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation counting
ChEMBL 383 8 0 5 4.6 c1cc(-c2nc(CN3CCCCC3)co2)ccc1OCCCN1CCCCC1 10.1039/C0MD00056F
CHEMBL3220124 116215 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation countingInverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation counting
ChEMBL 383 8 0 5 4.6 c1cc(-c2nc(CN3CCCCC3)co2)ccc1OCCCN1CCCCC1 10.1039/C0MD00056F
90666846 116217 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation countingInverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation counting
ChEMBL 370 5 0 6 3.8 COC(=O)c1oc(-c2ccc(O[C@H]3C[C@H](N4CCCCC4)C3)cc2)nc1C 10.1039/C0MD00056F
CHEMBL3220126 116217 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation countingInverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation counting
ChEMBL 370 5 0 6 3.8 COC(=O)c1oc(-c2ccc(O[C@H]3C[C@H](N4CCCCC4)C3)cc2)nc1C 10.1039/C0MD00056F
46222045 15553 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 243 4 2 2 3.4 CC(C)(C)c1ccc(NCCc2c[nH]cn2)cc1 10.1021/jm901890s
CHEMBL1096516 15553 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 243 4 2 2 3.4 CC(C)(C)c1ccc(NCCc2c[nH]cn2)cc1 10.1021/jm901890s
49799184 17742 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 291 3 1 2 4.0 c1ccc2cc(N3CCC(Cc4c[nH]cn4)CC3)ccc2c1 10.1016/j.bmc.2010.04.052
CHEMBL1173390 17742 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 291 3 1 2 4.0 c1ccc2cc(N3CCC(Cc4c[nH]cn4)CC3)ccc2c1 10.1016/j.bmc.2010.04.052
57403054 77521 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 341 4 1 4 2.9 C[C@H]1CC(=O)NN=C1c1ccc(OC2CCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2012.01.026
CHEMBL1950747 77521 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 341 4 1 4 2.9 C[C@H]1CC(=O)NN=C1c1ccc(OC2CCN(C3CCC3)CC2)cc1 10.1016/j.bmcl.2012.01.026
156013896 185019 0 None 3 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human H3R expressed in HEK293T-SP-FLAG-hH3R-CRE-CBR cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H3R expressed in HEK293T-SP-FLAG-hH3R-CRE-CBR cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4635634 185019 0 None 3 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human H3R expressed in HEK293T-SP-FLAG-hH3R-CRE-CBR cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H3R expressed in HEK293T-SP-FLAG-hH3R-CRE-CBR cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4650570 185019 0 None 3 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human H3R expressed in HEK293T-SP-FLAG-hH3R-CRE-CBR cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H3R expressed in HEK293T-SP-FLAG-hH3R-CRE-CBR cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
49799537 17332 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 270 4 2 3 2.9 CNc1ccc(N2CCC(Cc3c[nH]cn3)CC2)cc1 10.1016/j.bmc.2010.04.052
CHEMBL1169687 17332 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 270 4 2 3 2.9 CNc1ccc(N2CCC(Cc3c[nH]cn3)CC2)cc1 10.1016/j.bmc.2010.04.052
59651957 81578 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Inverse agonist activity at human H3 receptor by [35S]GTPgamma binding assayInverse agonist activity at human H3 receptor by [35S]GTPgamma binding assay
ChEMBL 353 5 0 5 2.8 C[C@@H]1CCCN1CCCOc1ccc2c(c1)CCc1cc(=O)n(C)nc1-2 10.1016/j.bmcl.2012.04.001
CHEMBL2031470 81578 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Inverse agonist activity at human H3 receptor by [35S]GTPgamma binding assayInverse agonist activity at human H3 receptor by [35S]GTPgamma binding assay
ChEMBL 353 5 0 5 2.8 C[C@@H]1CCCN1CCCOc1ccc2c(c1)CCc1cc(=O)n(C)nc1-2 10.1016/j.bmcl.2012.04.001
1223 7740 41 None -1 4 Mouse 8.8 pEC50 = 8.8 Functional
Inverse agonist activity at mouse histamine H3 receptor overexpressed in HEK293 cells by [35S]GTPgammaS binding assayInverse agonist activity at mouse histamine H3 receptor overexpressed in HEK293 cells by [35S]GTPgammaS binding assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1016/j.bmcl.2009.06.025
2790 7740 41 None -1 4 Mouse 8.8 pEC50 = 8.8 Functional
Inverse agonist activity at mouse histamine H3 receptor overexpressed in HEK293 cells by [35S]GTPgammaS binding assayInverse agonist activity at mouse histamine H3 receptor overexpressed in HEK293 cells by [35S]GTPgammaS binding assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1016/j.bmcl.2009.06.025
CHEMBL14690 7740 41 None -1 4 Mouse 8.8 pEC50 = 8.8 Functional
Inverse agonist activity at mouse histamine H3 receptor overexpressed in HEK293 cells by [35S]GTPgammaS binding assayInverse agonist activity at mouse histamine H3 receptor overexpressed in HEK293 cells by [35S]GTPgammaS binding assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1016/j.bmcl.2009.06.025
56954322 88855 0 None 3 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human H3R-Galphai2-Gbeta1gamma2-RGS4 expressed in Sf9 cells 0.1 nM to 1 mM by steady state GTPase activity assayAgonist activity at human H3R-Galphai2-Gbeta1gamma2-RGS4 expressed in Sf9 cells 0.1 nM to 1 mM by steady state GTPase activity assay
ChEMBL 500 17 6 4 1.7 N/C(=N\C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1 10.1021/jm201128q
CHEMBL2165642 88855 0 None 3 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human H3R-Galphai2-Gbeta1gamma2-RGS4 expressed in Sf9 cells 0.1 nM to 1 mM by steady state GTPase activity assayAgonist activity at human H3R-Galphai2-Gbeta1gamma2-RGS4 expressed in Sf9 cells 0.1 nM to 1 mM by steady state GTPase activity assay
ChEMBL 500 17 6 4 1.7 N/C(=N\C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1 10.1021/jm201128q
49857998 81954 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Inverse agonist activity at human histamine H3 receptor by [35S]-GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor by [35S]-GTPgammaS binding assay
ChEMBL 380 8 0 4 3.9 C[C@@H]1CCCN1CCCOc1ccc(C(=O)CN2CCC(F)(F)CC2)cc1 10.1016/j.bmcl.2012.02.081
CHEMBL2036643 81954 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Inverse agonist activity at human histamine H3 receptor by [35S]-GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor by [35S]-GTPgammaS binding assay
ChEMBL 380 8 0 4 3.9 C[C@@H]1CCCN1CCCOc1ccc(C(=O)CN2CCC(F)(F)CC2)cc1 10.1016/j.bmcl.2012.02.081
155540793 183061 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 221 4 2 5 0.6 CCC(C)NC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4516714 183061 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 221 4 2 5 0.6 CCC(C)NC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4595102 183061 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 221 4 2 5 0.6 CCC(C)NC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
24825522 194422 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 283 3 1 3 3.3 CC1CC(C)(C)N=C(c2cccc(Cc3c[nH]cn3)c2)O1 10.1021/jm7014149
CHEMBL494982 194422 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 283 3 1 3 3.3 CC1CC(C)(C)N=C(c2cccc(Cc3c[nH]cn3)c2)O1 10.1021/jm7014149
16059780 176173 0 None -1 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 334 4 0 4 4.0 Cc1nn(C)cc1-c1ccc2cc(CCN3CCC[C@H]3C)ccc2n1 10.1021/jm0705051
CHEMBL442242 176173 0 None -1 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 334 4 0 4 4.0 Cc1nn(C)cc1-c1ccc2cc(CCN3CCC[C@H]3C)ccc2n1 10.1021/jm0705051
90666844 116213 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation countingInverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation counting
ChEMBL 368 4 0 4 4.6 c1cc(C2=NC3(CCCCC3)CO2)ccc1O[C@H]1C[C@H](N2CCCCC2)C1 10.1039/C0MD00056F
CHEMBL3220122 116213 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation countingInverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation counting
ChEMBL 368 4 0 4 4.6 c1cc(C2=NC3(CCCCC3)CO2)ccc1O[C@H]1C[C@H](N2CCCCC2)C1 10.1039/C0MD00056F
11600849 147322 0 None - 1 Human 8.0 pEC50 = 8 Functional
Activity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cellsActivity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cells
ChEMBL 195 8 2 2 2.1 CCCNCCCCCc1c[nH]cn1 10.1021/jm0504353
CHEMBL381074 147322 0 None - 1 Human 8.0 pEC50 = 8 Functional
Activity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cellsActivity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cells
ChEMBL 195 8 2 2 2.1 CCCNCCCCCc1c[nH]cn1 10.1021/jm0504353
145951678 169727 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 406 2 1 3 2.7 O=C1C=C[C@]23C(c4ccccc4)=CC(=O)N2[C@H](c2cc(F)cc(F)c2)C(=O)N[C@@H]3C1 10.1016/j.ejmech.2018.04.020
CHEMBL4174591 169727 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 406 2 1 3 2.7 O=C1C=C[C@]23C(c4ccccc4)=CC(=O)N2[C@H](c2cc(F)cc(F)c2)C(=O)N[C@@H]3C1 10.1016/j.ejmech.2018.04.020
141272770 183168 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 193 2 2 5 -0.2 CNC1CN(c2cc(C)nc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4468740 183168 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 193 2 2 5 -0.2 CNC1CN(c2cc(C)nc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4595912 183168 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 193 2 2 5 -0.2 CNC1CN(c2cc(C)nc(N)n2)C1 10.1021/acs.jmedchem.9b01462
1238 8863 13 None 1258 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 2 2 2 0.3 C[C@@H](Cc1cnc[nH]1)N 10.1016/j.bmcl.2010.10.041
6603865 8863 13 None 1258 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 2 2 2 0.3 C[C@@H](Cc1cnc[nH]1)N 10.1016/j.bmcl.2010.10.041
CHEMBL11919 8863 13 None 1258 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 2 2 2 0.3 C[C@@H](Cc1cnc[nH]1)N 10.1016/j.bmcl.2010.10.041
145951678 169727 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 406 2 1 3 2.7 O=C1C=C[C@]23C(c4ccccc4)=CC(=O)N2[C@H](c2cc(F)cc(F)c2)C(=O)N[C@@H]3C1 10.1016/j.ejmech.2018.04.020
CHEMBL4174591 169727 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 406 2 1 3 2.7 O=C1C=C[C@]23C(c4ccccc4)=CC(=O)N2[C@H](c2cc(F)cc(F)c2)C(=O)N[C@@H]3C1 10.1016/j.ejmech.2018.04.020
155541911 179850 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 235 3 1 5 0.9 CC(C)c1cc(N2CC(N(C)C)C2)nc(N)n1 10.1021/acs.jmedchem.9b01462
CHEMBL4519616 179850 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 235 3 1 5 0.9 CC(C)c1cc(N2CC(N(C)C)C2)nc(N)n1 10.1021/acs.jmedchem.9b01462
10978141 11922 1 None 7 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@H]2CC[C@H](c3c[nH]cn3)O2)cc1 10.1016/j.bmcl.2010.10.041
CHEMBL105803 11922 1 None 7 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@H]2CC[C@H](c3c[nH]cn3)O2)cc1 10.1016/j.bmcl.2010.10.041
10678661 12134 1 None 309 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 167 2 2 3 0.6 NC[C@@H]1CC[C@@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
CHEMBL106931 12134 1 None 309 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 167 2 2 3 0.6 NC[C@@H]1CC[C@@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
1267 10576 49 None -9 5 Human 7.0 pEC50 = 7 Functional
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation countingInverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation counting
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1039/C0MD00056F
3035905 10576 49 None -9 5 Human 7.0 pEC50 = 7 Functional
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation countingInverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation counting
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1039/C0MD00056F
CHEMBL260374 10576 49 None -9 5 Human 7.0 pEC50 = 7 Functional
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation countingInverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation counting
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1039/C0MD00056F
10037650 11981 0 None -47 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
CHEMBL106158 11981 0 None -47 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
11043445 63253 1 None 1 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@H]2CC[C@@H](c3c[nH]cn3)O2)cc1 10.1016/j.bmcl.2010.10.041
CHEMBL1632410 63253 1 None 1 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@H]2CC[C@@H](c3c[nH]cn3)O2)cc1 10.1016/j.bmcl.2010.10.041
10945113 116406 1 None 1 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@@H]2CC[C@@H](c3c[nH]cn3)O2)cc1 10.1016/j.bmcl.2010.10.041
CHEMBL322256 116406 1 None 1 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@@H]2CC[C@@H](c3c[nH]cn3)O2)cc1 10.1016/j.bmcl.2010.10.041
10037650 11981 0 None -47 2 Human 5.0 pEC50 = 5.0 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptor
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL106158 11981 0 None -47 2 Human 5.0 pEC50 = 5.0 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptor
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
145953579 169230 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 486 5 1 3 5.2 O=C1C=CC2(C=C1)C(c1ccccc1)=CC(=O)N2C(C(=O)NC1CCCCC1)c1ccc(Cl)cc1 10.1016/j.ejmech.2018.04.020
CHEMBL4166645 169230 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 486 5 1 3 5.2 O=C1C=CC2(C=C1)C(c1ccccc1)=CC(=O)N2C(C(=O)NC1CCCCC1)c1ccc(Cl)cc1 10.1016/j.ejmech.2018.04.020
145952741 169281 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 544 8 1 5 5.6 COc1cc(N2C(=O)/C(=C\c3ccccc3)C2(C(=O)NC2CCCCC2)c2ccc(F)cc2)cc(OC)c1OC 10.1016/j.ejmech.2018.04.020
CHEMBL4167482 169281 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 544 8 1 5 5.6 COc1cc(N2C(=O)/C(=C\c3ccccc3)C2(C(=O)NC2CCCCC2)c2ccc(F)cc2)cc(OC)c1OC 10.1016/j.ejmech.2018.04.020
145953579 169230 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 486 5 1 3 5.2 O=C1C=CC2(C=C1)C(c1ccccc1)=CC(=O)N2C(C(=O)NC1CCCCC1)c1ccc(Cl)cc1 10.1016/j.ejmech.2018.04.020
CHEMBL4166645 169230 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 486 5 1 3 5.2 O=C1C=CC2(C=C1)C(c1ccccc1)=CC(=O)N2C(C(=O)NC1CCCCC1)c1ccc(Cl)cc1 10.1016/j.ejmech.2018.04.020
10678661 12134 1 None 309 2 Human 7.0 pEC50 = 7.0 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptor
ChEMBL 167 2 2 3 0.6 NC[C@@H]1CC[C@@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL106931 12134 1 None 309 2 Human 7.0 pEC50 = 7.0 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptor
ChEMBL 167 2 2 3 0.6 NC[C@@H]1CC[C@@H](c2c[nH]cn2)O1 10.1021/jm0300025
12769844 116255 0 None 3 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
ChEMBL 234 5 3 3 0.7 CN/C(=N/C#N)NCCCCc1nc[nH]c1C 10.1039/C3MD00245D
CHEMBL3220641 116255 0 None 3 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
ChEMBL 234 5 3 3 0.7 CN/C(=N/C#N)NCCCCc1nc[nH]c1C 10.1039/C3MD00245D
1267 10576 49 None 8 5 Mouse 8.0 pEC50 = 8.0 Functional
Inverse agonist activity at mouse histamine H3 receptor overexpressed in HEK293 cells by [35S]GTPgammaS binding assayInverse agonist activity at mouse histamine H3 receptor overexpressed in HEK293 cells by [35S]GTPgammaS binding assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmcl.2009.06.025
3035905 10576 49 None 8 5 Mouse 8.0 pEC50 = 8.0 Functional
Inverse agonist activity at mouse histamine H3 receptor overexpressed in HEK293 cells by [35S]GTPgammaS binding assayInverse agonist activity at mouse histamine H3 receptor overexpressed in HEK293 cells by [35S]GTPgammaS binding assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmcl.2009.06.025
CHEMBL260374 10576 49 None 8 5 Mouse 8.0 pEC50 = 8.0 Functional
Inverse agonist activity at mouse histamine H3 receptor overexpressed in HEK293 cells by [35S]GTPgammaS binding assayInverse agonist activity at mouse histamine H3 receptor overexpressed in HEK293 cells by [35S]GTPgammaS binding assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmcl.2009.06.025
49799507 17664 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 283 4 1 2 4.0 CC(C)c1ccc(N2CCC(Cc3c[nH]cn3)CC2)cc1 10.1016/j.bmc.2010.04.052
CHEMBL1172712 17664 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 283 4 1 2 4.0 CC(C)c1ccc(N2CCC(Cc3c[nH]cn3)CC2)cc1 10.1016/j.bmc.2010.04.052
16678620 24161 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 418 5 0 5 3.9 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCN(Cc3ccncc3)C2=O)CC1 10.1016/j.bmcl.2010.08.009
CHEMBL1257487 24161 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 418 5 0 5 3.9 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCN(Cc3ccncc3)C2=O)CC1 10.1016/j.bmcl.2010.08.009
155533940 178642 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 207 3 2 5 0.2 CCNC1CN(c2cc(C)nc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4469111 178642 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 207 3 2 5 0.2 CCNC1CN(c2cc(C)nc(N)n2)C1 10.1021/acs.jmedchem.9b01462
42623731 178749 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 221 3 2 5 0.6 CNC1CN(c2cc(C(C)C)nc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4470781 178749 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 221 3 2 5 0.6 CNC1CN(c2cc(C(C)C)nc(N)n2)C1 10.1021/acs.jmedchem.9b01462
10176370 50109 11 None - 1 Human 7.9 pEC50 = 7.9 Functional
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
ChEMBL 179 3 2 2 1.3 c1nc(CCC2CCNCC2)c[nH]1 10.1021/jm049475h
CHEMBL150701 50109 11 None - 1 Human 7.9 pEC50 = 7.9 Functional
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
ChEMBL 179 3 2 2 1.3 c1nc(CCC2CCNCC2)c[nH]1 10.1021/jm049475h
1204 8713 119 None -2 11 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
1247 8713 119 None -2 11 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
1375 8713 119 None -2 11 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
774 8713 119 None -2 11 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
CHEMBL90 8713 119 None -2 11 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
DB05381 8713 119 None -2 11 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
1269 6909 41 None -275 6 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1021/acs.jmedchem.6b00120
37463 6909 41 None -275 6 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1021/acs.jmedchem.6b00120
CHEMBL275443 6909 41 None -275 6 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1021/acs.jmedchem.6b00120
155527111 177901 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human H3R expressed on cells incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at recombinant human H3R expressed on cells incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 579 8 2 8 3.8 CCCCC(=O)O[C@@H]1C[C@H](C)N2C[C@]3(NC)C[C@]4(C(=O)Nc5c(C(=O)[C@H]6OC6(C)C)cccc54)[C@](C)(C=O)[C@H]3C[C@H]2C1 10.1021/acs.jmedchem.9b01462
CHEMBL4458116 177901 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human H3R expressed on cells incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at recombinant human H3R expressed on cells incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 579 8 2 8 3.8 CCCCC(=O)O[C@@H]1C[C@H](C)N2C[C@]3(NC)C[C@]4(C(=O)Nc5c(C(=O)[C@H]6OC6(C)C)cccc54)[C@](C)(C=O)[C@H]3C[C@H]2C1 10.1021/acs.jmedchem.9b01462
145957226 168920 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 686 9 1 6 7.1 COc1ccc(C(C(=O)NC2CCCCC2)N2C(=O)C(c3ccc(C(F)(F)F)cc3)=C(c3ccccc3)C23C=CC(=O)C=C3)c(OC)c1OC 10.1016/j.ejmech.2018.04.020
CHEMBL4161732 168920 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 686 9 1 6 7.1 COc1ccc(C(C(=O)NC2CCCCC2)N2C(=O)C(c3ccc(C(F)(F)F)cc3)=C(c3ccccc3)C23C=CC(=O)C=C3)c(OC)c1OC 10.1016/j.ejmech.2018.04.020
1204 8713 119 None -2 11 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
1247 8713 119 None -2 11 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
1375 8713 119 None -2 11 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
774 8713 119 None -2 11 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
CHEMBL90 8713 119 None -2 11 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
DB05381 8713 119 None -2 11 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
16678619 24160 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 418 5 0 5 3.9 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCN(Cc3cccnc3)C2=O)CC1 10.1016/j.bmcl.2010.08.009
CHEMBL1257486 24160 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 418 5 0 5 3.9 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCN(Cc3cccnc3)C2=O)CC1 10.1016/j.bmcl.2010.08.009
145957226 168920 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 686 9 1 6 7.1 COc1ccc(C(C(=O)NC2CCCCC2)N2C(=O)C(c3ccc(C(F)(F)F)cc3)=C(c3ccccc3)C23C=CC(=O)C=C3)c(OC)c1OC 10.1016/j.ejmech.2018.04.020
CHEMBL4161732 168920 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 686 9 1 6 7.1 COc1ccc(C(C(=O)NC2CCCCC2)N2C(=O)C(c3ccc(C(F)(F)F)cc3)=C(c3ccccc3)C23C=CC(=O)C=C3)c(OC)c1OC 10.1016/j.ejmech.2018.04.020
9877454 212392 2 None 11 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 159 2 1 2 1.4 c1ccc(Cc2c[nH]cn2)nc1 10.1021/jm100643t
CHEMBL81644 212392 2 None 11 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 159 2 1 2 1.4 c1ccc(Cc2c[nH]cn2)nc1 10.1021/jm100643t
11378681 18113 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Effect on specific [35S]GTP-gamma-S, Binding to HEK293 cell membranes expressing the human Histamine H3 receptorEffect on specific [35S]GTP-gamma-S, Binding to HEK293 cell membranes expressing the human Histamine H3 receptor
ChEMBL 164 5 1 2 1.0 C#CCOCCCc1c[nH]cn1 10.1021/jm031065q
CHEMBL1179608 18113 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Effect on specific [35S]GTP-gamma-S, Binding to HEK293 cell membranes expressing the human Histamine H3 receptorEffect on specific [35S]GTP-gamma-S, Binding to HEK293 cell membranes expressing the human Histamine H3 receptor
ChEMBL 164 5 1 2 1.0 C#CCOCCCc1c[nH]cn1 10.1021/jm031065q
CHEMBL88958 18113 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Effect on specific [35S]GTP-gamma-S, Binding to HEK293 cell membranes expressing the human Histamine H3 receptorEffect on specific [35S]GTP-gamma-S, Binding to HEK293 cell membranes expressing the human Histamine H3 receptor
ChEMBL 164 5 1 2 1.0 C#CCOCCCc1c[nH]cn1 10.1021/jm031065q
16678616 24123 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 435 5 0 4 4.7 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCN(Cc3ccc(F)cc3)C2=O)CC1 10.1016/j.bmcl.2010.08.009
CHEMBL1257376 24123 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 435 5 0 4 4.7 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCN(Cc3ccc(F)cc3)C2=O)CC1 10.1016/j.bmcl.2010.08.009
16678618 24124 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 418 5 0 5 3.9 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCN(Cc3ccccn3)C2=O)CC1 10.1016/j.bmcl.2010.08.009
CHEMBL1257377 24124 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 418 5 0 5 3.9 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCN(Cc3ccccn3)C2=O)CC1 10.1016/j.bmcl.2010.08.009
16679616 24276 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 341 3 1 4 3.0 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3C[C@H](C)NC2=O)CC1 10.1016/j.bmcl.2010.08.009
CHEMBL1257850 24276 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 341 3 1 4 3.0 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3C[C@H](C)NC2=O)CC1 10.1016/j.bmcl.2010.08.009
145954176 169416 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 680 7 1 6 6.6 COc1ccc(C2=C(c3ccccc3)C3(C=CC(=O)C=C3)N(C(C(=O)NC3CCCCC3)c3cc4c(cc3Br)OCO4)C2=O)cc1 10.1016/j.ejmech.2018.04.020
CHEMBL4169663 169416 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 680 7 1 6 6.6 COc1ccc(C2=C(c3ccccc3)C3(C=CC(=O)C=C3)N(C(C(=O)NC3CCCCC3)c3cc4c(cc3Br)OCO4)C2=O)cc1 10.1016/j.ejmech.2018.04.020
145954176 169416 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 680 7 1 6 6.6 COc1ccc(C2=C(c3ccccc3)C3(C=CC(=O)C=C3)N(C(C(=O)NC3CCCCC3)c3cc4c(cc3Br)OCO4)C2=O)cc1 10.1016/j.ejmech.2018.04.020
CHEMBL4169663 169416 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 680 7 1 6 6.6 COc1ccc(C2=C(c3ccccc3)C3(C=CC(=O)C=C3)N(C(C(=O)NC3CCCCC3)c3cc4c(cc3Br)OCO4)C2=O)cc1 10.1016/j.ejmech.2018.04.020
46929554 23526 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 349 5 1 3 4.7 FC(F)(F)c1ccc(SCC(c2ccncc2)c2c[nH]cn2)cc1 10.1021/jm100643t
CHEMBL1243367 23526 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 349 5 1 3 4.7 FC(F)(F)c1ccc(SCC(c2ccncc2)c2c[nH]cn2)cc1 10.1021/jm100643t
46929556 23529 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 337 5 1 3 5.0 CC(C)(C)c1ccc(SCC(c2ccncc2)c2c[nH]cn2)cc1 10.1021/jm100643t
CHEMBL1243393 23529 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 337 5 1 3 5.0 CC(C)(C)c1ccc(SCC(c2ccncc2)c2c[nH]cn2)cc1 10.1021/jm100643t
9812843 212023 1 None 204 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 159 2 1 2 1.4 c1cncc(Cc2c[nH]cn2)c1 10.1021/jm100643t
CHEMBL78838 212023 1 None 204 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 159 2 1 2 1.4 c1cncc(Cc2c[nH]cn2)c1 10.1021/jm100643t
16679704 24375 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 327 5 1 4 2.6 C[C@H]1CCCN1CCCOc1ccc2c(c1)cc1n2CCNC1=O 10.1016/j.bmcl.2010.08.009
CHEMBL1258194 24375 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 327 5 1 4 2.6 C[C@H]1CCCN1CCCOc1ccc2c(c1)cc1n2CCNC1=O 10.1016/j.bmcl.2010.08.009
46929551 23516 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 337 5 1 3 5.0 CC(C)(C)c1ccc(SCC(c2ccccn2)c2c[nH]cn2)cc1 10.1021/jm100643t
CHEMBL1243335 23516 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 337 5 1 3 5.0 CC(C)(C)c1ccc(SCC(c2ccccn2)c2c[nH]cn2)cc1 10.1021/jm100643t
10219715 20575 0 None - 1 Rat 7.8 pEC50 = 7.8 Functional
The compound was evaluated for agonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uMThe compound was evaluated for agonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uM
ChEMBL 184 3 3 3 0.8 CNC(=N)SCCc1c[nH]cn1 10.1016/S0960-894X(00)80219-X
CHEMBL1195600 20575 0 None - 1 Rat 7.8 pEC50 = 7.8 Functional
The compound was evaluated for agonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uMThe compound was evaluated for agonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uM
ChEMBL 184 3 3 3 0.8 CNC(=N)SCCc1c[nH]cn1 10.1016/S0960-894X(00)80219-X
CHEMBL554956 20575 0 None - 1 Rat 7.8 pEC50 = 7.8 Functional
The compound was evaluated for agonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uMThe compound was evaluated for agonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uM
ChEMBL 184 3 3 3 0.8 CNC(=N)SCCc1c[nH]cn1 10.1016/S0960-894X(00)80219-X
11600779 82823 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Activity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cellsActivity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cells
ChEMBL 181 7 2 2 1.7 CCCNCCCCc1c[nH]cn1 10.1021/jm0504353
CHEMBL205731 82823 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Activity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cellsActivity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cells
ChEMBL 181 7 2 2 1.7 CCCNCCCCc1c[nH]cn1 10.1021/jm0504353
155533291 178620 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 179 1 2 5 -0.5 Cc1cc(N2CC(N)C2)nc(N)n1 10.1021/acs.jmedchem.9b01462
CHEMBL4468827 178620 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 179 1 2 5 -0.5 Cc1cc(N2CC(N)C2)nc(N)n1 10.1021/acs.jmedchem.9b01462
24825510 194502 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 255 3 1 3 2.6 CC1(C)COC(c2cccc(Cc3c[nH]cn3)c2)=N1 10.1021/jm7014149
CHEMBL495376 194502 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 255 3 1 3 2.6 CC1(C)COC(c2cccc(Cc3c[nH]cn3)c2)=N1 10.1021/jm7014149
1204 8713 119 None -2 11 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assayAgonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm1013488
1247 8713 119 None -2 11 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assayAgonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm1013488
1375 8713 119 None -2 11 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assayAgonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm1013488
774 8713 119 None -2 11 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assayAgonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm1013488
CHEMBL90 8713 119 None -2 11 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assayAgonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm1013488
DB05381 8713 119 None -2 11 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assayAgonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm1013488
11418968 70127 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
ChEMBL 267 4 1 2 3.1 C(=C1CCN(CCc2ccccc2)CC1)c1c[nH]cn1 10.1021/jm049475h
CHEMBL179479 70127 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
ChEMBL 267 4 1 2 3.1 C(=C1CCN(CCc2ccccc2)CC1)c1c[nH]cn1 10.1021/jm049475h
11327520 139349 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
ChEMBL 255 4 1 2 2.9 c1ccc(CN2CCC(Cc3c[nH]cn3)CC2)cc1 10.1021/jm049475h
CHEMBL369819 139349 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
ChEMBL 255 4 1 2 2.9 c1ccc(CN2CCC(Cc3c[nH]cn3)CC2)cc1 10.1021/jm049475h
11702447 116209 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation countingInverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation counting
ChEMBL 316 6 0 4 3.5 CC1(C)COC(c2ccc(OCCCN3CCCCC3)cc2)=N1 10.1039/C0MD00056F
CHEMBL3220119 116209 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation countingInverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation counting
ChEMBL 316 6 0 4 3.5 CC1(C)COC(c2ccc(OCCCN3CCCCC3)cc2)=N1 10.1039/C0MD00056F
127052634 147087 0 None -6 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 272 4 3 3 1.5 N#C/N=C(\NC[C@@H]1CC[C@H](c2c[nH]cn2)C1)NC1CC1 10.1021/acs.jmedchem.6b00120
CHEMBL3806146 147087 0 None -6 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 272 4 3 3 1.5 N#C/N=C(\NC[C@@H]1CC[C@H](c2c[nH]cn2)C1)NC1CC1 10.1021/acs.jmedchem.6b00120
132938089 174350 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Antagonist activity at recombinant human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation after 30 mins by TR-FRET TR-FRET assayAntagonist activity at recombinant human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation after 30 mins by TR-FRET TR-FRET assay
ChEMBL 317 9 0 2 5.4 CCC(C)(C)c1ccc(OCCCCCN2CCCCC2)cc1 10.1016/j.bmc.2017.03.031
CHEMBL4227989 174350 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Antagonist activity at recombinant human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation after 30 mins by TR-FRET TR-FRET assayAntagonist activity at recombinant human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation after 30 mins by TR-FRET TR-FRET assay
ChEMBL 317 9 0 2 5.4 CCC(C)(C)c1ccc(OCCCCCN2CCCCC2)cc1 10.1016/j.bmc.2017.03.031
CHEMBL4300613 174350 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Antagonist activity at recombinant human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation after 30 mins by TR-FRET TR-FRET assayAntagonist activity at recombinant human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation after 30 mins by TR-FRET TR-FRET assay
ChEMBL 317 9 0 2 5.4 CCC(C)(C)c1ccc(OCCCCCN2CCCCC2)cc1 10.1016/j.bmc.2017.03.031
155513736 176565 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 235 4 2 5 1.0 CCNC1CN(c2cc(C(C)C)nc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4439165 176565 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 235 4 2 5 1.0 CCNC1CN(c2cc(C(C)C)nc(N)n2)C1 10.1021/acs.jmedchem.9b01462
145946358 174305 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Antagonist activity at recombinant human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation after 30 mins by TR-FRET TR-FRET assayAntagonist activity at recombinant human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation after 30 mins by TR-FRET TR-FRET assay
ChEMBL 331 9 0 2 5.7 CCC(C)(C)c1ccc(OCCCCCN2CCCC(C)C2)cc1 10.1016/j.bmc.2017.03.031
CHEMBL4225644 174305 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Antagonist activity at recombinant human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation after 30 mins by TR-FRET TR-FRET assayAntagonist activity at recombinant human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation after 30 mins by TR-FRET TR-FRET assay
ChEMBL 331 9 0 2 5.7 CCC(C)(C)c1ccc(OCCCCCN2CCCC(C)C2)cc1 10.1016/j.bmc.2017.03.031
CHEMBL4300100 174305 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Antagonist activity at recombinant human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation after 30 mins by TR-FRET TR-FRET assayAntagonist activity at recombinant human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation after 30 mins by TR-FRET TR-FRET assay
ChEMBL 331 9 0 2 5.7 CCC(C)(C)c1ccc(OCCCCCN2CCCC(C)C2)cc1 10.1016/j.bmc.2017.03.031
44249906 201699 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 382 4 0 4 3.6 CC(C)N1CCC(Oc2ccc3cc(C(=O)N4CCOCC4)ccc3c2)CC1 10.1016/j.bmcl.2009.03.100
CHEMBL541483 201699 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 382 4 0 4 3.6 CC(C)N1CCC(Oc2ccc3cc(C(=O)N4CCOCC4)ccc3c2)CC1 10.1016/j.bmcl.2009.03.100
1218 7017 52 None -19 2 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 330 4 0 3 5.0 N#Cc1ccc(cc1)c1ccc2c(c1)cc(o2)CCN1CCC[C@H]1C 10.1021/jm0705051
9818903 7017 52 None -19 2 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 330 4 0 3 5.0 N#Cc1ccc(cc1)c1ccc2c(c1)cc(o2)CCN1CCC[C@H]1C 10.1021/jm0705051
CHEMBL351231 7017 52 None -19 2 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 330 4 0 3 5.0 N#Cc1ccc(cc1)c1ccc2c(c1)cc(o2)CCN1CCC[C@H]1C 10.1021/jm0705051
1218 7017 52 None -19 2 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 330 4 0 3 5.0 N#Cc1ccc(cc1)c1ccc2c(c1)cc(o2)CCN1CCC[C@H]1C 10.1021/jm0705051
9818903 7017 52 None -19 2 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 330 4 0 3 5.0 N#Cc1ccc(cc1)c1ccc2c(c1)cc(o2)CCN1CCC[C@H]1C 10.1021/jm0705051
CHEMBL351231 7017 52 None -19 2 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 330 4 0 3 5.0 N#Cc1ccc(cc1)c1ccc2c(c1)cc(o2)CCN1CCC[C@H]1C 10.1021/jm0705051
127050434 147028 0 None -3 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 160 3 4 3 0.2 CC(=N)SCCNC(=N)N 10.1021/acs.jmedchem.6b00120
CHEMBL3805514 147028 0 None -3 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 160 3 4 3 0.2 CC(=N)SCCNC(=N)N 10.1021/acs.jmedchem.6b00120
49799215 17704 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 242 3 1 3 2.3 c1cncc(N2CCC(Cc3c[nH]cn3)CC2)c1 10.1016/j.bmc.2010.04.052
CHEMBL1173033 17704 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 242 3 1 3 2.3 c1cncc(N2CCC(Cc3c[nH]cn3)CC2)c1 10.1016/j.bmc.2010.04.052
49799509 17677 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 297 3 1 2 4.2 CC(C)(C)c1ccc(N2CCC(Cc3c[nH]cn3)CC2)cc1 10.1016/j.bmc.2010.04.052
CHEMBL1172776 17677 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 297 3 1 2 4.2 CC(C)(C)c1ccc(N2CCC(Cc3c[nH]cn3)CC2)cc1 10.1016/j.bmc.2010.04.052
46945057 24308 0 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 395 5 0 4 4.1 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3C[C@@H](C)N(CC3CC3)C2=O)CC1 10.1016/j.bmcl.2010.08.009
CHEMBL1257965 24308 0 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 395 5 0 4 4.1 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3C[C@@H](C)N(CC3CC3)C2=O)CC1 10.1016/j.bmcl.2010.08.009
46945057 24308 0 None -1 2 Rat 7.8 pEC50 = 7.8 Functional
Inverse agonist activity at rat histamine H3 receptorInverse agonist activity at rat histamine H3 receptor
ChEMBL 395 5 0 4 4.1 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3C[C@@H](C)N(CC3CC3)C2=O)CC1 10.1016/j.bmcl.2010.08.009
CHEMBL1257965 24308 0 None -1 2 Rat 7.8 pEC50 = 7.8 Functional
Inverse agonist activity at rat histamine H3 receptorInverse agonist activity at rat histamine H3 receptor
ChEMBL 395 5 0 4 4.1 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3C[C@@H](C)N(CC3CC3)C2=O)CC1 10.1016/j.bmcl.2010.08.009
145952531 169693 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 534 7 1 6 5.9 COc1cc(NC2(c3ccccc3Cl)C(=O)N(C(C)(C)C)C(=O)/C2=C/c2ccccc2)cc(OC)c1OC 10.1016/j.ejmech.2018.04.020
CHEMBL4174017 169693 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 534 7 1 6 5.9 COc1cc(NC2(c3ccccc3Cl)C(=O)N(C(C)(C)C)C(=O)/C2=C/c2ccccc2)cc(OC)c1OC 10.1016/j.ejmech.2018.04.020
145952531 169693 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 534 7 1 6 5.9 COc1cc(NC2(c3ccccc3Cl)C(=O)N(C(C)(C)C)C(=O)/C2=C/c2ccccc2)cc(OC)c1OC 10.1016/j.ejmech.2018.04.020
CHEMBL4174017 169693 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 534 7 1 6 5.9 COc1cc(NC2(c3ccccc3Cl)C(=O)N(C(C)(C)C)C(=O)/C2=C/c2ccccc2)cc(OC)c1OC 10.1016/j.ejmech.2018.04.020
46888006 15717 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 272 4 1 2 3.8 FC(F)(F)c1ccc(SCCc2c[nH]cn2)cc1 10.1021/jm901890s
CHEMBL1098002 15717 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 272 4 1 2 3.8 FC(F)(F)c1ccc(SCCc2c[nH]cn2)cc1 10.1021/jm901890s
11622672 81794 2 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cellsActivity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cells
ChEMBL 221 6 1 2 2.6 c1nc(CCCCCN2CCCCC2)c[nH]1 10.1021/jm0504353
CHEMBL203389 81794 2 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cellsActivity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cells
ChEMBL 221 6 1 2 2.6 c1nc(CCCCCN2CCCCC2)c[nH]1 10.1021/jm0504353
10934158 115354 1 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptor
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@@H]2CC[C@H](c3c[nH]cn3)O2)cc1 10.1021/jm0300025
CHEMBL320331 115354 1 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptor
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@@H]2CC[C@H](c3c[nH]cn3)O2)cc1 10.1021/jm0300025
24738376 194094 1 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 234 3 1 1 3.7 c1ccc(-c2cccc(Cc3c[nH]cn3)c2)cc1 10.1021/jm7014149
CHEMBL493012 194094 1 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 234 3 1 1 3.7 c1ccc(-c2cccc(Cc3c[nH]cn3)c2)cc1 10.1021/jm7014149
10934158 115354 1 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@@H]2CC[C@H](c3c[nH]cn3)O2)cc1 10.1016/j.bmcl.2010.10.041
CHEMBL320331 115354 1 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@@H]2CC[C@H](c3c[nH]cn3)O2)cc1 10.1016/j.bmcl.2010.10.041
11474535 70330 2 None - 1 Human 6.7 pEC50 = 6.7 Functional
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
ChEMBL 221 4 1 2 2.5 CC(C)N1CCC(CCc2c[nH]cn2)CC1 10.1021/jm049475h
CHEMBL180061 70330 2 None - 1 Human 6.7 pEC50 = 6.7 Functional
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
ChEMBL 221 4 1 2 2.5 CC(C)N1CCC(CCc2c[nH]cn2)CC1 10.1021/jm049475h
16059780 176173 0 None -1 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 334 4 0 4 4.0 Cc1nn(C)cc1-c1ccc2cc(CCN3CCC[C@H]3C)ccc2n1 10.1021/jm0705051
CHEMBL442242 176173 0 None -1 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 334 4 0 4 4.0 Cc1nn(C)cc1-c1ccc2cc(CCN3CCC[C@H]3C)ccc2n1 10.1021/jm0705051
49799183 17477 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 284 4 1 3 2.9 CN(C)c1ccc(N2CCC(Cc3c[nH]cn3)CC2)cc1 10.1016/j.bmc.2010.04.052
CHEMBL1170855 17477 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 284 4 1 3 2.9 CN(C)c1ccc(N2CCC(Cc3c[nH]cn3)CC2)cc1 10.1016/j.bmc.2010.04.052
44539973 75289 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Inverse agonist activity at human H3R expressed in CHO cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human H3R expressed in CHO cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 297 4 0 4 2.5 C[C@@H]1CCCN1CCc1ccc(-c2ccc(=O)n(C)n2)cc1 10.1016/j.bmcl.2011.08.104
CHEMBL1917464 75289 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Inverse agonist activity at human H3R expressed in CHO cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human H3R expressed in CHO cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 297 4 0 4 2.5 C[C@@H]1CCCN1CCc1ccc(-c2ccc(=O)n(C)n2)cc1 10.1016/j.bmcl.2011.08.104
52948255 24340 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 473 5 0 4 5.1 CC(C)N1CCC(Oc2cc3cc4n(c3cc2Br)[C@@H](C)CN(CC2CC2)C4=O)CC1 10.1016/j.bmcl.2010.08.009
CHEMBL1258079 24340 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 473 5 0 4 5.1 CC(C)N1CCC(Oc2cc3cc4n(c3cc2Br)[C@@H](C)CN(CC2CC2)C4=O)CC1 10.1016/j.bmcl.2010.08.009
11619260 194733 16 None - 1 Human 8.7 pEC50 = 8.7 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 447 5 0 4 5.3 CC(C)N1CCC(Oc2ccc3c(c2)cc(C(=O)N2CCC(F)(F)CC2)n3C(C)C)CC1 10.1016/j.bmcl.2010.08.009
CHEMBL497031 194733 16 None - 1 Human 8.7 pEC50 = 8.7 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 447 5 0 4 5.3 CC(C)N1CCC(Oc2ccc3c(c2)cc(C(=O)N2CCC(F)(F)CC2)n3C(C)C)CC1 10.1016/j.bmcl.2010.08.009
25070031 72159 18 None -1 2 Rat 8.7 pEC50 = 8.7 Functional
Inverse agonist activity at rat histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS bindingInverse agonist activity at rat histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS binding
ChEMBL 313 6 1 4 2.7 C[C@@H]1CCCN1CCCOc1ccc(-c2ccc(=O)[nH]n2)cc1 10.1021/jm200401v
CHEMBL1829335 72159 18 None -1 2 Rat 8.7 pEC50 = 8.7 Functional
Inverse agonist activity at rat histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS bindingInverse agonist activity at rat histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS binding
ChEMBL 313 6 1 4 2.7 C[C@@H]1CCCN1CCCOc1ccc(-c2ccc(=O)[nH]n2)cc1 10.1021/jm200401v
56677285 72184 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Antagonist activity at human histamine 3 receptor by [35S]GTPgammaS binding assayAntagonist activity at human histamine 3 receptor by [35S]GTPgammaS binding assay
ChEMBL 341 6 0 5 2.9 C[C@H](COc1ccc(-c2ccc(=O)n(C)n2)cc1)CN1CCC[C@H]1C 10.1016/j.bmcl.2011.06.108
CHEMBL1829485 72184 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Antagonist activity at human histamine 3 receptor by [35S]GTPgammaS binding assayAntagonist activity at human histamine 3 receptor by [35S]GTPgammaS binding assay
ChEMBL 341 6 0 5 2.9 C[C@H](COc1ccc(-c2ccc(=O)n(C)n2)cc1)CN1CCC[C@H]1C 10.1016/j.bmcl.2011.06.108
44540072 75293 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Inverse agonist activity at human H3R expressed in CHO cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human H3R expressed in CHO cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 377 5 0 4 4.1 C[C@@H]1CCCN1CCc1ccc(-c2ccc(=O)n(-c3ccc(F)cc3)n2)cc1 10.1016/j.bmcl.2011.08.104
CHEMBL1917468 75293 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Inverse agonist activity at human H3R expressed in CHO cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human H3R expressed in CHO cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
ChEMBL 377 5 0 4 4.1 C[C@@H]1CCCN1CCc1ccc(-c2ccc(=O)n(-c3ccc(F)cc3)n2)cc1 10.1016/j.bmcl.2011.08.104
53363442 71162 0 None -1 2 Rat 8.7 pEC50 = 8.7 Functional
Inverse agonist activity at rat histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS bindingInverse agonist activity at rat histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS binding
ChEMBL 313 6 1 4 2.7 C[C@@H]1CCCN1CCCOc1ccc(-c2cn[nH]c(=O)c2)cc1 10.1021/jm200401v
CHEMBL1813065 71162 0 None -1 2 Rat 8.7 pEC50 = 8.7 Functional
Inverse agonist activity at rat histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS bindingInverse agonist activity at rat histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS binding
ChEMBL 313 6 1 4 2.7 C[C@@H]1CCCN1CCCOc1ccc(-c2cn[nH]c(=O)c2)cc1 10.1021/jm200401v
23725172 71155 0 None -2 2 Rat 8.7 pEC50 = 8.7 Functional
Inverse agonist activity at rat histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS bindingInverse agonist activity at rat histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS binding
ChEMBL 327 6 0 5 2.7 C[C@@H]1CCCN1CCCOc1ccc(-c2ccc(=O)n(C)n2)cc1 10.1021/jm200401v
CHEMBL1813057 71155 0 None -2 2 Rat 8.7 pEC50 = 8.7 Functional
Inverse agonist activity at rat histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS bindingInverse agonist activity at rat histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS binding
ChEMBL 327 6 0 5 2.7 C[C@@H]1CCCN1CCCOc1ccc(-c2ccc(=O)n(C)n2)cc1 10.1021/jm200401v
11957573 8791 34 None 3 5 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm901890s
1250 8791 34 None 3 5 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm901890s
3692 8791 34 None 3 5 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm901890s
CHEMBL19439 8791 34 None 3 5 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm901890s
1204 8713 119 None -2 11 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01462
1247 8713 119 None -2 11 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01462
1375 8713 119 None -2 11 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01462
774 8713 119 None -2 11 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01462
CHEMBL90 8713 119 None -2 11 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01462
DB05381 8713 119 None -2 11 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01462
25149712 185765 0 None 6 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gsalpha2, Gbeta1gamma2 and RGS19 by steady-state GTPase activity assayAgonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gsalpha2, Gbeta1gamma2 and RGS19 by steady-state GTPase activity assay
ChEMBL 299 7 4 3 1.6 N=C(NCCCc1c[nH]cn1)NC(=O)CCc1ccccc1 10.1016/j.bmcl.2010.10.041
CHEMBL470790 185765 0 None 6 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gsalpha2, Gbeta1gamma2 and RGS19 by steady-state GTPase activity assayAgonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gsalpha2, Gbeta1gamma2 and RGS19 by steady-state GTPase activity assay
ChEMBL 299 7 4 3 1.6 N=C(NCCCc1c[nH]cn1)NC(=O)CCc1ccccc1 10.1016/j.bmcl.2010.10.041
25149335 191004 0 None 6 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gsalpha2, Gbeta1gamma2 and RGS19 by steady-state GTPase activity assayAgonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gsalpha2, Gbeta1gamma2 and RGS19 by steady-state GTPase activity assay
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1016/j.bmcl.2010.10.041
CHEMBL483406 191004 0 None 6 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gsalpha2, Gbeta1gamma2 and RGS19 by steady-state GTPase activity assayAgonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gsalpha2, Gbeta1gamma2 and RGS19 by steady-state GTPase activity assay
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1016/j.bmcl.2010.10.041
11336692 70067 1 None - 1 Human 8.6 pEC50 = 8.6 Functional
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
ChEMBL 177 1 1 2 1.5 CN1CCC(=Cc2c[nH]cn2)CC1 10.1021/jm049475h
CHEMBL179302 70067 1 None - 1 Human 8.6 pEC50 = 8.6 Functional
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
ChEMBL 177 1 1 2 1.5 CN1CCC(=Cc2c[nH]cn2)CC1 10.1021/jm049475h
145954725 169199 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 534 7 1 6 5.9 COc1cc(NC2(c3cccc(Cl)c3)C(=O)N(C(C)(C)C)C(=O)/C2=C/c2ccccc2)cc(OC)c1OC 10.1016/j.ejmech.2018.04.020
CHEMBL4166098 169199 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 534 7 1 6 5.9 COc1cc(NC2(c3cccc(Cl)c3)C(=O)N(C(C)(C)C)C(=O)/C2=C/c2ccccc2)cc(OC)c1OC 10.1016/j.ejmech.2018.04.020
145954725 169199 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 534 7 1 6 5.9 COc1cc(NC2(c3cccc(Cl)c3)C(=O)N(C(C)(C)C)C(=O)/C2=C/c2ccccc2)cc(OC)c1OC 10.1016/j.ejmech.2018.04.020
CHEMBL4166098 169199 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 534 7 1 6 5.9 COc1cc(NC2(c3cccc(Cl)c3)C(=O)N(C(C)(C)C)C(=O)/C2=C/c2ccccc2)cc(OC)c1OC 10.1016/j.ejmech.2018.04.020
145973591 169811 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 530 7 1 5 6.5 COc1ccc(NC2(c3cccc(Cl)c3)C(=O)N(C3CCCCC3)C(=O)/C2=C/c2ccccc2)cc1OC 10.1016/j.ejmech.2018.04.020
CHEMBL4175898 169811 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 530 7 1 5 6.5 COc1ccc(NC2(c3cccc(Cl)c3)C(=O)N(C3CCCCC3)C(=O)/C2=C/c2ccccc2)cc1OC 10.1016/j.ejmech.2018.04.020
145973591 169811 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 530 7 1 5 6.5 COc1ccc(NC2(c3cccc(Cl)c3)C(=O)N(C3CCCCC3)C(=O)/C2=C/c2ccccc2)cc1OC 10.1016/j.ejmech.2018.04.020
CHEMBL4175898 169811 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 530 7 1 5 6.5 COc1ccc(NC2(c3cccc(Cl)c3)C(=O)N(C3CCCCC3)C(=O)/C2=C/c2ccccc2)cc1OC 10.1016/j.ejmech.2018.04.020
1236 8848 25 None -1 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1021/jm901890s
1237 8848 25 None -1 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1021/jm901890s
156615 8848 25 None -1 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1021/jm901890s
CHEMBL268229 8848 25 None -1 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1021/jm901890s
56954515 88840 0 None 2 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human H3R-Galphai2-Gbeta1gamma2-RGS4 expressed in Sf9 cells 0.1 nM to 1 mM by steady state GTPase activity assayAgonist activity at human H3R-Galphai2-Gbeta1gamma2-RGS4 expressed in Sf9 cells 0.1 nM to 1 mM by steady state GTPase activity assay
ChEMBL 546 17 6 6 2.3 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm201128q
CHEMBL2165628 88840 0 None 2 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human H3R-Galphai2-Gbeta1gamma2-RGS4 expressed in Sf9 cells 0.1 nM to 1 mM by steady state GTPase activity assayAgonist activity at human H3R-Galphai2-Gbeta1gamma2-RGS4 expressed in Sf9 cells 0.1 nM to 1 mM by steady state GTPase activity assay
ChEMBL 546 17 6 6 2.3 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm201128q
11957573 8791 34 None 3 5 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human H3 receptor expressed in CHO cells assessed as increase in cAMP accumulation by measuring reduction in forskolin level incubated for 4 hrs by CRE/MRE-luciferase reporter gene assayAgonist activity at human H3 receptor expressed in CHO cells assessed as increase in cAMP accumulation by measuring reduction in forskolin level incubated for 4 hrs by CRE/MRE-luciferase reporter gene assay
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.ejmech.2020.112150
1250 8791 34 None 3 5 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human H3 receptor expressed in CHO cells assessed as increase in cAMP accumulation by measuring reduction in forskolin level incubated for 4 hrs by CRE/MRE-luciferase reporter gene assayAgonist activity at human H3 receptor expressed in CHO cells assessed as increase in cAMP accumulation by measuring reduction in forskolin level incubated for 4 hrs by CRE/MRE-luciferase reporter gene assay
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.ejmech.2020.112150
3692 8791 34 None 3 5 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human H3 receptor expressed in CHO cells assessed as increase in cAMP accumulation by measuring reduction in forskolin level incubated for 4 hrs by CRE/MRE-luciferase reporter gene assayAgonist activity at human H3 receptor expressed in CHO cells assessed as increase in cAMP accumulation by measuring reduction in forskolin level incubated for 4 hrs by CRE/MRE-luciferase reporter gene assay
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.ejmech.2020.112150
CHEMBL19439 8791 34 None 3 5 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human H3 receptor expressed in CHO cells assessed as increase in cAMP accumulation by measuring reduction in forskolin level incubated for 4 hrs by CRE/MRE-luciferase reporter gene assayAgonist activity at human H3 receptor expressed in CHO cells assessed as increase in cAMP accumulation by measuring reduction in forskolin level incubated for 4 hrs by CRE/MRE-luciferase reporter gene assay
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.ejmech.2020.112150
11610910 202530 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 394 6 0 3 5.0 CC1CCN(C(=O)c2ccc3cc(OCCCN4CCCCC4)ccc3c2)CC1 10.1016/j.bmcl.2009.03.100
CHEMBL557461 202530 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 394 6 0 3 5.0 CC1CCN(C(=O)c2ccc3cc(OCCCN4CCCCC4)ccc3c2)CC1 10.1016/j.bmcl.2009.03.100
44578637 188383 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgammaS assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgammaS assay
ChEMBL 394 5 1 3 5.2 CC(C)N1CCC(Oc2ccc3cc(C(=O)NC4CCCCC4)ccc3c2)CC1 10.1016/j.bmcl.2008.06.062
CHEMBL477181 188383 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgammaS assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgammaS assay
ChEMBL 394 5 1 3 5.2 CC(C)N1CCC(Oc2ccc3cc(C(=O)NC4CCCCC4)ccc3c2)CC1 10.1016/j.bmcl.2008.06.062
127050431 147093 0 None -3 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3806206 147093 0 None -3 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
46929553 23525 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 337 5 1 3 5.0 CC(C)(C)c1ccc(SCC(c2cccnc2)c2c[nH]cn2)cc1 10.1021/jm100643t
CHEMBL1243366 23525 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 337 5 1 3 5.0 CC(C)(C)c1ccc(SCC(c2cccnc2)c2c[nH]cn2)cc1 10.1021/jm100643t
145952665 169213 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 440 5 1 4 5.3 COc1ccc(NC2(c3ccccc3)C(=O)N(C(C)(C)C)C(=O)/C2=C/c2ccccc2)cc1 10.1016/j.ejmech.2018.04.020
CHEMBL4166386 169213 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 440 5 1 4 5.3 COc1ccc(NC2(c3ccccc3)C(=O)N(C(C)(C)C)C(=O)/C2=C/c2ccccc2)cc1 10.1016/j.ejmech.2018.04.020
46929647 23530 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 355 5 2 3 4.3 FC(F)(F)c1ccc(SC[C@H](c2c[nH]cn2)C2CCNCC2)cc1 10.1021/jm100643t
CHEMBL1243394 23530 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 355 5 2 3 4.3 FC(F)(F)c1ccc(SC[C@H](c2c[nH]cn2)C2CCNCC2)cc1 10.1021/jm100643t
16678615 24091 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 435 5 0 4 4.7 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCN(Cc3cccc(F)c3)C2=O)CC1 10.1016/j.bmcl.2010.08.009
CHEMBL1257257 24091 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 435 5 0 4 4.7 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCN(Cc3cccc(F)c3)C2=O)CC1 10.1016/j.bmcl.2010.08.009
145951920 169737 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 548 6 1 4 5.7 COc1ccc(N2C(=O)/C(=C\c3ccccc3)C2(C(=O)NC(C)(C)C)c2ccc(Br)cc2)cc1OC 10.1016/j.ejmech.2018.04.020
CHEMBL4174766 169737 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 548 6 1 4 5.7 COc1ccc(N2C(=O)/C(=C\c3ccccc3)C2(C(=O)NC(C)(C)C)c2ccc(Br)cc2)cc1OC 10.1016/j.ejmech.2018.04.020
16679611 24405 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 341 5 1 4 3.0 C[C@H]1CC[C@H](C)N1CCCOc1ccc2c(c1)cc1n2CCNC1=O 10.1016/j.bmcl.2010.08.009
CHEMBL1258309 24405 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 341 5 1 4 3.0 C[C@H]1CC[C@H](C)N1CCCOc1ccc2c(c1)cc1n2CCNC1=O 10.1016/j.bmcl.2010.08.009
46222044 15683 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 215 4 2 2 2.7 Cc1ccc(NCCc2c[nH]cn2)cc1C 10.1021/jm901890s
CHEMBL1097658 15683 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 215 4 2 2 2.7 Cc1ccc(NCCc2c[nH]cn2)cc1C 10.1021/jm901890s
16678214 24586 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 369 4 0 4 3.8 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCN(C(C)C)C2=O)CC1 10.1016/j.bmcl.2010.08.009
CHEMBL1258874 24586 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 369 4 0 4 3.8 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCN(C(C)C)C2=O)CC1 10.1016/j.bmcl.2010.08.009
11694543 82574 4 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cellsActivity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cells
ChEMBL 167 6 2 2 1.3 CCNCCCCc1c[nH]cn1 10.1021/jm0504353
CHEMBL204843 82574 4 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cellsActivity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cells
ChEMBL 167 6 2 2 1.3 CCNCCCCc1c[nH]cn1 10.1021/jm0504353
42623567 180470 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 207 3 2 5 0.0 CCc1cc(N2CC(NC)C2)nc(N)n1 10.1021/acs.jmedchem.9b01462
CHEMBL4535363 180470 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 207 3 2 5 0.0 CCc1cc(N2CC(NC)C2)nc(N)n1 10.1021/acs.jmedchem.9b01462
1204 8713 119 None -2 11 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gialpha-2-Gbeta-1-gamma-2 and RGS4 proteins protein by steady-state GTPase assayAgonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gialpha-2-Gbeta-1-gamma-2 and RGS4 proteins protein by steady-state GTPase assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm900526h
1247 8713 119 None -2 11 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gialpha-2-Gbeta-1-gamma-2 and RGS4 proteins protein by steady-state GTPase assayAgonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gialpha-2-Gbeta-1-gamma-2 and RGS4 proteins protein by steady-state GTPase assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm900526h
1375 8713 119 None -2 11 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gialpha-2-Gbeta-1-gamma-2 and RGS4 proteins protein by steady-state GTPase assayAgonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gialpha-2-Gbeta-1-gamma-2 and RGS4 proteins protein by steady-state GTPase assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm900526h
774 8713 119 None -2 11 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gialpha-2-Gbeta-1-gamma-2 and RGS4 proteins protein by steady-state GTPase assayAgonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gialpha-2-Gbeta-1-gamma-2 and RGS4 proteins protein by steady-state GTPase assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm900526h
CHEMBL90 8713 119 None -2 11 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gialpha-2-Gbeta-1-gamma-2 and RGS4 proteins protein by steady-state GTPase assayAgonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gialpha-2-Gbeta-1-gamma-2 and RGS4 proteins protein by steady-state GTPase assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm900526h
DB05381 8713 119 None -2 11 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gialpha-2-Gbeta-1-gamma-2 and RGS4 proteins protein by steady-state GTPase assayAgonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gialpha-2-Gbeta-1-gamma-2 and RGS4 proteins protein by steady-state GTPase assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm900526h
11416895 67299 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
ChEMBL 191 2 1 2 1.9 CCN1CCC(=Cc2c[nH]cn2)CC1 10.1021/jm049475h
CHEMBL175741 67299 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
ChEMBL 191 2 1 2 1.9 CCN1CCC(=Cc2c[nH]cn2)CC1 10.1021/jm049475h
145951920 169737 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 548 6 1 4 5.7 COc1ccc(N2C(=O)/C(=C\c3ccccc3)C2(C(=O)NC(C)(C)C)c2ccc(Br)cc2)cc1OC 10.1016/j.ejmech.2018.04.020
CHEMBL4174766 169737 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 548 6 1 4 5.7 COc1ccc(N2C(=O)/C(=C\c3ccccc3)C2(C(=O)NC(C)(C)C)c2ccc(Br)cc2)cc1OC 10.1016/j.ejmech.2018.04.020
51354301 65666 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assayAgonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assay
ChEMBL 259 5 1 4 2.4 c1nc(CCn2cc(CC3CCCCC3)nn2)c[nH]1 10.1021/jm1013488
CHEMBL1688969 65666 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assayAgonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assay
ChEMBL 259 5 1 4 2.4 c1nc(CCn2cc(CC3CCCCC3)nn2)c[nH]1 10.1021/jm1013488
44480959 12448 2 None -1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gialpha-2-Gbeta-1-gamma-2 and RGS4 proteins protein by steady-state GTPase assayAgonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gialpha-2-Gbeta-1-gamma-2 and RGS4 proteins protein by steady-state GTPase assay
ChEMBL 206 5 3 3 0.1 N#C/N=C(\N)NCCCCc1c[nH]cn1 10.1021/jm900526h
CHEMBL1077861 12448 2 None -1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gialpha-2-Gbeta-1-gamma-2 and RGS4 proteins protein by steady-state GTPase assayAgonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gialpha-2-Gbeta-1-gamma-2 and RGS4 proteins protein by steady-state GTPase assay
ChEMBL 206 5 3 3 0.1 N#C/N=C(\N)NCCCCc1c[nH]cn1 10.1021/jm900526h
16679701 24551 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 341 3 1 4 3.0 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCCNC2=O)CC1 10.1016/j.bmcl.2010.08.009
CHEMBL1258755 24551 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 341 3 1 4 3.0 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCCNC2=O)CC1 10.1016/j.bmcl.2010.08.009
10773349 14863 1 None 89 2 Human 6.6 pEC50 = 6.6 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptor
ChEMBL 165 2 2 3 0.4 NC[C@H]1C=C[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL109130 14863 1 None 89 2 Human 6.6 pEC50 = 6.6 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptor
ChEMBL 165 2 2 3 0.4 NC[C@H]1C=C[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
10702196 115345 1 None 1 2 Human 4.6 pEC50 = 4.6 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptor
ChEMBL 165 2 2 3 0.4 NC[C@@H]1C=C[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL320279 115345 1 None 1 2 Human 4.6 pEC50 = 4.6 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptor
ChEMBL 165 2 2 3 0.4 NC[C@@H]1C=C[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
52941269 24057 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 381 5 0 4 3.8 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCN(CC3CC3)C2=O)CC1 10.1016/j.bmcl.2010.08.009
CHEMBL1257138 24057 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 381 5 0 4 3.8 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCN(CC3CC3)C2=O)CC1 10.1016/j.bmcl.2010.08.009
16678514 24090 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 435 5 0 4 4.7 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCN(Cc3ccccc3F)C2=O)CC1 10.1016/j.bmcl.2010.08.009
CHEMBL1257256 24090 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 435 5 0 4 4.7 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCN(Cc3ccccc3F)C2=O)CC1 10.1016/j.bmcl.2010.08.009
10820929 114984 1 None 30 2 Human 5.6 pEC50 = 5.6 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptor
ChEMBL 165 2 2 3 0.4 NC[C@@H]1C=C[C@@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL319658 114984 1 None 30 2 Human 5.6 pEC50 = 5.6 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptor
ChEMBL 165 2 2 3 0.4 NC[C@@H]1C=C[C@@H](c2c[nH]cn2)O1 10.1021/jm0300025
16679612 24277 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 341 3 1 4 3.2 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3[C@H](C)CNC2=O)CC1 10.1016/j.bmcl.2010.08.009
CHEMBL1257851 24277 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
ChEMBL 341 3 1 4 3.2 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3[C@H](C)CNC2=O)CC1 10.1016/j.bmcl.2010.08.009
145952665 169213 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 440 5 1 4 5.3 COc1ccc(NC2(c3ccccc3)C(=O)N(C(C)(C)C)C(=O)/C2=C/c2ccccc2)cc1 10.1016/j.ejmech.2018.04.020
CHEMBL4166386 169213 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 440 5 1 4 5.3 COc1ccc(NC2(c3ccccc3)C(=O)N(C(C)(C)C)C(=O)/C2=C/c2ccccc2)cc1 10.1016/j.ejmech.2018.04.020
11647025 96248 0 None -3 2 Rat 8.5 pEC50 = 8.5 Functional
Agonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 401 5 0 5 4.6 Cc1nc(N2CCCC2)ncc1-c1ccc2cc(CCN3CCC[C@H]3C)ccc2n1 10.1021/jm0705051
CHEMBL237191 96248 0 None -3 2 Rat 8.5 pEC50 = 8.5 Functional
Agonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 401 5 0 5 4.6 Cc1nc(N2CCCC2)ncc1-c1ccc2cc(CCN3CCC[C@H]3C)ccc2n1 10.1021/jm0705051
155538222 183232 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 207 3 2 5 0.2 CC(C)NC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4476584 183232 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 207 3 2 5 0.2 CC(C)NC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4596412 183232 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 207 3 2 5 0.2 CC(C)NC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
1255 9969 19 None 19 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 216 6 1 2 2.6 C(CCc1cnc[nH]1)OCc1ccccc1 10.1016/j.bmcl.2010.10.041
6421522 9969 19 None 19 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 216 6 1 2 2.6 C(CCc1cnc[nH]1)OCc1ccccc1 10.1016/j.bmcl.2010.10.041
CHEMBL19173 9969 19 None 19 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 216 6 1 2 2.6 C(CCc1cnc[nH]1)OCc1ccccc1 10.1016/j.bmcl.2010.10.041
11788475 127812 4 None - 1 Human 8.5 pEC50 = 8.5 Functional
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
ChEMBL 163 1 2 2 1.2 C(=C1CCNCC1)c1c[nH]cn1 10.1021/jm049475h
CHEMBL356666 127812 4 None - 1 Human 8.5 pEC50 = 8.5 Functional
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
ChEMBL 163 1 2 2 1.2 C(=C1CCNCC1)c1c[nH]cn1 10.1021/jm049475h
90666845 116216 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation countingInverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation counting
ChEMBL 395 6 0 5 4.7 c1cc(-c2nc(CN3CCCCC3)co2)ccc1O[C@H]1C[C@H](N2CCCCC2)C1 10.1039/C0MD00056F
CHEMBL3220125 116216 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation countingInverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation counting
ChEMBL 395 6 0 5 4.7 c1cc(-c2nc(CN3CCCCC3)co2)ccc1O[C@H]1C[C@H](N2CCCCC2)C1 10.1039/C0MD00056F
1204 8713 119 None -2 11 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human H3R expressed in HEK293T-SP-FLAG-hH3R-CRE-CBR cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H3R expressed in HEK293T-SP-FLAG-hH3R-CRE-CBR cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1247 8713 119 None -2 11 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human H3R expressed in HEK293T-SP-FLAG-hH3R-CRE-CBR cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H3R expressed in HEK293T-SP-FLAG-hH3R-CRE-CBR cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1375 8713 119 None -2 11 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human H3R expressed in HEK293T-SP-FLAG-hH3R-CRE-CBR cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H3R expressed in HEK293T-SP-FLAG-hH3R-CRE-CBR cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
774 8713 119 None -2 11 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human H3R expressed in HEK293T-SP-FLAG-hH3R-CRE-CBR cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H3R expressed in HEK293T-SP-FLAG-hH3R-CRE-CBR cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
CHEMBL90 8713 119 None -2 11 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human H3R expressed in HEK293T-SP-FLAG-hH3R-CRE-CBR cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H3R expressed in HEK293T-SP-FLAG-hH3R-CRE-CBR cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
DB05381 8713 119 None -2 11 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human H3R expressed in HEK293T-SP-FLAG-hH3R-CRE-CBR cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H3R expressed in HEK293T-SP-FLAG-hH3R-CRE-CBR cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
11603648 154966 0 None -2 2 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 397 5 0 5 4.8 Cc1c(-c2ccc3cc(CCN4CCC[C@H]4C)ccc3n2)cnn1-c1ccccn1 10.1021/jm0705051
CHEMBL393581 154966 0 None -2 2 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 397 5 0 5 4.8 Cc1c(-c2ccc3cc(CCN4CCC[C@H]4C)ccc3n2)cnn1-c1ccccn1 10.1021/jm0705051
11603648 154966 0 None -2 2 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 397 5 0 5 4.8 Cc1c(-c2ccc3cc(CCN4CCC[C@H]4C)ccc3n2)cnn1-c1ccccn1 10.1021/jm0705051
CHEMBL393581 154966 0 None -2 2 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
ChEMBL 397 5 0 5 4.8 Cc1c(-c2ccc3cc(CCN4CCC[C@H]4C)ccc3n2)cnn1-c1ccccn1 10.1021/jm0705051
145951081 169754 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 502 6 1 4 6.1 COc1ccc(NC2(c3cc(F)cc(F)c3)C(=O)N(C3CCCCC3)C(=O)/C2=C/c2ccccc2)cc1 10.1016/j.ejmech.2018.04.020